Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/556)
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Publication number: 20120172350Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: September 9, 2010Publication date: July 5, 2012Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
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Publication number: 20120142665Abstract: The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Inventors: Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinden, Matthias Koerner, Jens-Uwe Peters
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Patent number: 8158619Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: May 29, 2007Date of Patent: April 17, 2012Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet ØStergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel, Jen Damsgaard Mikkelsen, Henrik Björk Hansen, John Paul Redrobe, Jeppe Kejser Christensen, Tino Dyhring
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Publication number: 20120071469Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.1]octane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: May 12, 2010Publication date: March 22, 2012Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
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Publication number: 20120028968Abstract: This invention relates to novel dibenzofuranyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 25, 2010Publication date: February 2, 2012Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
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Publication number: 20120028967Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 20, 2010Publication date: February 2, 2012Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Tino Dyhring, Jeppe Kejser Christensen
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Patent number: 8106042Abstract: This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: March 9, 2009Date of Patent: January 31, 2012Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Eva Dam Christoffersen
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Patent number: 8101598Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: August 23, 2010Date of Patent: January 24, 2012Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel
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Publication number: 20120003153Abstract: This invention relates to novel indolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 25, 2010Publication date: January 5, 2012Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Tino Dyhring, Jeppe Kejser Christensen, Elsebet Østergaard Nielsen
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Publication number: 20120004215Abstract: This invention relates to novel N-oxides of certain diazabicyclononyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 25, 2010Publication date: January 5, 2012Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen, Elsebet Østergaard Nielsen
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Publication number: 20120004214Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 20, 2010Publication date: January 5, 2012Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen
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Publication number: 20110319397Abstract: This invention relates to novel N-oxides of certain furanyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 25, 2010Publication date: December 29, 2011Applicant: NeuroSearch A/SInventors: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen
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Publication number: 20110263577Abstract: This invention relates to novel oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 8, 2009Publication date: October 27, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring, Jeppe Kejser Christensen
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Publication number: 20110257161Abstract: This invention relates to novel diazabicyclononyl-phenyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: December 3, 2009Publication date: October 20, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet ?stergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
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Publication number: 20110251177Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I) and (II): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.Type: ApplicationFiled: April 13, 2011Publication date: October 13, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Jiaxin Yu, Jeffrey Clough, Rajinder Singh
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Publication number: 20110152238Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.Type: ApplicationFiled: December 13, 2010Publication date: June 23, 2011Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Gabrieie Murineddu, Luca Pani, Gerard Aime Pinna
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Publication number: 20110130389Abstract: Fumarate salt of 4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate, crystalline forms thereof, methods of preparation thereof, and therapeutic use thereof.Type: ApplicationFiled: December 1, 2010Publication date: June 2, 2011Applicant: SANOFI-AVENTISInventors: Benoit ROBERT, Laurent SALLE
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Publication number: 20110124619Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: November 17, 2010Publication date: May 26, 2011Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20110112078Abstract: This invention relates to novel oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholin receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: June 9, 2009Publication date: May 12, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Ostergaard Nielsen, Gunnar M. Olsen, Philip K. Ahring, Tino Dyhring, Jeppe Kejser Christensen, John Paul Redrobe, Jens Damsgaard Mikkelsen
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Publication number: 20110105478Abstract: This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: March 9, 2009Publication date: May 5, 2011Applicant: NeuroSearch A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Eva Dam Christoffersen
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Patent number: 7932248Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: November 9, 2006Date of Patent: April 26, 2011Assignee: Memory Pharmaceuticals CorporationInventors: Richard Schumacher, Jianguo Ma, Brian Herbert, Mihaela Diana Danca, Wenge Xie, Truc Minh Nguyen, Ashok Tehim
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Patent number: 7910578Abstract: This invention relates to novel 8,10-diaza-bicyclo[4.3.1]decane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: May 21, 2007Date of Patent: March 22, 2011Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel, Jeppe Kejser Christensen, Tino Dyhring
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Publication number: 20110059955Abstract: The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application. The compounds of the present invention correspond to the formula (I): in which the variables are as set forth in the specification. These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V1a receptors and some compounds additionally exhibit a strong affinity for AVP V1b receptors.Type: ApplicationFiled: August 18, 2010Publication date: March 10, 2011Applicant: SANOFI-AVENTISInventors: Loic FOULON, Laurent GOULLIEUX, Brigitte POUZET, Claudine SERRADEIL-LE GAL, Gerard VALETTE
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Publication number: 20110046118Abstract: This invention relates to novel 1,4-diaza-bicyclo [3.2.2]nonyl pyrimidine derivatives of formula (I) and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: November 13, 2008Publication date: February 24, 2011Applicant: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen, John Paul Redrobe, Jens Damsgaard Mikkelsen
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Publication number: 20100324027Abstract: The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: June 18, 2010Publication date: December 23, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kevin B. Sippy
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Publication number: 20100305108Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: November 13, 2008Publication date: December 2, 2010Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen, John Paul Redrobe, Jens Damsgaard Mikkelsen
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Publication number: 20100298306Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds, which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. The novel compounds include compounds of formula I: wherein X, R1, and R2 are as herein defined.Type: ApplicationFiled: October 22, 2008Publication date: November 25, 2010Applicant: MEMORY PHARMACEUTICALS CORPORATIONInventors: Brian Herbert, Richard Schumacher, Guangxiu Dai, Wenge Xie
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Publication number: 20100286128Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: August 14, 2008Publication date: November 11, 2010Inventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Jeppe Kejser Christensen, John Paul Redrobe, Tino Dyhring
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Publication number: 20100280015Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: August 14, 2008Publication date: November 4, 2010Applicant: NeuroSearch A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen
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Patent number: 7807667Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: May 29, 2007Date of Patent: October 5, 2010Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B Timmermann, Steven Charles Loechel
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Publication number: 20100227848Abstract: The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: May 14, 2008Publication date: September 9, 2010Inventors: Christopher D. Cox, David B. Whitman
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Publication number: 20100222316Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: March 17, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
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Publication number: 20100216780Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: May 29, 2007Publication date: August 26, 2010Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel, Jens Damsgaard Mikkelsen, Henrik Björk Hansen, John Paul Redrobe, Jeppe Kejser Christensen, Timo Dyhring
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Publication number: 20100210625Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: August 14, 2008Publication date: August 19, 2010Applicant: NeuroSearch A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser
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Publication number: 20100196357Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: January 21, 2010Publication date: August 5, 2010Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20100196714Abstract: Methods for synthesizing tetrahydroquinoline-containing compounds are provided, along with synthetic intermediates and products associated with such methods.Type: ApplicationFiled: April 7, 2010Publication date: August 5, 2010Applicant: WyethInventors: Christoph Dehnhardt, Sreenivasulu Megati, Jerry Sun
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Publication number: 20100190770Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: January 22, 2010Publication date: July 29, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Sambaiah Thota, Rose Yen
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Publication number: 20100137288Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: February 5, 2010Publication date: June 3, 2010Inventors: Richard Schumacher, Mihaela Diana Danca, Jianguo Ma, Brian Herbert, True Minh Nguyen, Wenge Xie, Ashok Tehim
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Publication number: 20100130483Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 27, 2010Publication date: May 27, 2010Applicant: NeuroSearch A/SInventors: Dan PETERS, Gunnar M. Olsen, Elsebet Øtergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring
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Publication number: 20100130482Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: January 5, 2010Publication date: May 27, 2010Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring, Daniel B. Timmerman
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Publication number: 20100130420Abstract: The present invention provides novel chimeric receptors that have unique pharmacology. In particular, the chimeric receptors comprise a mutated ligand binding domain of the ?7 nicotinic acetylcholine receptor fused to a transmembrane or channel domain from a ligand-gated ion channel protein. The mutations in the ligand binding domain confer selective binding of compounds. Methods of using the novel chimeric receptors of the invention as well as compounds that preferentially bind and activate the chimeric receptors are also disclosed.Type: ApplicationFiled: October 9, 2009Publication date: May 27, 2010Applicant: Howard Hughes Medical InstituteInventors: Scott STERNSON, Loren Looger, Peter Lee
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Publication number: 20100113428Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: December 8, 2009Publication date: May 6, 2010Inventors: Dan PETERS, Gunnar M. OLSEN, Elsebet Østergaard NIELSEN, Tino Dyhring JØRGENSEN, Daniel B. TIMMERMANN
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Patent number: 7678788Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: February 4, 2004Date of Patent: March 16, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring
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Patent number: 7662812Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: February 13, 2006Date of Patent: February 16, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B Timmermann, Gunnar Olsen, Elsebet Østergaard Nielsen, Tino Dyhring
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Publication number: 20100022506Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: October 5, 2009Publication date: January 28, 2010Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
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Publication number: 20100004226Abstract: The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-IV, VI-XI, XV-XVIII and XX-XXI and a pharmaceutically-acceptable carrier.Type: ApplicationFiled: August 7, 2009Publication date: January 7, 2010Inventors: James M. Cook, Hao Zhou, Shengming Huang, P.V.V.S. Sarma, Chunchun Zhang
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Publication number: 20090325939Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: September 3, 2009Publication date: December 31, 2009Inventors: Wenge XIE, Brian Herbert, Richard A. Schumacher, Jianguo Ma, True Minh Nguyen, Carla Maria Gauss, Ashok Tehim
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Patent number: 7632831Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: May 6, 2005Date of Patent: December 15, 2009Assignee: Memory Pharmaceuticals CorporationInventors: Wenge Xie, Brian Herbert, Richard A. Schumacher, Jianguo Ma, Truc Minh Nguyen, Carla Maria Gauss, Ashok Tehim
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Publication number: 20090258864Abstract: This invention is directed to compounds of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, as isolated stereoisomers or mixtures thereof, or as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising the compounds of formula (I); and methods of using the compounds and the pharmaceutical compositions in treating diseases or conditions associated with JAK2 activity.Type: ApplicationFiled: February 13, 2009Publication date: October 15, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Somasekhar Bhamidipati, Jeffrey Clough, Ankush Argade, Rajinder Singh, Vadim Markovtosov, Pingyu Ding, Jiaxin Yu, Andy Atuegbu, Hui Hong, Ihab Darwish, Sambaiah Thota
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Publication number: 20090253685Abstract: A subject of the invention is a product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent for a therapeutic use which is simultaneous, separate or spread over time in the treatment of cancer.Type: ApplicationFiled: May 22, 2008Publication date: October 8, 2009Inventors: Gregoire Provost, Marie-Christine Brezak Pannetier, Christian Diolez