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)
  • Publication number: 20120172350
    Abstract: 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: Application
    Filed: September 9, 2010
    Publication date: July 5, 2012
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Publication number: 20120142665
    Abstract: 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: Application
    Filed: December 1, 2011
    Publication date: June 7, 2012
    Inventors: Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinden, Matthias Koerner, Jens-Uwe Peters
  • Patent number: 8158619
    Abstract: 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: Grant
    Filed: May 29, 2007
    Date of Patent: April 17, 2012
    Assignee: Neurosearch A/S
    Inventors: 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
  • Publication number: 20120071469
    Abstract: 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: Application
    Filed: May 12, 2010
    Publication date: March 22, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
  • Publication number: 20120028968
    Abstract: 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: Application
    Filed: January 25, 2010
    Publication date: February 2, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
  • Publication number: 20120028967
    Abstract: 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: Application
    Filed: January 20, 2010
    Publication date: February 2, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Tino Dyhring, Jeppe Kejser Christensen
  • Patent number: 8106042
    Abstract: 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: Grant
    Filed: March 9, 2009
    Date of Patent: January 31, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Eva Dam Christoffersen
  • Patent number: 8101598
    Abstract: 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: Grant
    Filed: August 23, 2010
    Date of Patent: January 24, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel
  • Publication number: 20120003153
    Abstract: 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: Application
    Filed: January 25, 2010
    Publication date: January 5, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Tino Dyhring, Jeppe Kejser Christensen, Elsebet Østergaard Nielsen
  • Publication number: 20120004215
    Abstract: 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: Application
    Filed: January 25, 2010
    Publication date: January 5, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen, Elsebet Østergaard Nielsen
  • Publication number: 20120004214
    Abstract: 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: Application
    Filed: January 20, 2010
    Publication date: January 5, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen
  • Publication number: 20110319397
    Abstract: 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: Application
    Filed: January 25, 2010
    Publication date: December 29, 2011
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen
  • Publication number: 20110263577
    Abstract: 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: Application
    Filed: October 8, 2009
    Publication date: October 27, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring, Jeppe Kejser Christensen
  • Publication number: 20110257161
    Abstract: 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: Application
    Filed: December 3, 2009
    Publication date: October 20, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet ?stergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
  • Publication number: 20110251177
    Abstract: 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: Application
    Filed: April 13, 2011
    Publication date: October 13, 2011
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Jiaxin Yu, Jeffrey Clough, Rajinder Singh
  • Publication number: 20110152238
    Abstract: 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: Application
    Filed: December 13, 2010
    Publication date: June 23, 2011
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Gabrieie Murineddu, Luca Pani, Gerard Aime Pinna
  • Publication number: 20110130389
    Abstract: 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: Application
    Filed: December 1, 2010
    Publication date: June 2, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Benoit ROBERT, Laurent SALLE
  • Publication number: 20110124619
    Abstract: 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: Application
    Filed: November 17, 2010
    Publication date: May 26, 2011
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Publication number: 20110112078
    Abstract: 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: Application
    Filed: June 9, 2009
    Publication date: May 12, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: 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
  • Publication number: 20110105478
    Abstract: 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: Application
    Filed: March 9, 2009
    Publication date: May 5, 2011
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Eva Dam Christoffersen
  • Patent number: 7932248
    Abstract: 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: Grant
    Filed: November 9, 2006
    Date of Patent: April 26, 2011
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Richard Schumacher, Jianguo Ma, Brian Herbert, Mihaela Diana Danca, Wenge Xie, Truc Minh Nguyen, Ashok Tehim
  • Patent number: 7910578
    Abstract: 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: Grant
    Filed: May 21, 2007
    Date of Patent: March 22, 2011
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel, Jeppe Kejser Christensen, Tino Dyhring
  • Publication number: 20110059955
    Abstract: 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: Application
    Filed: August 18, 2010
    Publication date: March 10, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Loic FOULON, Laurent GOULLIEUX, Brigitte POUZET, Claudine SERRADEIL-LE GAL, Gerard VALETTE
  • Publication number: 20110046118
    Abstract: 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: Application
    Filed: November 13, 2008
    Publication date: February 24, 2011
    Applicant: Neurosearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen, John Paul Redrobe, Jens Damsgaard Mikkelsen
  • Publication number: 20100324027
    Abstract: The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: June 18, 2010
    Publication date: December 23, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Michael R. Schrimpf, Kevin B. Sippy
  • Publication number: 20100305108
    Abstract: 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: Application
    Filed: November 13, 2008
    Publication date: December 2, 2010
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen, John Paul Redrobe, Jens Damsgaard Mikkelsen
  • Publication number: 20100298306
    Abstract: 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: Application
    Filed: October 22, 2008
    Publication date: November 25, 2010
    Applicant: MEMORY PHARMACEUTICALS CORPORATION
    Inventors: Brian Herbert, Richard Schumacher, Guangxiu Dai, Wenge Xie
  • Publication number: 20100286128
    Abstract: 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: Application
    Filed: August 14, 2008
    Publication date: November 11, 2010
    Inventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Jeppe Kejser Christensen, John Paul Redrobe, Tino Dyhring
  • Publication number: 20100280015
    Abstract: 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: Application
    Filed: August 14, 2008
    Publication date: November 4, 2010
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen
  • Patent number: 7807667
    Abstract: 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: Grant
    Filed: May 29, 2007
    Date of Patent: October 5, 2010
    Assignee: NeuroSearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B Timmermann, Steven Charles Loechel
  • Publication number: 20100227848
    Abstract: 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: Application
    Filed: May 14, 2008
    Publication date: September 9, 2010
    Inventors: Christopher D. Cox, David B. Whitman
  • Publication number: 20100222316
    Abstract: 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: Application
    Filed: March 17, 2010
    Publication date: September 2, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
  • Publication number: 20100216780
    Abstract: 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: Application
    Filed: May 29, 2007
    Publication date: August 26, 2010
    Inventors: 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
  • Publication number: 20100210625
    Abstract: 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: Application
    Filed: August 14, 2008
    Publication date: August 19, 2010
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser
  • Publication number: 20100196357
    Abstract: 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: Application
    Filed: January 21, 2010
    Publication date: August 5, 2010
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Publication number: 20100196714
    Abstract: Methods for synthesizing tetrahydroquinoline-containing compounds are provided, along with synthetic intermediates and products associated with such methods.
    Type: Application
    Filed: April 7, 2010
    Publication date: August 5, 2010
    Applicant: Wyeth
    Inventors: Christoph Dehnhardt, Sreenivasulu Megati, Jerry Sun
  • Publication number: 20100190770
    Abstract: 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: Application
    Filed: January 22, 2010
    Publication date: July 29, 2010
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Sambaiah Thota, Rose Yen
  • Publication number: 20100137288
    Abstract: 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: Application
    Filed: February 5, 2010
    Publication date: June 3, 2010
    Inventors: Richard Schumacher, Mihaela Diana Danca, Jianguo Ma, Brian Herbert, True Minh Nguyen, Wenge Xie, Ashok Tehim
  • Publication number: 20100130483
    Abstract: 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: Application
    Filed: January 27, 2010
    Publication date: May 27, 2010
    Applicant: NeuroSearch A/S
    Inventors: Dan PETERS, Gunnar M. Olsen, Elsebet Øtergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring
  • Publication number: 20100130482
    Abstract: 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: Application
    Filed: January 5, 2010
    Publication date: May 27, 2010
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring, Daniel B. Timmerman
  • Publication number: 20100130420
    Abstract: 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: Application
    Filed: October 9, 2009
    Publication date: May 27, 2010
    Applicant: Howard Hughes Medical Institute
    Inventors: Scott STERNSON, Loren Looger, Peter Lee
  • Publication number: 20100113428
    Abstract: 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: Application
    Filed: December 8, 2009
    Publication date: May 6, 2010
    Inventors: Dan PETERS, Gunnar M. OLSEN, Elsebet Østergaard NIELSEN, Tino Dyhring JØRGENSEN, Daniel B. TIMMERMANN
  • Patent number: 7678788
    Abstract: 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: Grant
    Filed: February 4, 2004
    Date of Patent: March 16, 2010
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring
  • Patent number: 7662812
    Abstract: 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: Grant
    Filed: February 13, 2006
    Date of Patent: February 16, 2010
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Daniel B Timmermann, Gunnar Olsen, Elsebet Østergaard Nielsen, Tino Dyhring
  • Publication number: 20100022506
    Abstract: 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: Application
    Filed: October 5, 2009
    Publication date: January 28, 2010
    Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
  • Publication number: 20100004226
    Abstract: 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: Application
    Filed: August 7, 2009
    Publication date: January 7, 2010
    Inventors: James M. Cook, Hao Zhou, Shengming Huang, P.V.V.S. Sarma, Chunchun Zhang
  • Publication number: 20090325939
    Abstract: 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: Application
    Filed: September 3, 2009
    Publication date: December 31, 2009
    Inventors: Wenge XIE, Brian Herbert, Richard A. Schumacher, Jianguo Ma, True Minh Nguyen, Carla Maria Gauss, Ashok Tehim
  • Patent number: 7632831
    Abstract: 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: Grant
    Filed: May 6, 2005
    Date of Patent: December 15, 2009
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Richard A. Schumacher, Jianguo Ma, Truc Minh Nguyen, Carla Maria Gauss, Ashok Tehim
  • Publication number: 20090258864
    Abstract: 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: Application
    Filed: February 13, 2009
    Publication date: October 15, 2009
    Applicant: 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
  • Publication number: 20090253685
    Abstract: 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: Application
    Filed: May 22, 2008
    Publication date: October 8, 2009
    Inventors: Gregoire Provost, Marie-Christine Brezak Pannetier, Christian Diolez