Bicyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/235)
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Patent number: 8247414Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: GrantFiled: July 25, 2007Date of Patent: August 21, 2012Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Robert L. Hudkins, Kurt A. Josef, Ming Tao, Allison L. Zulli
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Patent number: 8247409Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: November 11, 2009Date of Patent: August 21, 2012Assignee: Amgen Inc.Inventors: Fang-Tsao Hong, James R. Falsey, Seifu Tadesse, Andrew Tasker
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Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20120202815Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Y is a 5-membered, fully or partially unsaturated heterocyclic ring containing 2-4 carbon atoms and 2-3 nitrogen atoms as ring members, the ring substituted with Z on a ring member atom connected through an adjacent single ring member atom to the ring member atom attaching the heterocyclic ring to the phenyl ring of Formula 1, and optionally further substituted with up to 2 substituents independently selected from R5 on carbon atom ring members and from R6 on nitrogen atom ring members; Z is an 8-, 9-, 10- or 11-membered fused heterobicyclic ring system containing ring members selected from carbon atoms and 1 to 4 heteroatoms independently selected from up to 2O, up to 2S and up to 4 N atoms, wherein up to 3 carbon atom ring members are independently selected from C(?O) and C(?S), and the sulfur atom ring members are independently selected from S(?O)u(?NR7)z, the ring system optionally substituted wiType: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Applicant: E.I.DU PONT DE NEMOURS AND COMPANYInventors: John Lawrence Andreassi II, Andrew Edmund Taggi
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Patent number: 8236949Abstract: Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.Type: GrantFiled: July 17, 2008Date of Patent: August 7, 2012Assignee: University of DelawareInventors: Joseph Michael Fox, Melissa Blackman, Maksim Royzen, Ni Yan
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Patent number: 8236801Abstract: The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: GrantFiled: February 19, 2009Date of Patent: August 7, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Patent number: 8231888Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: June 9, 2011Date of Patent: July 31, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Publication number: 20120178927Abstract: The invention relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.Type: ApplicationFiled: July 12, 2011Publication date: July 12, 2012Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Stefan LEHR, Dieter FEUCHT, Eva-Maria FRANKEN, Olga MALSAM, Alfred ANGERMANN, Guido BOJACK, Christian ARNOLD, Martin Jeffery HILLS, Heinz KEHNE, Christopher Hugh ROSINGER
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Patent number: 8217029Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: GrantFiled: April 11, 2008Date of Patent: July 10, 2012Assignee: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8211890Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.Type: GrantFiled: December 11, 2009Date of Patent: July 3, 2012Assignee: Actelion PharmaceuticalsInventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20120165276Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: May 6, 2008Publication date: June 28, 2012Applicant: Mpex Pharmaceuticals, Inc.Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
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Patent number: 8207168Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition disorders.Type: GrantFiled: June 15, 2010Date of Patent: June 26, 2012Assignee: Cephalon, Inc.Inventors: Nadine C. Becknell, Derek Dunn, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Publication number: 20120149691Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.Type: ApplicationFiled: July 30, 2010Publication date: June 14, 2012Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Yarlagadda S. Babu, Pravin L. Kotian, V. Satish Kumar, Minwan Wu, Tsu-Hsing Lin
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Publication number: 20120135984Abstract: Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.Type: ApplicationFiled: May 1, 2010Publication date: May 31, 2012Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty, Geoffrey Richard Heintzelman, Jeffrey D. Yingling, Casey Kopczynski
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Patent number: 8188083Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are defined as herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: June 26, 2008Date of Patent: May 29, 2012Assignee: Abbott LaboratoriesInventors: David J. Calderwood, Dominique F. Bonafoux, Andrew Burchat, Ping Ding, Kristine E. Frank, Michael Z. Hoemann, Kelly D. Mullen, Heather M. Davis
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Publication number: 20120129864Abstract: The subject of the present invention is compounds corresponding to the formula (I) in which: X represents a divalent (C2-C5)alkylene radical which is unsubstituted or substituted one or more times by an Alk group; R1 represents a phenyl, a naphthyl, a pyridyl, a 1-benzothienyl or a 1,3-benzodioxolyl; R2 represents a hydrogen atom, a halogen atom, an Alk group, an OAlk group or else a group chosen from —S-Alk, —SO-Alk, —SO2-Alk, —CO—N(R4)-Alk, —N(R4)SO2-Alk, —N(R4)CO-Alk, —N(R4)SO2—N(Alk)2; R3 represents a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 represents a hydrogen atom or a (C1-C4)alkyl; Alk represents an unsubstituted or substituted (C1-C4)alkyl. Preparation process and therapeutic application.Type: ApplicationFiled: April 6, 2010Publication date: May 24, 2012Applicant: SANOFIInventors: Elodie Barbagallo, Carole Legeay, Murielle Rinaldi-Carmona, Pascale Roux, Claude Vernhet
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Publication number: 20120129833Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.Type: ApplicationFiled: August 19, 2011Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
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Patent number: 8178536Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: November 29, 2010Date of Patent: May 15, 2012Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch, Thomas Salzmann, David Armistead
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Publication number: 20120095006Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.Type: ApplicationFiled: December 16, 2011Publication date: April 19, 2012Inventors: Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
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Patent number: 8143253Abstract: Compounds of formula I in free or salt or solvate form, where R1, R2 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: July 24, 2008Date of Patent: March 27, 2012Assignee: Novartis AGInventors: Dimitrios Lizos, Sven Weiler, Nikolaus Johannes Stiefl
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Publication number: 20120046267Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.Type: ApplicationFiled: February 11, 2011Publication date: February 23, 2012Inventors: Keith R. Hornberger, Dan M. Berger, Xin Chen, Andrew P. Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Lifu Ma, Mark J. Mulvihill, Bijoy Panicker, Kam W. Siu, Arno G. Steinig, James G. Tarrant, Jing Wang, Qinghua Weng, Rajaram Sangem, Ramesh C. Gupta
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Patent number: 8119566Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.Type: GrantFiled: August 2, 2004Date of Patent: February 21, 2012Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
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Publication number: 20120040989Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; and salts of such compounds.Type: ApplicationFiled: April 8, 2010Publication date: February 16, 2012Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Patent number: 8114893Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: GrantFiled: December 17, 2009Date of Patent: February 14, 2012Assignees: Genentech, Inc., Abbott Laboratories, The Walter and Eliza Hall Medical Research InstituteInventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
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Publication number: 20120015952Abstract: The invention relates to compounds of formulae (1) and (2): and pharmaceutically acceptable salts thereof for the treatment of cancer, inflammation, auto-immune diseases, diabetes and diabetic complications, infection, cardiovascular disease and ischemia-reperfusion injuries.Type: ApplicationFiled: March 25, 2010Publication date: January 19, 2012Applicant: Profectus Biosciences, Inc.Inventors: Jie Zhang, Drago Robert Sliskovic, Charles E. Ducker
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Publication number: 20120004234Abstract: This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: February 4, 2010Publication date: January 5, 2012Applicant: Schering CorporationInventors: Jason L. Davis, Michael John Mayer, Hubert B. Josien
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Publication number: 20110312936Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.Type: ApplicationFiled: June 16, 2011Publication date: December 22, 2011Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
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Patent number: 8076331Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.Type: GrantFiled: July 29, 2010Date of Patent: December 13, 2011Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
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Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
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Patent number: 8063070Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.Type: GrantFiled: May 4, 2010Date of Patent: November 22, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Patent number: 8063049Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: September 10, 2010Date of Patent: November 22, 2011Assignee: Ardea Biosciences, Inc.Inventors: Yung-hyo Koh, Zhi Hong, Jean-Michel Vernier, Andreas Maderna
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Publication number: 20110281877Abstract: The present invention relates to new dithiinopyridazinedione derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinedione derivatives.Type: ApplicationFiled: April 14, 2011Publication date: November 17, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Jürgen Benting
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Patent number: 8058275Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: GrantFiled: October 22, 2010Date of Patent: November 15, 2011Assignee: Eisai Inc.Inventors: Weizheng Xu, Greg Delahanty, Jie Zhang
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Patent number: 8044053Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: October 10, 2007Date of Patent: October 25, 2011Assignee: Laboratories del Dr. Esteve, S.A.Inventors: Helmut Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
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Patent number: 8044198Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: February 15, 2008Date of Patent: October 25, 2011Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
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Publication number: 20110251199Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I and A1, A2, A3, A4, X, Z, Z?, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: June 17, 2011Publication date: October 13, 2011Applicant: Amgen Inc.Inventors: Frenel F. De Morin, Jian J. Chen, Elizabeth M. Doherty, Stephen Hitchcock, Qi Huang, Joseph L. Kim, Gang Liu, Thomas Nixey, Nick A. Paras, Jeffrey Petkus, Daniel M. Retz, Adrian L. Smith, Jiawang Zhu
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Publication number: 20110245259Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.Type: ApplicationFiled: December 11, 2009Publication date: October 6, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110212969Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Publication number: 20110212968Abstract: The invention relates to novel phenethylamide derivatives and their wherein A, B, R1, R2 and R3 are as described in the application, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: October 13, 2009Publication date: September 1, 2011Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen, Daniel Trachsel, Jodi T. Williams
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Publication number: 20110207737Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.Type: ApplicationFiled: November 11, 2009Publication date: August 25, 2011Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
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Patent number: 8003658Abstract: The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof for inhibiting the growth of cancer cells, a method for the preparation thereof and a pharmaceutical composition comprising same as an active ingredient.Type: GrantFiled: December 20, 2005Date of Patent: August 23, 2011Assignee: Hanmi Holdings Co., Ltd.Inventors: Young Jin Ham, Ji Hyeon Gong, Mi Young Cha, Jong Woo Kim, Maeng Sup Kim, Eun Young Kim, Ji Yeon Song, Chang In Kim, Se Young Kim, Gwan Sun Lee
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Publication number: 20110190272Abstract: The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-IR kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.Type: ApplicationFiled: May 6, 2009Publication date: August 4, 2011Applicant: ASTRAZENECA ABInventors: Kevin Daly, Del Valle David, David Scott, Qing Ye
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Publication number: 20110183983Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.Type: ApplicationFiled: August 28, 2009Publication date: July 28, 2011Applicant: NEOPHARM CO., LTD.Inventors: Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
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Patent number: 7977334Abstract: The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.Type: GrantFiled: May 1, 2008Date of Patent: July 12, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Thomas Trieselmann, Bradford S. Hamilton
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Patent number: 7977333Abstract: Substituted and pyridines and pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1 and R2 may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using these materials are also disclosed.Type: GrantFiled: November 24, 2003Date of Patent: July 12, 2011Assignee: Bayer Healthcare LLCInventors: Jacques P. Dumas, Stephen J. Boyer, Julie A. Dixon, Teddy K. Joe, Harold C. E. Kluender, Wendy Lee, Dhanapalan Nagarathnam, Robert N. Sibley, Ning Su
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Patent number: 7973159Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I. where R1, R1a, R1b, A, R3, R4, R5, R5b and R6 are as defined herein.Type: GrantFiled: October 19, 2010Date of Patent: July 5, 2011Assignee: Bristol-Myers Squibb CompanyInventors: William N. Washburn, Saleem Ahmad, Andres S. Hernandez
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Patent number: 7964204Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: December 28, 2006Date of Patent: June 21, 2011Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Publication number: 20110144115Abstract: The present invention is related to novel substituted 1-benzylcinnolin-4(1H)-one derivatives having affinity for cannabinoid CB2 receptors, their preparation and their therapeutic application.Type: ApplicationFiled: January 10, 2011Publication date: June 16, 2011Applicant: SANOFI-AVENTISInventors: Claude Vernhet, Elodie Barbagallo, Murielle Rinaldi-Carmona, Pascale Roux
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Publication number: 20110144331Abstract: This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of anxiety disorders, cognitive disorders, and/or mood disorders.Type: ApplicationFiled: February 22, 2011Publication date: June 16, 2011Applicant: AstraZeneca ABInventors: Marc J. Chapdelaine, Cyrus J. Ohnmacht, Christopher Becker, Hui-Fang Chang, Bruce T. Dembofsky