The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
-
Publication number: 20090209547Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: February 13, 2009Publication date: August 20, 2009Inventors: IN JONG KIM, GUOQIANG WANG, HEEJIN KIM, YAT SUN OR
-
Patent number: 7576209Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: December 4, 2007Date of Patent: August 18, 2009Assignee: Merck & Co., Inc.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
-
Publication number: 20090198063Abstract: Disclosed is a compound represented by the general formula: [wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.Type: ApplicationFiled: May 24, 2007Publication date: August 6, 2009Applicants: Toyama Chemical Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Taro Kiyoto, Junichi Ando, Tadashi Tanaka, Yasuhiro Tsutsui, Mai Yokotani, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri
-
Publication number: 20090192146Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: ApplicationFiled: February 9, 2009Publication date: July 30, 2009Applicant: ACEA BIOSCIENCES, INC.Inventors: Xiao XU, Haoyun An, Xiaobo Wang
-
Patent number: 7566726Abstract: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, Y and Z are defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. 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 chemokine receptors are involved.Type: GrantFiled: April 22, 2005Date of Patent: July 28, 2009Assignee: Merck & Co. Inc.Inventors: Lihu Yang, Sander G. Mills, Kothandaraman Shankaran
-
Publication number: 20090176807Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: ApplicationFiled: March 16, 2009Publication date: July 9, 2009Inventors: John Robinson REGAN, Thomas Wai-Ho Lee, David Thomson, Thomas Martin Kirrane, JR., Daniel Kuzmich, John Robert Proudfoot, Younes Bekkali, Renee Zindell
-
Patent number: 7557121Abstract: The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I?) in which A and R1 are as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: May 12, 2005Date of Patent: July 7, 2009Assignee: Pfizer IncInventors: Graham Lunn, John Paul Mathias, Ross Sinclair Strang
-
Publication number: 20090171089Abstract: Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: ApplicationFiled: March 6, 2009Publication date: July 2, 2009Applicant: BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.Inventors: Charles L. CYWIN, Scott E. JAKES, Joachim HEIDER, Mark A. BOBKO, Renee L. DES JARLAIS, Mark PLAYER, James RINKER, Michael WINTERS, Bao-ping ZHAO
-
Publication number: 20090170885Abstract: This invention provided compounds of formula I where W and Z are, independently, CH or N, and where other substituents are defined herein. Such compounds are potassium channel modulators. The invention also provides a composition comprising a pharmaceutically acceptable carrier or excipient and at least one of the following: a pharmaceutically effective amount of a compound of formula I; a pharmaceutically acceptable salt of a compound of formula I; a pharmaceutically acceptable ester of a compound of formula I. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt or ester or solvate thereof.Type: ApplicationFiled: July 28, 2008Publication date: July 2, 2009Applicant: VALEANT PHARMACEUTICALS INTERNATIONAL, INC.Inventors: JEAN-MICHEL VERNIER, MARTHA DE LA ROSA
-
Patent number: 7550480Abstract: Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.Type: GrantFiled: February 13, 2004Date of Patent: June 23, 2009Assignee: SmithKline Beecham CorporationInventors: Jeffrey Charles Boehm, James Francis Callahan, Ralph F. Hall, Xichen Lin, Katherine Louise Widdowson
-
Publication number: 20090156822Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.Type: ApplicationFiled: February 10, 2009Publication date: June 18, 2009Applicant: Boehringer Ingelheim International GmbHInventors: Murray D. BAILEY, Punit BHARDWAJ, Elise GHIRO, Nathalie GOUDREAU, Teddy HALMOS, Montse LLINAS-BRUNET, Marc-Andre POUPART, Jean RANCOURT
-
Publication number: 20090156578Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.Type: ApplicationFiled: December 1, 2006Publication date: June 18, 2009Inventors: Henry Pauls, Judd M. Berman
-
Patent number: 7547709Abstract: Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.Type: GrantFiled: November 2, 2004Date of Patent: June 16, 2009Assignee: Vanderbilt UniversityInventors: Derek A. Pratt, Luca Valgimigli, Gino A. DiLabio
-
Publication number: 20090149492Abstract: 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 DPP4 modulated disease or disorder such as, for example, diabetes, by administration of a therapeutically effective dose of a compound according to Formula I. wherein X, Z, A, R2, Y, R1, n, and b are as defined herein.Type: ApplicationFiled: November 16, 2007Publication date: June 11, 2009Inventors: John M. Fevig, Jianxin Feng
-
Publication number: 20090131444Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.Type: ApplicationFiled: May 23, 2006Publication date: May 21, 2009Applicant: ASTRAZENECA ABInventors: Folkert Reck, Marshall Morningstar, Hajnalka Hartl
-
Publication number: 20090124804Abstract: The present invention is directed to a process for enantioselectively preparing substituted piperidine alkanoic acid integrin antagonist compounds.Type: ApplicationFiled: October 30, 2008Publication date: May 14, 2009Inventors: William A. Kinney, Christopher A. Teleha, Shyamali Ghosh, Bruce E. Maryanoff
-
Publication number: 20090118298Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.Type: ApplicationFiled: September 25, 2008Publication date: May 7, 2009Inventors: Dawn M. George, Lu Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
-
Publication number: 20090118324Abstract: Compounds are provided for use with MEK that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 17, 2008Publication date: May 7, 2009Inventors: Qing DONG, Toufiko Kanounl, Michael B. Wallace
-
Publication number: 20090118233Abstract: A heterocyclic compound of the formula (I): wherein B1 is —C(R2)? or —N?; R1? is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R5 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is —C(—Y)?C(—RA)—C(—R3)?C(—R4)—, etc. wherein Y is OH, etc.; RA is —COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.Type: ApplicationFiled: February 26, 2008Publication date: May 7, 2009Inventors: Hitoshi Murai, Takeshi Endo, Noriyuki Kurose, Teruhiko Taishi, Hiroshi Yoshida
-
Publication number: 20090105215Abstract: The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.Type: ApplicationFiled: April 6, 2007Publication date: April 23, 2009Inventors: Brian Herbert, Wenge Xie, Truc Minh Nguyen, Allen T. Hopper, Ashok Tehim
-
Publication number: 20090104116Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.Type: ApplicationFiled: January 31, 2007Publication date: April 23, 2009Applicant: JERINI AGInventors: Gunter Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
-
Publication number: 20090105291Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH?C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof.Type: ApplicationFiled: December 3, 2008Publication date: April 23, 2009Applicant: Rigel Pharmaceuticals, Inc.Inventors: Stephen Brand, Stuart Bailey, Julien A. Brown, James A. Johnson, John R. Porter, John C. Head
-
Publication number: 20090091252Abstract: The present invention provides a novel binaphthyl compound and an organic light emitting element having a good light emitting efficiency and a high durability at a low driving voltage.Type: ApplicationFiled: October 2, 2008Publication date: April 9, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Tetsuya Kosuge, Jun Kamatani, Shigemoto Abe, Ryota Ooishi, Kengo Kishino
-
Patent number: 7511055Abstract: The present invention relates to heterocyclic derivatives of formula I wherein R1, R2 and R3 are as defined in the description and claims, which compounds are metabotropic glutamate receptor 5 antagonists.Type: GrantFiled: September 28, 2006Date of Patent: March 31, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Patrick Schnider, Eric Vieira
-
Publication number: 20090082390Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: July 8, 2008Publication date: March 26, 2009Inventors: Wai Ngor CHAN, Amanda Johns, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter
-
Publication number: 20090082358Abstract: Bicyclic 3,4-fused piperidine compounds, and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duoType: ApplicationFiled: September 22, 2008Publication date: March 26, 2009Inventors: Nobuko Nishimura, Mark H. Norman, Nuria Tamayo, Phi Tang, Yunxin Y. Bo
-
Publication number: 20090075978Abstract: The present invention relates to substituted propiolic acid amides, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
-
Publication number: 20090076065Abstract: The present application describes deuterium-enriched MK-0812, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 11, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Patent number: 7501437Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk—in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: March 28, 2007Date of Patent: March 10, 2009Assignee: UCB Pharma, S.A.Inventors: Stephen Brand, Stuart Bailey, Julien A. Brown, James A. Johnson, John R. Porter, John C. Head
-
Publication number: 20090062327Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: April 10, 2006Publication date: March 5, 2009Inventors: Chixu Chen, Brian W. Eastman, Essa H. Hu
-
Publication number: 20090062267Abstract: The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: January 29, 2008Publication date: March 5, 2009Applicant: ASTRAZENECA ABInventors: Jean-Claude Arnould, Benedicte Delouvrie, Christine Marie Paul Lambert-Van Der Brempt
-
Publication number: 20090054304Abstract: The present invention relates to compounds useful as modulators of TGR5 and methods for the treatment or prevention of metabolic, cardiovascular, and inflammatory diseases.Type: ApplicationFiled: August 8, 2008Publication date: February 26, 2009Applicant: KALYPSYS, INC.Inventors: Mark R. Herbert, Anthony B. Pinkerton, Dana L. Siegel
-
Publication number: 20090048224Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: September 5, 2008Publication date: February 19, 2009Applicants: Amgen, Inc., Array BioPharma, Inc.Inventors: Robert D. Groneberg, Benny C. Askew, JR., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
-
Patent number: 7491714Abstract: Quinoline and naphthridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.Type: GrantFiled: December 3, 2003Date of Patent: February 17, 2009Assignee: Glaxo Group LimitedInventors: Jeffrey Michael Axten, Catherine Genevieve Yvette Dartois, Guy Marguerite Marie Gerard Nadler, Neil David Pearson
-
Publication number: 20090042928Abstract: The modulator compounds described herein modulate muscarinic receptors and are useful for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: June 26, 2008Publication date: February 12, 2009Inventors: Peter D. J. Grootenhuis, Miguel Garcia-Guzman Blanco, Lewis R. Makings, Philip Martin Londo
-
Publication number: 20090029987Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.Type: ApplicationFiled: July 28, 2006Publication date: January 29, 2009Applicant: RESVERLOGIX CORP.Inventors: Norman C.W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
-
Publication number: 20090023769Abstract: Compounds of formula I in free or salt form for the preparation of a medicament for the treatment of pulmonary hypertension, where R1 and R2 have the meanings as indicated in the specification. Pharmaceutical compositions that contain the compounds are also described.Type: ApplicationFiled: January 29, 2007Publication date: January 22, 2009Inventors: Clive McCarthy, Neil John Press
-
Publication number: 20090012073Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 26, 2007Publication date: January 8, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
-
Patent number: 7473696Abstract: An efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl} cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt are provided. The succinate salt is crystalline and has superior properties.Type: GrantFiled: October 25, 2004Date of Patent: January 6, 2009Assignee: Merck & Co., Inc.Inventors: Mark Jensen, Robert Larsen, Daniel Richard Sidler
-
Patent number: 7470705Abstract: The present invention discloses compounds of formula (I) wherein A, n, q, K, W, X, Y; Z, R1, R2, R3, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and its sequelae.Type: GrantFiled: March 17, 2005Date of Patent: December 30, 2008Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Guoqing Cao, Ana Maria Escribano, Maria Carmen Fernandez, Peter Ambrose Lander, Nathan Bryan Mantlo, Eva Maria Martin de la Nava, Ana Isabel Mateo Herranz, Daniel Ray Mayhugh, Xiaodong Wang
-
Publication number: 20080318979Abstract: This invention provides potassium channel modulators which are compounds of formula I where at least one of W and Z is N; where the moiety is one of Groups A or B below A where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.Type: ApplicationFiled: June 12, 2008Publication date: December 25, 2008Applicant: VALEANT PHARMACEUTICALS INTERNATIONALInventors: Jean-Michel VERNIER, Samedy OUK, Martha A. DE LA ROSA
-
Patent number: 7468370Abstract: Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by of phosphodiesterase type 4 or the down-regulation or inhibition of TNF-? release, particularly obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: December 15, 2003Date of Patent: December 23, 2008Assignee: Novartis AGInventors: Alastair Denholm, Thomas Hugo Keller, Clive McCarthy, Neil John Press, Roger John Taylor
-
Publication number: 20080306088Abstract: Compounds of Formula I: wherein R1, R2, R3, R4 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: AstraZeneca ABInventors: Joshua Clayton, Ian Egle, James Empfield, James Folmer, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi
-
Publication number: 20080300246Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK2? 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR?, PKA, PKB?, PKD2, Rsk1, SAPK2?, SAPK2?, SAPK3, SGK, Tie2 and TrkB kinases.Type: ApplicationFiled: August 9, 2006Publication date: December 4, 2008Applicant: IRM LLCInventors: Yongping Xie, Guobao Zhang, Xing Wang, Nathanael S. Gray, Yi Liu
-
Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
-
Publication number: 20080293646Abstract: The invention relates to compounds of Formula (I): wherein R1, R2 and X are as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of Formula (I).Type: ApplicationFiled: March 12, 2008Publication date: November 27, 2008Inventors: Thomas V. Magee, Usa Reilly, Mark Carl Noe, Mark E. Flanagan, Zhengong Bryan Li, Richard Allen Buzon, Daniel William Widlicka
-
Publication number: 20080293743Abstract: The invention provides compounds of formula (I): wherein R1, R2, A, A1 and B are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.Type: ApplicationFiled: December 14, 2005Publication date: November 27, 2008Applicant: ASTRAZENECA ABInventors: Balint Gabos, Michael Lundkvist, Magnus Munck Af Rosenschold, Igor Shamovsky, Pavol Zlatoidsky
-
Patent number: 7456195Abstract: The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: GrantFiled: June 22, 2006Date of Patent: November 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Zhang, Alexandra A. Nirschl, Yan Zou, Eldon Scott Priestley
-
Patent number: 7449581Abstract: The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.Type: GrantFiled: January 9, 2007Date of Patent: November 11, 2008Assignee: Poche Palo Alto LLCInventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl
-
Patent number: 7446112Abstract: The modulator compounds described herein modulate muscarinic receptors and are useful for treating muscarinic receptor mediated diseases.Type: GrantFiled: December 7, 2004Date of Patent: November 4, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Peter D. J. Grootenhuis, Miguel Garcia-Guzman Blanco, Lewis R. Makings, Philip Martin Londo