The Additional Hetero Ring Is 1,3-diazine (including Hydrogenated) Patents (Class 540/600)
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Publication number: 20090186875Abstract: Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: February 19, 2009Publication date: July 23, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christoph HOENKE, Birgit JUNG, Domnic MARTYRES, Peter NICKOLAUS, Pascale POUZET
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Patent number: 7560450Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
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Patent number: 7557112Abstract: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.Type: GrantFiled: October 5, 2005Date of Patent: July 7, 2009Assignee: Astellas Pharma Inc.Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
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Patent number: 7544677Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: August 19, 2005Date of Patent: June 9, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Nicholas D. P. Cosford, John C. Hartnett, Yiwei Li, Jun Liang, Peter J. Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu
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Publication number: 20090137550Abstract: This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N?-substituted-N?-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-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: ApplicationFiled: March 24, 2006Publication date: May 28, 2009Inventors: Jeffrey C. Boehm, John J. Taggart
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Publication number: 20090124596Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: ApplicationFiled: January 10, 2008Publication date: May 14, 2009Inventors: Roger Victor Bonnert, Frank Burkamp, Rhona Jane Cox, Simon De Sousa, Mark Dickinson, Simon Fraser Hunt, Premji Meghani, Austen Pimm, Hitesh Jayantilal Sanganee
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Publication number: 20090124600Abstract: Compounds represented by Formula (I): and/or pharmaceutically acceptable salts, individual enantiomers and stereoisomers thereof, are effective as NMDA/NR2B antagonists useful for treating conditions such as pain, Parkinson's disease, Alzheimer's disease, epilepsy, depression, anxiety, ischemic brain injury including stroke.Type: ApplicationFiled: April 14, 2006Publication date: May 14, 2009Inventor: Mark E. Layton
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Publication number: 20090118261Abstract: The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf 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: August 26, 2005Publication date: May 7, 2009Applicant: ASTRAZENECA ABInventors: Brian Aquila, Leslie Dakin, Jayachandran Ezhuthachan, Stephen Lee, Paul Lyne, Timothy Pontz, XiaoLan Zheng
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Publication number: 20090105211Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: March 14, 2008Publication date: April 23, 2009Applicant: Exelixis, Inc.Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Publication number: 20090082336Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.Type: ApplicationFiled: November 4, 2008Publication date: March 26, 2009Inventors: Julius J. Matasi, Deen Tulshian, Duane A. Burnett, Wen-Lian Wu, Peter Korakas, Lisa S. Silverman, Thavalakulamgara K. Sasikumar, Li Qiang, Martin S. Donalski
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Publication number: 20090069298Abstract: The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc. Q is single bond, a methylene group or a group of the formula: —N(RQ)—, RQ is an alkyl group, Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), R3 and R4 are the same or different and a hydrogen atom, a cyano group etc. E is one of the following groups (i) to (v): R00 is an alkyl group, Q1 is a single bond etc., Q2 is a single bond or an alkylene group, one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., one of R50 and R60 is a hydrogen atom or an alkyl group and the other is a hydrogen atom, an alkyl group etc., R51 is an alkyl group or an optionally substituted arylsulfonyl group, R61 is an alkylamino group or an azido group, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 20, 2006Publication date: March 12, 2009Applicant: TANABE SEIYAKU CO., LTD.Inventors: Yasunori Moritani, Kimihiro Shirai, Mariko Oi
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Publication number: 20090047249Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable-salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.Type: ApplicationFiled: June 26, 2008Publication date: February 19, 2009Inventors: Micheal Graupe, Randall L. Halcomb
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Publication number: 20090029968Abstract: A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: ApplicationFiled: November 29, 2006Publication date: January 29, 2009Inventors: Bernard Christophe Barlaam, Robert Hugh Bradbury, Richard Ducray
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Publication number: 20090004185Abstract: The present invention relates to amino-substituted quinazoline derivatives as inhibitors of ?-catenin/tcf-4 pathway, which can be useful in the treatment of cancer; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.Type: ApplicationFiled: January 10, 2008Publication date: January 1, 2009Applicant: WYETHInventors: Aranapakam M. VENKATESAN, Christoph DEHNHARDT, Zecheng CHEN, Osvaldo Dos SANTOS, Efren Delos SANTOS, Kevin CURRAN, Semiramis AYRAL-KALOUSTIAN, Lei CHEN
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Publication number: 20080293697Abstract: This invention relates to compounds of formula (I).Type: ApplicationFiled: March 30, 2005Publication date: November 27, 2008Inventors: Andrew Simon Bell, David Graham Brown, David Nathan Abraham Fox, Ian Roger Marsh, Andrew Ian Morrell, Dafydd Rhys Owen, Michael John Palmer, Carol Ann Winslow, Hwang Fun Lu, Thomas Edward Rogers
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Patent number: 7456168Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4).Type: GrantFiled: April 11, 2007Date of Patent: November 25, 2008Assignee: Warner-Lambert CompanyInventors: Mark Barvian, Richard John Booth, John Quin, III, Joseph Thomas Repine, Derek J. Sheehan, Peter Laurence Toogood, Scott Norman Vanderwel, Hairong Zhou
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Publication number: 20080255095Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.Type: ApplicationFiled: June 18, 2007Publication date: October 16, 2008Applicant: BTG INTERNATIONAL LIMITEDInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
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Publication number: 20080221083Abstract: The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors.Type: ApplicationFiled: November 20, 2007Publication date: September 11, 2008Inventors: Matthias Hochgurtel, Harald Bluhm, Heiko Kroth, Michael Essers, Christian Gege, Arthur Taveras
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Publication number: 20080188454Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 28, 2007Publication date: August 7, 2008Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Thilo J. Heckrodt, Joane Litvak
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Patent number: 7393845Abstract: A heteroaryl derivative having the formula (I).Type: GrantFiled: June 5, 2007Date of Patent: July 1, 2008Assignee: H. Lundbeck A/SInventors: Mario Rottländer, Ejner Knud Moltzen, Ivan Mikkelsen, Thomas Ruhland, Kim Andersen, Christian Krog-Jensen
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Publication number: 20080119457Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein A, Q1, Q2, Q3, R31, and R41 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 24, 2007Publication date: May 22, 2008Inventors: Kenneth He Huang, John Mangette, Thomas Barta, Steven E. Hall, James Veal, Philip Hughes
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Patent number: 7326699Abstract: The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof-alone or in combination with one or more other pharmaceutically active compounds-for the treatment of a disease, especially a proliferative disease, such as a tumour disease, a method for the treatment of such diseases in mammals, especially in humans, and the use of such a compound-alone or in combination with one or more other pharmaceutically active compounds-for the preparation of a pharmaceutical composition (medicament) for the treatment especially of a proliferative disease, such as a tumour.Type: GrantFiled: May 13, 2002Date of Patent: February 5, 2008Assignee: Novartis AGInventors: Hans-Georg Capraro, Pascal Furet, Carlos Garcia-Echeverria, Paul William Manley
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Publication number: 20080004253Abstract: Certain TRPV1-modulating thiazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: June 28, 2007Publication date: January 3, 2008Inventors: Bryan James Branstetter, James Guy Breitenbucher, Alec D. Lebsack, Wei Xiao
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Patent number: 7304052Abstract: The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -{circle around (A)}- is substituted with R2 being hydrogen, hydroxy, C1-4alkyl, or C1-4alkyloxy; -a1=a2-a3=a4- represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1, C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR3, wherein R3 is hydrogen, C1-6alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl2 and optionally with hydroxy, C1-4alkylcarbonylC1-4alkyl suType: GrantFiled: December 14, 2000Date of Patent: December 4, 2007Assignee: Janssen Pharmaceuitca N.V.Inventors: Frans Eduard Janssens, Jérôme Emile Georges Guillemont, François Maria Sommen
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Patent number: 7294629Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, an optically active compound thereof, a racemate thereof or a diastereomer mixture thereof has a superior tyrosine-specific protein kinase inhibitory activity and is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of various cancers, psoriasis or diseases caused by arteriosclerosis, and the like.Type: GrantFiled: February 21, 2002Date of Patent: November 13, 2007Assignee: Mitsubishi Pharma CorporationInventors: Yasunori Kitano, Eiji Kawahara, Tsuyoshi Suzuki, Daisuke Abe, Masahiro Nakajou, Naoko Ueda
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Patent number: 7285557Abstract: A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are providedType: GrantFiled: October 15, 2002Date of Patent: October 23, 2007Assignee: SmithKline Beecham P.L.C.Inventors: Andrew J Carpenter, Joel P Cooper, Anthony L Handlon, Donald L Hertzog, Clifton E Hyman, Yu C Guo, Jason D Speake, David Richard Witty
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Publication number: 20070219183Abstract: The present invention relates to dihydropyrazolo[1,5-a]pyrimidine and dihydroimidazo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative and methods for treating or preventing cancer, comprising administering to a subject in need thereof an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative.Type: ApplicationFiled: March 15, 2007Publication date: September 20, 2007Applicant: WyethInventors: Jeremy Ian Levin, Zhong Li, Dennis Powell
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Patent number: 7265125Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.Type: GrantFiled: April 7, 2005Date of Patent: September 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Philippe Guerry, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7208489Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.Type: GrantFiled: January 28, 2005Date of Patent: April 24, 2007Assignee: Warner-Lambert CompanyInventors: Mark Barvian, Richard John Booth, John Quin, III, Joseph Thomas Repine, Derek J. Sheehan, Peter Laurence Toogood, Scott Norman Vanderwel, Hairong Zhou
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Patent number: 7192952Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesityType: GrantFiled: March 2, 2005Date of Patent: March 20, 2007Assignee: Novo Nordisk, A/SInventors: Anders Bendtz Kanstrup, Christian Klarner Sams, Jane Marie Lundbeck, Lise Brown Christiansen, Marit Kristiansen
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Patent number: 7157451Abstract: Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: GrantFiled: September 12, 2003Date of Patent: January 2, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Karnail S. Atwal, Wayne Vaccaro, John Lloyd, Heather Finlay, Lin Yan, Rao S. Bhandaru
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Patent number: 7098330Abstract: This invention describes novel pyrazole compounds of formula III: wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–8 membered carbocyclo ring; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: August 29, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M. C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert J. Davies
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Patent number: 6964957Abstract: Pyrazole compounds represented by the formula: are described. The pyrazole compounds and pharmaceutical compositions containing them may be used in inhibiting ERAB or HADH2 activity and in treating ERAB, HADH2 or amyloid-? mediated diseases and conditions.Type: GrantFiled: August 17, 2001Date of Patent: November 15, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Melwyn A. Abreo, Jerry J. Meng, Charles S. Agree
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Patent number: 6936612Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.Type: GrantFiled: January 16, 2003Date of Patent: August 30, 2005Assignee: Warner-Lambert CompanyInventors: Mark Barvian, Richard John Booth, John Quin, III, Joseph Thomas Repine, Derek J. Sheehan, Peter Laurence Toogood, Scott Norman Vanderwel, Hairong Zhou
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Patent number: 6936603Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: August 30, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Hui Cai, James P. Edwards, Steven P Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6900226Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.Type: GrantFiled: August 27, 2001Date of Patent: May 31, 2005Assignee: Hoffman-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Philippe Guerry, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 6887864Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.Type: GrantFiled: March 6, 2003Date of Patent: May 3, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher
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Patent number: 6869947Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesityType: GrantFiled: June 28, 2002Date of Patent: March 22, 2005Assignee: Novo Nordisk A/SInventors: Anders Bendtz Kanstrup, Christian Klarner Sams, Jane Marie Lundbeck, Lise Brown Christiansen, Marit Kristiansen
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Patent number: 6787554Abstract: The invention relates to triazolo[4,3-a]pyrido[2,3-d]pyrimidine-5-one derivatives, their regioisomers, their salts and their solvates if they exist, their preparation, compositions containing them and their use. These derivatives possess properties inhibiting PDE4 and/or the release of TNF&agr;, and may therefore be used for the treatment or prevention of numerous conditions by virtue of the inhibition of the PDE4 enzyme and the resulting increase in the cAMP level.Type: GrantFiled: November 22, 2002Date of Patent: September 7, 2004Assignee: Warner-Lambert LLCInventor: Bernard Gaudillière
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Publication number: 20040127483Abstract: This invention concerns compounds of formula 1Type: ApplicationFiled: September 19, 2003Publication date: July 1, 2004Applicant: Neurocrine Biosciences, Inc.Inventors: Chen Chen, Thomas R. Webb, James R. McCarthy, Terence J. Moran, Keith M. Wilcoxen, Charles Q. Huang
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Patent number: 6750214Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 4, 2003Date of Patent: June 15, 2004Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
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Publication number: 20040082569Abstract: An amide of the formula I 1Type: ApplicationFiled: October 20, 2003Publication date: April 29, 2004Applicant: Abbott GmbH & Co., KGInventors: Wilfried Lubisch, Achim Moller, Hans-Jorg Treiber, Monika Knopp
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Patent number: 6706720Abstract: Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: GrantFiled: December 5, 2000Date of Patent: March 16, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Karnail S. Atwal, Wayne Vaccaro, John Lloyd, Heather Finlay, Lin Yan, Rao S. Bhandaru
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Publication number: 20040048850Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) arc able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).Type: ApplicationFiled: September 12, 2003Publication date: March 11, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
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Publication number: 20040029859Abstract: Compounds of formula (I): 1Type: ApplicationFiled: March 12, 2003Publication date: February 12, 2004Applicant: Pfizer Inc.Inventors: Julian Blagg, Michael Jonathan Fray, Mark Llewellyn Lewis, John Paul Mathias, Mark Henryk Stefaniak, Alan Stobie
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Publication number: 20040024190Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: 1Type: ApplicationFiled: July 18, 2002Publication date: February 5, 2004Applicant: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
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Publication number: 20040019034Abstract: This invention relates to new therapeutically useful 8-(disubstituted)phenyl-6,9-dihydro-5H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-c]pyrimidine-5-one and 8-phenyl-6,9-dihydro-5H-pyrrolo[3,2-e][1,2,4]triazolo[4,3-c]pyrimidine-5-one derivatives of formula (I): wherein: —X—C—Y— represents (a) or (b) to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their medical uses as potent and selective inhibitors of phosphodiesterase 5 (PDE 5).Type: ApplicationFiled: August 15, 2003Publication date: January 29, 2004Inventors: Bernat Vidal Juan, Cristina Esteve Trias, Jordi Garcia Ferrer, Jose Manuel Prieto Soto
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Patent number: 6680314Abstract: Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cyType: GrantFiled: April 30, 2002Date of Patent: January 20, 2004Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
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Publication number: 20040006078Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: October 1, 2002Publication date: January 8, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Eugene R. Hickey, Weimin Liu, Usha R. Patel, Denice M. Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young
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Publication number: 20030229074Abstract: Melanin concentrating hormone receptor ligands (especially substituted 2-(4-benzyl-piperazin-1-ylmethyl)-1H-benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: ApplicationFiled: January 9, 2003Publication date: December 11, 2003Inventors: Robert W. DeSimone, John Peterson, Cheryl Steenstra, Yiping Shen, Linda Gustavson, Christopher Mach, Alan Hutchison