The Additional Hetero Ring Consists Of One Oxygen And Four Carbons Patents (Class 546/214)
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Publication number: 20090036439Abstract: The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.Type: ApplicationFiled: September 19, 2008Publication date: February 5, 2009Applicant: WyethInventors: Craig Eugene Caufield, Schuyler Adam Antane, Koi Michele Morris, Shaughnessy McGrath Naughton, Dominick Anthony Quagliato, Patrick Michael Andrae, Annmarie Enos, John F. Chiarello
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Publication number: 20090030041Abstract: An N-substituted N-(4-piperininyl)amide derivative represented by the following formula (I): (wherein R1 represents C1-6 alkyl, furyl, etc.; R2 represents amino, acetylamino, ureido, etc.; R3 represents hydrogen, C2-8 alkoxycarbonyl, etc.; R4 represents optionally substituted phenyl, etc.; R5 represents hydroxyl, benzyloxy, etc.; R6 represents hydrogen or methyl; and m is 1 or 2) or a salt of the derivative, and an analgesic containing the derivative or salt.Type: ApplicationFiled: September 13, 2005Publication date: January 29, 2009Inventors: Toshihiro Takahashi, Tsuyoshi Endo, Masatoshi Ushioda, Kunio Kobayashi, Tomio Yamakawa, Kiichi Shika, Toru Kawasaki, Toshiyasu Imai, Kenji Hirate, Takako Hirate
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Patent number: 7482459Abstract: The present invention extends to the compound of formula I: or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed to the use of a compound of formula I as an inhibitor of tryptase, comprising introducing the compound into a composition comprising tryptase. In addition, the present invention is directed to the use of a compound of formula I for treating a patient suffering from, or subject to, a physiological condition in need of amelioration of an inhibitor of tryptase comprising administering to the patient a therapeutically effective amount of the compound of claim 1 The present invention is directed also to the preparation of a compound of formula I.Type: GrantFiled: September 14, 2006Date of Patent: January 27, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Zhongli Gao, Larry Davis, Julian Levell, Mark Czekaj, Adam W. Sledeski
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Patent number: 7479562Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 9, 2006Date of Patent: January 20, 2009Assignee: Theravance, Inc.Inventors: Yu-Hua Ji, Craig Husfeld, Mathai Mammen, YongQi Mu, Eric L. Stangeland
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Publication number: 20080318907Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: ApplicationFiled: March 12, 2007Publication date: December 25, 2008Applicant: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Patent number: 7446195Abstract: Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.Type: GrantFiled: August 16, 2006Date of Patent: November 4, 2008Assignee: Schering CorporationInventors: Yongqi Deng, Lianyun Zhao, Gerald W. Shipps, Jr., Patrick J. Curran, M. Arshad Siddiqui, Rumin Zhang, Charles W. McNemar, Todd W. Mayhood, William T. Windsor, Emma M. Lees, David A. Parry
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Publication number: 20080269250Abstract: The invention provides compounds of formula (I) wherein the substituents are as defined in the description, processes and intermediates for their preparation and their use as pharmaceuticals.Type: ApplicationFiled: February 20, 2006Publication date: October 30, 2008Inventors: Ralf Glatthar, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
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Publication number: 20080255198Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.Type: ApplicationFiled: June 13, 2008Publication date: October 16, 2008Inventors: Chang An Chu, Paul Gillespie, Jefferson Wright Tilley
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Patent number: 7429603Abstract: The invention is directed to compounds of Formulae I, II and III: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.Type: GrantFiled: April 26, 2004Date of Patent: September 30, 2008Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Mark R. Player, Nand Baindur, Benjamin Brandt, Naresh Chadha, Raymond J. Patch, Davoud Asgari, Taxiarchis M. Georgiadis
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Patent number: 7390803Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.Type: GrantFiled: October 24, 2003Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
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Patent number: 7381721Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: March 17, 2003Date of Patent: June 3, 2008Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Publication number: 20080119488Abstract: Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: July 24, 2005Publication date: May 22, 2008Applicant: EXELIXIS, INC.Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Haixia Wang, Yinong Xie, Lynne Canne Bannen, Diva Sze-Ming Chan, Ping Huang, Vasu Jammalamadaka, Richard G. Khoury, Morrison B. Mac, Jason Jevious Parks, Yong Wang, Wei Xu
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Patent number: 7361666Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: April 11, 2002Date of Patent: April 22, 2008Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Patent number: 7358251Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 29, 2005Date of Patent: April 15, 2008Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Patent number: 7342027Abstract: Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an active ingredient, and processes for the preparation thereof.Type: GrantFiled: July 26, 2003Date of Patent: March 11, 2008Assignees: Yuhan Corporation, Dong-A Pharmaceutical Co., LtdInventors: Jong Wook Lee, Bong Yong Lee, Chun Ho Lee, Yun Hur, Tae Dong Han, Hyun Kyoung Ko, Suk Won Yun, Jae Young Shim, Joong In Lim, Moon Ho Son, Jae Sung Yang, Mi Kyung Kim
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Patent number: 7335670Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.Type: GrantFiled: April 17, 2006Date of Patent: February 26, 2008Assignee: Sanofi-AventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Maria-Carmen Renones
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Publication number: 20080045560Abstract: Compounds of the following structure are described: wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.Type: ApplicationFiled: August 13, 2007Publication date: February 21, 2008Applicant: WyethInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
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Patent number: 7326716Abstract: The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a piperidinyl prostaglandin E analog.Type: GrantFiled: November 29, 2004Date of Patent: February 5, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh, Karen M. Kedzie, Daniel W. Gil, Wha Bin Im
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Patent number: 7288657Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: October 30, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Patent number: 7205410Abstract: 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, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(?O)—R9, or -Alk-Y—C(?O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond or NR10; said R10 being hydrogen, or C1-6alkyl; R11 and RType: GrantFiled: January 29, 2003Date of Patent: April 17, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie André Bosmans, Ann Louise Gabriëlle Meulemans, Michel Anna Jozef De Cleyn, Henricus Jacobus Maria Gijsen
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Patent number: 7186719Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, cycloalkyl(C1–C6 alkyl)- or aryl(C1–C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: GrantFiled: September 30, 2004Date of Patent: March 6, 2007Assignee: British Biotech PharmaceuticalsInventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Patent number: 7125895Abstract: This invention relates to novel arylalkyl cyclic amine derivatives. This invention also relates to chemokine receptor antagonists that are be effective as therapeutic agents and/or preventive agents for diseases such as atherosclerosis, rheumatoid arthritis, transplant rejection, psoriasis, asthma, ulcerative colitis, glomerulonephritis, multiple sclerosis, pulmonary fibrosis, and myocarditis, in which tissue infiltration of blood monocytes and lymphocytes plays a major role in the initiation, progression or maintenance of the disease. Furthermore, chemokine receptor antagonists also inhibit the interaction of viruses, which attack blood monocytes and lymphocytes, through the use of a chemokine receptor. One such example is the HIV virus.Type: GrantFiled: May 12, 2000Date of Patent: October 24, 2006Assignee: Bristol-Myers Squibb Pharma Research Labs, Inc.Inventors: Christine M. Tarby, Wilna Moree
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Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
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Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
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Patent number: 7084144Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.Type: GrantFiled: May 19, 2004Date of Patent: August 1, 2006Assignee: The Jordanian Pharmaceutical MFG & Medical Equipment CO LTDInventor: Adnan Badwan
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Patent number: 7041682Abstract: Disclosed are NK1 antagonists having the formula: Also disclosed are methods for treating a number of physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough, using the compounds of formula (I).Type: GrantFiled: July 2, 2003Date of Patent: May 9, 2006Assignee: Schering CorporationInventors: Neng-Yang Shih, Steven Wang, Gregory Reichard, Dong Xiao, Cheng Wang
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Patent number: 7034110Abstract: A method for obtaining compounds having selected properties for a particular application by forming base modules having at least two structural diversity elements from the reaction of a first compound having at least one structural diversity element and a first reactive group, with a second compound having at least one structural diversity element and a second reactive group, wherein the first and second groups combine by an addition reaction; producing a first array of molecules by varying at least one of the structural diversity elements of the compounds when producing the base modules; and screening the array to determine a first suitable compound for the particular application. The base modules are preferably formed form oxazolone- and aminimide-derived compounds.Type: GrantFiled: January 23, 2004Date of Patent: April 25, 2006Assignee: ArQule, Inc.Inventor: Joseph C. Hogan, Jr.
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Patent number: 7019007Abstract: The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 27, 2002Date of Patent: March 28, 2006Assignee: Syntex (U.S.A.) LLCInventors: Daisy Joe Du Bois, Beihan Wang
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Patent number: 6995268Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: June 14, 2001Date of Patent: February 7, 2006Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Patent number: 6977263Abstract: Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.Type: GrantFiled: April 26, 2001Date of Patent: December 20, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Peter C. Astles, Paul R. Eastwood, Olivier Houille, Julian Levell, Heinz Pauls, Mark Czekaj, Guyan Liang, Yong Gong, James Pribish, Kent Neuenschwander
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Patent number: 6977260Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.Type: GrantFiled: January 22, 2004Date of Patent: December 20, 2005Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 6903120Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.Type: GrantFiled: December 22, 2000Date of Patent: June 7, 2005Assignee: A. Carlsson Research ABInventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
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Patent number: 6887870Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N. R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.Type: GrantFiled: September 25, 2000Date of Patent: May 3, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
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Patent number: 6887871Abstract: There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.Type: GrantFiled: February 20, 2001Date of Patent: May 3, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Peter Hamley, Antonio Mete, Austen Pimm
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Patent number: 6878723Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.Type: GrantFiled: April 6, 2000Date of Patent: April 12, 2005Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), BioprojetInventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
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Patent number: 6872735Abstract: The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.Type: GrantFiled: July 11, 2003Date of Patent: March 29, 2005Assignee: Genentech, Inc.Inventors: Daniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters
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Patent number: 6861530Abstract: This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.Type: GrantFiled: July 6, 2001Date of Patent: March 1, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
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Patent number: 6846825Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C4 alkenyloxy, amino, C1-C4 alkylamino, or di-(C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: GrantFiled: August 10, 2000Date of Patent: January 25, 2005Assignee: British Biotech Pharmaceuticals LimitedInventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Patent number: 6800628Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-26alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R4, —Alk—NR5R6, 1-R6-4-piperidinyl, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar—, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloaType: GrantFiled: November 19, 2002Date of Patent: October 5, 2004Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul RenĂ© Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
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Patent number: 6787650Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.Type: GrantFiled: April 5, 2002Date of Patent: September 7, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Osamu Kurasawa, Shinichi Imamura, Shohei Hashiguchi, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba
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Patent number: 6756387Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, triazolyl and thiazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: January 16, 2003Date of Patent: June 29, 2004Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Zhongyong Wei
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Patent number: 6747037Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.Type: GrantFiled: June 6, 2003Date of Patent: June 8, 2004Assignee: Allergan, Inc.Inventors: David W. Old, Thang D. Dinh
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Patent number: 6720336Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: July 10, 2001Date of Patent: April 13, 2004Assignees: Pfizer, Inc., Pfizer Products, Inc.Inventor: Spiros Liras
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Patent number: 6696443Abstract: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.Type: GrantFiled: November 20, 2001Date of Patent: February 24, 2004Assignee: Scios, Inc.Inventors: Babu Mavunkel, Sundeep Dugar, Gregory Luedtke, Xuefei Tan, Glenn McEnroe
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Patent number: 6680329Abstract: Compounds of formula [I] in which: W may represent a —(CH2)2—, —(CH2)3—, —CH2—C≡C— or —CH2—CH═CH— group, R2 may in particular represent a piperidyl group, an optionally substituted 1,2,3,6-tetrahydropyridyl group, a hexahydro-1H-azepinyl group, an optionally substituted piperazinyl group or a morpholinyl group, R3 may in particular represent a group —COR1, A may in particular represent an optionally substituted phenyl group, a heterocycle or a cyclopentyl group, and B may in particular represent a pyridyl group, an aminopyrazinyl group, an aminopyridazinyl group, a pyrimidinyl group optionally substituted with an amino group, piperidyl group or an aminopyridyl group optionally substituted on the pyridine with a (C1-C4)alkyl or (C1-C4)alkoxy group, the amino group possibly also being substituted with a (C1-C4)alkyl group, their preparation and their therapeutic application.Type: GrantFiled: September 12, 2002Date of Patent: January 20, 2004Assignee: Sanofi-SynthelaboInventors: Jean-Michel Altenburger, GĂ©rard Cremer, Gilbert Lassalle, Mostafa Matrougui
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Patent number: 6670379Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1,Type: GrantFiled: April 17, 2003Date of Patent: December 30, 2003Assignee: Novartis AGInventors: Trevor John Howe, Gurdip Bhalay, Darren Mark Le Grand, Thomas Storz
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Patent number: 6667318Abstract: The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.Type: GrantFiled: November 26, 2001Date of Patent: December 23, 2003Assignee: Genentech, Inc.Inventors: Daniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters
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Patent number: 6664273Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: November 25, 2002Date of Patent: December 16, 2003Assignee: Schering CorporationInventors: Duane A. Burnett, Wen-Lian Wu
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Patent number: 6645980Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: November 20, 2000Date of Patent: November 11, 2003Assignee: Sepracor Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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Patent number: 6638950Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 20, 2001Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng