The Additional Hetero Ring Consists Of One Sulfur And Four Carbons Patents (Class 546/212)
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Patent number: 7521462Abstract: The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.Type: GrantFiled: February 11, 2005Date of Patent: April 21, 2009Assignee: Eli Lilly and CompanyInventors: Serge Louis Boulet, Barry Peter Clark, John Fairhurst, Peter Thaddeus Gallagher, Anette Margareta Johansson, Maria Ann Whatton, Virginia Ann Wood
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Publication number: 20090082401Abstract: The present application describes deuterium-enriched tiagabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 18, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7491821Abstract: Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genitourinary, gastrointestinal, and respiratory disorders: wherein R1 is —C(?S)CH3, pyridyl, pyrimidinyl, pyrazinyl, thiazolyl, furyl, furylcarbonyl, acetyl, or carbamoyl; R2a and R2b are independently H, methyl, or ethyl; R3 is H or methyl; Y is a bond, —(CR4R5)n— or —CR4?CR5—; wherein R4 and R5 are each independently H or methyl and n is 1 or 2; X is N or CH; A is phenyl, 5-membered heterocyclyl, or 6-membered heterocyclyl; R6, R7 and R8 are each independently H, halo, lower alkyl, cycloalkyl, alkylthio, alkylthio-lower alkyl, alkylsulfonyl-lower alkyl, di(lower alkyl)amino-lower alkyl, morpholinyl-lower alkyl, 4-methyl-piperazinyl-methyl, trifluoromethyl, pyridyl, tetrazolyl, thiophenyl, phenyl, biphenyl, or benzyl (where thiophenyl, phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoromethyl, lower alkoxy or lower alkylthio) or R6 and R7 together form a 5-membered or 6-membered carbocyclType: GrantFiled: August 11, 2006Date of Patent: February 17, 2009Assignee: Roche Palo Alto LLCInventors: Christine E. Brotherton-Pleiss, Michael Patrick Dillon, Shelley K. Gleason, Clara Jeou Jen Lin, Ryan Craig Schoenfeld, Marzia Villa, Yansheng Zhai
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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: 20080269495Abstract: A process for preparing pure tiagabine, which is a piperidine carboxylic acid compound, via pharmaceutically acceptable salts of tiagabine ester is provided. Also, L(+) tartaric acid, oxalic acid and dibenzoyl L(+) tartaric acid salts of tiagabine esters are provided. Further, process for preparing acid addition salts of tiagabine esters is provided.Type: ApplicationFiled: August 4, 2005Publication date: October 30, 2008Inventors: Prosenjit Bose, Pramod Kumar, Shilpi Mittal, Yatendra Kumar
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Patent number: 7423052Abstract: A invention relates to N aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: June 25, 2002Date of Patent: September 9, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter
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Patent number: 7417058Abstract: The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3?, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.Type: GrantFiled: September 27, 2001Date of Patent: August 26, 2008Assignee: Laboratoires Serono S.A.Inventors: Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
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Publication number: 20080167346Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.Type: ApplicationFiled: November 15, 2007Publication date: July 10, 2008Applicant: SANOFI-AVENTISInventors: Michael WAGNER, Matthias URMANN, Volkmar WEHNER, Martin LORENZ, Armin BAUER, Marc NAZARE, Hans MATTER
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Patent number: 7348341Abstract: The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity.Type: GrantFiled: May 30, 2001Date of Patent: March 25, 2008Assignee: AstraZeneca ABInventors: Hitesh Sanganee, Brian Springthorpe
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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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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: 7276607Abstract: Substituted carbocyclic sulphonamide derivatives of formula (I), in which n is 0 or 1 and the other variables are as defined in the claims, are selective 5-HT7 receptor antagonists and are thereby effective in the treatment of a variety of neurological conditions, including depression and sleep disorders.Type: GrantFiled: November 29, 2002Date of Patent: October 2, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Neil Roy Curtis, Peter Alan Hunt, Janusz Jozef Kulagowski
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7223780Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.Type: GrantFiled: May 19, 2004Date of Patent: May 29, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volker Laux, Armin Bauer, Michael Wagner
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Patent number: 7217823Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.Type: GrantFiled: November 25, 2003Date of Patent: May 15, 2007Assignee: Sepracor Inc.Inventor: Michael Z. Hoemann
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Patent number: 7122675Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.Type: GrantFiled: August 1, 2002Date of Patent: October 17, 2006Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
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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: 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: 7022716Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: December 27, 2002Date of Patent: April 4, 2006Assignee: WyethInventors: Baihua Hu, Fuk-Wah Sum, Michael Sotirios Malamas
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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: 7015235Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 21, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner, Zhixiong Ye, Jonathan R. Young, Raman K. Bakshi
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Patent number: 7012084Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 14, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
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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: 6977265Abstract: The invention provides compounds of Formula (I): wherein: R1-R5, A, L, and X 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 29, 2002Date of Patent: December 20, 2005Assignee: Roche Palo Alto LLCInventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
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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: 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: 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: 6864249Abstract: The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagulants.Type: GrantFiled: November 1, 2002Date of Patent: March 8, 2005Assignee: LG Life Sciences, Ltd.Inventors: Koo Lee, Won Hyuk Jung, Cheol Won Park, Sang Koo Lee, Sun Hwa Lee, Hee Dong Park
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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: 6828318Abstract: Compounds of formula (1): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3,4,5,6,7 or 8-membered ring containing 0,1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups; and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, are useful for treating conditions generally associated with abnormalities in glutamatergic transmission.Type: GrantFiled: March 31, 2003Date of Patent: December 7, 2004Assignee: Vernalis Research LimitedInventors: Michael Frederick Snape, Roger John Gillespie, Claire Elizabeth Dawson, Steven Michael McAteer, Suneel Gaur
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Patent number: 6825217Abstract: Compositions and methods are provided for treating neuropathic pain or neuropathic dysfunction that include the administration of an effective amount of a defined carbinol or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: October 16, 2002Date of Patent: November 30, 2004Assignee: Endo Pharmaceuticals, Inc.Inventors: Richard Carliss, David A. H. Lee
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Publication number: 20040235897Abstract: Compounds of general formula I 1Type: ApplicationFiled: November 13, 2003Publication date: November 25, 2004Inventors: William Brown, Andrew Griffin, Christopher Walpole
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Publication number: 20040220223Abstract: Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK3 receptor antagonists.Type: ApplicationFiled: March 22, 2004Publication date: November 4, 2004Inventors: Daniel Bichon, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Publication number: 20040198742Abstract: Substituted 3-(benzoylureido)thiophene derivatives, processes for preparing them and their useType: ApplicationFiled: February 17, 2004Publication date: October 7, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Karl Schoenafinger, Elisabeth Defossa, Erich Von Roedern, Dieter Kadereit, Andreas Herling, Hans-Joerg Burger, Thomas Klabunde, Karl-Ulrich Wendt
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Patent number: 6784173Abstract: Compounds of formula I wherein A, R1 and R2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.Type: GrantFiled: June 11, 2002Date of Patent: August 31, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Ulrike Leser-Reiff, Tim Sattelkau, Gerd Zimmermann
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Publication number: 20040152734Abstract: Substituted C-furan-2-yl-methylamine and C-thiophen-2-yl-methylamine compounds, processes for their preparation, medicaments and pharmaceutical compositions containing them, and their use in treatment methods and in the preparation of analgesics, in the preparation of a local anaesthetic, an antiarrhythmic, an antiemetic, a nootropic agent and/or a medicament for the treatment and/or prophylaxis of cardiovascular diseases, urinary incontinence, diarrhea, pruritus and/or inflammations, and/or a medicament for the treatment of depression and/or alcohol and/or drug and/or medicament abuse, and/or a medicament for increasing vigilance.Type: ApplicationFiled: November 21, 2003Publication date: August 5, 2004Applicant: Gruenenthal GmbHInventors: Corrina Sundermann, Michael Przewosny
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Publication number: 20040147556Abstract: Compounds of general formula I: R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl and pyridine N-oxide; 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-C?6? 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; arc 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, anxiety and functional gastrointestinal disorders.Type: ApplicationFiled: November 13, 2003Publication date: July 29, 2004Inventors: William Brown, Christopher Walpole, Zhongyong Wei
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Publication number: 20040142966Abstract: Compounds of general formula I[Chemical formula should be inserted here. Please see paper copy] R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; 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-C6alkyl, NO2, CF3, C1-C6alkoxy, 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, anxiety and functional gastrointestinal disorders.Type: ApplicationFiled: November 13, 2003Publication date: July 22, 2004Inventors: William Brown, Andrew Griffin, Christopher Walpole
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Publication number: 20040142965Abstract: Compounds of general formula I [Chemical formula should be inserted here. Please see paper copy] R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; 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-C6alkyl, NO2, CF3, C1-C6alkoxy, 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, anxiety or functional gastrointestinal disorders.Type: ApplicationFiled: November 13, 2003Publication date: July 22, 2004Inventors: William Brown, Andrew Griffin, Christopher Walpole
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Publication number: 20040142967Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, pyrroloyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl and pyridine N-oxide; 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, anxiety and functional gastrointestinal disorders.Type: ApplicationFiled: November 13, 2003Publication date: July 22, 2004Inventors: Zhongyong Wei, William Brown, Christopher Walpole
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Publication number: 20040138259Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl, and pyridine N-oxide; 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, anxiety, and functional gastrointestinal disorders.Type: ApplicationFiled: November 13, 2003Publication date: July 15, 2004Inventors: William Brown, Christopher Walpole, Zhongyong Wei
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Publication number: 20040122234Abstract: This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.Type: ApplicationFiled: June 3, 2003Publication date: June 24, 2004Inventors: Kenneth Lee Hauser, Jeffrey Alan Dodge, Mark Louis Heiman, Scott Alan Jones, Charles Arthur Alt, Henry Uhlman Bryant, Jeffrey Daniel Cohen, James Densmore Copp, Kennan Joseph Fahey, William Harlan Gritton, Louis Nickolaus Jungheim, Joseph Henry Kennedy, Charles Willis Lugar, Brian Stephen Muehl, Alan David Palkowitz, Andrew Michael Ratz, Gary Anthony Rhodes, Roger Lewis Robey, David Edward Seyler, Timothy Alan Shepherd, Kenneth Jeff Thrasher, William George Trankle
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Patent number: 6753337Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: December 21, 2001Date of Patent: June 22, 2004Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Patent number: 6750231Abstract: There is provided a compound of formula I, wherein Het1, R1, R2, R3, X and n have meanings given in the description, which are useful in the prophylaxis and in the treatment of diseases mediated by opiate receptors, such as pruritus.Type: GrantFiled: March 19, 2002Date of Patent: June 15, 2004Assignee: Pfizer IncInventors: Stephen Paul Gibson, Ivan Tommasini, Kimberley Verrier, Christopher James Dutton, David Morris Gethin, Douglas James Critcher, Richard Edward Armer
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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: 6740647Abstract: Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.Type: GrantFiled: June 21, 2000Date of Patent: May 25, 2004Assignee: Abbott GmbH & Co., KGInventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Hans Wolfgang Höffken, Wilfried Hornberger