Ring Sulfur In The Polycyclo Ring System Patents (Class 546/202)
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Publication number: 20090042124Abstract: A resist composition includes (A) a compound represented by the following formula (I): wherein each of R1 to R13 independently represents a hydrogen atom or a substituent, provided that at least one of R1 to R13 is a substituent containing an alcoholic hydroxyl group; Z represents a single bond or a divalent linking group; and X? represents an anion containing a proton acceptor functional group.Type: ApplicationFiled: August 1, 2008Publication date: February 12, 2009Applicant: FUJIFILM CORPORATIONInventors: Sou KAMIMURA, Yasutomo KAWANISHI, Kenji WADA, Tomotaka TSUCHIMURA
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Publication number: 20090023917Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.Type: ApplicationFiled: January 18, 2005Publication date: January 22, 2009Applicant: Eli Lilly and CompanyInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
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Patent number: 7479500Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: June 1, 2005Date of Patent: January 20, 2009Assignee: WyethInventors: Michael Byron Webb, Gary Paul Stack, Magda Asselin, Deborah Ann Evrard
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Publication number: 20090018149Abstract: Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases.Type: ApplicationFiled: April 9, 2003Publication date: January 15, 2009Inventors: Andrea Missio, Gerald Bacher, Anil Koul, Axel Choidas, Peter Banhegyi, Zoltan Greff, Gyorgy Keri, Peter Marko, Laszlo Orfi, Janos Pato, Frigyes Waczek
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Publication number: 20090005375Abstract: The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula wherein the variables are as defined herein. In particular, the present invention relates to ACC1 and/or ACC2 inhibitors, compositions of matter, kits and articles of manufacture comprising these compounds, methods for inhibiting ACC1 and/or ACC2, and methods of making the inhibitors.Type: ApplicationFiled: March 21, 2008Publication date: January 1, 2009Inventors: Edcon Chang, Matthew H. McNeill
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Patent number: 7470710Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (I), wherein X represents a bond, oxygen, NR3 or a group (CH2), wherein n represents 1, 2 or 3; Y represents CH2, CO, CH(OH), or CH2CH(OH); Het is an optionally substituted bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; Ar2 represents an optionally substituted phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: June 25, 2002Date of Patent: December 30, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
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Patent number: 7468443Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.Type: GrantFiled: May 3, 2006Date of Patent: December 23, 2008Assignee: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Noboru Iwakami, Tamotsu Takamatsu
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Publication number: 20080306111Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: ApplicationFiled: August 7, 2008Publication date: December 11, 2008Inventors: John R. Carson, Scott L. Dax, Bart DeCorte, Li Liu, Mark McDonnell, James McNally
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Patent number: 7462630Abstract: The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc. comprising the compound represented by the following general formula (1) or its analogue to a patient in need of such treatment: wherein, A represents CH?CH, etc., a, b, c and d represents CH etc., R1, R2, R3, R4, R5 and R6 represents H etc., V—W represents C?C, etc., n represents 0 to 3, Y1 represents O etc., B represents —(CH2)vCHR21 wherein v is 0 to 3, R21 represents H, a lower alkyl group or the like, etc., G represents —CO—, a covalent bond, etc., m is 0 to 6, R7 and R8 represents H, a lower alkyl group, —COR18a, —COOR20 wherein R18a and R20 each represents a lower alkyl group or the like, etc.Type: GrantFiled: February 27, 2004Date of Patent: December 9, 2008Assignee: Ajinomoto Co., Inc.Inventors: Takashi Yamamoto, Seiji Niwa, Kayo Otani, Seiji Ohno, Hajime Koganei, Satoshi Iwayama, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Shinichi Fujita, Keiko Moki
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Publication number: 20080287498Abstract: Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of Ketotifen.Type: ApplicationFiled: April 30, 2007Publication date: November 20, 2008Inventors: A.K. Gunnar Aberg, George E. Wright, Jan L. Chen, Andrew T. Maioli
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Patent number: 7449481Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.Type: GrantFiled: April 12, 2005Date of Patent: November 11, 2008Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Marie-Edith Gourdel, Greg Hostetler, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet, Eric Riguet, Dominique Schweizer, Christophe Yue
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Patent number: 7449483Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: December 6, 2006Date of Patent: November 11, 2008Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
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Publication number: 20080227814Abstract: The present invention relates to a selective estrogen receptor modulator selected from the group consisting of: (I) or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.Type: ApplicationFiled: January 18, 2005Publication date: September 18, 2008Inventors: Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Owen Brendan Wallace
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Publication number: 20080207691Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.Type: ApplicationFiled: December 16, 2005Publication date: August 28, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace
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Patent number: 7375229Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe-, or —CH2—, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation, and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: February 17, 2006Date of Patent: May 20, 2008Assignee: Eli Lilly and CompanyInventor: Owen Brendan Wallace
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Patent number: 7345060Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: November 19, 2004Date of Patent: March 18, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham
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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: 7282497Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: GrantFiled: March 17, 2006Date of Patent: October 16, 2007Assignee: Glaxo Group LimitedInventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
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Patent number: 7271264Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: July 18, 2003Date of Patent: September 18, 2007Assignee: Eli Lilly and CompanyInventors: Ronald Jay Hinklin, Owen Brendan Wallace
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Patent number: 7238713Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.Type: GrantFiled: July 17, 2003Date of Patent: July 3, 2007Assignee: Acadia Pharmaceuticals, Inc.Inventors: Carl-Magnus A. Anderson, Bo Lennart M. Friberg, Niels Skjaerbaek, Tracy A. Spalding, Allan K. Uldam
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Patent number: 7226934Abstract: Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of ketotifen.Type: GrantFiled: September 12, 2000Date of Patent: June 5, 2007Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen, Andrew T. Maioli
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Patent number: 7208491Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.Type: GrantFiled: February 3, 2004Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7144883Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous systemType: GrantFiled: June 11, 2002Date of Patent: December 5, 2006Assignee: Biovitrum ABInventors: Patrizia Caldirola, Gary Johansson, Andrew Mott, Katarina Beierlien, Markus Thor, Lars Tedenborg, Ulf Bremberg, Annika Jenmalm Jensen
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Patent number: 7144898Abstract: The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.Type: GrantFiled: December 6, 2000Date of Patent: December 5, 2006Assignee: Eli Lilly and CompanyInventors: Marvin Martin Hansen, John Xiaoqiang He, Nicholas Allan Honigschmidt, Daniel James Koch, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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Patent number: 7112594Abstract: Compounds represented by the following general formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine, a derivative thereof, imidazole, a derivative thereof, etc.; the ring B represents benzene, cyclohexane, pyrrole or a derivative thereof, furan, thiophene, etc.; R1, R2 and R3 represent each hydrogen, alkyl, halogen, hydroxyl, alkoxy, etc.; W represents hydrogen, alkyl or hydroxycarbonylalkyl; X represents halogen, cyano, nitro, etc.; X? represents hydrogen, halogen, etc.; and Y represents alkyl, hydroxyalkyl, hydroxycarbonylalkyl, aminoalkyl, etc.; salt thereof, and drugs comprising these compounds. Because of having an exellent effect of inhibiting activated lymphocyte proliferation, these compounds are usefull as preventives or remedies for various autoimmune diseases.Type: GrantFiled: August 9, 2001Date of Patent: September 26, 2006Assignee: Mitsubishi Pharma CorporationInventors: Hiroyuki Ushio, Youichiro Naito, Naoki Sugiyama, Takafumi Kawaguchi, Makio Ohtsuki, Kenji Chiba
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Patent number: 7071201Abstract: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 2, 2001Date of Patent: July 4, 2006Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 7060711Abstract: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist.Type: GrantFiled: October 25, 2002Date of Patent: June 13, 2006Assignee: Biofrontera Bioscience GmbHInventors: Hermann Lubbert, Christoph Ullmer, Emile Bellott, Mark Froimowitz, Douglas Gordon
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Patent number: 6984637Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 21, 2003Date of Patent: January 10, 2006Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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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: 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: 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: 6949540Abstract: 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: September 27, 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: 6916831Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.Type: GrantFiled: February 24, 2003Date of Patent: July 12, 2005Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
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Patent number: 6908922Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions ins which endothelial dysfunction is known.Type: GrantFiled: November 12, 2002Date of Patent: June 21, 2005Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6897211Abstract: The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-?) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.Type: GrantFiled: November 18, 2002Date of Patent: May 24, 2005Assignee: Pliva-Istrazivacki Institut d.o.o.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic, Zeljko Zupanovic, Boska Hrvacic
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Patent number: 6894064Abstract: This invention provides compounds of formula I and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size range. The present invention further provides pharmaceutical compositions containing or formulated using compounds of formula I, and the use of such compounds for alleviating human pathologies, including osteoporosis, serum lipid lowering, and breast cancer.Type: GrantFiled: March 26, 2004Date of Patent: May 17, 2005Assignee: Eli Lilly and CompanyInventors: Gordon Nelson Arbuthnot, Brian Weston Dalder, Kerry John Hartauer, Wayne Douglas Luke, Robert Eugene Stratford, Jr.
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Patent number: 6878725Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: June 12, 2001Date of Patent: April 12, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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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: 6849658Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r?)(r?) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r? and r? are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of the compounds of formula (I).Type: GrantFiled: October 31, 2001Date of Patent: February 1, 2005Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Simon Trouille
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Patent number: 6844344Abstract: The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotineType: GrantFiled: December 6, 2000Date of Patent: January 18, 2005Assignee: Eli Lilly and CompanyInventors: John Xiaoqiang He, Nicholas Allan Honigschmidt, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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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: 6784180Abstract: The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.Type: GrantFiled: September 9, 2002Date of Patent: August 31, 2004Assignee: Eli Lilly and CompanyInventors: John Xiaoqiang He, Nicholas Allan Honigschmidt, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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Publication number: 20040157841Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1Type: ApplicationFiled: February 3, 2004Publication date: August 12, 2004Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 6768007Abstract: 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.Type: GrantFiled: March 13, 2002Date of Patent: July 27, 2004Assignees: Panacos Pharmaceuticals, Inc., The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Lan Xie, Graham P. Allaway, Carl T. Wild
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Patent number: 6767915Abstract: Certain novel 4-substituted piperidine compounds 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: January 27, 2003Date of Patent: July 27, 2004Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Khaled J. Barakat, Yingjie Lai, Ravi P. Nargund, Brenda L. Palucki, Min K. Park, Iyassu K. Sebhat, Zhixiong Ye, Arthur A. Patchett
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Publication number: 20040142971Abstract: Benzothiophene compounds such as 1Type: ApplicationFiled: June 6, 2002Publication date: July 22, 2004Applicant: GeneSoft, Inc.Inventors: Roland W. Burli, Eldon E. Baird, Matthew J. Taylor, Jacob A. Kaizerman, Wenhao Hu
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Patent number: 6756388Abstract: The invention is a compound of Formula (I): wherein R is —OH, R1 is —OH, R2 is —H, n is 2 or 3 and X is sulfur, or a pharmaceutically acceptable salt of a compound having Formula (1), or a pharmaceutical composition comprising a compound having Formula (1) or a pharmaceutically acceptable salt thereof, or methods of treating bone loss, breast cancer or prostate cancer comprising administering an effective amount of the compound having Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 1, 1996Date of Patent: June 29, 2004Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul Da Silva-Jardine, Eric R. Larson, James R. Hauske, Robert L. Rosati
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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