Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
-
Patent number: 7244746Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: February 4, 2004Date of Patent: July 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Han, Gene M. Dubowchik, John E. Macor
-
Patent number: 7241788Abstract: Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described hereinType: GrantFiled: May 12, 2006Date of Patent: July 10, 2007Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Robert L. Dow
-
Patent number: 7241741Abstract: The present invention provides methods for the treatment of respiratory tract mucositis in individuals in need of such treatment, the method comprising the systemic administration to the individual of therapeutically effective amounts of at least one anti-fungal agent and at least one anti-bacterial agent, wherein the treatment does not involve the cessation of use of emollients by the individual. The present invention also provides compositions suitable for use in the treatment of respiratory tract mucositis.Type: GrantFiled: July 23, 2004Date of Patent: July 10, 2007Assignee: Atopic Pty. Ltd.Inventor: Thomas J. Borody
-
Publication number: 20070154553Abstract: Provided are a gel including a compound represented by Formula 1 below and a method of preparing the same: wherein n, X, A1, and A2 are as defined in the specification.Type: ApplicationFiled: October 25, 2006Publication date: July 5, 2007Applicants: POSTECH FOUNDATION, POSTECH ACADEMY-INDUSTRY FOUNDATIONInventors: Kimoon KIM, Il Ha HWANG, Woo Sung JEON, Hee Joon KIM, Dongwoo KIM, Narayanan SELVAPALAM, Erumaipatty R. NAGARAJAN
-
Patent number: 7238699Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: February 4, 2004Date of Patent: July 3, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Bireshwar Dasgupta, Gene M. Dubowchik, John E. Macor
-
Patent number: 7230021Abstract: The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A—B, K, Q, X, Y, Z, R and R1 are as defined in Claim 1.Type: GrantFiled: March 13, 2003Date of Patent: June 12, 2007Assignee: The Texas A&M University SystemInventors: Daniel Romo, Jun Liu, Nam Song Choi, Zonggao Shi
-
Patent number: 7220757Abstract: Compounds of formula (I): are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.Type: GrantFiled: September 9, 2005Date of Patent: May 22, 2007Assignee: Replidyne, Inc.Inventors: John Berge, Andrew Forrest, Dieter Hamprecht, Richard Jarvest
-
Patent number: 7220769Abstract: A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: X represents oxygen, sulphur, or NRb; Y and Z each independently represent nitrogen, CH, CR1 or CR2; A represents an unsubstituted or substituted aryl group or an unsubstituted or substituted heterocyclyl group; Ra represents —C(O)NRsRt; R1 and R2 each independently represents hydrogen or specific substituents; and the use of such a compound in the treatment and/or prophylaxis of diseases associated with over activity of osteoclasts in mammals.Type: GrantFiled: June 14, 2004Date of Patent: May 22, 2007Assignee: Nikem Research S.R.L.Inventors: Carlo Farina, Stefania Gagliardi, Shahzad Sharooq Rahman
-
Patent number: 7211669Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: January 29, 2004Date of Patent: May 1, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta
-
Patent number: 7208629Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1–6alkyl and —(CH2)n-C3–7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1–6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitorsType: GrantFiled: October 16, 2002Date of Patent: April 24, 2007Assignee: Glaxo Group LimitedInventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, George Stuart Cockerill, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
-
Patent number: 7186740Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a] pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: September 19, 2003Date of Patent: March 6, 2007Assignee: Schering CorporationInventors: Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan
-
Patent number: 7186739Abstract: A carbamate compound is disclosed.Type: GrantFiled: March 11, 2005Date of Patent: March 6, 2007Assignee: ImmuPharma (France) SAInventors: Gilles Guichard, Marie-Christine Galas-Rodriguez, legal representative, Pierre Rodriguez, legal representative, Elisa Rodriguez, legal representative, Romain Rodriguez, legal representative, Vincent Semetey, Jean-Paul Briand, Marc Rodriguez, deceased
-
Patent number: 7173053Abstract: Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(?O) or formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(?O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1–C6) alkyl or phenyl(C1–C6)alkyl-; and R5 and R6 are as defined in the specification.Type: GrantFiled: November 8, 2001Date of Patent: February 6, 2007Assignee: British Biotech Pharmaceuticals LimitedInventors: Paul Raymond Beckett, Steven Launchbury, Gilles Pain, Lisa Marie Pratt
-
Patent number: 7169793Abstract: A process of preparation of optically pure or optically enriched isomers of omeprazole and structurally related sulfoxides is provided. Also provided are an amorphous form of esomeprazole, as well a pharmaceutical composition containing it and a method of using it for treatment of gastric disorders.Type: GrantFiled: June 27, 2003Date of Patent: January 30, 2007Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Kikkuru Srirami Reddy, Koilkonda Purandhar, Keshaboina Sreenath
-
Patent number: 7166583Abstract: The present invention relates to 1,3-diaza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumor necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: May 20, 2003Date of Patent: January 23, 2007Assignee: Pliva-Istrazivacki Institut d.o.o.Inventors: Mladen Mercep, Milan Mesic, Renata Rupcic, Dijana Pesic
-
Patent number: 7160914Abstract: Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.Type: GrantFiled: January 14, 2005Date of Patent: January 9, 2007Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: W. David Wilson, David W. Boykin, Richard R. Tidwell
-
Patent number: 7153873Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: June 6, 2006Date of Patent: December 26, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
-
Patent number: 7148215Abstract: The present invention concerns compounds of general formula (I): in which the substituents are as described herein.Type: GrantFiled: March 18, 2004Date of Patent: December 12, 2006Assignee: Aventis Pharma S.A.Inventors: Andrew James Ratcliffe, Roger John Aitchison Walsh, Tahir Nadeem Majid, Sukanthini Thurairatnam, Shelley Amendola, David John Aldous, John Edward Souness, Conception Nemecek, Sylvie Wentzler, Corinne Venot
-
Patent number: 7148234Abstract: Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.Type: GrantFiled: April 10, 2003Date of Patent: December 12, 2006Assignee: Pfizer Inc.Inventors: Masato Shimojo, Kana Taniguchi
-
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
-
Patent number: 7141598Abstract: The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula: wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.Type: GrantFiled: November 16, 2001Date of Patent: November 28, 2006Assignee: Takeda Pharmaceutical Company, Ltd.Inventors: Akihiro Tasaka, Takenori Hitaka, Nobuyuki Matsunaga, Masami Kusaka
-
Patent number: 7132439Abstract: The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.Type: GrantFiled: May 13, 2003Date of Patent: November 7, 2006Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Alan B. Fulp, Albert M. van Rhee, Kerry L. Spear
-
Patent number: 7122567Abstract: Heterocyclic amides of formula (1) wherein: Z is CH or nitrogen; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are selected from for example hydrogen, halo, C1-4alkyl, and C1-4alkanoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is —NR2R3 or —OR3; R2 and R3 are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have vaType: GrantFiled: March 4, 2003Date of Patent: October 17, 2006Assignee: AstraZeneca ABInventors: Paul Whittamore, Stuart Norman Lile Bennett, Iain Simpson
-
Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
-
Patent number: 7105513Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: July 31, 2003Date of Patent: September 12, 2006Assignee: Sanofi-Avertis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
-
Patent number: 7105550Abstract: This invention concerns the use of a compound of formula (I?) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.Type: GrantFiled: February 20, 2001Date of Patent: September 12, 2006Inventors: Christopher Love, Jean Pierre Frans Van Wauwe, Marc De Brabander, Ludwig Cooymans, Nele Vandermaesen, Ludo Edmond Josephine Kennis
-
Patent number: 7057042Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1 are as described in the specification.Type: GrantFiled: May 23, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Steven P. Latshaw, Sherry L. Nelson, Andrew O. Stewart
-
Patent number: 7041303Abstract: A method of treating myocardial damage secondary to myocardial infarction using moxonidine or a physiologically compatible salt thereof. Pharmaceutical preparations containing moxonidine and its physiologically compatible acid addition salts are suitable for use in acute myocardial infarction and/or postmyocardial infarction management. In addition to a beneficial influence, promoting recovery and/or rehabilitation, on the myocardial status following myocardial infarction, moxonidine and its physiologically compatible acid addition salts, especially when used in the management of postmyocardial infarction patients in the chronic stage, also show a preventive effect against the progression of heart failure after myocardial infarction.Type: GrantFiled: July 31, 2001Date of Patent: May 9, 2006Assignee: Solvay Pharmaceuticals GmbHInventor: Regina Geertruida Schoemaker
-
Patent number: 7034034Abstract: Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.Type: GrantFiled: October 21, 2002Date of Patent: April 25, 2006Assignee: Neurogen CorporationInventors: Charles A. Blum, Harry L. Brielmann, Stephane De Lombaert, Xiaozhang Zheng
-
Patent number: 7030149Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.Type: GrantFiled: April 19, 2002Date of Patent: April 18, 2006Assignee: Allergan, Inc.Inventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
-
Patent number: 7030139Abstract: Compounds of general formula (I), 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 painType: GrantFiled: April 18, 2002Date of Patent: April 18, 2006Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Miroslaw Tomaszewski, Christopher Walpole, Hua Yang
-
Patent number: 7022728Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.Type: GrantFiled: March 8, 2002Date of Patent: April 4, 2006Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Pramila A. Bhatia, Jerome F. Daanen, Andrew O. Stewart, Meena V. Patel, Teodozyj Kolasa, Jorge D. Brioni, Jeffrey Rohde
-
Patent number: 7012087Abstract: The therapeutic use of temporary p53 inhibitors in the treatment of p53-mediated diseases, conditions, and injuries is disclosed.Type: GrantFiled: June 13, 2001Date of Patent: March 14, 2006Assignee: The Board of Trustees of the University of IllinoisInventors: Andrei V. Gudkov, Pavel G. Komarov, Elena A. Komarova
-
Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
-
Patent number: 6956050Abstract: This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents a hydrogen atom, an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.Type: GrantFiled: April 9, 2003Date of Patent: October 18, 2005Assignee: Pfizer, Inc.Inventors: Misato Hirano, Satoru Iguchi, Kazunari Nakao, Tatsuya Yamagishi
-
Patent number: 6943175Abstract: Compounds of formula (I): are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.Type: GrantFiled: December 5, 2003Date of Patent: September 13, 2005Assignee: Replidyne, Inc.Inventors: John Berge, Andrew Forrest, Dieter Hamprecht, Richard Jarvest
-
Patent number: 6943149Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.Type: GrantFiled: March 17, 2003Date of Patent: September 13, 2005Assignees: Ortho McNeil Pharmaceutical, Inc., Millennium Pharmaceuticals, Inc.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly B. White
-
Patent number: 6936613Abstract: The present invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.Type: GrantFiled: July 15, 2003Date of Patent: August 30, 2005Assignee: Neurosearch A/SInventors: Lene Teuber, Frank Watjen
-
Patent number: 6936631Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, wherein X denotes CR5, N or S, and Y in the case where X denotes S, denotes CR6 or N and in all other cases denotes N, and methods for preparation thereof are disclosed. Also disclosed are methods for treating pain using the compound of Formula I, and pharmaceutical compositions comprising the compound of Formula I.Type: GrantFiled: August 5, 2003Date of Patent: August 30, 2005Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
-
Patent number: 6933295Abstract: The invention relates to the field of blood clotting, to novel compounds of formula (I), to a method for their production and to the use of these compounds as active ingredients in medicaments for preventing and/or treating diseases. The compounds are factor Xa inhibitors.Type: GrantFiled: July 3, 2002Date of Patent: August 23, 2005Assignee: Bayer AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Stephan Jordan, Elisabeth Perzborn, Karl-Heinz Schlemmer
-
Patent number: 6927217Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.Type: GrantFiled: October 16, 2002Date of Patent: August 9, 2005Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
-
Patent number: 6916827Abstract: Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).Type: GrantFiled: May 15, 2003Date of Patent: July 12, 2005Assignee: Neurogen CorporationInventors: George D. Maynard, Jun Yuan, George P. Luke, Kevin Currie
-
Patent number: 6911462Abstract: This invention relates to a family of phenylbenzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.Type: GrantFiled: March 20, 2002Date of Patent: June 28, 2005Assignee: Avanir PharmaceuticalsInventors: Jagadish C. Sircar, Mark L. Richards, Michael G. Campbell, Michael W. Major
-
Patent number: 6900216Abstract: The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds including pharmaceutically acceptable salts thereof which have an affinity for 5-HT1A receptors and which inhibit neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses including schizophrenia, tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snaking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemiaType: GrantFiled: March 10, 2001Date of Patent: May 31, 2005Assignee: Knoll GmbHInventors: Kevin James Doyle, Frank Kerrigan, John Paul Watts
-
Patent number: 6897208Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.Type: GrantFiled: October 24, 2002Date of Patent: May 24, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael L. Edwards, Paul J. Cox, Shelley Amendola, Stephanie D. Deprets, Timothy A. Gillespy, Christopher D. Edlin, Andrew D. Morley, Charles J. Gardner, Brian Pedgrift, Herve Bouchard, Didier Babin, Laurence Gauzy, Alain Le-Brun, Tahir N. Majid, John C. Reader, Lloyd J. Payne, Nawaz M. Khan, Michael Cherry
-
Patent number: 6894068Abstract: The present invention provides compositions and methods for the treatment of HIV infection. In particular, the present invention provides non-nucleoside inhibitors of reverse transcriptase (RT), as well as methods to treat HIV infection using these non-nucleoside inhibitors of RT. In preferred embodiments, the present invention provides a novel class of substituted benzimidazoles, effective in the inhibition of human immunodeficiency virus (HIV) RT.Type: GrantFiled: April 9, 2002Date of Patent: May 17, 2005Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Christopher J. Michejda, Marshall Morningstar, Thomas Roth
-
Patent number: 6888004Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Gene M. Dubowchik, Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta, John E. Macor
-
Patent number: 6884811Abstract: An antifungal composition comprising 3-iodo-2-propynyl butylcarbamate, 4,5-dichloro-2-octyl-isothiazolin-3-one and methyl 2-benzimidazolylcarbamate is useful as industrial antifungal composition, particularly for wood protection.Type: GrantFiled: August 30, 2002Date of Patent: April 26, 2005Assignee: Shinto Fine Co., Ltd.Inventor: Kazuhide Fujimoto
-
Patent number: 6861434Abstract: Compounds of the formula: useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: March 1, 2005Assignee: WyethInventor: Gary P. Stack
-
Patent number: 6858630Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted naphthimidazole derivative.Type: GrantFiled: December 6, 2000Date of Patent: February 22, 2005Assignee: SmithKline Beecham CorporationInventors: Juan I. Luengo, Kevin J. Duffy, Alan T. Price, Lihua Zhang