The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
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Publication number: 20080200455Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: August 20, 2007Publication date: August 21, 2008Applicant: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Publication number: 20080200471Abstract: The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: February 19, 2008Publication date: August 21, 2008Applicant: MEMORY PHARMACEUTICALS CORPORATIONInventors: Robert Dunn, Truc Minh Nguyen, Wenge Xie, Ashok Tehim
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Patent number: 7414067Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: March 24, 2004Date of Patent: August 19, 2008Assignees: Merck & Co. Inc., Evotec OAIInventors: Edward Andrew Boyd, Michael H. Fisher, Maria L. Garcia, Gregory J. Kaczorowski, Peter T. Meinke, William H. Parsons, Stephen Price, John Stibbard
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Publication number: 20080188487Abstract: The present invention relates to compounds of formula I wherein A, G and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 28, 2008Publication date: August 7, 2008Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20080188486Abstract: The present invention relates to compounds of formula I wherein one of R1 and R2 is hydrogen and the other one is and wherein A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 23, 2008Publication date: August 7, 2008Inventors: Matthias Nettekoven, Olivier Roche
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Patent number: 7405300Abstract: The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: GrantFiled: September 1, 2004Date of Patent: July 29, 2008Assignee: Aventis Pharmaveuticals Inc.Inventors: John Z. Jiang, Jack Roger Koehl, Shujaath Mehdi, Neil David Moorcroft, Kwon Yon Musick, Philip Marvin Weintraub, Paul Robert Eastwood
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Patent number: 7396830Abstract: This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and azaindole piperazine diamide derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: GrantFiled: October 2, 2006Date of Patent: July 8, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell, Zhongxing Zhang, Zhiwei Yin, Clint A. James, Edward H. Ruediger, Bradley C. Pearce
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Publication number: 20080161320Abstract: The present invention relates to fused bicyclic pyrimidine containing zinc-binding moiety based derivatives that have unique properties as protein tyrosine kinase (PTK) inhibitors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2007Publication date: July 3, 2008Inventors: Xiong Cai, Changgeng Qian, Stephen Gould
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Publication number: 20080161323Abstract: The present invention is concerned with new indol-2-one derivatives of Formula (I), which have favourable activity profile for the prophylaxis and treatment of disorders in the central nervous or in the cadiovascular system.Type: ApplicationFiled: May 11, 2005Publication date: July 3, 2008Applicant: EGIS GYOGYSZERGYAR RT.Inventors: Balazs Volk, Jozsef Barkoczy, Gyula Simig, Tibor Mezei, Rita Kapillerne Dezsofi, Istvan Gacsalyi, Katalin Pallagi, Gabor Gigler, Gyorgy Levay, Krisztina Moricz, Csilla Leveleki, Nora Sziray, Gabor Szenasi, Andras Egyed, Laszlo Gabor Harsing
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Patent number: 7390799Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: GrantFiled: May 12, 2006Date of Patent: June 24, 2008Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Patent number: 7381726Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: GrantFiled: June 5, 2002Date of Patent: June 3, 2008Assignee: Merck Patentgesellschaft mit Beschrankter HaftungInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Publication number: 20080125590Abstract: An azulene compound is provided. The azulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. One of R1, R2, R3, R4, R5, R6, R7, and R8 in formula (I) is a moiety of formula (II). The compound can be used to treat cancer.Type: ApplicationFiled: October 31, 2007Publication date: May 29, 2008Applicant: Industrial Technology Research InstituteInventors: On Lee, Chrong-Shiong Hwang, Chih-Hung Chen, Yuan-Jang Tsai, Chih Peng Liu, Ching-Huai Ko, Hsin-Hsin Shen, Ling-Mei Wang, Kuei-Tai Lai, Ying-Chu Shih, Ting-Shou Chen, Yen-Chun Chen, Lain-Tze Lee
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Publication number: 20080119465Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.Type: ApplicationFiled: November 30, 2007Publication date: May 22, 2008Applicant: Laboratories Fournier S.A.Inventors: Luc LEBRETON, Christine Dumas, Christine Massardier, Michel Bondoux
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Patent number: 7365077Abstract: Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same.Type: GrantFiled: November 6, 2002Date of Patent: April 29, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Christopher Norbert Johnson, David John Nash, Geoffrey Stemp
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Patent number: 7351822Abstract: 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: March 18, 2004Date of Patent: April 1, 2008Assignee: 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, Peter Robert Guzzo, Michael John Mayer
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Patent number: 7342041Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: March 11, 2008Assignee: Schering CorporationInventors: F. George Njoroge, Srikanth Venkatraman, Ashok Arasappan, Francisco Velazquez, Viyyoor M. Girijavallabhan
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Patent number: 7342015Abstract: A heteroaryl derivative having the formula (I).Type: GrantFiled: June 27, 2002Date of Patent: March 11, 2008Assignee: H. Lundbeck A/SInventors: Mario Rottländer, Ejner Knud Moltzen, Ivan Mikkelsen, Thomas Ruhland, Kim Andersen, Christian Krog-Jensen
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Publication number: 20080044881Abstract: Hydroxy carboxy pyrrolyl-indolinone derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: November 26, 2004Publication date: February 21, 2008Inventor: Congxin Liang
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Patent number: 7329749Abstract: Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).Type: GrantFiled: December 24, 2001Date of Patent: February 12, 2008Assignee: Merck Patent GesellschaftInventors: Henning Boettcher, Gerd Bartoszyk, Juergen Harting, Christoph van Amsterdam, Christoph Seyfried
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Patent number: 7319098Abstract: The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein R1 is a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C1-C6 alkoxy, a C1-C6 alkyl, and a cyano group; R2 is a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C1-C6 alkyl group; and n is 1 or 2.Type: GrantFiled: November 16, 2006Date of Patent: January 15, 2008Assignee: Korea Institute of Science and TechnologyInventors: Yong Seo Cho, Hyunah Choo, Ae Nim Pae, Joo Hwan Cha, Hun Yeong Koh, Hwa-Sil Kim, Hyewhon Rhim, Seon Hee Seo
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Patent number: 7314879Abstract: The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunctionType: GrantFiled: January 21, 2003Date of Patent: January 1, 2008Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Caño Ivan Collado, Oscar De Frutos-Garcia, Christopher William Doecke, Matthew Joseph Fisher, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Jeffrey Thomas Mullaney, Paul Leslie Ornstein, Chaoyu Xie
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Patent number: 7304064Abstract: The present invention relates to 1-[(indol-3-yl)carbonyl]piperazine derivative according to the general formula I or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said 1-[(indol-3-yl)carbonyl]piperazine derivatives, and to the use of these derivatives in the treatment of pain, such as peri-operative pain, chronic pain neuropathic pain, cancer pain, and pain and spasticity associated with multiple sclerosis.Type: GrantFiled: June 13, 2003Date of Patent: December 4, 2007Assignee: N.V. OrganonInventors: Phillip Martin Cowley, Wilson Caulfield, Jason Tierney, James Cairns, Julia Adam-Worrall, Mark York
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Publication number: 20070270423Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds of the present invention are useful for the treatment and/or prevention of diseases which are associated with the modulation of histamine 3 (H3) receptors.Type: ApplicationFiled: April 26, 2007Publication date: November 22, 2007Inventors: Matthias Heinrich Nettekoven, Olivier Roche
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Patent number: 7297692Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.Type: GrantFiled: August 3, 2006Date of Patent: November 20, 2007Assignee: Sanofi-AventisInventors: Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
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Publication number: 20070259867Abstract: The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein R1 is a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C1-C6 alkoxy, a C1-C6 alkyl, and a cyano group; R2 is a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C1-C6 alkyl group; and n is 1 or 2.Type: ApplicationFiled: November 16, 2006Publication date: November 8, 2007Inventors: Yong Seo Cho, Hyunah Choo, Ae Nim Pae, Joo Hwan Cha, Hun Yeong Koh, Hwa-Sil Kim, Hyewhon Rhim, Seon Hee Seo
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Patent number: 7291619Abstract: The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: November 6, 2007Assignee: Eli Lilly and CompanyInventors: Christopher Kelly Biggers, Karin Briner, Christopher William Doecke, Matthew Joseph Fisher, Larry Wayne Hertel, Vincent Mancuso, Michael John Martinelli, John Philip Mayer, Paul Leslie Ornstein, Timothy Ivo Richardson, Jikesh Arvind Shah, Qing Shi, Zhipei Wu, Chaoyu Xie
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Publication number: 20070249624Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with 4-squarylpiperazine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: ApplicationFiled: April 19, 2007Publication date: October 25, 2007Inventors: Carol Bachand, Daniel H. Deon, Edward H. Ruediger
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Publication number: 20070244125Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: April 5, 2007Publication date: October 18, 2007Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Patent number: 7256188Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity.Type: GrantFiled: May 8, 2002Date of Patent: August 14, 2007Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Patent number: 7253172Abstract: Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitusType: GrantFiled: June 19, 2002Date of Patent: August 7, 2007Assignee: Merck & Co., Inc.Inventors: Linda Brockunier, Emma Parmee, Ann E. Weber
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Patent number: 7244846Abstract: Compounds of the formula (I), in which D, R1, R2 and n are defined in Claim 1, are potent 5-HT1A agonists and 5-HT reuptake inhibitors and are suitable for the treatment of depression, anxiety states, panic attacks, obsessive-compulsive disorders, psychiatric illnesses, cerebral infarction, cerebral ischaemia, tension states, side-effects in the treatment of high blood pressure, for the prophylaxis and therapy of cerebral illnesses, acromegaly, hypogonadism, secondary amenorrhoea, premenstrual syndrome, undesired puerperal lactation, pain, sleep disorders, narcolepsy, bipolar illnesses, mania, dementia, addiction illnesses, sexual dysfunction, eating disorders, obesity or fibromyalgiaType: GrantFiled: February 27, 2002Date of Patent: July 17, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Henning Boettcher, Christoph van Amsterdam, Wilfried Rautenberg, Gerd Bartoszyk
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Patent number: 7223765Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.Type: GrantFiled: March 15, 2006Date of Patent: May 29, 2007Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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Patent number: 7205330Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: April 17, 2007Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
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Patent number: 7189726Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.Type: GrantFiled: May 14, 2002Date of Patent: March 13, 2007Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
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Patent number: 7186724Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: April 6, 2004Date of Patent: March 6, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: James A Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Jospeh T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Fancois Sabuco, Yulin Chiang, Nicola Collar
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Patent number: 7186715Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: March 6, 2007Assignee: Eli Lilly and CompanyInventors: Karin Briner, Christopher William Doecke, Vincent Mancuso, Michael John Martinelli, Timothy Ivo Richardson, Roger Ryan Rothhaar, Qing Shi, Chaoyu Xie
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Patent number: 7169777Abstract: The present invention relates to melanocortin receptor agonist of the formula I useful in the treatment of obesity, diabetes, and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: January 30, 2007Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Karin Briner, Ivan Collado Caño, Oscar De Frutos Garcia, Christopher William Doecke, Matthew Joseph Fisher, Cristina Garcia-Paredes, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Ana Isabel Mateo Herranz, Jeffrey Thomas Mullaney, Paul Leslie Ornstein, Zhipei Wu, Chaoyu Xie
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Patent number: 7157577Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: March 8, 2004Date of Patent: January 2, 2007Assignee: Sugen Inc.Inventors: Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
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Patent number: 7157463Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: January 2, 2007Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Karin Briner, Christopher William Doecke, Matthew Joseph Fisher, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Jeffrey Thomas Mullaney, Chaoyu Xie
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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: 7141574Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; - - - - - represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7and R8 and Q are as defined herein; Y2is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all oType: GrantFiled: July 18, 2002Date of Patent: November 28, 2006Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-André Poupart, Jean Rancourt
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Patent number: 7141568Abstract: Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: July 1, 2004Date of Patent: November 28, 2006Assignee: Pfizer Italia S.r.l.Inventors: Daniele Fancelli, Barbara Forte, Jürgen Moll, Mario Varasi, Paola Vianello
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Patent number: 7135473Abstract: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH?CH, CH?N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.Type: GrantFiled: August 13, 2003Date of Patent: November 14, 2006Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
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Patent number: 7129240Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.Type: GrantFiled: April 29, 2004Date of Patent: October 31, 2006Assignee: Sanofi-AventisInventors: Richard Roux, Claudine Serradeil-le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 7119093Abstract: The present invention relates to the compound 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycabonyl-2-indolinone-monoethanesulphonate of formula I and the use thereof as a pharmaceutical compositionType: GrantFiled: July 21, 2003Date of Patent: October 10, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Gerald J. Roth, Guenter Linz, Peter Sieger, Werner Rall, Frank Hilberg, Thomas Bock
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Patent number: 7115607Abstract: Selected substituted piperazine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: July 24, 2002Date of Patent: October 3, 2006Assignee: Amgen Inc.Inventors: Christopher H. Fotsch, Premilla Arasasingham, Yunxin Bo, Ning Chen, Martin H. Goldberg, Nianhe Han, Feng-Yin Hsieh, Michael G. Kelly, Qingyian Liu, Mark H. Norman, Duncan M. Smith, Markian Stec, Nuria Tamayo, Ning Xi, Shimin Xu
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Patent number: 7109201Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: in which Ra is a group of formula (i) wherein P2 is phenyl, naphthyl, heteroaryl or a 5 to 7 membered heterocyclic ring; P3 is phenyl, naphthyl or heteroaryl; R1 is NR4COR5, NR4SO2R5, CH2NR4SO2R5, CH2NR4COR5 or CH2NR4CO2R5 where R4 and R5 are independently hydrogen or C1-6alkyl; R2 and R3 are independently halogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, COC1-6alkyl, haloC1-6alkyl, cyano or NR6R7 where R6 and R7 are independently hydrogen or C1-6alkyl; b and c are independently 0, 1, 2 or 3; Y is a single bond, CH2 or NH; W is —(CR9R10)t—where t is 2, 3 or 4 and R9 and R10 are independently hydrogen or C1-6alkyl or W is a group CH?CH; Rb is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, COC1-6alkyl, cyano or C1-6alkoxy; and Rc is hydrogen or C1-6alkyl. Processes for preparation of the compounds and their uses in therapy, particularly depression, are also disclosed.Type: GrantFiled: March 11, 2002Date of Patent: September 19, 2006Assignee: SmithKline Beecham plcInventors: Mervyn Thompson, Paul Adrian Wyman
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Patent number: 7105515Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.Type: GrantFiled: November 13, 2002Date of Patent: September 12, 2006Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 7094779Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.Type: GrantFiled: July 3, 2002Date of Patent: August 22, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Wouter I. Iwema Bakker, Jan H. van Maarseveen, Hein K. A. C. Coolen, Martinus Th. M. Tulp, Arnoldus H. J. Herremans, Andrew C. Mccreary, Gustaaf J. M. van Scharrenburg, Adrianus van den Hoogenband
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Patent number: 7087750Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.Type: GrantFiled: October 22, 2001Date of Patent: August 8, 2006Assignee: Biovitrum ABInventors: Patrizia Caldirola, Björn M. Nilsson, Gary Johansson