Plural Hetero Atoms In The Additional Hetero Ring Patents (Class 540/603)
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Patent number: 7151175Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.Type: GrantFiled: March 21, 2005Date of Patent: December 19, 2006Assignee: N-Gene Research Laboratories Inc.Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
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Patent number: 7125877Abstract: This invention provides compounds which are represented by a general formula [I] [in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands for a 3–10 membered aliphatic nitrogen-containing heterocyclic group; R3, R4 and R5 may be same or different, and each stands for hydrogen, lower alkyl optionally having substituent group(s) and the like; and a is 0 or 1]. These compounds exhibit high affinity to nociceptin receptors and whereby inhibit actions of nociceptin, and are useful as an analgesic, antiobestic, agent for ameliorating brain function, treating agents for Alzheimer's disease and dementia, and therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like.Type: GrantFiled: May 14, 2003Date of Patent: October 24, 2006Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kensuke Kobayashi, Hirobumi Takahashi, Hiroshi Kawamoto, Tetsuya Kato, Satoru Itoh, Takashi Yoshizumi, Osamu Okamoto
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7087593Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.Type: GrantFiled: September 30, 2002Date of Patent: August 8, 2006Assignee: ACADIA Pharmaceuticals Inc.Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
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Patent number: 7071182Abstract: The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.Type: GrantFiled: December 22, 2004Date of Patent: July 4, 2006Assignee: Abbott LaboratoriesInventors: Andrew J. Souers, Christine A. Collins, Ju Gao, Andrew S. Judd, Philip R. Kym, Mathew M. Mulhern, Hing L. Sham, Dariusz Wodka
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Patent number: 7071184Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Patent number: 7049307Abstract: The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.Type: GrantFiled: December 22, 2004Date of Patent: May 23, 2006Assignee: Abbott LaboratoriesInventors: Andrew J. Souers, Christine A. Collins, Ju Gao, Andrew S. Judd, Philip R. Kym, Mathew M. Mulhern, Hing L. Sham, Dariusz Wodka
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Patent number: 7034029Abstract: 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 receptorType: GrantFiled: January 16, 2004Date of Patent: April 25, 2006Assignee: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Patent number: 7030150Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.Type: GrantFiled: May 9, 2002Date of Patent: April 18, 2006Assignee: Trimeris, Inc.Inventors: John William Lackey, Daniel S Kinder, Nicolai A Tvermoes
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Patent number: 7008957Abstract: The invention relates to compounds of the formula I in which the radicals have the stated meanings, their stereoisomeric forms and their physiologically tolerated salts and process for their preparation. The compounds are suitable for the treatment of metabohlic disorders such as type 2 diabetes.Type: GrantFiled: July 26, 2004Date of Patent: March 7, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Holger Wagner, Karl Schoenafinger, Gerhard Jaehne, Holger Gaul, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7001901Abstract: This invention relates to novel tetrazolyl-propionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby resulting in prevention and treatment of the neuropathology associated with production of A?-peptide. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease.Type: GrantFiled: August 27, 2003Date of Patent: February 21, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Michael G. Yang
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Patent number: 6982259Abstract: N-Heterocyclic derivatives of the following formula: where m, n, p, A1, R1, R2, R3 and R4 are described herein, as well as other N-heterocyclic derivatives, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: April 23, 2003Date of Patent: January 3, 2006Assignee: Schering AktiengesellschaftInventors: David D. Davey, Raju Mohan, Gary B. Phillips, Guo Ping Wei, Wei Xu
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Patent number: 6953793Abstract: 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: August 10, 2001Date of Patent: October 11, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Christopher R. Butler, Hui Cai, James P. Edwards, Cheryl A. Grice, Darin J. Gustin, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Clark A. Sehon, Kevin L. Tays, Jianmei Wei
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Patent number: 6919329Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: GrantFiled: February 24, 2003Date of Patent: July 19, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh
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Patent number: 6906090Abstract: The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.Type: GrantFiled: March 4, 1999Date of Patent: June 14, 2005Assignee: AstraZeneca ABInventor: Ramachandran Janakiraman
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Patent number: 6887865Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: April 12, 2002Date of Patent: May 3, 2005Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6887864Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.Type: GrantFiled: March 6, 2003Date of Patent: May 3, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher
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Patent number: 6861432Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.Type: GrantFiled: November 22, 2002Date of Patent: March 1, 2005Assignee: Schering AktiengesellschaftInventors: Arwed Cleve, Christoph Huwe, Volker Schulze, Helmut Morack, Dieter Zopf, Jens Hoffmann, Andreas Reichel
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Patent number: 6833375Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: September 10, 2002Date of Patent: December 21, 2004Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Publication number: 20040254164Abstract: Compounds according to formula (I) wherein n is 0-3, R′ is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from hydrogen and optionally substituted C1-6 alkyl, or R5 and R8 are an alkylene chain, are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.Type: ApplicationFiled: March 29, 2004Publication date: December 16, 2004Applicant: Pfizer Inc.Inventors: Charlotte Moira Norfor Allerton, David John Bull, Mark Edward Bunnage, Robert John Maguire, John Steele
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Patent number: 6828315Abstract: The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives.Type: GrantFiled: October 25, 2001Date of Patent: December 7, 2004Assignee: Warner-Lambert LLCInventors: Bernard Gaudilliere, Remi Lavalette, Charles Andrianjara, Francine Breuzard
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Publication number: 20040242563Abstract: The present invention provides substituted 3,3-phenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.Type: ApplicationFiled: June 1, 2004Publication date: December 2, 2004Applicants: Children's Medical Center Corporation, President and Fellows of Harvard College, Nuchem Pharmaceuticals Inc.Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Publication number: 20040235824Abstract: The present invention relates to a compound of the formula I 1Type: ApplicationFiled: May 19, 2004Publication date: November 25, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, Volker Laux, Matthias Urmann, Armin Bauer, Hans Matter
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Publication number: 20040220170Abstract: Compounds of the present invention modulate PN3 in mammals and are useful in treating pain in mammals.Type: ApplicationFiled: May 1, 2003Publication date: November 4, 2004Inventors: Robert N. Atkinson, Irene Drizin, Robert J. Gregg, Michael F. Gross, Michael E. Kort, Lei Shi
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Publication number: 20040214816Abstract: This invention relates to substituted imidazoles of Formula I 1Type: ApplicationFiled: October 17, 2001Publication date: October 28, 2004Inventors: Scott Beers, Michael P. Wachter
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Publication number: 20040192667Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: ApplicationFiled: March 1, 2004Publication date: September 30, 2004Applicant: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally
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Publication number: 20040167121Abstract: The present invention provides compounds of formula I: 1Type: ApplicationFiled: October 27, 2003Publication date: August 26, 2004Inventors: Alex Aronov, David J. Lauffer, Huan Qui Li, Ronald Charles Tomlinson, Pan Li
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Patent number: 6767912Abstract: 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: GrantFiled: December 20, 2001Date of Patent: July 27, 2004Assignee: WyethInventors: Ping Zhou, Derek Cecil Cole, Michael Gerard Kelly, William Joseph Lennox
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Publication number: 20040127484Abstract: Benzotriazoles of formula I 1Type: ApplicationFiled: October 14, 2003Publication date: July 1, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Stefan Petry, Karl-Heinz Baringhaus, Norbert Tennagels, Guenter Mueller, Hubert Heuer
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Publication number: 20040110736Abstract: The present application describes modulators of MCP-1 of formula (I): 1Type: ApplicationFiled: November 12, 2003Publication date: June 10, 2004Inventor: Robert Cherney
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Publication number: 20040082568Abstract: This invention relates to novel tetrazolylpropionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I): 1Type: ApplicationFiled: August 27, 2003Publication date: April 29, 2004Inventor: Michael G. Yang
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Publication number: 20040082563Abstract: Novel compounds of the formula (I) formula (I) in which W, E, X, Y, T, R1, R2, R2′, and R2″ are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.Type: ApplicationFiled: September 16, 2003Publication date: April 29, 2004Inventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20040063691Abstract: This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.Type: ApplicationFiled: September 24, 2002Publication date: April 1, 2004Inventors: Roger A. Smith, Stephen J. O'Connor, Stephan-Nicholas Wirtz, Wai C. Wong, Soongyu Choi, Harold C.E. Kluender, Ning Su, Gan Wang, Furahi Achebe, Shihong Ying
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Publication number: 20040048844Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): 1Type: ApplicationFiled: May 1, 2003Publication date: March 11, 2004Applicant: Bristol-Myers Squibb Pharma CompanyInventors: David Nugiel, David Carini, Susan DiMeo, Anup Vidwans, Eddy Yue
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Patent number: 6696437Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.Type: GrantFiled: March 25, 2002Date of Patent: February 24, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Uta Holzenkamp, Sabine Schult, Reinhold Mueller
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Publication number: 20040034008Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: June 30, 2003Publication date: February 19, 2004Applicant: Schering CorporationInventors: Andrew W. Stamford, Yusheng Wu
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Publication number: 20040023950Abstract: N-Heterocyclic derivatives of the following formula: 1Type: ApplicationFiled: April 23, 2003Publication date: February 5, 2004Applicant: Schering AktiengesellschaftInventors: David D. Davey, Raju Mohan, Gary B. Phillips, Guo Ping Wei, Wei Xu
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Publication number: 20040014741Abstract: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.Type: ApplicationFiled: October 26, 2001Publication date: January 22, 2004Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
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Patent number: 6680314Abstract: Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cyType: GrantFiled: April 30, 2002Date of Patent: January 20, 2004Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
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Patent number: 6667303Abstract: Aryl substituted 1,4-diazepanes are provided such as derivatives of 6-(1,4-diazepan-1-yl)benzo[cd]indol-2(1H)-one, 6-(1,4-diazepan-1-yl)acenaphthylen-1(2H)-one and 5-(1,4-diazepan-1-yl)-2H-naphtho[1,8-cd]isothiazole-1,1-dioxide. Also provided are pharmaceutical compositions containing one or more of the aryl substituted 1,4-diazepanes. The aryl substituted 1,4-diazepanes are useful for treating disorders or deficiencies associated with the 5-HT2C receptor.Type: GrantFiled: July 30, 2002Date of Patent: December 23, 2003Assignee: WyethInventors: Yansong Gu, Jeffrey Claude Pelletier
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Publication number: 20030229076Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: September 16, 2002Publication date: December 11, 2003Inventors: Stanislaw Rachwal, Alan Hutchison, Kenneth Shaw, George D. Maynard, Xiao-Shu He, Robert DeSimone, Kevin Hodgetts
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Publication number: 20030229075Abstract: 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: ApplicationFiled: March 28, 2003Publication date: December 11, 2003Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Publication number: 20030220319Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: 1Type: ApplicationFiled: January 31, 2003Publication date: November 27, 2003Inventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
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Publication number: 20030191107Abstract: Compounds according to formula (I) wherein n is 1-4, R1 is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7 and R8 are each independently selected from hydrogen and optionally substituted C1-6 alkyl are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.Type: ApplicationFiled: January 22, 2003Publication date: October 9, 2003Applicant: Pfizer Inc.Inventors: Charlotte Moira Norfor Allerton, Mark Edward Bunnage, John Steele
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Patent number: 6627626Abstract: The present invention relates to 5-heterocyclo-pyrazoles of the formula I: wherein ring W, m, n, and R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: September 30, 2003Assignee: Pfizer Inc.Inventors: Martha L. Minich, Subas M. Sakya
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Patent number: 6627624Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.Type: GrantFiled: March 31, 2000Date of Patent: September 30, 2003Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, Daniel L. Rosewater
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Publication number: 20030162771Abstract: The present invention relates to compounds of formula: 1Type: ApplicationFiled: June 12, 2002Publication date: August 28, 2003Inventors: Michel Geslin, Danielle Gully, Jean-Pierre Maffrand, Pierre Roger
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Publication number: 20030134801Abstract: The present invention relates to a compound having formula I: 1Type: ApplicationFiled: November 1, 2002Publication date: July 17, 2003Applicant: LG Life Sciences, Ltd.Inventors: Koo Lee, Won Hyuk Jung, Cheol Won Park, Sang Koo Lee, Sun Hwa Lee, Hee Dong Park
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Publication number: 20030114508Abstract: This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof.Type: ApplicationFiled: July 1, 2002Publication date: June 19, 2003Inventors: Akira Matsuhisa, Isao Kinoyama, Akira Toyoshima, Takahito Nakahara, Masahiro Takeuchi, Minoru Okada
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Publication number: 20030100545Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.Type: ApplicationFiled: September 30, 2002Publication date: May 29, 2003Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf