Ring Nitrogen In The Polycyclo Ring System Patents (Class 546/200)
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Patent number: 7423058Abstract: 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: December 21, 2006Date of Patent: September 9, 2008Assignee: 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: 7419989Abstract: The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: December 21, 2005Date of Patent: September 2, 2008Assignee: Theravance, Inc.Inventors: Paul Fatheree, Roland Gendron, Adam A Goldblum, Daniel D Long, Daniel Marquess, S. Derek Turner, Seok-Ki Choi
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Publication number: 20080188478Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents a group selected from H, CF3, and C1-6 alkyl (optionally substituted by C1-6 alkyloxy or triazolyl); R2 represents halo; Ring A represents a 5- or 6-membered heterocyclic ring containing at least one N atom (the ring being optionally bridged with two or more carbon atoms); R3 represents a 5- or 6-membered heterocyclic ring containing at least one atom selected from N, O or S, the heterocyclic ring being optionally substituted by one or more groups selected from C1-6 alkyl oxo or NH2, the heterocyclic ring being further optionally fused to a 5- or 6-membered aryl or heterocyclic ring containing at least one atom selected from N, O or S, the fused aryl or heterocyclic ring being substituted by one or more halo atoms; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhea.Type: ApplicationFiled: April 18, 2006Publication date: August 7, 2008Inventors: Justin Stephen Bryans, Mark Edward Bunnage, Patrick Stephen Johnson, Helen Janet Mason, Lee Richard Roberts, Thomas Ryckmans, Alan Stobie, Toby James Underwood
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Publication number: 20080132496Abstract: Substituted carboxylic acid amides of general formula wherein A, B, and R1 to R5 are as defined herein, and the tautomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, such as antithrombotic activity and factor Xa-inhibiting activity.Type: ApplicationFiled: November 30, 2007Publication date: June 5, 2008Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: James Gillard, Sandra Ruth Handschuh, Herbert Nar, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Mario Schuler-Metz, Eckhart Bauer, Georg Dahmann, Kai Gerlach
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Patent number: 7378526Abstract: This invention relates to novel azacyclic ethynyl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: May 6, 2003Date of Patent: May 27, 2008Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring
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Publication number: 20080119516Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrom, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.Type: ApplicationFiled: July 29, 2004Publication date: May 22, 2008Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Antoni Torrens Jover, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
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Patent number: 7345060Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: November 19, 2004Date of Patent: March 18, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham
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Patent number: 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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Publication number: 20080009628Abstract: One-pot condensation-reduction methods for preparing substituted allylic alcohols as well as highly selective extractive methods to separate isomeric alcohols produced in the one-pot condensation-reduction processes are provided for preparing, for example, a quinolone.Type: ApplicationFiled: June 13, 2007Publication date: January 10, 2008Inventors: Michael Reuman, Roger Faessler, Armin Roessler, Kirk Sorgi, Xun Li, Jeffrey S. Grimm
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Patent number: 7314883Abstract: The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors using pharmaceutical compositions comprising compounds of Formula (I)Type: GrantFiled: January 5, 2007Date of Patent: January 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ling Chen, Prasad V. Chaturvedula, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, George N. Karageorge, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
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Patent number: 7297711Abstract: The present invention relates to novel tetracyclic arylalkyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylalkyl of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention also relates to process/es for preparing such compound/s of general formula (I), composition/s containing effective amount/s of such a compound and the use of such a compound/composition in therapy.Type: GrantFiled: June 19, 2003Date of Patent: November 20, 2007Assignee: Suven Life Sciences LimitedInventors: Venkateswarlu Jasti, Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Srinivasa Reddy Battula, Venkata Satya Veerabhadra Vadlamudi Rao
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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: 7271264Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: July 18, 2003Date of Patent: September 18, 2007Assignee: Eli Lilly and CompanyInventors: Ronald Jay Hinklin, Owen Brendan Wallace
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Publication number: 20070142434Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: ApplicationFiled: August 3, 2006Publication date: June 21, 2007Applicant: DECODE CHEMISTRY, INC.Inventors: Vincent Sandanayaka, Jasbir Singh, Lei Zhao, Mark E. Gurney
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Patent number: 7232834Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them.Type: GrantFiled: September 10, 2003Date of Patent: June 19, 2007Assignee: Novexel SAInventors: Eric Bacque, Antony Bigot, Youssef El Ahmad, Jean-Luc Malleron, Serge Mignani, Baptiste Ronan, Michel Tabart, Fabrice Viviani
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Patent number: 7220862Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: December 5, 2003Date of Patent: May 22, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, George N. Karageorge, Guanglin Luo, John E. Macor, Graham Poindexter, George Tora
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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: 7189701Abstract: Tetrapeptide L-alanyl-L-glutamyl-L-asparagyl-L-proline of the general formula L-Ala-L-Glu-Asp-L-Pro is proposed as a biologically active compound stimulating the functional activity of neurones. The application of L-Ala-L-Glu-L-Asp-L-Pro tetrapeptide in medicine is proposed for the preparation of a drug stimulating the functional activity of neurones. There is proposed a pharmacological agent, which contains as its active base an effective amount of L-Ala-L-Glu-L-Asp-L-Pro tetrapeptide for its salts of the amino acid group (acetate, hydrochloride, oxalate) or its salts of carboxyl groups (the salts of sodium, potassium, calcium, lithium, zinc, magnesium, and also the salts of organic and inorganic cations-ammonium, triethylammonium). The agent is proposed for parenteral, intranasal and oral administration.Type: GrantFiled: May 25, 2000Date of Patent: March 13, 2007Assignee: Sankt-Petersburgskaya Obschestvennaya Organizatsiya “Institut Bioregulyatsii I Gerontologii Szo Ramn”Inventors: Vladimir K. Khavinson, Vyacheslav G. Morozov, Vladimir V. Malinin, Evgeny I. Grigoriev
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Patent number: 7166617Abstract: Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.Type: GrantFiled: February 26, 2001Date of Patent: January 23, 2007Assignee: Mitsubishi Pharma CorporationInventors: Haruko Yamabe, Masahiro Okuyama, Akira Nakao, Mitsuru Ooizumi, Ken-ichi Saito
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Patent number: 7153848Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.Type: GrantFiled: July 14, 2005Date of Patent: December 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7125887Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: October 9, 2001Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: Jeffrey J. Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Yuan Cheng, legal representative, Christopher A. Willoughby, deceased
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Patent number: 7112594Abstract: Compounds represented by the following general formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine, a derivative thereof, imidazole, a derivative thereof, etc.; the ring B represents benzene, cyclohexane, pyrrole or a derivative thereof, furan, thiophene, etc.; R1, R2 and R3 represent each hydrogen, alkyl, halogen, hydroxyl, alkoxy, etc.; W represents hydrogen, alkyl or hydroxycarbonylalkyl; X represents halogen, cyano, nitro, etc.; X? represents hydrogen, halogen, etc.; and Y represents alkyl, hydroxyalkyl, hydroxycarbonylalkyl, aminoalkyl, etc.; salt thereof, and drugs comprising these compounds. Because of having an exellent effect of inhibiting activated lymphocyte proliferation, these compounds are usefull as preventives or remedies for various autoimmune diseases.Type: GrantFiled: August 9, 2001Date of Patent: September 26, 2006Assignee: Mitsubishi Pharma CorporationInventors: Hiroyuki Ushio, Youichiro Naito, Naoki Sugiyama, Takafumi Kawaguchi, Makio Ohtsuki, Kenji Chiba
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Patent number: 7105544Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject.Type: GrantFiled: January 14, 2003Date of Patent: September 12, 2006Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, John M. Wetzel, Chien-An Chen, Yu Jiang, Kai Lu
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Patent number: 7094800Abstract: The invention relates to compounds of the formula I in which the radicals have the meanings stated in the text, their stereoisomeric forms, and their physiologically tolerated salts, physiologically functional derivatives and process for their preparation. The compounds are suitable for the treatment of disorders of metabolism, such as type 2 diabetes.Type: GrantFiled: July 26, 2004Date of Patent: August 22, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Holger Wagner, Gerhard Jaehne, Holger Gaul, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7091353Abstract: The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-? in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases.Type: GrantFiled: December 21, 2001Date of Patent: August 15, 2006Assignee: Celgene CorporationInventors: Michael J. Robarge, Roger Shen-Chu Chen, George W. Muller, Hon-Wah Man
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Patent number: 7071201Abstract: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 2, 2001Date of Patent: July 4, 2006Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 6987188Abstract: Compounds of the formula: are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system.Type: GrantFiled: July 28, 2004Date of Patent: January 17, 2006Inventors: Scott Dax, James McNally
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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
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Patent number: 6908922Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions ins which endothelial dysfunction is known.Type: GrantFiled: November 12, 2002Date of Patent: June 21, 2005Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6852725Abstract: The present invention is directed to imidazolyl derivatives of the formula: where the substituents are defined in the specification, or a pharmaceutically acceptable salt thereof. The derivatives bind selectively to the somatostatin subtype receptors and elicit either an agonist or antagonist effect from the somatostatin subtype receptors.Type: GrantFiled: June 8, 1999Date of Patent: February 8, 2005Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S. A. S.Inventors: Christophe Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Christophe Philippe Moinet, Thomas D. Gordon, Barry A. Morgan
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Patent number: 6844344Abstract: The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotineType: GrantFiled: December 6, 2000Date of Patent: January 18, 2005Assignee: Eli Lilly and CompanyInventors: John Xiaoqiang He, Nicholas Allan Honigschmidt, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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Patent number: 6841552Abstract: Compounds of the formula: are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system.Type: GrantFiled: April 20, 2000Date of Patent: January 11, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Scott Dax, James McNally
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Publication number: 20040215019Abstract: The invention relates to coagulation of the blood.Type: ApplicationFiled: January 30, 2004Publication date: October 28, 2004Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer
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Publication number: 20040180923Abstract: Certain novel bridged piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of (MC-4R), such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: January 14, 2004Publication date: September 16, 2004Inventors: Zhixiong Ye, Khaled J. Barakat, Liangqin Guo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 6787650Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.Type: GrantFiled: April 5, 2002Date of Patent: September 7, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Osamu Kurasawa, Shinichi Imamura, Shohei Hashiguchi, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba
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Publication number: 20040147497Abstract: A compound or composition comprising N-formyl paroxetine of formula (1) is useful as a pharmaceutical and as a synthetic intermediate. The N-formyl paroxetine can be an impurity in paroxetine substances and methods of assaying for such an impurity are also useful.Type: ApplicationFiled: January 20, 2004Publication date: July 29, 2004Inventors: Hans J. Hoorn, Theodorus H.A. Peters, Frantisek Picha
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Publication number: 20040127517Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: October 20, 2003Publication date: July 1, 2004Inventors: Marco Baroni, Bernard Bourrie, Pierre Casellas
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Publication number: 20040122052Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with a 2,6-dioxo-3-hydroxypiperidin-5-yl group, which may be further substituted in the 5-position with alkyl or halogeno, and in the 4-position with alkyl or a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF&agr;. A typical embodiment is 2-(2,6-dioxo-3-hydroxy-5-fluoro-piperidin-5-yl)-4-aminoisoindolin-1-one.Type: ApplicationFiled: December 9, 2003Publication date: June 24, 2004Applicant: Celgene CorporationInventors: George Muller, Hon-Wah Man, David I. Stirling
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These 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, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6727264Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: July 3, 2002Date of Patent: April 27, 2004Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, John Wetzel, John E. DeLeon, Yu Jiang, Chien-An Chen, Kai Lu
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Patent number: 6713473Abstract: A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents —S—, —O—, —NR4—, —NR5—CO— and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof.Type: GrantFiled: February 19, 2002Date of Patent: March 30, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoyuki Nishikawa, Masaharu Sugai, Kozo Aoki, Makoto Suzuki, Akihiko Ikegawa, Kazunobu Takahashi, Fukuichi Ohsawa, Naomi Masuda, Nobukazu Kakui, Jiro Tanaka, Yuji Tabata, Kenji Asai
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Publication number: 20040024023Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: July 17, 2003Publication date: February 5, 2004Applicant: WyethInventors: Ronald Charles Bernotas, Steven Edward Lenicek
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Publication number: 20040019207Abstract: The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is (a), wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino; or aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, aminoacyl, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitrType: ApplicationFiled: July 17, 2003Publication date: January 29, 2004Applicant: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon Feldback Nielsen, Elsebet Ostergaard Nielsen
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Patent number: 6677338Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.Type: GrantFiled: February 28, 2002Date of Patent: January 13, 2004Assignees: President and Fellows of Harvard College, Organix, Inc.Inventors: Bertha K. Madras, Peter C. Meltzer
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Publication number: 20030212141Abstract: The present invention is directed to a new class of serotonin 5HT2 antagonists and thier use in the treatment of a variety of diseases.Type: ApplicationFiled: April 9, 2003Publication date: November 13, 2003Inventors: Thaddeus R. Nieduzak, Mark W. Dudley, John H. Kehne
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Publication number: 20030212094Abstract: Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: 1Type: ApplicationFiled: December 30, 2002Publication date: November 13, 2003Inventors: Haruko Yamabe, Masahiro Okuyama, Akira Nakao, Mitsuru Ooizumi, Ken-ichi Saito
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Publication number: 20030207861Abstract: 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: ApplicationFiled: January 21, 2003Publication date: November 6, 2003Applicant: SCHERING CORPORATIONInventors: Ashok Arasappan, Frank Bennett, Stephane L. Bogen, Kevin X. Chen, Edwin Jao, Yi-Tsung Liu, Raymond G. Lovey, Vincent S. Madison, Latha G. Nair, F. George Njoroge, Anil K. Saksena, Mousumi Sannigrahi, Srikanth Venkatraman, Viyyoor M. Girijavallabhan
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Patent number: 6642228Abstract: There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1 is hydrogen etc., B is bond, or B—N—R1 forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and &agr;1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for &agr;1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which &agr;1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by &agr;1B adrenoceptor.Type: GrantFiled: April 13, 2001Date of Patent: November 4, 2003Assignee: Toray Industries, Inc.Inventors: Ryoji Hayashi, Eiji Ohmori, Masafumi Isogaya, Mitsuhiro Moriwaki, Hiroki Kumagai
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Publication number: 20030195191Abstract: Compounds of formula (I): wherein R1 is bicyclyl or heterobicyclyl, R2 and R3 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, (C1-6)alkylthio, (C2-6)alkenylthio, (C2-6)alkynylthio, aryloxy, arylthio, heterocyclyloxy, heterocyclythio, (C1-6)alkoxy, (C1-6)alkenyloxy, aryl(C1-6)alkoxy, aryl(C1-6)alkylthio, amino, mono- or di-(C1-6)alkylamino, acylamino, sulfonylamino, cycloalkyl, cycloalkenyl, carboxylic acid (C1-6) ester, hydroxy, halogen, carboxamide: CONR8R9 where R8 and R9 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and heterocyclyl and includes R8 and R9 as part of a heterocyclyl group, or R2 and R3 together form a cyclic alkyl or alkenyl; R4 and R5 are each independently aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino; R6 and R7 are each hydrogen or together form a fused aryl ring; and m and n are each independently from 0 to 2; with the proviso that when n=1 neither R4 nor RType: ApplicationFiled: May 12, 2003Publication date: October 16, 2003Inventors: Gordon Burton, Barry Sidney Orlek