Carbocyclic Ring Containing Patents (Class 546/194)
-
Patent number: 6699890Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2 , R3 and R4 are as defined herein.Type: GrantFiled: January 22, 2002Date of Patent: March 2, 2004Assignee: Memory Pharmaceuticals Corp.Inventors: Richard A. Schumacher, William F. Brubaker, Michael De Vivo, Hans-Jürgen Ernst Hess, Allen Hopper, Ashok Tehim, Ruiping Liu, Axel Unterbeck
-
Patent number: 6696443Abstract: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.Type: GrantFiled: November 20, 2001Date of Patent: February 24, 2004Assignee: Scios, Inc.Inventors: Babu Mavunkel, Sundeep Dugar, Gregory Luedtke, Xuefei Tan, Glenn McEnroe
-
Publication number: 20040034028Abstract: The present invention relates to compounds of the formula (I): in which: Z represents biphenyl optionally substitute in position 2′, 3′, 4′, 5′ and 6′ with one or more substitutents chosen from trihalomethyl and trihalomethoxy; Het represents quinolyl, quinoxalyl or pyridyl optionally substituted with one or more substitutents chosen from halo, cyano, nitro, (C1-C6)alkyl, (C6-C12)aryl, (C1-C6)alkoxy, hydroxyl, (C1-C6)thioalkoxy, carboxyl and (C1-C6)alkoxycarbonyl, or pharmaceutically acceptable salts thereof. These compounds are useful as inhibitors of microsomal triglyceride transfer protein and as inhibitors of the secretion of B apoproteins.Type: ApplicationFiled: May 22, 2003Publication date: February 19, 2004Inventors: Alyx-Caroline Guevel, Didier Festal, Francois Collonges, Daniel Guerrier, Olivier Chevreuil
-
Patent number: 6689794Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: May 10, 2002Date of Patent: February 10, 2004Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
-
Patent number: 6689779Abstract: The present invention relates to novel oxazolidinone derivatives, their pharmaceutically acceptable salts and a process for the preparation thereof. More particularly, the present invention relates to oxazolidinone derivatives having pyridine or pyrimidine moeity substituted by heterocycle and heteroaromaticcycle at 4-position of phenyl ring. The compounds of the present invention have wide antibacterial spectrum, superior antibacterial activity and low toxicity, such that the compound of this invention can be used as an antibacterial agent.Type: GrantFiled: November 27, 2002Date of Patent: February 10, 2004Assignee: Dong A Pharm. Co., Ltd.Inventors: Jae-Gul Lee, Won-Bin Leem, Jong-Hwan Cho, Sung-Hak Choi, Jong-Jin Lee, Sang-Kuk Park, Tae-Hoo Lee, Dong-Goo Kim, Hyun-Jung Sung
-
Patent number: 6689793Abstract: The present invention is directed to derivatives of piperidinylethyl, phenoxyethyl, and fluorophenethyl bromopyridyl thioureas, which have been found to be effective non-nucleoside inhibitors (NNRTI) of NNI-resistant and multi-drug resistant human immunodeficiency virus (HIV)-1 reverse transcriptase (RT). The present invention is further directed to methods of using the above derivatives to treat patients with NNI-resistant or multi-drug resistant human immunodeficiency virus (HIV)-1.Type: GrantFiled: December 6, 2001Date of Patent: February 10, 2004Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Venkatachalam
-
Patent number: 6686503Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula: wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.Type: GrantFiled: June 13, 2001Date of Patent: February 3, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Wenying Chai, William V. Murray
-
Patent number: 6683079Abstract: 3-(amino- or aminoalkyl) pyridinone derivatives having the formula (1) wherein Q, X, Y, and R3-R6 are as defined, which derivatives are useful for the treatment of HIV related diseases.Type: GrantFiled: July 15, 2002Date of Patent: January 27, 2004Assignees: Centre National de la Recherche Scientifique, Insitut CurieInventors: Emile Bisagni, Valerie Dolle, Chi Hung Nguyen, Claude Monneret, David Grierson, Anne-Marie Aubertin
-
Patent number: 6683074Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: September 26, 2001Date of Patent: January 27, 2004Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
-
Patent number: 6680329Abstract: Compounds of formula [I] in which: W may represent a —(CH2)2—, —(CH2)3—, —CH2—C≡C— or —CH2—CH═CH— group, R2 may in particular represent a piperidyl group, an optionally substituted 1,2,3,6-tetrahydropyridyl group, a hexahydro-1H-azepinyl group, an optionally substituted piperazinyl group or a morpholinyl group, R3 may in particular represent a group —COR1, A may in particular represent an optionally substituted phenyl group, a heterocycle or a cyclopentyl group, and B may in particular represent a pyridyl group, an aminopyrazinyl group, an aminopyridazinyl group, a pyrimidinyl group optionally substituted with an amino group, piperidyl group or an aminopyridyl group optionally substituted on the pyridine with a (C1-C4)alkyl or (C1-C4)alkoxy group, the amino group possibly also being substituted with a (C1-C4)alkyl group, their preparation and their therapeutic application.Type: GrantFiled: September 12, 2002Date of Patent: January 20, 2004Assignee: Sanofi-SynthelaboInventors: Jean-Michel Altenburger, Gérard Cremer, Gilbert Lassalle, Mostafa Matrougui
-
Publication number: 20040009988Abstract: The present invention relates to A compound of formula (I) wherein A, U, V, X, Z, R1, Y, R2 and R3 are defined in the description or a physiologically acceptable salt, solvate or derivative thereof, to compositions and processes for making said compounds and their use in treating conditions ameliorated by an apoB-100 and/or MTP inhibitor.Type: ApplicationFiled: May 20, 2003Publication date: January 15, 2004Inventor: Nerina Dodic
-
Publication number: 20040009967Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: ApplicationFiled: July 30, 2002Publication date: January 15, 2004Applicant: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Loser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
-
Patent number: 6677454Abstract: Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.Type: GrantFiled: January 28, 2003Date of Patent: January 13, 2004Assignee: Biostream Therapeutics, Inc.Inventors: John W. Babich, Miles P. Smith
-
Patent number: 6677354Abstract: Disclosed are compounds of formula (I): wherein: Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered heteroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, OType: GrantFiled: December 16, 2002Date of Patent: January 13, 2004Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Christopher Norbert Johnson, Geoffrey Stemp, Kevin Thewlis
-
Patent number: 6677369Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: April 25, 2002Date of Patent: January 13, 2004Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Publication number: 20040006086Abstract: The present invention relates to compounds represented by the structural Formula I: 1Type: ApplicationFiled: June 20, 2002Publication date: January 8, 2004Inventors: Andrew Stamford, Youhao Dong, Stuart W. McCombie, Yusheng Wu
-
Publication number: 20030236250Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: ApplicationFiled: November 13, 2002Publication date: December 25, 2003Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
-
Patent number: 6664277Abstract: The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.Type: GrantFiled: January 3, 2003Date of Patent: December 16, 2003Assignee: PPD Discovery, Inc.Inventors: Bradley B. Brown, Kenneth S. Rehder, Jon-Paul Strachan, Jeron H. Eaves, Christopher T. Lowden
-
Publication number: 20030225077Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.Type: ApplicationFiled: April 28, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
-
Publication number: 20030225059Abstract: The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: ApplicationFiled: November 13, 2002Publication date: December 4, 2003Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain, Lihu Yang
-
Publication number: 20030225133Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: ApplicationFiled: March 28, 2003Publication date: December 4, 2003Inventor: Aloke A Dutta
-
Patent number: 6656954Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: November 29, 2001Date of Patent: December 2, 2003Assignee: Pharmacia CorporationInventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
-
Patent number: 6656959Abstract: The present invention concerns pyridine derivatives having the formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein L is hydrogen; C1-6alkyl; C1-6alkyl carbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidyl; substituted piperidyl; C1-6alkylsulfonyl or arylsulfonyl; —A—B— is —CR8═CR5— or—CHR4—CHR5—; D is O or NR6; R1 is a hydrogen or C1-4alkyl; R2 is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyl oxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or substituted C1-6alkyl; or R2 is —O—R9 or —NH—R10; R3 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R2 and R1, or R2 and R3 taken together may form a bivalent radical; Q is disubstituted pyridine; R7 and R8 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cyclo alkyl; aType: GrantFiled: September 29, 2000Date of Patent: December 2, 2003Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Freyne, Gaston Stanislas Diels, Maria Encarnacion Matesanz-Ballesteros, Adolfo Diaz-Martinez
-
Patent number: 6649627Abstract: The invention concerns compounds of formula (Ia) wherein R1a represents hydrogen, an —S(O)z —(C1-C4)Alk group, a —CO(C1-C4)Alk group, an —NHSO2—(C1-C4)Alk group, an NCHl (C1-C4) Alk group, a 2-furyl group or a halogen; R2 represents hydrogen or a (C1-C4)Alk group, a (C1-C4) alkoxyl group, a halogen, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NH2, —NHSO2(C1-C4)Alk; m and n are independently 0, 1 or 2; R3 and R4 independently represent hydrogen or a (C1-C4)Alk group; Z is 1 or 2 and their salts or solvates, the pharmaceutical compositions that contain them, the process for their preparation, and intermediate synthesis products.Type: GrantFiled: March 26, 2001Date of Patent: November 18, 2003Assignee: Sanofi-SynthelaboInventors: Roberto Cecchi, Tiziano Croci, Umberto Guzzi, Eric Marsault
-
Patent number: 6645980Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: November 20, 2000Date of Patent: November 11, 2003Assignee: Sepracor Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
-
Publication number: 20030208078Abstract: Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.Type: ApplicationFiled: January 28, 2003Publication date: November 6, 2003Inventors: John W. Babich, Miles P. Smith
-
Patent number: 6642385Abstract: In one embodiment, the present invention describes the synthesis of 4-(piperidyl)(2-pyridyl)methanone-(E)-O-methyloxime dihydrochloride, monohydrochloride and free base, and similar compounds, in high stereochemical purity.Type: GrantFiled: October 11, 2002Date of Patent: November 4, 2003Assignee: Schering CorporationInventors: Wenxue Wu, Hongbiao Liao, David J Tsai
-
Patent number: 6642226Abstract: The invention relates to compounds of the formula wherein R1 is optionally substituted phenyl, morpholinyl, piperazinyl, pyrrolidinyl, piperidinyl or is thiomorpholinyl, 1-oxo-thiomorpholinyl or 1,1-dioxothiomorpholinyl. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable in the control or treatment of diseases, related to this receptor.Type: GrantFiled: January 25, 2002Date of Patent: November 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Stephan Roever, Patrick Schnider
-
Patent number: 6638946Abstract: The invention relates to a compound of formula (I): wherein: A represents pyridine, pyridinium or piperidine R1, R2, R3 and R4 are as defined in the description R5 represents hydrogen, a nitrogen-containing heterocycle or a group of formula (II): R6 represents hydrogen or linear or branched (C1-C6)alkyl. and medicinal products containing the same which are useful in treating pain or deficiencies in memory.Type: GrantFiled: September 25, 2001Date of Patent: October 28, 2003Assignee: Les Laboratoires ServierInventors: Otto Meth-Cohn, Chu-Yi Yu, Pierre Lestage, Marie-Cécile Lebrun, Daniel-Henri Caignard, Pierre Renard
-
Patent number: 6638950Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 20, 2001Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
-
Publication number: 20030199505Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: ApplicationFiled: February 26, 2003Publication date: October 23, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Pineiro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Publication number: 20030199504Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: ApplicationFiled: February 28, 2003Publication date: October 23, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Pineiro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Patent number: 6635657Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: June 8, 2001Date of Patent: October 21, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Piñeiro-Núñez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Patent number: 6635640Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.Type: GrantFiled: June 29, 2001Date of Patent: October 21, 2003Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
-
Patent number: 6632828Abstract: Compounds of the formula I or a pharmaceutically acceptable salt, solvate or N-oxide thereof, wherein X is ═CH— or ═N—; Y is H, halogen, trihaloalkyl, alkyl, alkenyl, cycloalkyl, cycloalkyl, SH, —S-alkyl, or —CN. R is alkyl, —CF3, cycloalkyl, heterocycloalkyl, heterocycloalkyl-alkyl, heteroarylalky or adamantyl, or optionally substituted phenyl, phenoxyalkyl, phenylthioalkyl, pyridyl, thienyl, thiazolyl, pyrazinyl, 1,2,5,6-tetrahydropyridine or wherein R10 and R11 are hydrogen, alkyl or together form a cycloalkyl, are disclosed, as well as pharmaceutical compositions and methods of using said compounds in the treatment of eating disorders and diabetes.Type: GrantFiled: July 23, 2002Date of Patent: October 14, 2003Assignee: Schering CorporationInventors: Andrew W. Stamford, Craig D. Boyle, Ying Huang
-
Publication number: 20030187023Abstract: A compound represented by the formula: 1Type: ApplicationFiled: January 16, 2003Publication date: October 2, 2003Inventors: Keiji Kubo, Toshio Miyawaki, Masaki Kawamura
-
Publication number: 20030187022Abstract: Compounds of general formula I 1Type: ApplicationFiled: January 16, 2003Publication date: October 2, 2003Inventors: William Brown, Christopher Walpole, Zhongyong Wei
-
Patent number: 6627629Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 29, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
-
Patent number: 6624176Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.Type: GrantFiled: October 29, 2002Date of Patent: September 23, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Torsten Hoffmann, Patrick Schnider, Heinz Stadler
-
Patent number: 6620815Abstract: This invention is directed to oxazolidinone compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: August 10, 2000Date of Patent: September 16, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, T. G. Murali Dhar, Dhanapalan Nagarathnam, Yoon T. Jeon, Mohammad R. Marzabadi, Wai C. Wong, Charles Gluchowski
-
Patent number: 6617325Abstract: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: May 15, 2002Date of Patent: September 9, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
-
Publication number: 20030166644Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.Type: ApplicationFiled: December 13, 2002Publication date: September 4, 2003Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
-
Patent number: 6610704Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermidates thereof.Type: GrantFiled: June 8, 2001Date of Patent: August 26, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Pineiro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Patent number: 6608087Abstract: The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.Type: GrantFiled: July 18, 2002Date of Patent: August 19, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, Dean Stamos, Michael Badia, Anne-Laure Grillot, Steven Ronkin, Martin Trudeau
-
Patent number: 6608072Abstract: Compounds of formula (I) and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof, wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.Type: GrantFiled: April 22, 2002Date of Patent: August 19, 2003Assignee: Novartis AGInventor: Lászlo Révész
-
Patent number: 6608086Abstract: This invention provides dihydropyridines useful for treatment of prostatic hyperplasia, inhibition of cholesterol synthesis, and/or reduction of intraocular pressure.Type: GrantFiled: October 5, 2001Date of Patent: August 19, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Charles Gluchowski, John M. Wetzel, George Chiu, Mohammed R. Marzabadi, Wai C. Wong, Dhanapalan Nagarathnam
-
Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Patent number: 6605608Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: December 22, 2000Date of Patent: August 12, 2003Assignee: Ono Pharmaceutical Co., LtdInventors: Takuya Seko, Masashi Kato
-
Patent number: 6605620Abstract: A cyclic amine compound by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.Type: GrantFiled: March 28, 2002Date of Patent: August 12, 2003Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
-
Publication number: 20030149017Abstract: The present invention relates to 2-aminopyridine derivatives of the formula 1Type: ApplicationFiled: December 6, 2002Publication date: August 7, 2003Applicant: Pfizer Inc.Inventor: John Adams Lowe