The Additional Hetero Ring Contains Nitrogen As The Only Ring Hetero Atom [e.g., 2-(2-imidazolin-2-yl)-benzimidazole; 1-p-chlorophenyl-3- Pyrrolidin-1- Yl-propyl Benzimidazolone, Etc.] Patents (Class 548/306.1)
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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: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7122674Abstract: The invention relates to a process for preparing hydroxyindolylglyoxylamides in high yields and particularly pure form.Type: GrantFiled: July 31, 2003Date of Patent: October 17, 2006Assignee: Elbion AGInventors: Hans-Joachim Jänsch, Helge Hartenhauer, Hans Stange, Norbert Höfgen, Jürgen Schäfer
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Patent number: 7118811Abstract: A compound represented by formula (IA) or (IIA): wherein R11, R12 and R13 each represents a hydrogen atom, an aliphatic hydrocarbon group, an aryl group or a heterocyclic group; L1 represents a connecting group; R11 and R12, R11 and L1 and R12 and L1 may each combine with each other to form a ring when possible; R14, R15, R16 and R17 each represents a hydrogen atom or a substituent; and R13 to R17 may each combine with each of R11 to R17 or L1 to form a ring when possible; wherein R13 to R17 and L1 have the same meaning as in formula (IA); Q represents an atomic group necessary for forming a 5-, 6- or 7-membered ring with N; and R13, R14, R15, R16 and R17 may each combine with each of R13 to R17, the connecting group L1 or the atomic group Q to form a ring.Type: GrantFiled: July 24, 2003Date of Patent: October 10, 2006Assignee: Fuji Photo Film Co., Ltd.Inventors: Toshihiro Ise, Hisashi Okada
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Patent number: 7115644Abstract: Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease.Type: GrantFiled: September 3, 2003Date of Patent: October 3, 2006Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Antonio Jose del Moral Barbosa, Jr., Daniel R. Goldberg, Abdelhakim Hammach, Pingrong Liu, Neil Moss, Mark Stephen Ralph, Gregory Paul Roth, Christopher Ronald Sarko, Fariba Soleymanzadeh, Andre White
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Patent number: 7056918Abstract: The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; s is an integer from 0–5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: March 11, 2002Date of Patent: June 6, 2006Assignee: Pfizer, Inc.Inventors: Mark A. Dombroski, Michael A. Letavic, Kim F. McClure
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Patent number: 7034048Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors.Type: GrantFiled: May 4, 2001Date of Patent: April 25, 2006Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Caroline Minli Rachel Low, Matthew John Tozer
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Patent number: 7030139Abstract: Compounds of general formula (I), are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of painType: GrantFiled: April 18, 2002Date of Patent: April 18, 2006Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Miroslaw Tomaszewski, Christopher Walpole, Hua Yang
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Patent number: 7022714Abstract: This invention relates aryl substituted benzimidazoles of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1, R2, R10 and n are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: July 31, 2003Date of Patent: April 4, 2006Assignee: Euro-Celtique S.A.Inventors: Qun Sun, Xiaoming Zhou, Donald J. Kyle
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Patent number: 7019004Abstract: The invention provides compounds of formula (I) wherein X, Y, R1, R2, R3 and R4 are as defined in the description, and the preparation thereof.Type: GrantFiled: May 7, 2001Date of Patent: March 28, 2006Assignee: Novartis AGInventors: Daniel Berney, Robin Breckenridge, Peter Neumann, Gideon Shapiro, Max Peter Seiler, Thomas J. Troxler
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Patent number: 7002021Abstract: Diketopyrrolopyrroles of the formula (I): wherein R1, R2, R3 and R4 independently of one another are a C1–C4 alkyl radical or a substituted or unsubstituted phenyl radical, wherein the phenyl radical can be substituted by 1, 2, 3 or 4 substituents from the group C1–C4 alkyl, C1–C4 alkoxy, CN, F, Cl, Br, NO2, CF3, S—C1–C4 alkyl, phenyl or (C1–C2)alkylenephenyl, with the proviso that at least one of the radicals, R1, R2, R3, or R4, is one of the stated substituted or unsubstituted phenyl radicals.Type: GrantFiled: June 6, 2003Date of Patent: February 21, 2006Assignee: Clariant GmbHInventors: Felix W. Grimm, Hans Joachim Metz, Joachim Weber, Andreas Wacker
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Patent number: 6989384Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: July 23, 2003Date of Patent: January 24, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Ye Hua, Hiep The Luu, Fora P. Chan, Theodore O. Johnson, Jr., Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Shao Song Chu, Brian Walter Eastman
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Patent number: 6969712Abstract: This invention relates to the compounds represented by a general formula [I]: [in which A1 and A2 represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C3-C20 aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.Type: GrantFiled: November 14, 2001Date of Patent: November 29, 2005Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Osamu Okamoto, Hiroshi Kawamoto, Kensuke Kobayashi, Satoru Itoh, Tetsuya Kato, Izumi Yamamoto, Yoshikazu Iwasawa
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Patent number: 6960591Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: July 4, 2001Date of Patent: November 1, 2005Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Patent number: 6949550Abstract: The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 26, 2002Date of Patent: September 27, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Mimi L. Quan, Ruth R. Wexler
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Patent number: 6916827Abstract: Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).Type: GrantFiled: May 15, 2003Date of Patent: July 12, 2005Assignee: Neurogen CorporationInventors: George D. Maynard, Jun Yuan, George P. Luke, Kevin Currie
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Patent number: 6916810Abstract: The present invention relates to cyclic urea derivatives, their synthesis, and their use as ?v integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.Type: GrantFiled: September 7, 2001Date of Patent: July 12, 2005Assignee: Merck & Co., Inc.Inventors: John H. Hutchinson, Aiwen Li
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Patent number: 6916819Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: GrantFiled: December 21, 2001Date of Patent: July 12, 2005Assignee: Neurogen CorporationInventors: Guiying Li, John M. Peterson, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, Vinod Singh, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu
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Patent number: 6911462Abstract: This invention relates to a family of phenylbenzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.Type: GrantFiled: March 20, 2002Date of Patent: June 28, 2005Assignee: Avanir PharmaceuticalsInventors: Jagadish C. Sircar, Mark L. Richards, Michael G. Campbell, Michael W. Major
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Patent number: 6906070Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: August 8, 2001Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 6906075Abstract: Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: January 9, 2003Date of Patent: June 14, 2005Assignee: Neurogen Corp.Inventors: Robert W. DeSimone, Cheryl Steenstra, Linda Gustavson, Rajagopal Bakthavatchalam, Alan Hutchison
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Patent number: 6894173Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: May 17, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6855714Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.Type: GrantFiled: July 5, 2002Date of Patent: February 15, 2005Assignee: Schering AktiengesellschaftInventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger
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Patent number: 6849620Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 17, 2002Date of Patent: February 1, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, Eric Jon Jacobsen, David W. Piotrowski, Brad A. Acker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, Vincent E. Groppi, Jr.
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Patent number: 6841566Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein R1 is selected from: H, haloalkyl, (C1-6)alkyl, (C2-6)alkenyl, (C3-7)cycloalkyl, (C2-6)alkynyl, (C5-7)cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C6-10)bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR5, wherein R5 is H, halogen, haloalkyl, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; X is N or CR5; D is N or CR5; each of Y1 and Y2 is independently O or S; Z is O, N, or NRZ wherein RZ is H, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; R3 and R4 are each independently H, (C1-6)alkyl, first (C3-7)cycloalkyl or 6- or 10-membered aryl, Het (C1-6)alkyl-6- or 10-membered aryl, (C1-6)alkyl-Het; or each R3 and R4 are independently covalently bonded together to form second (C3-7)cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R3 or R4Type: GrantFiled: July 18, 2002Date of Patent: January 11, 2005Assignee: Boehringer Ingelheim, Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos
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Patent number: 6841563Abstract: Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group. R4 and R5 are independently —H, a C1-C4 straight chained or branched alkyl group or, taken together with the nitrogen atom to which each is bonded, a non-aromatic heterocyclic ring. Ring A and Ring B are independently further substituted with zero, one or two substituents. Physiologically acceptable salts of structural formula shown above are also included. Also disclosed is a method promoting growth, efficiency of feed utilization and/or production of lean body mass in a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by the structural formula as shown or a physiologically acceptable salt thereof.Type: GrantFiled: November 13, 2000Date of Patent: January 11, 2005Assignee: Eli Lilly and CompanyInventors: Randall Bruce Hopkins, Deana Lori Hancock, Michael Eugene Quimby
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Patent number: 6833381Abstract: TNF-&agr; inhibitors containing a heterocyclic compound having angiotensin II antagonistic activity which are useful as preventives/remedies for inflammatory diseases, etc.Type: GrantFiled: August 14, 2002Date of Patent: December 21, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Kazuaki Ikeya, Takahito Kitayoshi
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Publication number: 20040214857Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.Type: ApplicationFiled: April 16, 2004Publication date: October 28, 2004Inventors: Michael K. Ameriks, Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher
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Publication number: 20040209929Abstract: Fused heteroarylcarboxylic acids of formula (I): 1Type: ApplicationFiled: February 19, 2004Publication date: October 21, 2004Applicant: Agouron Pharmaceuticals, Inc.Inventors: Donald Skalitzky, Wei-Guo Su, Luke Raymond Zehnder
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Publication number: 20040192749Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: January 16, 2004Publication date: September 30, 2004Applicant: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Publication number: 20040142948Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: ApplicationFiled: November 7, 2003Publication date: July 22, 2004Inventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
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Patent number: 6759425Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to benzimidazole molecules that are cellular proliferation inhibitors and thus are useful as anticancer agents.Type: GrantFiled: February 27, 2002Date of Patent: July 6, 2004Assignee: Avanir PharmaceuticalsInventors: Jagadish C. Sircar, Mark L. Richards
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Patent number: 6747028Abstract: This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.Type: GrantFiled: December 27, 2001Date of Patent: June 8, 2004Assignee: Hanssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Koenraad Jozef Lodewijk Marcel Andries
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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: 6740649Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.Type: GrantFiled: September 16, 2002Date of Patent: May 25, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
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Patent number: 6737421Abstract: Compounds of the formula I or II and their tautomeric forms, possible enantiomeric and diastereomeric forms, possible cistrans isomers on the rings in A and prodrugs thereof, pharmaceutical compositions containing these compounds and methods of treating neurodegenerative diseases or neuronal damage with these compounds.Type: GrantFiled: April 4, 2002Date of Patent: May 18, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubish, Michael Kock, Thomas Hoeger, Roland Grandel, Sabine Schult, Reinhold Mueller
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Publication number: 20040077856Abstract: PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 29, 2003Publication date: April 22, 2004Inventors: Jia-Ning Xiang, Siegfried B. Christensen IV, Xiangmin Liao, Maxwell D. Cummings
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Publication number: 20040063642Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.Type: ApplicationFiled: March 17, 2003Publication date: April 1, 2004Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly B. White
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Publication number: 20040063768Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds 1Type: ApplicationFiled: September 15, 2003Publication date: April 1, 2004Inventors: Derek John Denhart, Jonathan L. Ditta, Dalton King, John E. Macor, Lawrence R. Marcin, Ronald J. Mattson, Zhaoxing Meng
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Publication number: 20040063939Abstract: The invention relates to a process for preparing hydroxyindolylglyoxylamides in high yields and particularly pure form.Type: ApplicationFiled: July 31, 2003Publication date: April 1, 2004Inventors: Hans-Joachim Jansch, Helge Hartenhauer, Hans Stange, Norbert Hofgen, Jurgen Schafer
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Patent number: 6710054Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N, and S, etc.; A is 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl; etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.Type: GrantFiled: October 15, 2001Date of Patent: March 23, 2004Assignee: Pfizer IncInventors: Kazunari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
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Patent number: 6706735Abstract: 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 26, 2002Date of Patent: March 16, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Paul S. Watson, Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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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: 20040023993Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: June 30, 2003Publication date: February 5, 2004Applicant: Neurogen Corporation A Corporation of the State of DelawareInventors: Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, Daniel L. Rosewater
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Patent number: 6683188Abstract: The present invention provides organic dye compounds having their absorption maxima in a region ranging from the ultraviolet region to a relatively short wavelength visible region and uses thereof. The present invention provides specific monomethine cyanine dyes, light absorbents and optical recording media comprising the monomethine cyanine dyes, and a process for producing the monomethine cyanine dyes which comprises a step of reacting a quaternary ammonium salt of nitrogen atom-containing heterocyclic compound having a reactive methyl group with a quaternary ammonium salt of nitrogen atom-containing heterocyclic compound having an appropriate leaving group.Type: GrantFiled: August 17, 2001Date of Patent: January 27, 2004Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Chiaki Kasada, Yasushi Aizawa, Toshio Kawata, Shigeo Yasui
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Publication number: 20040010017Abstract: 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: ApplicationFiled: January 17, 2003Publication date: January 15, 2004Inventors: Douglas Wade Beight, John Joseph Masters, Jason Scott Sawyer, Robert Theodore Shuman, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20040010026Abstract: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.Type: ApplicationFiled: June 17, 2003Publication date: January 15, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Guenter Linz, Peter Sieger, Gunnar Schreiner, Werner Rall, Rolf Schmid
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Publication number: 20040002524Abstract: This invention relates to compounds, in particular benzimidazoles, that are useful as estrogen agonists and/or antagonists and pharmaceutical uses thereof. The present invention also relates to benzimidazoles that are selective for the ER&bgr; receptor and pharmaceutical uses thereof.Type: ApplicationFiled: June 11, 2003Publication date: January 1, 2004Inventors: Richard Chesworth, Laura D. Gegnas
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Publication number: 20030225053Abstract: Disclosed are amide compounds of formula(I): 1Type: ApplicationFiled: April 10, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
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Patent number: 6649609Abstract: The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.Type: GrantFiled: December 12, 2001Date of Patent: November 18, 2003Assignee: Neurosearch A/SInventors: Lene Teuber, Frank Watjen