Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Nitrogen Patents (Class 549/69)
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Publication number: 20080269481Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.Type: ApplicationFiled: February 4, 2008Publication date: October 30, 2008Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Bettina Hamelin, Oswy Z. Pereira, Carl Poisson, Melaine Proulx, Thumkunta Jagadeeswar Reddy, Zhang Ming-Qiang
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Publication number: 20080261952Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
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Patent number: 7423061Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: GrantFiled: August 12, 2004Date of Patent: September 9, 2008Assignee: AstraZeneca ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Stephanie Springer, Mei Su, Dingwei Yu
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Publication number: 20080200468Abstract: Therapeutically active heteroaryl carboxylic acid derivatives of Formula (I) wherein R1, R2, W, X, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.Type: ApplicationFiled: February 14, 2006Publication date: August 21, 2008Inventors: Juliet Kay Simpson, Ivan Leo Pinto
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Patent number: 7402696Abstract: The present invention provides novel benzene compounds presented by the following formulas, and analogs thereof, that exert an ACC activity-inhibiting effect that is effective in the treatment of obesity, hyperlipemia, fatty liver, hyperglycemia, impaired glucose tolerance, diabetes, diabetic complications (diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, and diabetic macroangiopathy, hypertension, arteriosclerosis), hypertension, and arteriosclerosis.Type: GrantFiled: October 13, 2006Date of Patent: July 22, 2008Assignee: Ajinomoto Co., Inc.Inventors: Nobuyasu Suzuki, Yukio Nihei, Hidehiro Ichinose, Hideyuki Tanaka, Noriko Yasa, Toshihiro Hatanaka, Yoko Masuzawa, Eiji Nakanishi, Nobuo Kondo
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Patent number: 7375131Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.Type: GrantFiled: May 29, 2003Date of Patent: May 20, 2008Assignee: SmithKlineBeecham Corp.Inventors: James F. Callahan, Yue Hu Li
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Patent number: 7358376Abstract: The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: February 7, 2001Date of Patent: April 15, 2008Assignee: AstraZeneca ABInventors: Andrew Baxter, Stephen Brough, Alan Faull, Craig Johnstone, Thomas McInally
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Patent number: 7326729Abstract: The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.Type: GrantFiled: May 11, 2005Date of Patent: February 5, 2008Assignee: Schering CorporationInventors: Jianhua Chao, Arthur G. Taveras, Cynthia J. Aki
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Patent number: 7196114Abstract: Substituted 3-(benzoylureido)thiophene derivatives, processes for preparing them and their use The invention relates to compounds of the formula I where the radicals are as defined, and their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.Type: GrantFiled: February 17, 2004Date of Patent: March 27, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Elisabeth Defossa, Erich Von Roedern, Dieter Kadereit, Andreas Herling, Hans-Joerg Burger, Thomas Klabunde, Karl-Ulrich Wendt
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Patent number: 7196207Abstract: A method for reducing a sulfur-containing compound by hydrogenation using a noble metal catalyst which method is exemplified by an industrial method for producing a 2-alkyl-3-aminothiophene derivative with high economical efficiency by hydrogenating a 2-alkenyl-3-aminothiophene derivative using the noble metal catalyst. 2-Alkyl-3-aminothiophene derivatives are useful compounds in the fields of medicine and agriculture, and in particular, useful in bactericides for agriculture or gardening, or intermediates of the bactericides. The hydrogenation reaction temperature is controlled at 150° C. to 300° C. and the method allows the used noble metal catalyst to be recovered and reused.Type: GrantFiled: July 22, 2003Date of Patent: March 27, 2007Assignee: Mitsui Chemicals, Inc.Inventors: Daisuke Ura, Hiroyuki Katsuta, Toshio Kitashima, Kenichi Sato
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Patent number: 7157585Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: May 11, 2005Date of Patent: January 2, 2007Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Patent number: 7049271Abstract: The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of processes for their preparation and to their use as herbicides and pesticides.Type: GrantFiled: April 25, 2001Date of Patent: May 23, 2006Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jutta Böhmer, Ralf Wischnat, Mark Wilhelm Drewes, Peter Dahmen, Rolf Pontzen, Peter Lösel, Christoph Erdelen, Dieter Feucht
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6927290Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: May 10, 2004Date of Patent: August 9, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Patent number: 6869606Abstract: Biotinylated pharmacologically active agents and complexes containing same are disclosed. In particular, biotinylated-chemokines are described. The complexes further include an anti-biotin antibody that selectively binds to biotin. The complex can be dissociated by contact with free biotin. The complexes are particularly useful for enhancing an immune response to tumor cells and virus-infected cells, in vivo or in vitro.Type: GrantFiled: February 18, 2000Date of Patent: March 22, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: Walter Newman, Dominic Picarella, Dulce Soler
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Patent number: 6849733Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.Type: GrantFiled: August 22, 1997Date of Patent: February 1, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
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Patent number: 6835745Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, R3, X, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 10, 2003Date of Patent: December 28, 2004Assignee: WyethInventors: Richard D. Coghlan, William F. Fobare, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
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Patent number: 6821960Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.Type: GrantFiled: November 16, 2001Date of Patent: November 23, 2004Assignee: Noyo Nordisk Pharmaceuticals, Inc.Inventors: Anker Steen Jørgensen, Peter Madsen
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Publication number: 20040180948Abstract: The present invention relates to a compound of formula (I): 1Type: ApplicationFiled: March 23, 2004Publication date: September 16, 2004Inventors: Joel M. Linden, Ray A. Ollson, Peter J. Scammells
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Publication number: 20040180947Abstract: A sulfonamide compound of the formula (I):Type: ApplicationFiled: March 30, 2004Publication date: September 16, 2004Applicant: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Tsuyoshi Mizutani, Teruo Oku, Noritsugu Yamasaki, Osamu Onomura, Masahiro Nishikawa, Takahiro Hiramura, Takafumi Imoto
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Patent number: 6790866Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: July 30, 2002Date of Patent: September 14, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Patent number: 6774233Abstract: 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: August 10, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Publication number: 20040127548Abstract: Novel anthelmintic compositions containing thiophene derivatives as active ingredients are disclosed.Type: ApplicationFiled: October 16, 2003Publication date: July 1, 2004Inventor: Byung Hyun Lee
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Patent number: 6753337Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: December 21, 2001Date of Patent: June 22, 2004Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Publication number: 20040102636Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: February 1, 2002Publication date: May 27, 2004Applicant: BAYER CORPORATIONInventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
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Publication number: 20040048864Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.Type: ApplicationFiled: December 2, 2002Publication date: March 11, 2004Inventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
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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
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Patent number: 6673967Abstract: A method for processing of hydrogen for the reductive acylation of nitro, azido and cyano arenes is disclosed. More particularly, improved process for the preparation of amides and anilides using C3-C7 carboxylic acids as proton source/acylating agents employing Fe3+-montmorillonite as a catalyst is disclosed.Type: GrantFiled: November 29, 2002Date of Patent: January 6, 2004Assignee: Council of Scientific and Industrial ResearchInventors: Boyapati Manoranjan Choudary, Venkati Sri Ranganath Kalluri, Lakshmi Kantam Mannepalli
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Patent number: 6660732Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: September 25, 2001Date of Patent: December 9, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
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Publication number: 20030225274Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.Type: ApplicationFiled: February 27, 2003Publication date: December 4, 2003Inventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
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Patent number: 6656933Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: September 25, 2001Date of Patent: December 2, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Eugene R. Hickey
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Patent number: 6653483Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: April 17, 2000Date of Patent: November 25, 2003Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20030195354Abstract: An amide compound given by formula [I]: 1Type: ApplicationFiled: December 12, 2002Publication date: October 16, 2003Inventor: Hiroshi Sakaguchi
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Patent number: 6620963Abstract: Compounds of the formula where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR&agr; retinoid receptors.Type: GrantFiled: September 19, 2002Date of Patent: September 16, 2003Assignee: Allergan, Inc.Inventors: Tien T. Duong, Richard Beard, Roshantha A. Chandraratna
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Publication number: 20030162818Abstract: This invention provides a novel acylsulfonamide derivative which can be used as an ACC activity inhibitor effective for the treatment of visceral fat syndrome that becomes the risk-factor of diseases of adult people such as myocardial infarction, cerebral infarction and diabetes.Type: ApplicationFiled: March 4, 2003Publication date: August 28, 2003Applicant: AJINOMOTO CO. INC.Inventors: Hiroshi Ikawa, Masato Nishimura, Keiji Okada, Takashi Nakamura
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Patent number: 6596752Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.Type: GrantFiled: July 12, 2002Date of Patent: July 22, 2003Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn CompanyInventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
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Patent number: 6586459Abstract: 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 28, 2001Date of Patent: July 1, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Junior, 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
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Patent number: 6583282Abstract: 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: July 6, 2000Date of Patent: June 24, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6583173Abstract: 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 28, 2001Date of Patent: June 24, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffrey Bernard Franciskovich, Theodore Goodson, Junior, 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
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Patent number: 6545152Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.Type: GrantFiled: July 18, 2000Date of Patent: April 8, 2003Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Venkatachalam
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Patent number: 6538144Abstract: The invention relates to p-thienylbenzylamides of formula (I) in which R(1), R(2), R(3), R(4), R(5), R(6) and X have the meanings given in the description. The compounds of formula (I) are potent agonists of angiotensin-(1-7) receptors and are useful as pharmaceutically active compounds to treat and/or prevent hypertension; cardiac hypertrophy; cardiac insufficiency; coronary heart diseases, such as angina pectoris; and endothelial dysfunction or endothelial damage as a consequence, for example, of atherosclerotic processes or in association with diabetes mellitus.Type: GrantFiled: March 13, 2002Date of Patent: March 25, 2003Assignee: Aventis Pharma Deutschland GmbHInventor: Holger Heitsch
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Patent number: 6482849Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.Type: GrantFiled: June 23, 1998Date of Patent: November 19, 2002Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn CompanyInventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
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Publication number: 20020165223Abstract: Compounds represented by structural formula I 1Type: ApplicationFiled: September 12, 2001Publication date: November 7, 2002Inventors: William J. Greenlee, Ying Huang, Joseph M. Kelly, Stuart W. McCombie, Andrew W. Stamford, Yusheng Wu
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Patent number: 6476023Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.Type: GrantFiled: November 20, 2000Date of Patent: November 5, 2002Assignee: Boehringen Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan
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Patent number: 6455684Abstract: A method for analyzing an objective substance, comprising reacting a labeled probe with an objective substance on a biological sample, said probe comprising a label substance of the formula (I): wherein A1 is an aromatic group, R1 is a hydrogen or —COCH2COCnF2n+1 and n is an integer of 1-6, which is bonded to a probe selected from the group consisting of nucleic acid, nucleic acid binding protein, low molecular ligand and receptor for ligand (except antibody) to give a fluorescent complex, reacting the complex with an objective substance on a biological sample and assaying fluorescence of the resultant fluorescent complex, a labeled nucleic acid probe and a labeled nucleotide. According to the method of the present invention, defects such as hindrance of fluorescence due to contaminant substance, low sensitivity and the like can be resolved, thereby enabling analysis on a tissue.Type: GrantFiled: September 28, 2001Date of Patent: September 24, 2002Assignees: Toyo Boseki Kabushiki KaishaInventors: Kazuhiro Matsui, Katsunori Ikeda, Shinichi Teshima, Yoshihisa Kawamura, Kazuko Matsumoto
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Patent number: 6448290Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: June 18, 1999Date of Patent: September 10, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Patent number: 6358945Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: February 16, 2000Date of Patent: March 19, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Proudfoot, John R. Regan, Alan D. Swinamer, Hidenori Takahashi
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Patent number: 6350761Abstract: This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.Type: GrantFiled: July 24, 2000Date of Patent: February 26, 2002Assignee: Berlex Laboratories, Inc.Inventors: William J. Guilford, Steven T. Sakata, Kenneth J. Shaw, Shung Wu, Wei Xu, Zuchun Zhao
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Publication number: 20020002199Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.Type: ApplicationFiled: March 11, 1999Publication date: January 3, 2002Inventors: LONE JEPPESEN, HENRIK SUNE ANDERSEN, OLE HVILSTED OLSEN, LUKE MILBURN JUDGE, DANIEL DALE HOLSWORTH, FARID BAKIR, FRANK URBAN AXE, YU GE