Nitrogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/254)
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Publication number: 20030176399Abstract: The present invention is directed to formulations comprising 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Methods of treating diseases related to abnormal PK activity utilizing the formulations comprising these compounds and methods of making these formulations are also disclosed.Type: ApplicationFiled: November 21, 2002Publication date: September 18, 2003Applicant: SUGEN INCORPORATEDInventors: Ping Gao, Anand Sistla, Narmada Shenoy
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Patent number: 6608210Abstract: A method for producing a compound represented by the formula: wherein the ring A is a benzene ring which may be substituted in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.Type: GrantFiled: January 16, 2002Date of Patent: August 19, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Publication number: 20030153567Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: ApplicationFiled: January 29, 2003Publication date: August 14, 2003Applicant: SmithKline Beecham CorporationInventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
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Publication number: 20030149015Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula 1Type: ApplicationFiled: December 10, 2002Publication date: August 7, 2003Inventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
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Publication number: 20030144253Abstract: The present invention relates to acyclic and cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 30, 2002Publication date: July 31, 2003Inventors: Michael Mullican, David Lauffer, Roger Tung
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Publication number: 20030144281Abstract: Disclosed are substituted benzimidazole compounds of formula(I): 1Type: ApplicationFiled: November 5, 2002Publication date: July 31, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles Cywin, Jinbo Lee, Steven S. Pullen, Gregory Paul Roth, Christopher Ronald Sarko, Roger John Snow, Noel Stewart Wilson
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Publication number: 20030144290Abstract: Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.Type: ApplicationFiled: October 21, 2002Publication date: July 31, 2003Applicant: NEUROGEN CORPORATIONInventors: Charles A. Blum, Harry L. Brielmann, Stephane De Lombaert, Xiaozhang Zheng
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Patent number: 6593355Abstract: Novel benzimidazoles having antithrombotic activity. Exemplary are: (a) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, (b) 2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, and (c) (R)-2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(isobutyloxycarbonylmethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole.Type: GrantFiled: July 3, 2002Date of Patent: July 15, 2003Assignee: Boehringer Ingelehim Pharma KGInventors: Uwe Ries, Iris Kaufmann-Hefner, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6589914Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 4, 2002Date of Patent: July 8, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Publication number: 20030109547Abstract: An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.Type: ApplicationFiled: June 5, 2002Publication date: June 12, 2003Applicant: AJINOMOTO CO. INCInventors: Masayuki Sugiki, Kazuyuki Sagi, Kohichi Fujita, Takashi Kayahara, Shunji Takehana, Kuniya Sakurai, Kazumi Tashiro
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Publication number: 20030083315Abstract: The present invention provides a benzimidazole derivative or its. pharmaceutically permissible salt expressed by the following formula (1). Further, the present invention provides a human chymase activity inhibitor containing the substance as an active ingredient.Type: ApplicationFiled: September 14, 2001Publication date: May 1, 2003Inventors: Naoki Tsuchiya, Yoshiyuki Matsumoto, Hiroshi Saitou, Tsuyoshi Mizuno
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Patent number: 6521650Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: April 4, 2000Date of Patent: February 18, 2003Assignee: Pfizer, Inc.Inventors: Thomas Richard Belliotti, Justin Stephen Bryans, Thomas Capiris, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
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Patent number: 6518289Abstract: Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.Type: GrantFiled: April 3, 2000Date of Patent: February 11, 2003Assignee: Pfizer, Inc.Inventors: Justin Stephen Bryans, Thomas Capiris, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
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Publication number: 20030018013Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: October 11, 2001Publication date: January 23, 2003Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Publication number: 20030009034Abstract: This invention relates to a transition metal mediated process for the preparation of optionally substituted 2-amino-benzoxazoles and or 2-amino-benzimidazoles, which are useful as therapeutic agents or as intermediates in the synthesis of therapeutic agents.Type: ApplicationFiled: March 22, 2002Publication date: January 9, 2003Inventors: Neil Wishart, Kurt Ritter
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Publication number: 20030004356Abstract: Novel benzimidazoles having antithrombotic activity.Type: ApplicationFiled: July 3, 2002Publication date: January 2, 2003Applicant: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Iris Kaufmann-Hefner, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6479518Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.Type: GrantFiled: September 21, 2001Date of Patent: November 12, 2002Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
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Publication number: 20020151574Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1Type: ApplicationFiled: October 5, 2001Publication date: October 17, 2002Inventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao
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Publication number: 20020151723Abstract: A method for producing a compound represented by the formula: 1Type: ApplicationFiled: January 16, 2002Publication date: October 17, 2002Applicant: TAKEDA CHEMICAL INDUSTRIES, LTD.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6451833Abstract: A class of N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders.Type: GrantFiled: November 1, 2000Date of Patent: September 17, 2002Assignee: Pharmacia CorporationInventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
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Patent number: 6451832Abstract: Novel benzimidazoles having antithrombotic activity. Exemplary are: (a) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, (b) 2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, and (c) (R)-2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(isobutyloxycarbonylmethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole.Type: GrantFiled: December 12, 2000Date of Patent: September 17, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Iris Kaufmann-Hefner, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6444840Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: September 3, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
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Patent number: 6444701Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: November 8, 2001Date of Patent: September 3, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini
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Patent number: 6441015Abstract: The present invention relates to tetrazole compounds of Formula I, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, and pharmaceutically acceptable salts of the prodrugs. The invention also relates to compositions comprising the tetrazole compounds and to methods of treating obesity, diabetes, atherosclerosis, hypertension, coronary heart disease, hypercholesterolemia, hyperlipidemia, thyroid disease, thyroid cancer, hypothyroidism, depression, glaucoma, cardiac arrhythmias, congestive heart failure, and osteoporosis using the tetrazole compounds.Type: GrantFiled: January 23, 2001Date of Patent: August 27, 2002Assignee: Pfizer Inc.Inventors: Gary E. Aspnes, Yuan-Ching P. Chiang
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Patent number: 6441177Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.Type: GrantFiled: December 16, 1999Date of Patent: August 27, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
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Patent number: 6436974Abstract: The instant invention is a novel series of amino heterocycles useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, and sleep disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: November 30, 2001Date of Patent: August 20, 2002Assignee: Warner-Lambert CompanyInventors: Thomas Richard Belliotti, Andrew John Thorpe, David Juergen Wustrow
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Patent number: 6426359Abstract: This invention relates to the use of EP2 receptor subtype selective prostaglandin E2 agonists to augment bone mass including the prevention and treatment of skeletal disorders in mammals, including humans.Type: GrantFiled: June 11, 1999Date of Patent: July 30, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L Rosati, David D. Thompson
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Patent number: 6426360Abstract: A class of compounds is described for treating inflammation and inflammation-related disorders.Type: GrantFiled: May 15, 2000Date of Patent: July 30, 2002Assignee: G D Searle & Co.Inventors: Richard M Weier, Paul W Collins, Michael A Stealey, Thomas E Barta, Renee M Huff
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Patent number: 6417215Abstract: Novel calcilytic compounds are provided.Type: GrantFiled: July 26, 2001Date of Patent: July 9, 2002Assignee: SmithKline Beecham CorporationInventor: Amparo Maria Lago
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Patent number: 6410780Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: June 25, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
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Patent number: 6388088Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: October 11, 2001Date of Patent: May 14, 2002Assignee: Hoffman-La Roche Inc.Inventor: Achyutharao Sidduri
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Patent number: 6376532Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: GrantFiled: January 25, 2001Date of Patent: April 23, 2002Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Publication number: 20020045650Abstract: The present invention provides novel compounds of Formula I: 1Type: ApplicationFiled: August 10, 2001Publication date: April 18, 2002Inventor: Richard Laurence Mackman
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Patent number: 6369232Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: August 8, 2001Date of Patent: April 9, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Achyutharao Sidduri
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Publication number: 20020038028Abstract: Compounds of the formula 1Type: ApplicationFiled: November 21, 2001Publication date: March 28, 2002Inventors: Daniel Yohannes, Mark W. Bundesmann
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Publication number: 20020037912Abstract: The present invention provides novel compounds of Formula I: 1Type: ApplicationFiled: August 10, 2001Publication date: March 28, 2002Inventor: Ellen M. Leahy
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Publication number: 20020035262Abstract: Compounds of the formula 1Type: ApplicationFiled: November 21, 2001Publication date: March 21, 2002Inventors: Daniel Yohannes, Mark W. Bundesmann
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Publication number: 20020035267Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: ApplicationFiled: October 11, 2001Publication date: March 21, 2002Inventor: Achyutharao Sidduri
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Publication number: 20020032224Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: ApplicationFiled: September 14, 2001Publication date: March 14, 2002Applicant: ICOS CorporationInventors: Kerry W. Fowler, Joshua Odingo
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Patent number: 6355808Abstract: Benzimidazole derivatives of the formula (I): wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin Π antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.Type: GrantFiled: March 27, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Publication number: 20020028748Abstract: There are provided 3-heterocyclic substituted benzisothiazole and benzisoxazole compounds having the structural formula I 1Type: ApplicationFiled: April 17, 2001Publication date: March 7, 2002Applicant: Intellectual Property Department BASF AktiengesellschaftInventors: Peter John Wepplo, Richard Anthony Rampulla, Gavin David Heffernan, Michael Vernie Cossette, Charles Malcolm Langevine, Venkataraman Kameswaran, Robert Eugene Diehl, James Joseph Fiordeliso, Gregory Jay Haley, Michael Anthony Guaciaro
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Publication number: 20020025961Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 5, 2001Publication date: February 28, 2002Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
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Patent number: 6350880Abstract: The present invention provides a crystalline or crystallized acid addition salt of Losartan useful for obtaining highly pure 2-n-butyl-4-chloro-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol (Losartan), and a purification method of Losartan that includes production of the crystalline or crystallized acid addition salt.Type: GrantFiled: November 16, 2000Date of Patent: February 26, 2002Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Tadashi Katsura, Hiroshi Shiratani, Nobushige Itaya
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Patent number: 6350774Abstract: This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.Type: GrantFiled: January 24, 2000Date of Patent: February 26, 2002Assignee: Eli Lilly And CompanyInventors: Nicholas J Bach, Jolie A. Bastian, Nickolay Y Chirgadze, Michael L Denney, Robert J. Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Publication number: 20020022647Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula 1Type: ApplicationFiled: August 16, 2001Publication date: February 21, 2002Inventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
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Patent number: 6323230Abstract: Derivatives of general chemical formula L(I) and (IV) are used in the topical treatment of diseases of the epithelial tissues, like psoriasis (epidermis) and ulcerative colitis L(lower intestine). These compounds display a high efficacy when administered for example by epicuaneous route in the case of dermatological illnesses like psoriasis, atopic dermatitis and other similar affections, or when administered by oral or rectal route in the case of diseases of the epithelia of the lower intestine like the ulcerative colitis and Crohn's disease.Type: GrantFiled: April 24, 2000Date of Patent: November 27, 2001Assignee: Geange Ltd.Inventor: Carla Rossi
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Publication number: 20010039290Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: ApplicationFiled: March 14, 2001Publication date: November 8, 2001Inventors: John R. Regan, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
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Patent number: 6300364Abstract: Pharmaceutical compositions having a cholesterol-lowering effect which comprises as the active ingredient a compound having a PPAR (peroxisome proliferator-activated receptor)&dgr; activating effect or a PPAR&dgr;- and PPAR&ggr;-activating effect or a pharmaceutically acceptable salt thereof; pharmaceutical compositions wherein the cholesterol-lowering effect is an LDL-cholesterol-lowering effect; and a method for identifying a compound having a cholesterol-lowering effect characterized by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect thereof. Means for Solution: It is found out that a compound exerting an excellent cholesterol-lowering effect on higher animals such as humans and ape has an effect of activating PPAR&dgr; or PPAR&dgr; and PPAR&ggr;.Type: GrantFiled: January 24, 2000Date of Patent: October 9, 2001Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Teruhiko Shimokawa, Satomi Nishijima, Koyo Matsuda, Yuichi Iizumi, Seiichi Hashimoto
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Patent number: 6271237Abstract: The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D is substituted ortho to G on E and may be CH2NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: December 21, 1998Date of Patent: August 7, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Robert A. Galemmo, Jr., Lori L. Bostrom, Donald J. P. Pinto, Karen A. Rossi