Chalcogen Or Nitrogen Attached Directly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/251)
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Patent number: 6756378Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are pharmaceutical compositions, methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion, which involve compounds of Formula I.Type: GrantFiled: December 28, 2001Date of Patent: June 29, 2004Assignees: Pharmacopeia Drug Discovery, Inc., Daiichi Pharmaceutical Co., Ltd.Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Shin Iimura, Yoshiyuki Yoneda
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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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Publication number: 20040006236Abstract: A compound of formula 1a 1Type: ApplicationFiled: January 22, 2003Publication date: January 8, 2004Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Publication number: 20030224943Abstract: The instant invention relates to novel tetrazole derivatives of the formula (I) wherein R1 represents halogen, methyl, ethyl, halomethyl, methoxy, ethoxy, C1-2 haloalkoxy, methylthio, ethylthio, C1-3 alkylsulfonyl, methylsulfonyloxy, ethylsulfonyloxy, nitro or cyano, R2 represents C1-6 alkyl, C3-6 cycloalkyl which may be optionally substituted with halogen or C1-3 alkyl, C1-4 haloalkyl, C2-6 alkenyl, or phenyl which may be optionally substituted with halogen, C1-3 alkyl, C1-4 haloalkyl, C2-6 alkenyl, or phenyl which may be optionally substituted with halogen, C1-3 alkyl, C1-2 haloalkyl or nitro, m represents 0, 1 or 2, two R1 s may be identical or different, in case m represents 2, n represents 1 or 2, Q represents one the cyclic groups which are mentioned in the specification, to intermediates and several processes for their preparation, to their use as herbicides and to novel compositions containing them.Type: ApplicationFiled: February 20, 2003Publication date: December 4, 2003Inventors: Akihiko Yanagi, Shinichi Narabu, Toshio Goto, Chieko Ueno, Shinichi Shirakura
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Publication number: 20030212116Abstract: A heterocyclic imino compound of the formula (1) and an agrochemically acceptable salt thereof; and an agricultural chemical, fungicide and insecticide containing at least one member selected from the group of such compounds as an active ingredient: 1Type: ApplicationFiled: June 25, 2002Publication date: November 13, 2003Inventors: Toshio Niki, Takashi Mizukoshi, Hiroaki Takahashi, Jun Satow, Tomoyuki Ogura, Kazuhiro Yamagishi, Hiroyuki Suzuki, Fumio Hayasaka
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Patent number: 6624121Abstract: Novel tetrazolinones with herbicidal activity are disclosed. The tetrazolinones of the present invention are represented by the general formula (I) wherein R1, R2, m, n and Q are as defined in the specification. A process for making the tetrazolinones of the present invention is also disclosed.Type: GrantFiled: February 5, 2002Date of Patent: September 23, 2003Assignee: Nihon Bayer Agrochem K.K.Inventors: Akihiko Yanagi, Shinichi Narabu, Toshio Goto, Seishi Ito, Chieko Ueno
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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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Patent number: 6583165Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: February 21, 2001Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Publication number: 20030113132Abstract: A novel charge transport compound, a novel process using that novel compound and an organophotoreceptor includes:Type: ApplicationFiled: August 9, 2002Publication date: June 19, 2003Applicant: Samsung Information Systems AmericaInventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait
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Publication number: 20030114681Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.Type: ApplicationFiled: August 30, 2002Publication date: June 19, 2003Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6576632Abstract: The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.Type: GrantFiled: April 13, 2000Date of Patent: June 10, 2003Assignee: Pfizer IncInventors: Steven W. Goldstein, Kelly P. Longo, James F. Blake, Mohamed M. A. Awad, Kenneth P. Raiche, Kevin W. Kramer
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Patent number: 6570022Abstract: A process of preparing bis-(1(2)H-tetrazol-5-yl)-amine monohydrate is provided including combining a dicyanamide salt, an azide salt and water to form a first reaction mixture, adding a solution of a first strong acid characterized as having a pKa of less than about 1 to said first reaction mixture over a period of time characterized as providing a controlled reaction rate so as to gradually form hydrazoic acid without loss of significant quantities of hydrazoic acid from the solution while heating the first reaction mixture at temperatures greater than about 65° C., heating the resultant reaction mixture at temperatures greater than about 65° C. for a period of time sufficient to substantially completely form a reaction product, treating the reaction product with a solution of a second strong acid to form a product of bis-(1(2)H-tetrazol-5-yl)-amine monohydrate, and, recovering the bis-(1(2)H-tetrazol-5-yl)-amine monohydrate product.Type: GrantFiled: September 21, 2001Date of Patent: May 27, 2003Assignee: The Regents of the University of CaliforniaInventors: Darren L. Naud, Michael A. Hiskey
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Publication number: 20030092685Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.Type: ApplicationFiled: October 25, 2002Publication date: May 15, 2003Inventors: Theodore J. Nitz, Daniel C. Pevear
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Patent number: 6552051Abstract: Novel compounds are provided having the structural formula R[—N(NO2)—L—R1]n wherein R, L, R1 and n are defined herein. The compounds are useful in a variety of contexts, but are primarily to be used as high energy oxidizing agents in explosive compositions, propellant formulations, gas-generating compositions and the like. The compounds are also useful as pharmaceutical agents. Compositions containing the compounds are also provided, including energetic compositions, as are methods for using the novel compounds and compositions.Type: GrantFiled: June 7, 2001Date of Patent: April 22, 2003Assignee: SRI InternationalInventors: Jeffrey C. Bottaro, Robert J. Schmitt, Mark A. Petrie, Paul E. Penwell
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Publication number: 20030073839Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: ApplicationFiled: March 7, 2000Publication date: April 17, 2003Inventors: Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Anne-Marie Campbell, Timothy G. Lease, James H. Cook
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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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Publication number: 20030060634Abstract: A process of preparing bis-(1(2)H-tetrazol-5-yl)-amine monohydrate is provided including combining a dicyanamide salt, an azide salt and water to form a first reaction mixture, adding a solution of a first strong acid characterized as having a pKa of less than about 1 to said first reaction mixture over a period of time characterized as providing a controlled reaction rate so as to gradually form hydrazoic acid without loss of significant quantities of hydrazoic acid from the solution while heating the first reaction mixture at temperatures greater than about 65° C., heating the resultant reaction mixture at temperatures greater than about 65° C. for a period of time sufficient to substantially completely form a reaction product, treating the reaction product with a solution of a second strong acid to form a product of bis-(1(2)H-tetrazol-5-yl)-amine monohydrate, and, recovering the bis-(1(2)H-tetrazol-5-yl)-amine monohydrate product.Type: ApplicationFiled: September 21, 2001Publication date: March 27, 2003Inventors: Darren L. Naud, Michael A. Hiskey
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Publication number: 20030032626Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: 1Type: ApplicationFiled: June 13, 2002Publication date: February 13, 2003Inventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
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Patent number: 6515124Abstract: Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and accordingly reduce or eliminate inflammatory skin disease psoriasis.Type: GrantFiled: January 5, 2001Date of Patent: February 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Publication number: 20030004193Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.Type: ApplicationFiled: July 23, 2002Publication date: January 2, 2003Inventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Lu-Yan Zhang
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Patent number: 6498004Abstract: This invention provides a photographic element comprising at least one silver halide emulsion layer in which the silver halide is sensitized with a compound of the formula (a): &Dgr;−(t)m−XY′ (a) XY′−(t)m−&Dgr; (b) &Dgr;−(t)m−XY′−(t)m−&Dgr; (c) wherein &Dgr; is protective group that is eliminated during development of the photographic element, t is a timing group, m is an integer from 0 to 3, and XY′ is a fragmentable electron donor moiety in which X is an electron donor group and Y′ is a leaving proton H or a leaving group Y, with the proviso that if Y′ is a proton, a base, &bgr;−, is present in the emulsion or is covalently linked directly or indirectly to X, and wherein: 1) X—Y′ has an oxidation potential between 0 and about 1.Type: GrantFiled: December 28, 2000Date of Patent: December 24, 2002Assignee: Eastman Kodak CompanyInventors: Jerome R. Lenhard, Annabel A. Muenter, Stephen A. Godleski, Paul A. Zielinski, Deepak Shukla, Donald R. Diehl
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Patent number: 6495580Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.Type: GrantFiled: October 18, 1999Date of Patent: December 17, 2002Assignee: ViroPharma IncorporatedInventors: Theodore J. Nitz, Daniel C. Pevear
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Publication number: 20020161224Abstract: Diaryl ether compounds useful in the control of weeds are described.Type: ApplicationFiled: February 9, 2001Publication date: October 31, 2002Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Hiroshi Shimoharada, Masamitsu Tsukamoto
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Patent number: 6458580Abstract: A method for promoting the growth of at least one anaerobic fungus in the rumen of a ruminant animal, the method comprising the step of administering to the rumen an effective amount of a degradation resistant sulphur source.Type: GrantFiled: September 27, 2000Date of Patent: October 1, 2002Assignees: Commonwealth Scientific and Industrial Research Organisation, Australian Wool Research and Promotion OrganizationInventors: Geoffrey Leslie Raymond Gordon, Michael William Phillips
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Publication number: 20020133007Abstract: Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) 1Type: ApplicationFiled: August 16, 2001Publication date: September 19, 2002Applicant: ISK AMERICAS INCORPORATEDInventors: Sandeep Gupta, Shao-Yong Wu, Masamitsu Tsukamoto, David A. Pulman, Bai-Ping Ying
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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: 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: 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: 6436965Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts and hydrates thereof are disclosed as useful for treating or preventing diseases and conditions mediated by PDE-IV. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: March 1, 2001Date of Patent: August 20, 2002Assignee: Merck Frosst Canada & Co.Inventors: Marc Labelle, Claudio Sturino, Nicolas Lachance, Dwight Macdonald
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Patent number: 6437169Abstract: 1. A 1-naphthol compound represented by formula (I) below: wherein A represents the moiety of a compound having an acidic proton the pKa of a corresponding protonated form (AH) of which is 0 to 14, R1 represents an aliphatic group, aryl group, or heterocyclic group, R2 represents a substituent, n represents an integer of 0 to 5, X represents a hydrogen atom, halogen atom, R11—, R11O—, R11S—, R11OCOO—, R12COO—, R12(R13)NCOO—, R12CON(R13)—, —NO, —NO2, or —N═N—R11, wherein R11 represents an aliphatic group, aryl group, or heterocyclic group, and each of R12 and R13 independently represents a hydrogen atom, aliphatic group, aryl group, or heterocyclic group, and Y represents an oxygen atom or sulfur atom.Type: GrantFiled: June 19, 2000Date of Patent: August 20, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Takayuki Ito, Koji Takaku
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Publication number: 20020082283Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: ApplicationFiled: September 13, 2001Publication date: June 27, 2002Applicant: Gliatech, Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
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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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Publication number: 20020077486Abstract: Novel compounds of formulae (I) to (VIII), 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) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 2, 2001Publication date: June 20, 2002Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-MaGuire
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Patent number: 6399641Abstract: The present invention is a series of 2H-tetrazole-5-yl-amide derivatives showing activity as ligands of metabotropic glutamate receptors.Type: GrantFiled: June 27, 2001Date of Patent: June 4, 2002Assignee: Hoffmann-la Roche Inc.Inventors: Synese Jolidon, Vincent Mutel, Eric Vieira, Juergen Wichmann
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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: 20020022648Abstract: The present invention is a series of 2H-tetrazole-5-yl-amide derivatives showing activity as ligands of metabotropic glutamate receptors.Type: ApplicationFiled: June 27, 2001Publication date: February 21, 2002Inventors: Synese Jolidon, Vincent Mutel, Eric Vieira, Juergen Wichmann
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Patent number: 6342245Abstract: The present invention is concerned with novel pharmaceutical compositions of lipid lowering agents which can be administered to a mammal suffering from hyperlipidemia, obesitas or atherosclerosis, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising a lipid lowering agent and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.Type: GrantFiled: April 24, 2000Date of Patent: January 29, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Baert, Geert Verreck
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Publication number: 20020006946Abstract: The present invention relates to tetrazole compounds of Formula I, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, and pharmaceutically acceptable salts of the prodrugs.Type: ApplicationFiled: January 23, 2001Publication date: January 17, 2002Inventors: Gary E. Aspnes, Yuan-Ching P. Chiang
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Publication number: 20020006947Abstract: This invention relates to compounds having the Formula I: 1Type: ApplicationFiled: March 22, 2001Publication date: January 17, 2002Inventors: Derk J. Hogenkamp, Phong Nguyen, Ji Yang
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Patent number: 6335459Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor agonists, and which are represented by Formula I: wherein R1, R2, R3, R4, R5, A, and B are as defined in the specification, and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: December 7, 1999Date of Patent: January 1, 2002Assignee: Syntex (U.S.A.) LLCInventors: Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Daniel Lee Severance
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Publication number: 20010053855Abstract: Compounds of the invention having general formula (I) 1Type: ApplicationFiled: December 22, 2000Publication date: December 20, 2001Applicant: ISIS Pharmaceuticals, Inc.Inventor: Muthiah Manoharan
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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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Patent number: 6306852Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 oType: GrantFiled: April 24, 2000Date of Patent: October 23, 2001Assignee: Pfizer Inc.Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
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Patent number: 6300498Abstract: The 1,5′-bitetrazole of the invention comprises 1,5′-bitetrazole, and ammonia or an amine. The 1,5′-bitetrazole of the invention decomposes sharply and generates a nontoxic gas.Type: GrantFiled: July 23, 1999Date of Patent: October 9, 2001Assignee: Toyo Kasei Kogyo Company LimitedInventors: Hiroaki Tanaka, Kunihiro Shimamoto, Atuhiro Onishi
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Patent number: 6277790Abstract: Tetrazolinonecarboxamides of formula I wherein Het is oxetan-3-yl, thietan-3-yl, tetrahydrofuran-3-yl, furan-3-yl, tetrahydrothiophen-3-yl, thiophen-3-yl, tetrahydro-2H-pyran-3-yl, tetrahydro-2H-thiopyran-3-yl, tetrahydro-2H-pyran-4-yl or tetrahydro-2H-thiopyran-4-yl, in each case with or without substitution; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, or 3- to 7-membered heterocyclyl; R2 is hydrogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, or is optionally substituted cycloalkyl, cycloalkylalkyl, phenyl, phenylalkyl, 3- to 7-membered heterocyclyl, or 3- to 7-membered heterocyclylalkyl, their preparation and herbicidal compositions comprising them.Type: GrantFiled: February 1, 2000Date of Patent: August 21, 2001Assignee: BASF AktiengesellschaftInventors: Cyrill Zagar, Gerhard Hamprecht, Markus Menges, Olaf Menke, Robert Reinhard, Peter Schäfer, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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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
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Patent number: 6232334Abstract: 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 II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes,Type: GrantFiled: August 18, 1999Date of Patent: May 15, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6184383Abstract: There is disclosed a method of producing acetals, which comprises reacting a compound of formula (I), at least one compound selected from a group consisting of a compound of formula (II), paraformaldehyde, and trioxane; and a compound of formula (III), to synthesize an acetal of formula (IV), wherein the reaction is carried out in the presence of an oxidizing agent and an acid: wherein R1 is an alkyl group etc., R2 is an alkyl or aryl group, R3 and R4 each independently are a hydrogen atom, an alkyl group or an aryl group, X1 and X2 each are a group of nonmetal atoms necessary to form a 5- or 6-membered N-containing heteroring, and M is a hydrogen atom or a cation. This method can give acetal compounds with good efficiency and a high yield.Type: GrantFiled: November 18, 1999Date of Patent: February 6, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Atsuo Kondoh, Fumio Iwamoto
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Patent number: 6174839Abstract: The invention is related to a novel phenylacetylene derivates of formula: wherein X represents hydrogen, halogen, optionally substituted C1-6 alkyl; Y represents hydrogen, halogen, cyano, nitro, optionally substituted C1-6 alkyl, C1-6 alkoxy, C3-8 cycloalkoxy, optionally substituted C1-6 alkylthio, C3-8 cycloalkylthio, C1-6 alkylsulfinyl, optionally substituted C1-6 alkylsulfonyl, C3-8 cycloalkylsulfonyl, C1-6 alkylsulfonyloxy, optionally substituted sulfonamide, optionally substituted carboxamide, etc., or Y may form together with Z which is bonded to the vicinal carbon atom a 5- or 6-membered ring; n is 0 or 1; Z represents hydrogen or halogen; m is 1 or 2; R represents hydrogen, halogen, C1-6 alkyl, tri(C1-6 alkyl)silyl, COORc or CONRdRe; Q represents a heterocyclic group, and their use as herbicid.Type: GrantFiled: February 23, 1999Date of Patent: January 16, 2001Assignee: Nihon Bayer Agrochem K.K.Inventors: Akihiko Yanagi, Shin-ichi Narabu, Toshio Goto, Seishi Ito, Natsuko Minegishi, Tatsuya Yamaoka, Chieko Ueno
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Patent number: 6172057Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: February 19, 1998Date of Patent: January 9, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell