Additional Ring Containing Patents (Class 546/337)
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Publication number: 20040147569Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: ApplicationFiled: January 9, 2004Publication date: July 29, 2004Applicant: Schering AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi
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Publication number: 20040122063Abstract: The invention relates a compound represented by the formula (1):Type: ApplicationFiled: July 30, 2003Publication date: June 24, 2004Inventors: Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Kenji Yoshikawa, Hideyuki Kanno, Masatoshi Nagamochi
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Publication number: 20040077694Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.Type: ApplicationFiled: October 10, 2003Publication date: April 22, 2004Inventors: Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
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Patent number: 6720335Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: March 8, 2002Date of Patent: April 13, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
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Patent number: 6696456Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, R4, R5, R6, G and Z have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: October 13, 2000Date of Patent: February 24, 2004Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Norman Eugene Ohler, Kelly Michelle Solinsky, Neil Gregory Almstead, Biswanath De, Michael George Natchus
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Patent number: 6677360Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: April 6, 2001Date of Patent: January 13, 2004Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6660885Abstract: The invention relates to polycyclic aryl and heteroaryl substituted benzene compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: March 13, 2001Date of Patent: December 9, 2003Assignee: Pharmacia CorporationInventors: Michael S. South, John J. Parlow
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Patent number: 6656958Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.Type: GrantFiled: February 1, 2001Date of Patent: December 2, 2003Assignee: Abbott LaboratoriesInventors: Nan-Horng Lin, Liming Dong
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Patent number: 6632823Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.Type: GrantFiled: December 22, 1997Date of Patent: October 14, 2003Assignee: Merck & Co., Inc.Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
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Patent number: 6630495Abstract: Compounds of formula (I) or (II): or salts therefor are used as phytopathogenic fungicides wherein the various radicals and substitutents are as defined in the description. Pesticidal compositions contain these compounds together with an agriculturally acceptable diluent or carrier. The compounds and compositions are applied in methods for combating pests.Type: GrantFiled: July 22, 2002Date of Patent: October 7, 2003Assignee: Bayer Cropscience GmbHInventors: Tracey Cooke, Tennyson Ekwuru, David Hardy, Peter Millward, Brian Moloney, Andrew Pettinger, Peter Stanley Thomas, Richard Michael Turner
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Patent number: 6624309Abstract: Benzoic acid derivatives of the formula where X is oxygen, sulfur, —NH, —NR1, —N—CN, —N—OR1 or —N—NO2; Y is a single bond, —C═C—, or —NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo, or (heterocyclo)alkyl; and R2 is aryl or heterocyclo. The compounds of formula I are useful in the treatment of arrhythmia.Type: GrantFiled: September 25, 2002Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss
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Patent number: 6605625Abstract: Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters. Compounds of the invention include compounds of the formula I in which: A1, A2, A3, A4, A5, A6, A7 and A8 independently of one another are chosen from nitrogen, CH and CR(5), at least four of these groups being CH, and wherein all other variables are as defined here.Type: GrantFiled: November 29, 2001Date of Patent: August 12, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Patent number: 6586598Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.Type: GrantFiled: May 8, 2002Date of Patent: July 1, 2003Assignee: Geneva Pharmaceuticals, Inc.Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
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Patent number: 6570020Abstract: A process for preparing a compound of the formula useful as a non-steroidal glucocorticoid receptor modulator.Type: GrantFiled: October 22, 2001Date of Patent: May 27, 2003Assignee: Pfizer Inc.Inventors: Jerry A. Murry, Timothy D. White
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Patent number: 6566380Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.Type: GrantFiled: July 24, 2001Date of Patent: May 20, 2003Assignee: ICAgen, Inc.Inventors: Aimee Dolores Reed, Michael Francis Gross, Serge Beaudoin
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Patent number: 6555562Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Ar is an optionally substituted aromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: February 26, 1999Date of Patent: April 29, 2003Assignee: Celltech R&D LimitedInventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
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Patent number: 6534499Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: March 18, 2003Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
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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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Patent number: 6512121Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: June 11, 2001Date of Patent: January 28, 2003Assignee: G.D. Searle & Co.Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6503928Abstract: Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.Type: GrantFiled: September 18, 2001Date of Patent: January 7, 2003Assignee: WyethInventors: Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Wayne E. Childers
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Patent number: 6503933Abstract: Compounds of formula (I) and salts thereof as phytopathogenic fungicides wherein A1 is substituted 2-pyridyl; A2 is optionally substituted phenyl; L is —(C═O)—, —SO2— or —(C═S)—; R1 is hydrogen, optionally substituted alkyl or acyl; and R2 is hydrogen or optionally substituted alkyl are useful phytopathogenic fungicides.Type: GrantFiled: September 21, 2000Date of Patent: January 7, 2003Assignee: Aventis CropScience UK LimitedInventors: Brian Anthony Moloney, David Hardy, Elizabeth Anne Saville-Stones
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Patent number: 6500832Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 14, 2000Date of Patent: December 31, 2002Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Patent number: 6489364Abstract: Compounds of formula (I), wherein A′ and A″ are independently the same or different group of formula (II) wherein: R′ is H, CH3, C(CH3)2, —ORa, —N(Ra)2, —N(Ra)ORa or —DP; R′″ is H or CH3; Ra is H, C1-C3 alkyl; D is a bond, alkylene, —C(═O)—, —S(O)— or S(O)2—; P is an optionally substituted, mono or bicyclic carbo- or hetereocycle; R″ is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or —C(═O)N(R′″)—; Q is absent, a bond, —CH(OH)— or CH2—; or R″ together with Q, M and R′ define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R′ is —ORa, —, N(Ra)2, —N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH3, Y is H, OH, OCH3, but X and Y areType: GrantFiled: June 21, 2001Date of Patent: December 3, 2002Assignee: Medivir ABInventors: Bjorn Classon, Ingemar Sven-Anders Kvarnstrom, Bengt Bertil Samuelsson
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Patent number: 6486193Abstract: The present invention provides novel 3-substituted pyrrolidines of the formula useful in as inhibitors of matrix metallo-proteinases (MMPs). Pharmaceutical compositions containing said compounds as well as methods of treating disease states responding to inhibition of matrix metalloproteinase are also claimed herein.Type: GrantFiled: March 23, 2001Date of Patent: November 26, 2002Assignee: Aventis Pharmaceuticals Inc.Inventor: Gary A. Flynn
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Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
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Patent number: 6476056Abstract: An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are the same or different, and are each a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyridyl group or a naphthyl group, provided that Ar1 and Ar2 are not both phenyl or both naphthyl and are not phenyl and naphthyl, R1 is a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a substituted or unsubstituted phenyl group or a group of the formula: —NR2(R3) (wherein R2 and R3 are the same or different, and are each a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, X1 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a halogen atom, a trifluoromethyl group, a carbamoyl group or an aminosulfonyl group, Y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; and pharmaceutically acceptablType: GrantFiled: August 7, 2001Date of Patent: November 5, 2002Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshio Nakamura, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Kenji Yamamoto, Koichiro Harada, Masanori Yoshida
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Patent number: 6472413Abstract: One embodiment of the present invention relates to heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which R(1), R(2), R(3), R(4), Het, X, Y and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an at inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart, or vagal dysfunction of the heart, or for the prevention of sudden cardiac death.Type: GrantFiled: November 2, 2001Date of Patent: October 29, 2002Assignee: Adventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert
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Patent number: 6472349Abstract: Pyridine-2,3-dicarboxamides of the formula I in which the variables are as defined in the description, which are suitable for use as herbicides or for the desiccation or defoliation of plants are described.Type: GrantFiled: September 28, 2001Date of Patent: October 29, 2002Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Markus Menges, Olaf Menke, Robert Reinhard, Ingo Sagasser, Cyrill Zagar, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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Patent number: 6472414Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X, are as defined herein.Type: GrantFiled: May 18, 1999Date of Patent: October 29, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Patent number: 6465471Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: July 1, 1999Date of Patent: October 15, 2002Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
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Patent number: 6462158Abstract: Disclosed herein are polymerizable compounds represented by the following formula (1): wherein one of R1 and R2 represents an alkyl group, which has 1 to 4 carbon atoms and is other than a tert-butyl group, and the other represents a hydrogen atom or an alkyl group which has 1 to 4 carbon atoms and is other than a tert-butyl group, R3 to R9 each independently represent a hydrogen atom, a silyl group, a cyano group, a hydroxyl group, a halogen atom or a monovalent nonpolymerizable organic substituent group, and A represents a polymerizable group having a carbon-carbon double bond; polymers obtained by singly polymerizing the polymerizable compounds or copolymerizing them with copolymerizable compounds; and resist compositions comprising the polymers. These polymers are useful as base polymers for resist materials for an exposure light source of a short wavelength.Type: GrantFiled: August 16, 2000Date of Patent: October 8, 2002Assignee: Maruzen Petrochemical Co., Ltd.Inventors: Takuya Miwa, Nobuyuki Oka, Masao Kaneko
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Patent number: 6451791Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: September 17, 2002Assignee: Monsanto CompanyInventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
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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: 6436925Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be aromType: GrantFiled: October 3, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Publication number: 20020103239Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: ApplicationFiled: November 29, 2001Publication date: August 1, 2002Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
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Patent number: 6426348Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).Type: GrantFiled: May 23, 2001Date of Patent: July 30, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth Gregory Hull, Achytharao Sidduri, Jefferson Wright Tilley
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Patent number: 6423728Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are usefull in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (IBD).Type: GrantFiled: May 23, 2001Date of Patent: July 23, 2002Assignee: Hoffman-La Roche Inc.Inventors: Kenneth Gregory Hull, Achytharao Sidduri, Jefferson Wright Tilley
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Patent number: 6413947Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an, optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.Type: GrantFiled: September 13, 2000Date of Patent: July 2, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Publication number: 20020082218Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula 1Type: ApplicationFiled: February 21, 2002Publication date: June 27, 2002Inventors: Stephane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
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Patent number: 6407120Abstract: The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.Type: GrantFiled: January 28, 2000Date of Patent: June 18, 2002Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Marlys Hammond, Richard F. Hank
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Patent number: 6392046Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: September 30, 1999Date of Patent: May 21, 2002Assignee: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
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Patent number: 6384220Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: GrantFiled: May 1, 2001Date of Patent: May 7, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Nancy-Ellen Haynes, Ramakanth Sarabu
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Patent number: 6355805Abstract: The present invention is directed to multibinding compounds which are &bgr;3 adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.Type: GrantFiled: June 8, 1999Date of Patent: March 12, 2002Assignee: Advanced Medicine, Inc.Inventors: Seok-Ki Choi, Edmund J. Moran
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Patent number: 6350907Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitorsType: GrantFiled: April 11, 2000Date of Patent: February 26, 2002Assignee: Pfizer IncInventors: Michael Jonathan Fray, Roger Peter Dickinson, Kevin Neil Dack
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Patent number: 6329523Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: March 10, 1999Date of Patent: December 11, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Haoyun An
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Patent number: 6326380Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—, optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is —OH or —NHR20 when the bond is absent; Y is ═O, ═S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ═O, (H, H), (H, OH), (H, SH) or (H, C1-CType: GrantFiled: April 7, 2000Date of Patent: December 4, 2001Assignee: Schering CorporationInventors: Samuel Chackalamannil, Theodros Asberom, Yan Xia, Dario Doller, Martin C. Clasby, Michael F. Czarniecki
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Patent number: 6316627Abstract: A process for the preparation of trifluoroethoxy benzoic acid derivatives, in particular Flecainide, and their pharmaceutically acceptable salts, starting with commercially available halobenzoic acids and involving the use of simple reagents and low cost solvents, to afford high overall yield of the product. The above object is achieved in accordance with the present invention which, in one aspect thereof, provides a process for preparing a compound of formula (A): and pharmaceutically acceptable salts thereof, which process comprises the steps of: a) reacting a halobenzoic acid or a salt thereof of the formula [II ] with 2,2,2-trifluoroethanol in the presence of a strong base and a copper containing material, if desired followed by acidification to obtain a compound of formula [I] b) converting the product obtained in step a) above into the compound of formula (A) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 21, 1999Date of Patent: November 13, 2001Assignee: Fine Tech Ltd.Inventors: Arie L. Gutman, Genady Nisnevich, Eleonora Shkolnik, Igor Zaltzman, Boris Tishin
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Patent number: 6316459Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyType: GrantFiled: October 25, 1994Date of Patent: November 13, 2001Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 6306859Abstract: Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.Type: GrantFiled: March 1, 2000Date of Patent: October 23, 2001Assignee: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Edward J. Podlesny
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Patent number: 6306873Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: July 20, 1999Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino