Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 546/175)
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Patent number: 6645957Abstract: The invention relates to compounds represented by the following general formula (1): wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a lower alkylene group which may be substituted, or the like, Y is a single bond or the like; Z is a divalent residue of benzene which may be substituted, or the like, and m and n are independently an integer of 1 to 4, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.Type: GrantFiled: June 19, 2002Date of Patent: November 11, 2003Assignee: Kowa Co., Ltd.Inventors: Hiroyuki Ishiwata, Seiichi Sato, Mototsugu Kabeya, Soichi Oda, Yukio Hattori, Makoto Suda, Manabu Shibasaki, Hiroshi Nakao, Takao Nagoya
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Patent number: 6642228Abstract: There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1 is hydrogen etc., B is bond, or B—N—R1 forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and &agr;1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for &agr;1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which &agr;1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by &agr;1B adrenoceptor.Type: GrantFiled: April 13, 2001Date of Patent: November 4, 2003Assignee: Toray Industries, Inc.Inventors: Ryoji Hayashi, Eiji Ohmori, Masafumi Isogaya, Mitsuhiro Moriwaki, Hiroki Kumagai
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Patent number: 6635657Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: June 8, 2001Date of Patent: October 21, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Piñeiro-Núñez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6632840Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) isType: GrantFiled: March 24, 2000Date of Patent: October 14, 2003Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Patent number: 6610701Abstract: Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.Type: GrantFiled: February 8, 2002Date of Patent: August 26, 2003Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Craig Coburn, Harold G. Selnick, Phung L. Ngo
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Patent number: 6605722Abstract: Compounds which can be represented by general formula (I) indicated below and in which: R1 and R2 are selected, independently, from hydrogen, an alkyl group having from 1 to 4 carbon atoms, a halogen group such as a fluoro, chloro or bromo group, the methoxy group, the cyano group, or the trifluoromethyl group, and R3 is selected, independently, from a phenyl or a 2 (or 3 or 4)-pyridyl group, unsubstituted or mono- or di-substituted with an alkyl or alkoxy group having from 1 to 4 carbon atoms, with a halogen group such as a fluoro or chloro group, with the trifluoromethyl group, with the cyano group, with the nitro group, with the amino group, or with the phenyl group, a 1 (or 2)-naphthyl group, a 2 (or 3)-indolyl group as such or N-alkylated with an alkyl group having from 1 to 3 carbon atoms, a 2 (or 3, 4, 5, 6, 7 or 8)-quinolinyl or a 1 (or 3, 4, 5, 6, 7 or 8)-isoquinolinyl group, unsubstituted or mono- or di-substituted with a group selected, independently, from the methyl, ethyl, propType: GrantFiled: August 8, 2002Date of Patent: August 12, 2003Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Walter Peris, Lucio Claudio Rovati
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Patent number: 6586430Abstract: Compounds of Formula 1 [Region &agr;]-[Region &bgr;]-[Region &ggr;]-[Region &dgr;] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: December 1, 1999Date of Patent: July 1, 2003Assignee: Pfizer Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Patent number: 6576642Abstract: Compounds having the formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyindeny, pyridyl, indolyl,isoindolyl, quinolyl or isoquinolyl group which are optionally substituted; X is optionally substituted alicyclic, aromatic, imino or heterocyclic groups or —S— or —O—; Y is a single bond or an alkylene group; Z is an unsubstituted aliphatic group or divalent residue of benzene or pyridine, which is optionally substituted; anis hydrogen, lower alkyl, cycloalkyl, aryl or aralkyl; with certain provisos. These compounds exhibit an inhibitory effect on the production of IgE antibodies and are, hence, useful as antiallergic agents.Type: GrantFiled: May 17, 2001Date of Patent: June 10, 2003Assignee: Kowa Co., Ltd.Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
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Publication number: 20030087897Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: ApplicationFiled: May 10, 2002Publication date: May 8, 2003Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
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Patent number: 6559163Abstract: Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: August 16, 2001Date of Patent: May 6, 2003Assignee: Neurogen CorporationInventors: Guolin Cai, Jun Yuan, Kevin Currie, Pamela Albaugh, Alan Hutchison
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Patent number: 6552196Abstract: The present invention relates to quinolonecarboxylic acid derivatives having more excellent and broad antibacterial activities than the existing quinolone-series antibiotic. More specifically, it pertains to novel quinolonecarboxylic acid derivative represented by following formula 1, which have a derivative of 7-[8-(alkoxyimino)-2,6-diazaspiro[3.4]oct-6-yl] as a substituent, and pharmaceutically acceptable salts and isomers thereof: Wherein A is C—H, C—F, C—Cl, C—O—CH3 or N; Y is H or amino; R1 is cyclopropyl or 2,4-difluorsophenyl R2 is C1-4 alkyl; and R3 is H or C1-4 alkyl.Type: GrantFiled: September 6, 2001Date of Patent: April 22, 2003Assignee: Dong Wha Pharmaceutical Industrial Co., Ltd.Inventors: Sung-Joon Yoon, Yong-Ho Chung, Chi-Woo Lee, Yoon-Seok Oh, Nam-Doo Kim, Jae-Kyung Lim, Yoon-Ho Jin
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Publication number: 20030065007Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1Type: ApplicationFiled: October 9, 2002Publication date: April 3, 2003Inventors: Mark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
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Patent number: 6525036Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.Type: GrantFiled: January 5, 2001Date of Patent: February 25, 2003Assignee: Merck & Co., Inc.Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Publication number: 20030036653Abstract: Compounds of the formula 1Type: ApplicationFiled: March 15, 2002Publication date: February 20, 2003Applicant: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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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: 6509468Abstract: The invention relates to a vitreous form of the compound, FR 173657, having the structure of formula (I). This vitreous form has good solid stability and is therefore useful for producing and supplying FR 173657 products whose quality is stable enough to be suitable for medicine.Type: GrantFiled: April 20, 2001Date of Patent: January 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Norio Ohnishi, Osamu Aoki, Atsuo Ohike, Kazuto Okimoto, Hiroshi Ishikuro
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Patent number: 6506751Abstract: Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing; A is S, S═O or O═S═O; R1 and R2 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R5 represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R5 is (CR6R7)—(CH2)n—XR8R9; X is S or N; R6, R7, R8, R9, and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.Type: GrantFiled: November 2, 2000Date of Patent: January 14, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Stephanie Elizabeth Ault Justus, Helen Tsenwhei Lee, Jason Keith Pontrello, Bruce David Roth, Karen Elaine Sexton, Michael William Wilson
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Patent number: 6495548Abstract: The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered lactam containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.Type: GrantFiled: March 31, 2000Date of Patent: December 17, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Jingwu Duan
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Patent number: 6495568Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: December 17, 2002Assignee: Warner-Lambert CompanyInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6495565Abstract: The present application describes novel &bgr;-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3, R4, and R4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-&agr; inhibitors.Type: GrantFiled: March 16, 2001Date of Patent: December 17, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jingwu Duan, Bryan W. King, Carl Decicco, Thomas P. Maduskuie, Jr., Matthew E. Voss
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Patent number: 6492401Abstract: NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.Type: GrantFiled: August 18, 1999Date of Patent: December 10, 2002Assignee: Pfizer, Inc.Inventors: Ernest S. Hamanaka, Angel Guzman-Perez, Roger B. Ruggeri, Ronald T. Webster, Christian J. Mularski
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Patent number: 6489339Abstract: A compound according to Formula (I): wherein: A represents C1-4 alkylene, unsubstituted or optionally substituted by C1-4 alkyl or aryl; or A forms a 5-8 membered fused aliphatic ring with the adjacent phenyl ring; m is an integer from 1 to 3; each R1 is independently selected form the group consisting of halo, C1-4 alkyl, methanesulfonyl, alkoxy, nitrile, dimethylamine, methylenedioxy and CF3; and R2 is hydrogen or methyl is provided.Type: GrantFiled: February 7, 2001Date of Patent: December 3, 2002Assignee: SmithKline Beecham CorporationInventors: Dennis Lee, William E. Bondinell, Anthony J. Jurewicz
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Patent number: 6472394Abstract: Disclosed are compounds represented by structural formula I: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein W is R1—CR3R12NR4C(O)— or R11C(O)NR4—; the dotted line is an optional double bond; X is —CHR8—, —C(O)—, or —C(═NOR9)—; Y is R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkyl-alkyl; R2 is optionally substituted aryl or heteroaryl; R3 is alkyl, aryl or heteroaryl; R4 and R12 are H or alkyl; R8 is H, alkyl or alkoxyalkyl; R9 is H, alkyl or arylalkyl; R10 is H, alkyl or aryl; R11 is or, when R2 is R6-heteroaryl or R10 is not H, R11 can also be R5-phenylalkyl; n is 1-3 and m is 1-5; and R14 is 1-3 substituents selected from H, alkyl, halogen, —OH, alkoxy and CF3; and pharmaceutical compositions containing the compounds and methods of using the compounds in the trType: GrantFiled: December 17, 2001Date of Patent: October 29, 2002Assignee: Schering CorporationInventors: Brian A. McKittrick, Jing Su, John W. Clader, Shengjian Li, Guihau Guo
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Patent number: 6469029Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1-3 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 13, 2000Date of Patent: October 22, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6455545Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: January 18, 2001Date of Patent: September 24, 2002Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: 6444809Abstract: Compounds of formula I wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: September 22, 2000Date of Patent: September 3, 2002Assignee: Zeneca LimitedInventor: Scott Carson Miller
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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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Patent number: 6436999Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 18, 1997Date of Patent: August 20, 2002Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Patent number: 6429312Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R5 is hydrogen or C1-C6 alkyl; and R represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.Type: GrantFiled: March 19, 2001Date of Patent: August 6, 2002Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 6403577Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: November 17, 1993Date of Patent: June 11, 2002Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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Patent number: 6399631Abstract: Carbazoles of the formula which are effective in treating conditions associated with neuropeptide Y-5 neurotransmission.Type: GrantFiled: July 21, 2000Date of Patent: June 4, 2002Assignee: Pfizer Inc.Inventors: Richard L. Elliott, David A. Griffith, Marlys Hammond
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Patent number: 6387931Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: May 14, 2002Assignee: Pfizer INCInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Publication number: 20020052323Abstract: This invention concerns compounds and a pharmaceutical composition of the structure:Type: ApplicationFiled: May 29, 2001Publication date: May 2, 2002Inventor: Jinhai Wang
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Patent number: 6380214Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein Z, X, X1, R1, R2 and R3 are as defined herein as it relates to pharmaceutical compositions containing the above compounds for the treatment of disorders mediated by angiogenesis in mammals by administration of the above compounds.Type: GrantFiled: April 17, 2000Date of Patent: April 30, 2002Assignee: Pfizer Inc.Inventors: Thomas George Gant, Mark Carl Noe
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Publication number: 20020040002Abstract: 1 Compounds of formula (I), wherein: n is 1 to 6; Het is a nitrogen containing ring fused to the benzene ring on two adjacent carbon atoms to form a bicyclic ring system which ring system may be optionally substituted; R1 is hydrogen, C1-8alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, aryl, heteroaryl, heterocyclyl, arylC1-6alkyl, heteroarylC1-6alkyl, heterocyclylC1-6alkyl or C3-8cycloalkylC1-6alkyl; R2 is C1-6alkyl, C2-6alkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R3 is hydrogen, C1-6alkyl, C3-8cycloalkyl, C4-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R4 is hydrogen or C1-6alkyl; or R3 and R4 together with the nitrogen atom to which they are joined form a heterocyclic ring; wherein any group or ring, in R1-R4, is optionally substituted; and pharmceutically acceptable salts and in vivo hydrolysable esters thereof, are described as inhibitors of the production of Tumour Necrosis Factor and/or one or more matrix metalType: ApplicationFiled: March 22, 2001Publication date: April 4, 2002Applicant: ZENECA LIMITEDInventor: Thomas Geoffrey Colerick Bird
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Patent number: 6342602Abstract: Compounds of the formula wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: August 4, 2000Date of Patent: January 29, 2002Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6342633Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner, or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are hyType: GrantFiled: September 27, 2000Date of Patent: January 29, 2002Assignee: Bayer AktiengesellschaftInventor: René Zurflüh
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Patent number: 6323180Abstract: A racemate, diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a satuType: GrantFiled: August 5, 1999Date of Patent: November 27, 2001Assignee: Boehringer Ingelheim (Canada) LtdInventors: Montse Llinas-Brunet, Murray D. Bailey, Dale Cameron, Elise Ghiro, Nathalie Goudreau, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic, Bruno Simoneau
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Patent number: 6297283Abstract: The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.Type: GrantFiled: April 9, 1999Date of Patent: October 2, 2001Assignee: Kowa Co., Ltd.Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
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Patent number: 6281211Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n isType: GrantFiled: September 21, 2000Date of Patent: August 28, 2001Assignee: Euro-Celtique S.A.Inventors: Sui Xiong Cai, Nancy C. Lan, Soo Hong-Bae
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Patent number: 6262123Abstract: Ortho-substituted benzoylguanidines of the formula I in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.Type: GrantFiled: September 17, 1999Date of Patent: July 17, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Udo Albus, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Wolfgang Scholz, Jan-Robert Schwark, Andreas Weichert
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Patent number: 6229011Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: May 8, 2001Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6211240Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4-alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner; or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are hType: GrantFiled: October 29, 1996Date of Patent: April 3, 2001Assignee: Novartis CorporationInventor: René Zurflüh
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Patent number: 6211196Abstract: Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of liver cirrhosis or Alzheimer's disease. This application describes such compounds, as well as processes for their preparation and use. The compounds according to this invention include compounds of formula (I) in which B, D, R1, and R2 have the meanings indicated herein.Type: GrantFiled: March 26, 1998Date of Patent: April 3, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Adalbert Wagner, Klaus Wirth, Bernward Schölkens
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Patent number: 6175015Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: R1 and R2 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1 and R2 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R3 is hydrogen, C1-C6 alkyl, or —COR′″ where R′″ is C1-C6 alkyl; R4 is hydrogen or C1-C6 alkyl; and R represents an azacycloalkylalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dysronia, and other disorders which respond to dopaminergiType: GrantFiled: October 28, 1999Date of Patent: January 16, 2001Assignee: Neurogen CorporationInventors: Jun Yuan, Jan Wasley
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Patent number: 6143744Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 5, 1999Date of Patent: November 7, 2000Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
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Patent number: 6130238Abstract: The present invention relates to novel 3-(cyclohexanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: June 19, 1998Date of Patent: October 10, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6124332Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6124333Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett