Ring Oxygen In The Additional Hetero Ring Patents (Class 514/254.1)
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Publication number: 20030125557Abstract: Novel 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds which are antagonistic to tachykinin receptors, of the general formula I, 1Type: ApplicationFiled: September 13, 2002Publication date: July 3, 2003Applicant: Solvay Pharmaceuticals GmbHInventors: Daniel Jasserand, Ulf Preuschoff, Jochen Antel, Samuel David, Holger Sann, Reinhard Brueckner, Dania Reiche, Christian Eeckhout
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Publication number: 20030109532Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR5, SO2R5, COR5, CN, NO2, CONHR5, CF3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)—R6; R3 and R4 are independently selected from the group consisting of H and C1-C4 alkyls, however both R3 and R4 cannot be H at the same time; R5 is C1-C3 alkyls, CF3, or N(R2)2; R6 is a C3-C6 cycloalkyl, 2-tetrahydrofurane, or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used are disclosed.Type: ApplicationFiled: November 20, 2002Publication date: June 12, 2003Inventors: Clas Sonesson, Bengt Andersson, Susanna Waters, Nicholas Waters, Ingela Marianne Svan, Liselott Lilja Ronnqvist
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Patent number: 6573266Abstract: This invention is directed to acyl piperazine derivatives of the following formula (Id): wherein R1b, R3, R4, R5, R6 and R10 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.Type: GrantFiled: November 16, 2000Date of Patent: June 3, 2003Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
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Patent number: 6555537Abstract: This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.Type: GrantFiled: November 29, 2000Date of Patent: April 29, 2003Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
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Patent number: 6552022Abstract: The invention relates to therapeutic benzamide compounds of formula (I) wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present invention also provides pharmaceutical compositions, processes for the preparation of compounds of formula (I) and their use in the treatment of conditions mediated by ApoB-100 regulation.Type: GrantFiled: May 15, 2001Date of Patent: April 22, 2003Assignee: SmithKline Beecham CorporationInventor: Alain Claude-Marie Daugan
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Patent number: 6541477Abstract: The invention is directed to methods for treating conditions mediated by by P38&agr; kinase using compounds of the formula wherein Ar1 and Ph are limited to specific embodiments or wherein the compound of formula (3) is a compound set forth in FIGS. 1A-1T.Type: GrantFiled: February 28, 2001Date of Patent: April 1, 2003Assignee: Scios, Inc.Inventors: R. Richard Goehring, Babu J. Mavunkel, David Y. Liu, George F. Schreiner, Gregory Leudtke, John A. Lewicki
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Patent number: 6531503Abstract: Benzofurane derivatives of formula (I), wherein R and R′ have the meanings given in claim no. (1), and salts thereof are suitable for use as intermediate products in the synthesis of medicaments.Type: GrantFiled: January 9, 2002Date of Patent: March 11, 2003Assignee: Merck Patent GmbHInventors: Andreas Bathe, Bernd Helfert, Henning Böttcher
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Patent number: 6518272Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionallyType: GrantFiled: March 27, 2002Date of Patent: February 11, 2003Assignee: WyethInventors: Wayne E. Childers, Michael G. Kelly, Yvette L. Palmer, Edward J. Podlesny
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Publication number: 20030004169Abstract: New substituted 4-phenyl N-alkyl)-piperazine and 4-phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bind at the dotted line; R1 is CF3, OSO2CF3, OSO2CH3, SOR7, SO2R7, COR7, CN, OR3, NO2, CONHR3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, and NH2; R3 and R4 are independently H or a C1-C4 alkyl; R5 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)—R6; R6 is a C3-C6 cycloalkyl, 2-tetrahydrofurane, or 3-tetrahydrofurane; R7 is a C1-C3 alkyl, CF3, or N(R4)2, and pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.Type: ApplicationFiled: June 18, 2002Publication date: January 2, 2003Inventors: Clas Sonesson, Bengt Andersson, Susanna Waters, Nicholas Waters, Joakim Tedroff
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Publication number: 20020165256Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.Type: ApplicationFiled: January 29, 2002Publication date: November 7, 2002Inventors: Hans Hofmann, Marion Mahnke, Klaus Memmert, Frank Petersen, Thomas Schupp, Ernst Kusters, Michael Mutz
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Publication number: 20020143020Abstract: The present invention is a chemical compound of formula (I) 1Type: ApplicationFiled: December 7, 2001Publication date: October 3, 2002Inventors: David Reginald Adams, Jonathan Mark Bentley, James Edward Paul Davidson, Claire Elizabeth Dawson, Ashley Roger George, Howard Langham Mansell, Patrizio Mattei, Jacques Mizrahi, Matthias Heinrich Nettekoven, Robert Mark Pratt, Stephan Roever, Jonathan Richard Anthony Roffey, Jean-Luc Specklin, Henri Stalder, Kerry Wilkinson
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Publication number: 20020137736Abstract: There are provided novel compounds of formula (I) 1Type: ApplicationFiled: February 27, 2001Publication date: September 26, 2002Inventors: Kenneth Mattes, Robert Murray, Eifion D Phillips, Hans Schmitthenner
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Publication number: 20020137754Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: January 9, 2002Publication date: September 26, 2002Inventor: Jackson B. Hester
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Patent number: 6451801Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl peperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferable asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: GrantFiled: March 24, 2000Date of Patent: September 17, 2002Assignee: UCB, S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Publication number: 20020115671Abstract: The invention is directed to prepare medicaments for treatment of and to methods to treat conditions mediated by kinase using compounds of the formula 1Type: ApplicationFiled: February 28, 2001Publication date: August 22, 2002Inventors: R. Richard Goehring, Babu J. Mavunkel, David Y. Liu, George F. Schreiner, Gregory Leudtke, John A. Lewicki
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Patent number: 6395738Abstract: The present invention relates to benzofuran derivatives represented by following general formula (I): wherein R1 represents lower alkyl, R2 represents hydrogen or substituted or unsubstituted lower alkyl, R3, R4, R5 and R6 independently represent hydrogen or lower alkyl, X represents CH2 or C═O, and Y represents CH2 or NH, or pharmaceutically acceptable salts thereof.Type: GrantFiled: March 29, 2000Date of Patent: May 28, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Tohru Matsuzaki, Haruhiko Manabe
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Patent number: 6387389Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.Type: GrantFiled: June 30, 1999Date of Patent: May 14, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa
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Patent number: 6387908Abstract: Epoxysuccinamide derivatives of the formula (1): wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or aralkyl; R2 is alkyl, alkenyl, alkynyl, aryl, or aralkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl; X is —O— or —NR4— (R4 is hydrogen, alkyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl); Y1 is OR5, SR6, or NR7R8; and Y2 is hydrogen or alkyl. The compounds are useful as remedies for bone diseases and arthritis.Type: GrantFiled: May 5, 2000Date of Patent: May 14, 2002Assignee: Nippon Chemiphar Co., Ltd.Inventors: Yutaka Nomura, Toshihiro Takahashi, Yasushi Yoshino, Koichiro Nishioka
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Patent number: 6387906Abstract: The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 7, 2000Date of Patent: May 14, 2002Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
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Patent number: 6376540Abstract: Disclosed are furan nitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compounds are useful as analytical reagents for detecting free radicals and as therapeutics for treating a wide variety of medical dysfunctions and diseases.Type: GrantFiled: December 17, 1999Date of Patent: April 23, 2002Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Lowell David Waterbury, Allan L. Wilcox, Hong Xu, Yong-Kang Zhang
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Patent number: 6346533Abstract: The particle diameter of itraconazole, insoluble drug, is reduced and crystallinity thereof is changed from crystalline into amorphous, increasing water solubility and a dissolution rate thereof. The improved itraconazole is applied to an oral adminstration drug.Type: GrantFiled: December 14, 1999Date of Patent: February 12, 2002Assignee: Dong-A Pharmaceutical Co., Ltd.Inventors: Bong-Jin Cha, Jun-Gyo Oh, Su-Eon Kim
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Patent number: 6344458Abstract: Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, migraine, obesity, cognitive disorders, and neurodegenerative diseases.Type: GrantFiled: December 13, 1999Date of Patent: February 5, 2002Assignee: American Home Products CorporationInventors: Michael G. Kelly, Yvette L. Palmer
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Publication number: 20020002168Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: January 3, 2002Inventor: Harry R. Howard
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Patent number: 6333324Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 26, 1999Date of Patent: December 25, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masahiro Neya, Hitoshi Yamazaki, Natsuko Kayakiri, Kentaro Sato, Teruo Oku
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Patent number: 6323207Abstract: Novel benzoylguanidine derivatives of general formula I useful for the treatment or reduction of tissue damage due to ischaemia.Type: GrantFiled: September 15, 1999Date of Patent: November 27, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Christian Eickmeier, Erich Buerger, Stefan Matthias Blech, Otto Roos
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Publication number: 20010041705Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: November 15, 2001Inventor: Harry R. Howard
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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: 6281215Abstract: New 4-(1-piperazinyl)benzoic acid derivatives of the formula (I) are described. Also described is methods for making these compounds and their use as therapeutic agents. In particular, the compounds find use in the treatment of diabetes.Type: GrantFiled: October 20, 1999Date of Patent: August 28, 2001Assignee: Merck Patent GmbHInventors: Gérard Moinet, Gérard Botton, Liliane Doare, Micheline Kergoat, Didier Messangeau
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Patent number: 6281214Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.Type: GrantFiled: October 5, 1998Date of Patent: August 28, 2001Assignee: Eisai Co., LtdInventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
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Patent number: 6277852Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof, wherein Z is oxygen, S(O)m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C1-C6)alkyl or phenyl; X is hydrogen, chloro, fluoro, bromo, iodo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, (C1-C6)alkyl S(O)a wherein a is 0, 1 or 2; or phenyl wherein the phenyl group is optionally substituted; Y is wherein M is oxygen or sulfur; X2 is hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkyl S(O)c wherein c is 0, 1 or 2; R1 is selected from wherein R6 is selected from the group consisting of hydrogen, optionally substituted (C1-C6)alkyl; and wherein R6 in G5 together with R7 form a 2 carbon chain; and R9 and R10 are independently hydrogen or (C1-C6)alkyl; R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally substituted; and R3 is —(CH2)tB, wherein t is 0-3 and B is hydrogType: GrantFiled: April 14, 1999Date of Patent: August 21, 2001Assignee: Pfizer INCInventor: Harry R. Howard
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Patent number: 6274582Abstract: Human growth hormone is used in combination with a cortisol synthesis inhibitor, in particular ketoconazole, for prevention or treatment of conditions related to Metabolis Syndrome (Neuroendocrine Syndrome). Administration can be supplemented by a sex hormone selected from testosterone and natural or synthetic estrogen. Also disclosed are corresponding pharmaceutical compositions.Type: GrantFiled: August 24, 1999Date of Patent: August 14, 2001Assignee: Cortendo ABInventor: Per Mårin
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Patent number: 6268381Abstract: The present invention relates to taxane derivatives each represented by the following formula (1): [wherein, A1 represents a group (in which R1 represents H or a (substituted) alkyl group) or a group (in which R2 represents an amino group, a mono- or di-alkylamino group, a piperidino group, a pyrrolidino group or a morpholino group), X represents H, an alkoxycarbonyl group or a benzoyl group, Y represents H or a trialkylsilyl group, A2 represents a furyl group, an alkylfuryl group, an alkyl group or a fluorophenyl group, Ac represents an acetyl group, and Bz represents a benzoyl group] or salts thereof; and drugs containing the same as an active ingredient. These compounds have excellent water solubility and antitumor activity.Type: GrantFiled: June 19, 2000Date of Patent: July 31, 2001Assignee: Kabushiki Kaisha Yakult HonshaInventors: Hideaki Shimizu, Atsuhiro Abe, Takanori Ogawa, Hiroshi Nagata, Seigo Sawada
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Patent number: 6225312Abstract: The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1-3 heteroatoms from the group O, N and S are present; R1 is hydrogen or fluoro; R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2; Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R3 and R4 independently are hydrogen or C1-4-alkyl; n has the value 1 or 2; R5 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl; and salts thereof show high affinity for both the dopamine D2 and serotonin 5-HT1A receptors.Type: GrantFiled: March 4, 1999Date of Patent: May 1, 2001Assignee: Duphar International Research B.V.Inventors: Roelof Willem Feenstra, Cornelis Gerrit Kruse, Martinus Theodorus Maria Tulp, Wilma Kuipers, Stephen Kenneth Long
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Patent number: 6207665Abstract: This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.Type: GrantFiled: June 9, 1998Date of Patent: March 27, 2001Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Guo Ping Wei, Wei Xu, Wei Zheng
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Patent number: 6187924Abstract: Compounds of formula (I) are useful as therapeutic agents, by virtue of having MMP and TNF inhibitory activity.Type: GrantFiled: November 12, 1998Date of Patent: February 13, 2001Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson