Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperidine Ring Patents (Class 546/225)
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Patent number: 7026510Abstract: (R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: where R, R1, R2, R3, X and Z are as defined in the description. The process for their preparation and pharmaceutical preparations thereof are also described. The quaternary salts of the invention are useful in the inhibition of chemotaxis of neutrophils and monocytes induced by the fraction C5a of the complement and are used in the treatment of psoriasis, pemphigus and pemphigoid, rheumatoid arthritis, intestinal chronic inflammatory pathologies including ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, cystic fibrosis, chronic obstructive pulmonary disease and glomerulonephritis. The compounds of the invention are advantageously used in the prevention and the treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: September 25, 2002Date of Patent: April 11, 2006Assignee: Dompé S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta
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Patent number: 6979691Abstract: Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is X is N or CH, W is —NR16R17, —NR16C(?O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.Type: GrantFiled: March 4, 2002Date of Patent: December 27, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Guixue Yu, John Macor, Timothy Herpin, R. Michael Lawrence, George C. Morton, Rejean Ruel, Graham S. Poindexter, Edward H. Ruediger, Carl Thibault
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Patent number: 6962998Abstract: Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a method for producing optically-active piperidine derivatives or their acid salts by optically resolving the racemic piperidine derivatives obtained in the former method.Type: GrantFiled: June 4, 2001Date of Patent: November 8, 2005Assignee: Toray Industries, Inc.Inventors: Toshihiro Fujino, Haruyo Sato
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Patent number: 6958352Abstract: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus. The compounds have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein W1, W2, X, R1, R2, R3, R4, m and n are defined herein.Type: GrantFiled: February 10, 2003Date of Patent: October 25, 2005Assignee: SmithKline Beecham CorporationInventors: Yazhong Pei, Soumitra S. Ghosh, Ian William James
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Patent number: 6958331Abstract: The invention relates to sulfonyl amine derivatives of formula IA wherein R5A, X1, X2, R9 and R10 are as defined herein, which derivatives are useful as bradykinin B1 receptor antagonists.Type: GrantFiled: June 2, 2000Date of Patent: October 25, 2005Assignee: Novartis AGInventors: Christopher Thomas Brain, William Cantrell, Andrew James Culshaw, Edward Karol Dziadulewicz, Terance William Hart, Timothy John Ritchie, Liladhar Waykole
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Patent number: 6946478Abstract: The invention provides compounds of general formula wherein R1, m, Q, T, n, R2, R3, V, W, X and R4 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: January 9, 2003Date of Patent: September 20, 2005Assignee: AstraZeneca ABInventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas McInally, Bryan Roberts, Stephen Thom
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Patent number: 6943177Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.Type: GrantFiled: August 30, 2002Date of Patent: September 13, 2005Assignee: University of Kentucky Research FoundationInventors: Linda P. Dwoskin, Peter A. Crooks, Marlon D. Jones
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Patent number: 6872735Abstract: The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.Type: GrantFiled: July 11, 2003Date of Patent: March 29, 2005Assignee: Genentech, Inc.Inventors: Daniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters
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Patent number: 6867221Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.Type: GrantFiled: July 10, 2002Date of Patent: March 15, 2005Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
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Patent number: 6858626Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.Type: GrantFiled: June 20, 2002Date of Patent: February 22, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Chu-Biao Xue, Carl P. Decicco, Xiaohua He
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Patent number: 6855706Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents for various diseases concerning ? 4 integrin.Type: GrantFiled: May 20, 2002Date of Patent: February 15, 2005Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Publication number: 20040210051Abstract: Compounds of the formula: 1Type: ApplicationFiled: April 21, 2004Publication date: October 21, 2004Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Publication number: 20040198989Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: ApplicationFiled: November 19, 2003Publication date: October 7, 2004Applicant: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Publication number: 20040198982Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: August 28, 2003Publication date: October 7, 2004Inventors: Petpihoon Prasit, Christopher Ian Bayly, Joel Stephane Robichaud, W. Cameron Black, Eduardo L. Setti, Robert M. Rydzewski, James T. Palmer
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Patent number: 6784186Abstract: This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of opioid compounds, particularly morphine and related compounds, in which an opioid compound is linked via the nitrogen at position 17 to a spacer group, which in turn is linked to a charged group, or a pharmaceutically acceptable salt thereof. In particularly preferred embodiments the opioid compound is morphine, codeine, or buprenorphine.Type: GrantFiled: November 20, 2000Date of Patent: August 31, 2004Inventors: Roy W. Jackson, Kamani R. Subasinghe, Alan L. A. Boura
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Patent number: 6777428Abstract: The present invention relates to a compound of formula I and a process for making: or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal.Type: GrantFiled: December 4, 2001Date of Patent: August 17, 2004Assignee: Eli Lilly and CompanyInventors: Joseph Herman Krushinski, Jr., Vincent Mancuso, Freddy Andre Napora, John Mehnert Schaus
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Patent number: 6770659Abstract: Provided herein are racemic or enantiomerically enriched benzoyl piperidine compounds and pharmaceutically useful salts thereof, pharmaceutical compositions comprising an effective amount of racemic or enantiomerically enriched benzoyl piperidine compounds to treat central nervous system diseases and methods of treating central nervous system diseases in a mammal, in particular psychoses and cognition disorders.Type: GrantFiled: August 26, 2002Date of Patent: August 3, 2004Assignee: SK CorporationInventors: Yong-Moon Choi, Yong-Kil Kim, Jin-Uk Yoo, Eun-Ah Paek, Chun-Eung Park, Sung-Yong Seo, Coo-Min Chung, Joon Heo
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Patent number: 6770656Abstract: The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.Type: GrantFiled: December 26, 2002Date of Patent: August 3, 2004Assignee: Applied Research Systems ARS Holding N.V.Inventors: Serge Halazy, Matthias Schwarz, Bruno Antonsson, Agnes Bombrun, Jean-Claude Martinou, Dennis Church
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Patent number: 6750228Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: GrantFiled: May 12, 2000Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Thomas E Barta, Daniel P Becker, Louis J Bedell, Terri L Boehm, Jeffrey N Carroll, Gary A DeCrescenzo, Yvette M Fobian, John N Freskos, Daniel P Getman, Joseph J McDonald, Madeleine H Li, Susan L Hockerman, Susan C Howard, Steve A Kolodziej, Deborah A Mischke, Joseph G Rico, Nathan W Stehle, Michael B Tollefson, William F Vernier, Clara I Villamil
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Publication number: 20040106646Abstract: The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.Type: ApplicationFiled: November 18, 2003Publication date: June 3, 2004Inventors: Yoshiko Takayama, Yukuo Yoshida, Masayoshi Uehata
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Publication number: 20040097487Abstract: An aromatic sulfonyl alpha-cycloamino hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-cycloamino hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: ApplicationFiled: October 27, 2003Publication date: May 20, 2004Applicant: G.D. Searle & Co.Inventors: Hui Li, Daniel P. Becker, Clara I. Villamil, Terri L. Boehm, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo
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Publication number: 20040087570Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: ApplicationFiled: October 16, 2003Publication date: May 6, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
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Publication number: 20040067981Abstract: A compound of the formula (I): 1Type: ApplicationFiled: July 28, 2003Publication date: April 8, 2004Applicant: SANKYO COMPANY, LIMITEDInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
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Patent number: 6716986Abstract: The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.Type: GrantFiled: July 22, 2002Date of Patent: April 6, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Ronald Charles Bernotas, Paul Wayne Brown, Gary Thomas Emmons, Chi-Hsin Richard King
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Publication number: 20040063725Abstract: The present invention relates to novel N-(phenylsulphonyl)glycyl-glycine compounds, which are defined by formula I and the description, as well as their method of preparation and their use in therapeutics 1Type: ApplicationFiled: June 20, 2003Publication date: April 1, 2004Inventors: Martine Barth, Michel Bondoux, Christophe Matt, Pierre Dodey, Jean-Michel Luccarini, Jean-Luc Paquet, Didier Pruneau
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Patent number: 6713492Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.Type: GrantFiled: May 24, 2001Date of Patent: March 30, 2004Assignees: Daiichi Radioisotope Laboratories, Ltd., Yamagata Public Corporation for the Development of IndustryInventors: Osamu Itoh, Heitaro Obara, Hidekatsu Yokoyama, Masaaki Aoyama
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Publication number: 20040044033Abstract: Provided herein are racemic or enantiomerically enriched benzoyl piperidine compounds and pharmaceutically useful salts thereof, pharmaceutical compositions comprising an effective amount of racemic or enantiomerically enriched benzoyl piperidine compounds to treat central nervous system diseases and methods of treating central nervous system diseases in a mammal, in particular psychoses and cognition disorders.Type: ApplicationFiled: August 26, 2002Publication date: March 4, 2004Inventors: Yong-Moon Choi, Yong-Kil Kim, Jin-Uk Yoo, Eun-Ah Paek, Chun-Eung Park, Sung-Yong Seo, Coo-Min Chung, Joon Heo
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Publication number: 20040024021Abstract: The prevent invention describes a new method for the separation of bupivacaine enantiomers consisting in a continous separation process performed without heating, by the selective precipitation of their diastereomeric salts with tartaric acid. This heatless process avoids the degradation of the reagents granting a continuous process feature to the procedure. Another embodiment of the present invention is related to the enantiomeric manipulation of bupivacaine enantiomers in order to obtain pharmaceutical compositions presenting several enantiomeric excess of levobupivacaine to quantify and determinate the role of the dextrobupivacaine on its anesthetic and cardiotoxic effects. These enantiomeric manipulated compositions showed to present an expressive improvement on its anesthetic properties that has shown to be similar to racemic bupivacaine presenting a cardiotoxic profile similar to enantiomeric pure levobupivacaine.Type: ApplicationFiled: October 7, 2002Publication date: February 5, 2004Inventors: Roberto T. Sudo, Valter F. T. Russo, Elisa M. S. Russo
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Patent number: 6686467Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokinesType: GrantFiled: October 8, 2002Date of Patent: February 3, 2004Assignee: Zeneca LimitedInventors: Dearg S Brown, George R Brown, Philip Cohen
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Patent number: 6683142Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalkyl group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X. derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.Type: GrantFiled: December 11, 2001Date of Patent: January 27, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Andreas Kramer, Peter Nesvadba
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Publication number: 20040010030Abstract: Novel anti-infectives and methods of using them are provided.Type: ApplicationFiled: November 5, 2002Publication date: January 15, 2004Inventors: Dashyant Dhanak, Thomas Carr
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Patent number: 6677451Abstract: A new process is described for the preparation of a compound of the formula I wherein R1, R2, R3 and R4, independently of each other, are C1-C8alkyl or C1-C5hydroxyalkyl, or R1 and R2 together with the carbon atom they are attached to are C5-C12cycloalkyl, or R3 and R4 together with the carbon atom they are attached to are C5-C12cycloalkyl; R5, R6, R7, R8 and R9, independently of each other, are H, C1-C8alkyl, C2-C8alkenyl, C5-C12aryl, C1-C4haloalkyl, an electron withdrawing group, or C6-C12aryl which is substituted by a residue selected from C1-C4alkyl, C1-C4alkoxy, halogen; and R7 and R8 together may also form a chemical bond; and R is an organic linking group containing 2-500 carbon atoms and forming, together with the carbon atoms it is directly connected to and the nitrogen atom, a substituted, 5-, 6 or 7-membered cyclic ring structure; characterized in that a compound of the formula II is oxidized.Type: GrantFiled: November 20, 2001Date of Patent: January 13, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Alessandro Zedda, Gianluca Ferri, Massimiliano Sala
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Patent number: 6673817Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: May 20, 2000Date of Patent: January 6, 2004Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6670379Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1,Type: GrantFiled: April 17, 2003Date of Patent: December 30, 2003Assignee: Novartis AGInventors: Trevor John Howe, Gurdip Bhalay, Darren Mark Le Grand, Thomas Storz
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Patent number: 6664271Abstract: Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal an effective amount of an immunopotentiating compound of Formula I or Formula II, or a physiologically acceptable salt.Type: GrantFiled: November 15, 2001Date of Patent: December 16, 2003Assignee: Eli Lilly and CompanyInventors: Lawrence Camillo Creemer, Janice Rhea Herring, Edward Deorsey McGruder
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Publication number: 20030225076Abstract: Diarylanines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: ApplicationFiled: September 13, 2002Publication date: December 4, 2003Inventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
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Patent number: 6645980Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: November 20, 2000Date of Patent: November 11, 2003Assignee: Sepracor Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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Patent number: 6638950Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 20, 2001Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
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Publication number: 20030195230Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 10, 2002Publication date: October 16, 2003Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
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Publication number: 20030176460Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R4 and R5 are each independently with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5-6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3, or 4,Type: ApplicationFiled: April 17, 2003Publication date: September 18, 2003Inventors: Trevor John Howe, Gurdip Bhalay, Darren Mark Le Grand, Thomas Storz
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Publication number: 20030166683Abstract: The invention is concerned with water soluble N—(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I) 1Type: ApplicationFiled: January 24, 2003Publication date: September 4, 2003Inventors: Leo Alig, Katrin Groebke Zbinden, Ulrike Obst
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Patent number: 6605620Abstract: A cyclic amine compound by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.Type: GrantFiled: March 28, 2002Date of Patent: August 12, 2003Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
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Patent number: 6599890Abstract: A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: November 8, 2000Date of Patent: July 29, 2003Assignee: Pfizer IncInventors: Kim F. McClure, Mark C. Noe, Michael A. Letavic, Louis S. Chupak
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Patent number: 6586602Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, wherein the disease may be, for example, asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: January 14, 2002Date of Patent: July 1, 2003Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Louis John Lombardo, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen
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Patent number: 6579971Abstract: A process for preparing compounds of the formula I in which R is hydrogen, C1-C6-alkoxy, —NHC1-C6-alkyl, —N(C1-C6-alkyl)2, OH, NH2 R1 is hydrogen, C1-C6-alkyl, Me3Si, C1-C6-alkyl-S R2 is Boc, C1-C6-acyl, mesyl, benzenesulfonyl, tosyl, trifluoroacetyl, A1-A3-peptide n is 1, 2 R4 is H, C1-C6-alkyl, is described.Type: GrantFiled: March 12, 2002Date of Patent: June 17, 2003Assignee: BASF AktiengesellschaftInventors: Bernd Schäfer, Günter Helmchen, Uli Kazmaier, Simone Schleich, Helmut Stahr, Volker Wolfart
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Patent number: 6548504Abstract: The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C) below: in which P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s); A is a single bond, a C1-6alkylene or a C2-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; n is 0, 1, 2 or 3; and R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or in which Ra is an alkyl group containing 1 to 20 carbon atoms oType: GrantFiled: July 19, 2000Date of Patent: April 15, 2003Assignee: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Stephen Frederick Moss
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Patent number: 6541489Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.Type: GrantFiled: July 31, 2000Date of Patent: April 1, 2003Assignee: G. D. Searle & CompanyInventors: Thomas E. Barta, Daniel P. Becker, Terri L. Boehm, Gary A. De Crescenzo, Clara I. Villamil, Joseph J. McDonald, John N. Freskos, Daniel P. Getman
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Publication number: 20030055052Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug having a cleavage site which is recognised by FAP&agr;, and said drug being cytotoxic or cytostatic under physiological conditions.Type: ApplicationFiled: November 9, 2001Publication date: March 20, 2003Inventors: Stefan Peters, Dietmar Leipert, John Edward Park, Martin Lenter, Pilar Garin-Chesa
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Patent number: 6525069Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 21, 2000Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
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Patent number: 6518286Abstract: The invention provides compounds of general formula (I) wherein: R1 represents optionally substituted, C1-C12 alkyl or optionally substituted 3- to 10-membered saturated or unsaturated ring system comprising up to two ring carbon atoms that form carbonyl groups and comprising up to 4 ring heteroatoms independently selected from nitrogen, oxygen and sulfur; m is 0-1; Q represents OCH2, C1-C4 alkylene or C2-C4 alkenylene; T represents C(O)NH, or when m is 0, T may additionally represent a bond or NH, or when m is 1 and Q represents C1-C4 alkylene, T may additionally represent NH; n is 1-4; each R2 and R3 independently represents H or C1-C4 alkyl; V represents N, and W represents N or CH; X represents O, C(O), CH(OH), SO2, NH or N(C1-C6 alkyl), provided that when W represents N, then X represents either C(O) or SO2 and when W represents CH, then X is other than SO2; R4 represents optionally substituted phenyl; R5 and R6 each independently represent H, C1-C6 alkyl or hydroxyC1-C6 alkyl, or R5 and R6 together withType: GrantFiled: June 1, 2000Date of Patent: February 11, 2003Assignee: AstraZeneca ABInventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas McInally, Bryan Roberts, Stephen Thom