The Chalcogen Is Bonded Directly To A Ring Carbon Of The Five-membered Hetero Ring Which Is Adjacent To The Ring Nitrogen (e.g., 2-indolinones, Etc.) Patents (Class 548/486)
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Patent number: 6268391Abstract: Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.Type: GrantFiled: April 7, 2000Date of Patent: July 31, 2001Assignee: Glaxo Wellcome Inc.Inventors: Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, David Kendall Jung, Karen Elizabeth Lackey, Robert Walton McNutt, Jr., Michael Robert Peel, James Marvin Veal
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Patent number: 6265591Abstract: A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA2 and novel intermediates useful in the preparation of such compounds.Type: GrantFiled: September 27, 2000Date of Patent: July 24, 2001Assignee: Eli Lilly and CompanyInventors: Benjamin Alan Anderson, Nancy Kay Harn
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Publication number: 20010007033Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to e useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: ApplicationFiled: March 1, 2000Publication date: July 5, 2001Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6248771Abstract: The present invention features formulations, including liquid, semi-solid or solid pharmaceutical formulations, that improve the oral bioavailability of hydrophobic pharmaceutical agents, such as quinazoline-, nitrothiazole-, and indolinone-based compounds. Also featured are formulations for parenteral delivery of such hydrophobic pharmaceutical agents, as well as methods of making and using both types of formulations.Type: GrantFiled: March 4, 1998Date of Patent: June 19, 2001Assignee: Sugen, Inc.Inventors: Narmada Shenoy, Gregory S. Wagner
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Patent number: 6245761Abstract: This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel substituted indoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these substituted indoles.Type: GrantFiled: August 29, 1996Date of Patent: June 12, 2001Assignee: Eli Lilly and CompanyInventors: Thomas C. Britton, Robert F. Bruns, Jr., Donald R. Gehlert, Philip A. Hipskind, Karen L. Lobb, James A. Nixon, Paul L. Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M. Zimmerman
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Patent number: 6228880Abstract: Compounds having dopaminegic activity are provided, having the formula: wherein R1 and R2 are each, independently, hydrogen, C1-10 alkyl, or (CH2)mR4, wherein R4 is phenyl or naphthyl which may be substituted by one or two substituents selected from the group consisting of C1-6 alkyl, halogen, C1-6 alkoxide and trifluoromethyl and m is 1 to 5; and R3 is hydrogen or C1-6 alkyl; or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 7, 1999Date of Patent: May 8, 2001Assignee: American Home Products CorpInventors: James A. Nelson, Mira A. Kanzelberger, Richard E. Mewshaw
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Patent number: 6225335Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: December 15, 1998Date of Patent: May 1, 2001Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6218421Abstract: A method for promoting smoking cessation, which method comprises administrating an effective, non-toxic amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof to a human in need thereof. Said ropinirole is preferably administered orally or transdermally. Also provided is a medicament for use in smoking cessation that comprises ropinirole. Said medicament may be a tablet for oral use or a transdermal patch containing ropinirole.Type: GrantFiled: July 1, 1999Date of Patent: April 17, 2001Assignee: SmithKline Beecham p.l.c.Inventor: Stephen Eldon King
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Patent number: 6207697Abstract: The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.Type: GrantFiled: September 8, 1998Date of Patent: March 27, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Qi Han, Celia Dominguez, Eugene C. Amparo, Jeongsook M. Park, Mimi L. Quan, Karen A. Rossi
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Patent number: 6194586Abstract: This invention discloses an efficient process for selectively sulfonating the primary alcohol of a diol containing both primary and secondary alcohols.Type: GrantFiled: February 25, 1998Date of Patent: February 27, 2001Assignees: Eli Lilly and Company, Wayne State University, University of HawaiiInventors: Michael J. Martinelli, Eric D Moher
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Patent number: 6174883Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: June 7, 1995Date of Patent: January 16, 2001Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6150394Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: July 22, 1998Date of Patent: November 21, 2000Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6147073Abstract: A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R.sub.1, R.sub.2 and R.sub.3 the said two being the same or different, are selected from:a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.4 R.sub.5 or --X--(CH.sub.2).sub.m --NHR.sub.6, in which X is --O--, --S-- or --NH--, m is an integer of 2 to 4, one of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.4 and R.sub.5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R.sub.6 is C.sub.2 -C.sub.6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a --NR.sub.4 R.sub.5 group in which R.sub.4 and R.sub.5 are as defined above.Type: GrantFiled: January 12, 1998Date of Patent: November 14, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Carlo Battistini, Antonella Ermoli, Sergio Vioglio, Franco Buzzetti, Dario Ballinari
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Patent number: 6143902Abstract: A chemic compound having the formula: ##STR1## wherein P.sub.1 is a hydroxyl protecting group, R.sub.1 is an alkyl group, an olefinic group, an aromatic group, Ph, PhCH.sub.2, an O-alkyl group, an O-olefinic group, an O-aromatic group, O--Ph, or O--CH.sub.2 Ph, and wherein Z is an N-imido group. In particular, P.sub.1 may be selected from the group consisting of benzyl, benzyloxymethyl and benzoyl, and Z may be a heterocyclic N-imido group, preferably having 5 to 7 atoms in the ring and alternatively substituted with at least one electron withdrawing group, preferably selected from the group consisting of a chloro group, a fluoro group and a nitro group. In particular, it is contemplated that Z may be succinimido, phthalimido, 5-norbornene-2,3-dicarboxyimido, maleimido and substituted derivatives thereof.Type: GrantFiled: June 21, 1999Date of Patent: November 7, 2000Assignee: NaPro BioTherapeutics, Inc.Inventors: Jan Zygmunt, James D. McChesney, Madhavi C. Chander
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Patent number: 6133305Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: September 25, 1998Date of Patent: October 17, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6100397Abstract: A process for the preparation of SB 207266 or a pharmaceutically acceptable salt thereof, which process comprises the reaction of N-(1-.sup.n butyl-4-piperidyl)methylamine with a compound of formula (A), ##STR1## wherein R is alkyl.Type: GrantFiled: February 16, 1999Date of Patent: August 8, 2000Assignee: Smithkline Beecham plcInventors: Michael Fedouloff, Gillian Elizabeth Smith, David William Guest, John Bryce Strachan
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Patent number: 6090839Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.Type: GrantFiled: December 19, 1997Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
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Patent number: 6083515Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: January 22, 1999Date of Patent: July 4, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6051593Abstract: The present invention relates to novel 3-(cycloalkanoheteroarylidenyl)-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: April 18, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5998463Abstract: This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.Type: GrantFiled: February 16, 1999Date of Patent: December 7, 1999Assignee: Pfizer IncInventors: Bernard Hulin, Reinhard Sarges
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Patent number: 5986106Abstract: A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA.sub.2 and novel intermediates useful in the preparation of such compounds.Type: GrantFiled: June 26, 1998Date of Patent: November 16, 1999Assignee: Eli Lilly and CompanyInventors: Vien Van Khau, Michael John Martinelli, Joseph Matthew Pawlak
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Patent number: 5977130Abstract: The present invention is directed to an intimal hypertrophy inhibitor containing as the active ingredient an oxyindole derivative represented by the following formula (I) or a salt thereof: ##STR1## (wherein R.sup.1 represents a hydrogen atom; a phenyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, or a halogen atom; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.2 represents a phenyl group which may be substituted; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.Type: GrantFiled: September 10, 1997Date of Patent: November 2, 1999Assignee: Taiho Pharmeutical Co., Ltd.Inventors: Atsushi Sato, Tetsuji Asao, Yuichi Hagiwara, Makoto Kitade, Yasundo Yamazaki
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Patent number: 5973165Abstract: A process for preparing 2-oxindole includes catalytically reacting isatin with hydrazine hydrate in a polar solvent containing a dissolved weak base at an elevated temperature to form the 2-oxindole product.Type: GrantFiled: March 17, 1999Date of Patent: October 26, 1999Assignee: Sinon CorporationInventors: Lung-Huang Kuo, Jaan-Pyng Hsu, Chin-Tsai Chen
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Patent number: 5965600Abstract: The present invention is directed to an oxindole derivative represented by formula (1): ##STR1## (wherein R represents a methyl group or a methoxy group), and pharmaceuticals containing the compound. The compound exhibits excellent granulation inhibiting activity while providing minimal liver toxicity and is useful as a pharmaceutical in the prevention and treatment of articular rheumatism, arteriosclerosis, hepatocirrhosis, etc., and also in the prevention and treatment of arthrosis deformans, psoriasis, gout, nephritis, angiitis, inflammatory intestinal diseases (ulcerative colitis, Crohn's disease), bronchitis, and chronic granulomatosis, etc.Type: GrantFiled: September 10, 1997Date of Patent: October 12, 1999Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Atsushi Sato, Tetsuji Asao, Yuichi Hagiwara, Makoto Kitade, Yasundo Yamazaki
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Patent number: 5952511Abstract: A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed.Type: GrantFiled: November 3, 1997Date of Patent: September 14, 1999Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Toru Esaki, Takashi Emura, Eiichi Hoshino
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Patent number: 5948808Abstract: Provided in the present invention are compounds and compositions of substituted indole-3-carbinols and diindolylmethane suitable for treating estrogen-dependent tumors. Also provided are methods of treating such cancerous-conditions.Type: GrantFiled: March 7, 1997Date of Patent: September 7, 1999Assignee: The Texas A&M University SystemInventor: Stephen H. Safe
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Patent number: 5919809Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: November 4, 1993Date of Patent: July 6, 1999Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5919790Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.Type: GrantFiled: October 2, 1997Date of Patent: July 6, 1999Assignees: Warner-Lambert Company, BASF AktiengesellsschaftInventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
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Patent number: 5898075Abstract: A process is described for obtaining a single enantiomer from a racemic mixture of the bicyclic lactam 2-azabicyclo?2.2. 1! hept-5-en-one by seeding a supersaturated solution of the lactam and a solvent with a single enantiomer of the lactam.Type: GrantFiled: March 13, 1997Date of Patent: April 27, 1999Assignee: Chirotech Technology LimitedInventors: Raymond McCague, Gerard Andrew Potter, Stephen John Clifford Taylor, Brian Michael Adger
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Patent number: 5891902Abstract: The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, --O--(CH.sub.2).sub.n --OR.sup.5, or ##STR2## R.sup.3 represents hydrogen, lower alkyl, or ##STR3## R.sup.4 represents hydroxy, lower alkoxy, substituted or unsubstituted aryloxy, or --NR.sup.10 R.sup.11, and X represents CO or SO.sub.2, with the proviso that when R.sup.3 is hydrogen or lower alkyl, and X is CO, R.sup.4 is --NR.sup.10 R.sup.11, or pharmaceutically acceptable salts thereof.Type: GrantFiled: July 15, 1996Date of Patent: April 6, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Daisuke Machii, Haruki Takai, Nobuo Kosaka, Hisakatsu Seo, Tomomi Sugiyama, Joji Nakamura, Hiroyuki Ishida, Katsushige Gomi, Soichiro Sato, Masako Uchii, Koji Suzuki
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Patent number: 5886020Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: March 23, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5885967Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 4, 1994Date of Patent: March 23, 1999Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5883113Abstract: The present invention relates to organic molecules apable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal ell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: March 16, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5883116Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: March 16, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5880141Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5849780Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.Type: GrantFiled: October 17, 1994Date of Patent: December 15, 1998Assignee: SanofiInventors: Alain Di Malta, Loic Foulon, Georges Garcia, Dino Nisato, Richard Roux, Claudine Serradeil-Legal, Gerard Valette, Jean Wagnon
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Patent number: 5849710Abstract: The present invention relates to indol-3-ylmethylene-2-oxindole derivatives which are useful as tyrosine kinase inhibitors. The compounds are suitable for use as anti-proliferative agents, anti-metastatic agents, anti-cancer agents, and in the control of angiogenesis and in inhibiting the development of atheromatous and an immunomogulating agents.Type: GrantFiled: December 4, 1996Date of Patent: December 15, 1998Assignee: Pharmacia & Upjohn S.p.A.Inventors: Carlo Battistini, Dario Ballinari, Antonella Ermoli, Sergio Penco, Sergio Vioglio
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Patent number: 5840738Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: June 25, 1997Date of Patent: November 24, 1998Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Christine Ann Droste, Cynthia Darshini Jesudason, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
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Patent number: 5840745Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.Type: GrantFiled: September 25, 1996Date of Patent: November 24, 1998Assignee: Pharmacia S. p. A.Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
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Patent number: 5840915Abstract: A process for the stereoselective synthesis of ?R!- and ?S!-2,3-dihydro-1,3-dimethyl-2-oxo-1H-indole-3-acetonitriles comprises reacting racemic and 5-alkoxy-substituted (.+-.)-1,3-dimethyloxindoles with a halogenated acetonitrile in the presence of a substituted N-benzyl cinchoninium, quinidinium, cinchonidinium, or quininium catalyst. The resulting alkylated oxindoles can be converted to primary amines by catalytic reduction in the presence of hydrogen gas. One of the primary amines, such as enantiomers of 3-(2-aminoethyl)-1,3-dihydro-1,3-dimethyl-5-methoxy-2H-indol-2-one, can be enriched by contact with a chiral tartaric acid in an amount sufficient to preferentially precipitate a salt of the chiral acid and one of the enantiomers. The product can be used in the synthesis of stereospecific forms of physostigmine and related compounds having pharmaceutical activity.Type: GrantFiled: June 12, 1997Date of Patent: November 24, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Thomas Bing Kin Lee, George Seung-Kit Wong
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Patent number: 5834504Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: November 10, 1998Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5821256Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.Type: GrantFiled: August 15, 1996Date of Patent: October 13, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
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Patent number: 5808095Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.Type: GrantFiled: October 7, 1997Date of Patent: September 15, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Yadagiri R. Pendri, Eduardo J. Martinez, John K. Thottathil, Piyasena Hewawasam
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Patent number: 5792786Abstract: The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non.about.steroidal anti.about.inflammatory agents which include a carboxylic acid group. The compounds involve the use of tromethamine or ethanolamine derivative to link the acyl groups derived from fatty acids to the therapeutic compounds.Type: GrantFiled: April 12, 1996Date of Patent: August 11, 1998Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Robert George Whittaker, Veronika Judith Bender, Wayne Gerrard Reilly
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Patent number: 5780498Abstract: The present invention provides novel compounds represented by the general formula I: ##STR1## wherein R.sub.1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R.sub.2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R.sub.3 and R.sub.3 ' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR.sub.3 and R.sub.3 ' together form a ring structure;R.sub.3 " is hydrogen, lower alkyl or an aryl; orR.sub.2 and R.sub.3 " together form a lower alkylene group --(CH.sub.2).sub.n -- wherein n is an integer of 1, 2 or 3; orR.sub.2 and R.sub.3 " together form a group represented by the formula: --(CH.sub.2).sub.p --Ar-- or --Ar--(CH.sub.2).sub.p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C(.dbd.X) is C(.dbd.Type: GrantFiled: April 30, 1996Date of Patent: July 14, 1998Assignee: Ciba-Geigy Japan LimitedInventors: Hideyuki Saika, Toshiki Murata, Thomas Pitterna, Thomas Fruh, Lene D. Svensson, Yoshihiro Urade, Takaki Yamamura, Toshikazu Okada
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Patent number: 5760248Abstract: A description is given of tachykinin receptor antagonists having general formula (I) ##STR1## their preparation and use in pharmaceutical formulations.Type: GrantFiled: May 31, 1996Date of Patent: June 2, 1998Assignee: A.Menarini Industrie Farmaceutiche Riunite S.r.l.Inventors: Alessandro Sisto, Christopher Fincham, Edoardo Potier, Stefano Manzini, Federico Arcamone, Paolo Lombardi
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Patent number: 5739324Abstract: A process for preparing cyclic lactams by reacting amino carbonitriles with water in liquid phase in the presence of heterogeneous catalysts based on titanium dioxide, zirconium oxide, cerium oxide and aluminum oxide.Type: GrantFiled: May 16, 1996Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Eberhard Fuchs, Tom Witzel
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Patent number: 5734063Abstract: The present invention provides a method for preparation of a compound of the formula (I) useful as a fog restrainer for a silver halide light-sensitive material, especially for a heat-developing light-sensitive material and a synthetic intermediate for the fog restrainer. The method makes it possible to obtain the fog restrainer in good yield and in short steps. ##STR1## wherein, R.sup.1 is alkyl, cycloalkyl, or aryl, R.sup.2 and R.sup.3 are hydrogen atom or alkyl, R.sup.4 is hydrogen atom or acyl, and R.sup.1 and R.sup.4 may be bonded together to form 5- or 6-membered ring.Type: GrantFiled: October 24, 1996Date of Patent: March 31, 1998Assignee: Fuji Photo Film Co.,Ltd.Inventors: Katsuyoshi Yamakawa, Tadahisa Sato