The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/341.5)
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Patent number: 6951948Abstract: The invention relates to methods of synthesizing libraries of diverse and complex 2-substituted azole compounds of the general formula (I) or (II) wherein X, R2 and the ring components are as described herein, novel intermediates useful for synthesizing such substituted azole compounds and methods for identifying and isolating the compounds.Type: GrantFiled: May 22, 2001Date of Patent: October 4, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Yijun Deng, Dennis Hlasta
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Patent number: 6812349Abstract: The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their preparation and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.Type: GrantFiled: September 23, 2003Date of Patent: November 2, 2004Assignee: Altana Pharma AGInventors: Wolf-Rüdiger Ulrich, Christian Scheufler, Thomas Fuchss, Jörg Senn-Bilfinger
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Patent number: 6787552Abstract: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.Type: GrantFiled: February 11, 2003Date of Patent: September 7, 2004Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shogo Sakuma, Tsuyoshi Endo, Atsushi Tendo, Toshihiro Takahashi, Shinichi Yoshida, Kunio Kobayashi, Nobutaka Mochizuki, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
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Publication number: 20040171844Abstract: Disclosed are compounds of the Formula I 1Type: ApplicationFiled: February 19, 2004Publication date: September 2, 2004Inventors: Daniele Marie Leonard, Joseph Thomas Repine, Gordon William Rewcastle
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Patent number: 6750352Abstract: A polymerizable molten salt monomer represented by the following general formula (I): wherein Q represents a nitrogen-containing aromatic heterocyclic atomic group which can form a cation; Y1 represents a divalent interlocking group or a bonding hand; Y2 represents a substituted or unsubstituted alkyl group; n represents an integer of from 2 to 20; m represents an integer of 2 or more; X− represents an anion; plural Y1's and plural Y2's may be the same or different, respectively, with the proviso that at least one of Y2's has a polymerizable substituent group; and a plurality of the compounds of the general formula (I) may be connected to each other at Q or Y2 to form a dimer, trimer or tetramer. Also disclosed are an electrolyte composition containing a polymer compound obtained by the polymerization of the molten salt monomer, and a cell containing the electrolyte composition.Type: GrantFiled: January 22, 2001Date of Patent: June 15, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Michio Ono, Chang-yi Qian
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Patent number: 6737418Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: April 30, 2002Date of Patent: May 18, 2004Assignee: Euro-Celtique S.A.Inventors: Derk Hogenkamp, Ravindra Upasani, Phong Nguyen
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Patent number: 6727098Abstract: A novel achiral biaryl-type compound and a circular dichroism (CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.Type: GrantFiled: February 26, 2002Date of Patent: April 27, 2004Assignee: Kanazawa UniversityInventors: Tomihisa Ohta, Shinzo Hosoi
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Patent number: 6716990Abstract: The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their preparation and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.Type: GrantFiled: June 11, 2002Date of Patent: April 6, 2004Assignee: Altana Pharma AGInventors: Wolf-Rüdiger Ulrich, Christian Scheufler, Thomas Fuchss, Jörg Senn-Bilfinger
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Patent number: 6713632Abstract: A method for producing a compound of the formula: wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group and ring A is an imidazole ring which is optionally substituted further, or a salt thereof, which method comprises reacting a compound of the formula: wherein ring A is as defined above, or a salt thereof, and a compound of the formula: R—M1 (II) wherein M1 is an alkali metal atom or a group of the formula: —Mg—Y1 where Y1 is a halogen atom, and R is as defined above, or a salt thereof, and bringing the resulting product into contact with an acid.Type: GrantFiled: April 12, 2002Date of Patent: March 30, 2004Assignee: Takeda Chemical Industries, Ltd.Inventor: Jun-ichi Kawakami
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Publication number: 20030216403Abstract: 1Type: ApplicationFiled: May 14, 2003Publication date: November 20, 2003Inventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Patent number: 6649643Abstract: Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterine myoma, mastopathy and polycystic ovary syndrome are disclosed.Type: GrantFiled: April 12, 2002Date of Patent: November 18, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Akio Ojida, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
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Patent number: 6645991Abstract: The invention describes novel compounds of the formula I which are biologically active as ligands of integrin &agr;v&bgr;3 X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5 in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.Type: GrantFiled: June 21, 2002Date of Patent: November 11, 2003Assignee: Merck Patent GmbHInventors: Alfred Jonczyk, Oliver Schadt, Simon Goodman
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Publication number: 20030199522Abstract: Compounds according to formula (I) wherein n is 0-3, R1 is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from hydrogen and optionally substituted C1-6 alkyl, or R5 and R8 are an alkylene chain, are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.Type: ApplicationFiled: January 22, 2003Publication date: October 23, 2003Applicant: Pfizer Inc.Inventors: Charlotte Moira Norfor Allerton, David John Bull, Mark Edward Bunnage, Robert John Maguire, John Steele
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Patent number: 6603019Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoidsType: GrantFiled: February 21, 2002Date of Patent: August 5, 2003Assignee: Allergan, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
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Patent number: 6573289Abstract: A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.Type: GrantFiled: October 18, 2000Date of Patent: June 3, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Akio Ojida, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
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Patent number: 6562846Abstract: The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.Type: GrantFiled: April 23, 2002Date of Patent: May 13, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, Kai Xie
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Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6545009Abstract: 1,3-Azole derivatives, pharmaceutical compositions thereof and methods for regulating the function of retinoid-related receptors with 1,3-azole derivatives are disclosed. Such regulation may be useful for preventing or treating diabetes, preventing or treating hyperlipidemia, preventing or treating impaired glucose tolerance (IGT) or for preventing transition from impaired glucose tolerance to diabetes.Type: GrantFiled: December 28, 2000Date of Patent: April 8, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuo Sugiyama, Yu Momose, Hiroyuki Kimura, Junichi Sakamoto, Hiroyuki Odaka
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Patent number: 6518257Abstract: To provide a composition having a steroid C17,20-lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic hydrocarbon group, R2 is an aromatic hydrocarbon group optionally having substituents or an aromatic heterocyclic group optionally having substituents, R3 is a hydrocarbon group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, and n is an integer of 0 to 4, and a salt thereof have a steroid C17,20-lyase inhibitory activity, and are useful as an agent for the pophylaxis or treatment of prostatism and tumors such as beast cancer and the like.Type: GrantFiled: April 18, 2002Date of Patent: February 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Tomohiro Kaku, Masami Kusaka
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Patent number: 6514966Abstract: NPY antagonists, methods of using such NPY antagonists and pharmaceutical compositions containing such NPY antagonists. The NPY antagonists are useful for the treatment of NPY mediated disease/conditions including obesity.Type: GrantFiled: January 4, 2001Date of Patent: February 4, 2003Assignee: Pfizer Inc.Inventors: Richard L. Elliott, Richard F. Hank, Marlys Hammond
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Publication number: 20030004358Abstract: 1 The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their prepration and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.Type: ApplicationFiled: June 11, 2002Publication date: January 2, 2003Inventors: Wolf- Rudiger Ulrich, Christian Scheufler, Thomas Fuchss, Jorg Senn-Bilfinger
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Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
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Patent number: 6465646Abstract: Compounds of Formula 1 and of Formula 2 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.Type: GrantFiled: August 4, 2000Date of Patent: October 15, 2002Assignee: Allergan, Inc.Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
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Patent number: 6465647Abstract: Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.Type: GrantFiled: August 4, 2000Date of Patent: October 15, 2002Assignee: Allergan, Inc.Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
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Publication number: 20020147229Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: August 17, 2001Publication date: October 10, 2002Inventors: Charlotte Moira Norfor Allerton, Julian Blagg, Mark Edward Bunnage, John Steele
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Patent number: 6459003Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: GrantFiled: March 31, 2000Date of Patent: October 1, 2002Assignee: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Publication number: 20020133023Abstract: The present invention relates to a class of compounds represented by the Formula I 1Type: ApplicationFiled: June 15, 2001Publication date: September 19, 2002Inventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B. Mohler, Barbara Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark Laurence Boys, Nizal Samuel Chandrakumar, Hung-Fun Lu
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Publication number: 20020086985Abstract: Novel linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye are provided. These linkers faciliate the efficient transfer of energy between a donor and acceptor dye in an energy transfer dye. One of these linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye has the general structure R21Z1C(O)R22R28 where R21 is a C1-5 alkyl attached to the donor dye, C(O) is a carbonyl group, Z1 is either NH, sulfur or oxygen, R22 is a substituent which includes an alkene, diene, alkyne, a five and six membered ring having at least one unsaturated bond or a fused ring structure which is attached to the carbonyl carbon, and R28 includes a functional group which attaches the linker to the acceptor dye.Type: ApplicationFiled: October 29, 2001Publication date: July 4, 2002Inventors: Linda G. Lee, Sandra L. Spurgeon, Barnett Rosenblum
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Patent number: 6407258Abstract: The invention relates to a process for the preparation of compounds of the formula (I) in which R(2) and R(3) independently of one another are —SR(4) or —COOR(5) and R(1), R(4) and R(5) have the meaning indicated in the description, which comprises cyclizing compounds of the formula II in which R(1), R(2) and R(3) have the meaning defined above, in the presence of alkylphosphonic anhydrides to give compounds of the formula (I), then purifying these in as is known per se by salt formation and, if appropriate, subsequent recrystallization and optionally removing radicals introduced for the protection of other functional groups in a manner known per se; and their use as intermediate for the synthesis of active compounds.Type: GrantFiled: July 26, 2000Date of Patent: June 18, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Bernd Napierski, Heinz-Peter Rebenstock, Wolfgang Holla
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Patent number: 6380396Abstract: The present invention provides intermediates for the preparation of compounds of the formula wherein R, R1, W, X, Y, Ar and ZA are defined herein.Type: GrantFiled: December 11, 2000Date of Patent: April 30, 2002Assignee: Pfizer Inc.Inventors: Sandra Marina Monaghan, David Alker, Christopher John Burns
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Publication number: 20020045760Abstract: A new process for the catalytic conversion of hydroxymethyl imidazoles to formylimidazoles is described. The reaction takes place in the presence of a peroxide. Formylimidazoles are important intermediate products for pharmaceutical substances.Type: ApplicationFiled: December 5, 2001Publication date: April 18, 2002Applicant: Lonza AGInventors: Yves Bessard, Josef Heveling
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Patent number: 6372693Abstract: The invention relates to 2-(3-alkenylbenzoyl)cyclohexane-1,3-diones of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR6, —OCOR7, —OSO2R7, —SH, —S(O)nR8, —SO2OR6, —SO2NR6R9, —NR9SO2R7 or —NR9COR7; R3 is hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl; R4, R5 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, alkoxy, alkylthio, haloalkoxy, —COR10, —CO2R10, —COSR10, —CONR10R11, —C(R12)═NR13, —PO(OR10)(OR11); unsubstituted or substituted alkyl, heterocyclyl, heterocyclylalkyl, phenyl, phenylalkyl, hetaryl or hetarylalkyl; or R4 and R5 together form an alkanediyl chain which can be substituted and/or can be interrupted by a hetero atom; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring whType: GrantFiled: November 2, 1999Date of Patent: April 16, 2002Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Michael Rack, Joachim Rheinheimer, Matthias Witschel, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Publication number: 20020032202Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1Type: ApplicationFiled: July 23, 2001Publication date: March 14, 2002Applicant: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
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Publication number: 20010047100Abstract: Novel intermediates useful in the preparation of optically active H3 histamine receptor antagonist 2-(4-imidazoyl)-cyclopropyl derivatives are disclosed.Type: ApplicationFiled: March 26, 2001Publication date: November 29, 2001Inventors: Hans Joergen Kjaersgaard, Jim Phillips, Syed M. Ali
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Patent number: 6313311Abstract: Imidazole derivatives of formula (I) wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is —CHR9—(CHR10)m—, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described.Type: GrantFiled: February 2, 1999Date of Patent: November 6, 2001Assignee: Orion CorporationInventors: Arto Karjalainen, Paavo Huhtala, Juha-Matti Savola, Siegfried Wurster, Maire Eloranta, Maarit Hillilä, Raimo Saxlund, Victor Cockcroft, Arja Karjalainen
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Patent number: 6310067Abstract: Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R2 denotes hydrogen or lower alkyl, R3 denotes nitro, amino, cyano or COOR2, wherein R2 in said COOR2 is as defined above, and Q denotes carbon or nitrogen.Type: GrantFiled: August 3, 2000Date of Patent: October 30, 2001Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Kazuhiko Ito, Takahiro Sakaue, Sachiko Inoue, Shinya Ogino
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Patent number: 6284756Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: September 4, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Richard W Harper, Todd J Kohn, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Michael R Wiley, Minsheng Zhang
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Patent number: 6277849Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eacType: GrantFiled: August 24, 1999Date of Patent: August 21, 2001Assignee: Syngenta Crop Protection, Inc.Inventor: Martin Zeller
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Patent number: 6265422Abstract: The present invention provides compounds of Formula I The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.Type: GrantFiled: April 28, 2000Date of Patent: July 24, 2001Assignee: Warner-Lambert CompanyInventors: Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
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Patent number: 6258834Abstract: The present invention relates to an agent for the prophylaxis and treatment of diabetic complications comprising, as an active ingredient, 4-[&agr;-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid, an optically active compound thereof or a pharmaceutically acceptable salt thereof. The present invention further relates to a method for the prophylaxis and treatment of diabetic complications comprising administering an effective amount of this compound. The medicament of the present invention is useful for the prophylaxis and treatment of diabetic complications, namely, diabetic neuropathy, nephropathy, ophthalmopathy, arteriosclerosis and the like. The action of the drug is long-lasting for very small doses and a single administration a day is sufficient.Type: GrantFiled: February 4, 2000Date of Patent: July 10, 2001Assignee: Welfide CorporationInventors: Yoshiharu Hayashi, Nobuharu Goto
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Patent number: 6184244Abstract: This invention is directed to novel (N-substituted) indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury.Type: GrantFiled: June 30, 1999Date of Patent: February 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Xu Bai
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Patent number: 6174906Abstract: Novel to isooxazoles, oxazoles, thiazoles, isothiazoles and imidazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: October 1, 1999Date of Patent: January 16, 2001Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Juan Ignacio Luengo, Jia-Ning Xiang
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Patent number: 6172239Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.Type: GrantFiled: August 16, 1999Date of Patent: January 9, 2001Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis JeanJean, Jean-Charles Molimard, Robert Boigegrain