The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/340)
-
Patent number: 6358965Abstract: The invention relates to the use of compounds of formula for the preparation of medicines designed for the treatment of neuronal and cerebral disorders. The invention also relates to the compounds of formula: a process for their preparation and the pharmaceutical compositions containing them.Type: GrantFiled: August 5, 1999Date of Patent: March 19, 2002Assignee: Sanofi-SynthelaboInventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi, Alessandra Ielmini
-
Publication number: 20020028945Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: June 11, 2001Publication date: March 7, 2002Inventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffrey S. Carter, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
-
Patent number: 6353110Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.Type: GrantFiled: November 24, 1999Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
-
Patent number: 6342505Abstract: The invention relates to the use of a compound of formula (I): for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-&bgr;1.Type: GrantFiled: April 10, 2000Date of Patent: January 29, 2002Assignee: Sanofi-SynthelaboInventors: Françoise Bono-Combie, Jacqueline Fournier, Jean Marc Herbert, Isabelle Lamarche, Umberto Guzzi
-
Publication number: 20020010344Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: April 10, 2001Publication date: January 24, 2002Inventors: Michael S. South, John J. Parlow
-
Patent number: 6333082Abstract: Liquid crystalline compounds useful in super twisted nematic liquid crystal displays are described and have the formula: wherein n is 1-5; m is 0-5; p is 0, 1 or 2; q is 0, 1 or 2 p+q is less than or equal to 3; A1, A2, A3 are independently chosen from 1,4-disubstituted benzene, 2,5-disubstituted pyrimidine, 1,5-disubstituted pyridine, 2,6-disubstituted naphthalene which may be laterally substituted with F, Cl, Br or CN, trans-1,4-disubstituted cyclohexane, 2,5-disubstituted dioxane, 2,5-disubstituted thiophene, 2,5-disubstituted furan, 2,5-disubstituted thiodiazole Z1 may be COO, OOC, OCH2, O; Z2, Z3 are independently chosen from a direct bond, COO, OOC, C2H4, CH2O, OCH2, C4H8, C3H6O, (E)—CH═CHC2H4, (E)—CH═CHCH2O, —C≡C—; R1 is alkyl, and may contain up to 20 carbon atoms and may be branched or a straight chain; provided that at least one of, A1, A2, A3 is selected from 1,4-disubstituted thiophene.Type: GrantFiled: June 30, 2000Date of Patent: December 25, 2001Assignee: QinetiQ LtdInventors: Warren L Duffy, John W Goodby, Stephen M Kelly
-
Patent number: 6326492Abstract: Described are compounds of the Formula VII: wherein Het, R1, R7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: May 26, 2000Date of Patent: December 4, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Tianbao Lu, Bruce E. Tomczuk, Richard M. Soll, John Spurlino, Roger Bone
-
Patent number: 6316630Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.Type: GrantFiled: June 6, 2000Date of Patent: November 13, 2001Assignee: Sloan Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
-
Patent number: 6307087Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.Type: GrantFiled: January 13, 1999Date of Patent: October 23, 2001Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
-
Patent number: 6300352Abstract: The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations containing them and methods for their preparation.Type: GrantFiled: May 11, 1998Date of Patent: October 9, 2001Assignee: AstraZeneca ABInventors: David Cheshire, David Cladingboel, Simon Hirst, Carol Manners, Michael Stocks
-
Patent number: 6281231Abstract: The object is to provide a novel compound, with which there is little possibility of phytotoxicity for crop plants, and which is greatly effective in controlling various plant diseases caused by viruses pathogenic to plants, by bacteria, and by molds, and to provide agricultural chemicals, particularly agents for controlling plant diseases, containing this compound, 2,6-dichloro-4-pyridinemethanol, and/or a benzoic acid ester thereof as an active ingredient.Type: GrantFiled: March 9, 2000Date of Patent: August 28, 2001Assignee: Dainippon Ink and Chemical, Inc.Inventors: Toru Asada, Mika Iiyama, Hiroyuki Tsuboi, Takashi Gotou
-
Patent number: 6271386Abstract: This invention relates to stable, quaternized vinlypyridine carboxylate home-, co- and ter-polymers, useful as dye transfer inhibitors and polymers complexable with active agrochemical, pharmaceutical or cosmetic agents for controlled release thereof, and to a commercial process for the synthesis of said polymers in high yield and purity.Type: GrantFiled: September 22, 1999Date of Patent: August 7, 2001Assignee: ISP Investments Inc.Inventors: Jenn S. Shih, Eduardo T. Yap, John C. Hornby, Bala Srinivas
-
Patent number: 6268503Abstract: A series of compounds capable of deriving an intermediate for the production of compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N′-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.Type: GrantFiled: July 7, 2000Date of Patent: July 31, 2001Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Kozo Matsui, Kiyoshi Sugi, Yoshihide Umemoto, Tetsuya Shintaku, Nobushige Itaya
-
Patent number: 6265409Abstract: The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations including them and methods for their preparation.Type: GrantFiled: May 11, 1998Date of Patent: July 24, 2001Assignee: AstraZeneca ABInventors: David Cheshire, David Cladingboel, Simon Hirst, Carol Manners, Michael Stocks
-
Patent number: 6252081Abstract: The present invention provides a novel industrially or economically preferable process for production of a hydrogen halogenide salt of a Donepezil derivative having an excellent pharmacological action as medicament, namely, reaction of 1-indanone derivative with carbonate ester to obtain 2-alkoxycarbonyl-1-indanone derivative, followed by reaction with halogenated (4-pyridyl)methyl or a salt thereof and decarboxylation successively to obtain 2-(4-pyridyl)methyl-1-indanone derivative, then reaction with halogenated benzyl to obtain quaternary ammonium salt, then reduction, and synthetic intermediates thereof. (Wherein R1 represents a hydrogen atom or lower alkoxy; n represents an integer of 1 to 4; R2 represents lower alkyl group; and X represents a halogen atom.Type: GrantFiled: June 27, 2000Date of Patent: June 26, 2001Assignee: Eisai Co., Ltd.Inventor: Yoichi Iimura
-
Patent number: 6239175Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.Type: GrantFiled: December 21, 1999Date of Patent: May 29, 2001Assignee: Smithkline Beecham p.l.c.Inventors: Jeremy David Hinks, Andrew Kenneth Takle, Eric Hunt
-
Patent number: 6232319Abstract: The invention relates to compounds of general formula (I): in which R, R1, R2, X and Y are as defined in the description, their geometrical and/or optical isomers, and their addition salts with a pharmaceutically-acceptable acid or base, as well as to medicaments containing the same.Type: GrantFiled: June 4, 1999Date of Patent: May 15, 2001Assignee: Adir et CompagnieInventors: Christian Marazano, Delphine Compere, Bhupesh Chandra Das, Jean Lepagnol
-
Patent number: 6228848Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: GrantFiled: November 22, 1999Date of Patent: May 8, 2001Assignee: Allergan, Inc.Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
-
Patent number: 6218539Abstract: The present invention relates to the use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: May 10, 1999Date of Patent: April 17, 2001Assignee: SmithKline Beecham CorporationInventor: Katherine L. Widdowson
-
Patent number: 6204388Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.Type: GrantFiled: February 24, 1999Date of Patent: March 20, 2001Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin, Scott Kuduk, Christina Harris, Xiu-Guo Zhang, Joseph R. Bertino
-
Patent number: 6174905Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: GrantFiled: September 26, 1997Date of Patent: January 16, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
-
Patent number: 6118004Abstract: A cyclobutenedione derivative. It comprises substituted or non-substituted aromatic group A; conjugated chain B which may contain an aromatic bonding group; and hydrogen bonding or ion bonding cyclobutenedionyl group C having an aromatic group which is bonded to the conjugated chain B, wherein A and B and C are bonded in the form of A-B-C. Crystal of the derivative is used as a non-linear optical device.Type: GrantFiled: November 6, 1998Date of Patent: September 12, 2000Assignee: Fuji Xerox Co., Ltd.Inventors: Yasunari Nishikata, Lyong Sun Pu
-
Patent number: 6106908Abstract: Liquid crystalline compounds useful in super twisted nematic liquid crystal displays are described and have the formula: ##STR1## wherein n is 1-5;m is 0-5;p is 0, 1 or 2;q is 0, 1 or 2p+q is less than or equal to 3;A.sub.1, A.sub.2, A.sub.3 are independently chosen from 1,4-disubstituted benzene 2,5-disubstituted pyrimidine, 1,5-disubstituted pyridine, 2,6-disubstituted naphthalene which may be laterally substituted with F, Cl, Br or CN, trans-1,4-disubstituted cyclohexane 2,5-disubstituted dioxane, 2,5-disubstituted thiophene, 2,5-disubstituted furan, 2,5-disubstituted thiodiazoleZ.sub.1 may be COO, OOC, OCH.sub.2, O;Z.sub.2, Z.sub.3 are independently chosen from a direct bond, COO, OOC, C.sub.2 H.sub.4, CH.sub.2 O, OCH.sub.2, C.sub.4 H.sub.8, C.sub.3 H.sub.6 O, (E)--CH.dbd.CHC.sub.2 H.sub.4, (E)--CH.dbd.CHCH.sub.2 O, --C.tbd.C--;R.sub.1 is alkyl, and may contain up to 20 carbon atoms and may be branched or a straight chain; provided that at least one of, A.sub.1, A.sub.2, A.sub.Type: GrantFiled: March 19, 1999Date of Patent: August 22, 2000Assignee: The Secretary of State for Defence in Her Britannic Majesty's Government of the United Kingdom of Great Britain and Northern IrelandInventors: Warren L Duffy, John W Goodby, Stephen M Kelly
-
Patent number: 6100403Abstract: A method of producing a compound represented by the formula: ##STR1## wherein R.sup.1 stands for hydrogen or an optionally substituted alkyl or acyl group, which comprises reacting a compound represented by the formula: ##STR2## wherein R.sup.1 is of the same meaning as defined above, and R.sup.2 stands for an optionally halolgenated alkyl group or an optionally substituted phenyl group with a compound represented by the formula: ##STR3## in a lower alcohol in the presence of an alkali metal or alkaline earth metal carbonate; the compound (III) being useful as starting compounds for producing thiazolidinedione derivatives having hypoglycemic and hypolipidemic activities.Type: GrantFiled: April 12, 1999Date of Patent: August 8, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Yuzuru Saito, Hideya Mizufune, Makoto Yamashita
-
Patent number: 6080839Abstract: The invention relates to a novel labeling reactant, suitable for labeling of a biospecific binding reactant using solid-phase synthesis. The invention further concerns new labeling methods. The novel labeling reactant has the formula (I) ##STR1## wherein -A- is a bivalent aromatic structure capable of absorbing light or energy and transferring the excitation energy to a lanthanide ion after the product made by the said solid-phase synthesis has been released from the used solid support, deprotected and converted to a lanthanide chelate;-G- is a bridge replacing a hydrogen atom in A;R is a protected amino acid residue --CH(NHX)COOH, where X is a transient protecting group, or its active ester, where said ester is e.g. an N-hydroxysuccinimido, p-nitrophenol or pentafluorophenol ester; andR' is --COOR'" where R'" is an alkyl of 1 to 4 carbon atoms, phenyl or benzyl, which phenyl or benzyl can be substituted or unsubstituted.Type: GrantFiled: June 25, 1998Date of Patent: June 27, 2000Assignee: Wallac OyInventors: Harri Takalo, Jari Hovinen, Veli-Matti Mukkala, Paivi Liitti, Heikki Mikola
-
Patent number: 6046227Abstract: 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..sub.3 receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: December 4, 1998Date of Patent: April 4, 2000Assignee: Eli Lilly and CompanyInventors: Thomas Alan Crowell, Charles David Jones, Anthony John Shuker
-
Patent number: 6034090Abstract: The invention relates to compounds of the formula in which: Y is --CH-- or --N--; R.sub.1 is hydrogen, a halogen or a CF.sub.3, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy group; R.sub.2 is a methyl or ethyl group; R.sub.3 and R.sub.4 are each hydrogen or a (C.sub.1 -C.sub.3)alkyl; and X is:(a) a (C.sub.1 -C.sub.6)alkyl, a (C.sub.1 -C.sub.6)alkoxy, a (C.sub.3 -C.sub.7)carboxyalkyl, a (C.sub.1 -C.sub.4)alkoxy-carbonyl(C.sub.1 -C.sub.6)alkyl, a (C.sub.3 -C.sub.7)carboxyalkoxy or a (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.6)alkoxy;(b) a radical selected from (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkoxy, (C.sub.3 -C.sub.7)-cycloalkylmethyl, (C.sub.3 -C.sub.7)cycloalkylamino and cyclohexenyl, it being possible for said radical to be substituted by a halogen, hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, amino or mono- or di-(C.sub.1 -C.sub.4)-alkylamino; or(c) a group selected from a phenyl, phenoxy, phenylamino, N-(C.sub.1 -C.sub.Type: GrantFiled: July 27, 1999Date of Patent: March 7, 2000Assignee: Sanofi-SynthlaboInventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi
-
Patent number: 6020368Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.Type: GrantFiled: December 4, 1998Date of Patent: February 1, 2000Inventors: Jeremy David Hinks, Andrew Kenneth Takle, Eric Hunt
-
Patent number: 6013795Abstract: Briefly, in one aspect, the present invention provides compositions of open-chain, .alpha.-branched fluoroalkylcarbonyl fluorides, and derivatives thereof.Type: GrantFiled: November 4, 1996Date of Patent: January 11, 2000Assignee: 3M Innovative Properties CompanyInventors: Anthony P. Manzara, Wei-Qiang Fan, Richard M. Stern, George G. I. Moore
-
Patent number: 6004903Abstract: Benzoyl derivatives of the formula I ##STR1## where Z is a 5-membered or 6-membered heterocyclic, saturated or unsaturated radical containing one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen,Q is a cyclohexane-1, 3-dione ring bonded in the 2-position and of the formula II, ##STR2## or conventional agricultural salts of the compounds I.Type: GrantFiled: August 14, 1997Date of Patent: December 21, 1999Assignee: Basf AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Franz Rohl, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
-
Patent number: 6005113Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.Type: GrantFiled: May 14, 1997Date of Patent: December 21, 1999Assignee: Molecular Probes, Inc.Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
-
Patent number: 5998625Abstract: This invention relates to a process for the preparation of a key intermediate using an chiral additive to effect an asymmetric conjugate addition.Type: GrantFiled: January 5, 1998Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Richard D. Tillyer, David M. Tschaen, Feng Xu
-
Patent number: 5994539Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.Type: GrantFiled: December 18, 1997Date of Patent: November 30, 1999Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro
-
Patent number: 5990314Abstract: This invention relates to a compound of formula I ##STR1## These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.Type: GrantFiled: June 7, 1996Date of Patent: November 23, 1999Assignee: SmithKline Beecham CorporationInventor: Robert A. Daines
-
Patent number: 5977105Abstract: A compound of formula I, ##STR1## wherein--X represents (CH.sub.2).sub.n O, (CH.sub.2).sub.n S or C.sub.2 alkylene;n represents 1 or 2;Ar.sup.1 represents indanyl, tetrahydronaphthyl, naphthyl or phenyl, which latter two groups may be substituted by one or more substituents selected from chloro, fluoro, OR.sup.1, O(CH.sub.2).sub.m CONR.sup.20 R.sup.21, C(O)R.sup.2, C.sub.1-6 alkyl (optionally substituted by one or more fluorine atoms), pyridyl, thiazinyl, phenyl or C.sub.7-9 alkylphenyl which latter two groups are optionally substituted by one or more substituent selected from halo, nitro, OR.sup.3, C.sub.1-6 alkyl (optionally substituted by one or more fluorine atoms), C(O)R.sup.4, C(O)OR.sup.5, C(O)N(R.sup.6)R.sup.7, CN, CH.sub.2 OR.sup.14, CH.sub.2 NR.sup.15 R.sup.16, N(R.sup.8)R.sup.9, N(R.sup.10)SO.sub.2 R.sup.11, N(R.sup.12)C(O)R.sup.13, OC(O)R.sup.19 and SO.sub.2 NR.sup.17 R.sup.18 ;m represents an integer 1 to 3;R.sup.1, R.sup.2 and R.sup.3 independently represent H, C.sub.Type: GrantFiled: March 3, 1997Date of Patent: November 2, 1999Assignee: Astra Pharmaeuticals Ltd.Inventors: David Cheshire, David Cladingboel, David Hardern, Michael Stocks
-
Patent number: 5952509Abstract: A method of producing a compound represented by the formula: ##STR1## wherein R.sup.1 stands for hydrogen or an optionally substituted alkyl or acyl group, which comprises reacting a compound represented by the formula: ##STR2## wherein R.sup.1 is of the same meaning as defined above, and R.sup.2 stands for an optionally halolgenated alkyl group or an optionally substituted phenyl group with a compound represented by the formula: ##STR3## in a lower alcohol in the presence of an alkali metal or alkaline earth metal carbonate; the compound (III) being useful as starting compounds for producing thiazolidinedione derivatives having hypoglycemic and hypolipidemic activities.Type: GrantFiled: June 23, 1997Date of Patent: September 14, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Yuzuru Saito, Hideya Mizufune, Makoto Yamashita
-
Patent number: 5948915Abstract: A cyclobutenedione derivative. It comprises substituted or non-substituted aromatic group A; conjugated chain B which may contain an aromatic bonding group; and hydrogen bonding or ion bonding cyclobutenedionyl group C having an aromatic group which is bonded to the conjugated chain B, wherein A and B and C are bonded in the form of A--B--C. Crystal of the derivative is used as a non-linear optical device.Type: GrantFiled: September 29, 1997Date of Patent: September 7, 1999Assignee: Fuji Xerox Co., Ltd.Inventors: Yasunari Nishikata, Lyong Sun Pu
-
Patent number: 5925645Abstract: The 2-aryl-substituted pyridines are prepared by reacting pyridylaldehydes with organometallic compounds and then selectively reducing the products. The 2-aryl-substituted pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis.Type: GrantFiled: March 13, 1997Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Rolf Angerbauer, Arndt Brandes, Michael Logers, Matthias Muller-Gliemann, Hilmar Bischoff, Delf Schmidt, Stefan Wohlfeil
-
Patent number: 5922742Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: April 2, 1997Date of Patent: July 13, 1999Assignee: Merck Frosst CanadaInventors: Cameron Black, Zhaoyin Wang, Greg Hughes
-
Patent number: 5919937Abstract: The invention encompasses a novel process for the formation of enantiomerically enriched mixtures of compounds of Formula I, which are useful precursors in the synthesis of phosphodiestersae IV inhibitors.Type: GrantFiled: October 7, 1998Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Joseph E. Lynch, Kenneth M. Wells, Yao-Jun Shi
-
Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
-
Patent number: 5908851Abstract: Compounds of formula (I), ##STR1## wherein X is a --CO.sub.2 H or --CONHOH group; R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.Type: GrantFiled: October 7, 1997Date of Patent: June 1, 1999Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Andrew Miller, Zoe Marie Spavold, Mark Whittaker
-
Patent number: 5906989Abstract: The invention relates to 7-?5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)! heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.Type: GrantFiled: May 26, 1998Date of Patent: May 25, 1999Assignee: Allergan Sales, Inc.Inventor: Robert M. Burk
-
Patent number: 5863926Abstract: The present invention relates to novel 4,4-(disubstituted)cyclohexan-1-carboxylate monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: October 6, 1997Date of Patent: January 26, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
-
Patent number: 5861421Abstract: This invention relates to derivatives of 4,4-(disubstituted)cyclohexan-1-ones and related compounds which are useful for treating allergic and inflammatory diseases.Type: GrantFiled: June 23, 1997Date of Patent: January 19, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
-
Patent number: 5851427Abstract: Photocross-linkable naphthyl derivatives include compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each independently signify a cross-linkable group;S.sup.1 and S.sup.2 signify --(CY.sub.2).sub.m -, --O(CY.sub.2).sub.m -, --(CY.sub.2).sub.m O--, --(CY.sub.2).sub.m COO--, --(CY.sub.2).sub.m OOC--, --(Si?(CH.sub.3).sub.2 !O).sub.m -, --OCH.sub.2 (Si?(CH.sub.3).sub.2 !O).sub.m Si?(CH.sub.3).sub.2 !CH.sub.2 O-- or --NHCH.sub.2 (Si?(CH.sub.3).sub.2 !O).sub.m Si?(CH.sub.3).sub.2 !CH.sub.2 NH--;Y signifies hydrogen, fluorine or methyl;a signifies 0 or 1;b signifies 1 or 2, with the proviso that a+b=2;m signifies a whole number of 1 to 16;A.sup.1 and A.sup.2 each independently signify 1,4-phenylene, which is optionally mono- or multiply-substituted with halogen, cyano, methyl, methoxy and/or acetyl, pyridine-2,5-diyl, pyrimidine-2,5-diyl, trans-1,4-cyclohexylene or trans-1,3-dioxane-2,5-diyl; andZ.sup.1 and Z.sup.2 each independently signify a single bond, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.Type: GrantFiled: February 23, 1996Date of Patent: December 22, 1998Assignee: Rolic AGInventor: Stephen Kelly
-
Patent number: 5849923Abstract: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH=CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.C is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl.Type: GrantFiled: June 4, 1996Date of Patent: December 15, 1998Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, Nicholas A. Meanwell
-
Patent number: 5817836Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.Type: GrantFiled: May 12, 1997Date of Patent: October 6, 1998Assignee: AllerganInventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
-
Patent number: 5817842Abstract: Process for the epoxidation of olefins with oxygen and/or air and a redox system, in the presence of titanium silicalite, characterized in that the redox system is selected from:1) quinone/hydroquinone derivatives having the general formula (Ia) and (Ib) ##STR1## 2) acetophenone/1-phenyl ethanol derivatives having the general formula (IIa) and (IIb) ##STR2##Type: GrantFiled: July 9, 1997Date of Patent: October 6, 1998Assignee: Enichem S.p.A.Inventors: Mario Gabriele Clerici, Alberto de Angelis, Patrizia Ingallina
-
Patent number: RE36575Abstract: A compound of the formula: ##STR1## (wherein R.sup.1 is hydrogen or a lower alkyl) can be produced advantageously by (1) reacting a compound of the formula: ##STR2## (wherein R.sup.1 has the meaning given above) with a halogenating agent or sulfonyl halide to give a compound of the formula: ##STR3## (wherein R.sup.1 has the meaning given above and X is a halogen or an alkyl- or aryl-sulfonyloxy), (2) reacting the resulting compound with a compound of the formula: ##STR4## to give a compound of the formula: ##STR5## (wherein R.sup.1 has the meaning given above), (3) reacting the resulting compound with a compound of the formula: ##STR6## to give a compound of the formula: ##STR7## (wherein R.sup.1 has the meaning given above), and (4) subjecting the resulting compound to catalytic reduction.Type: GrantFiled: October 10, 1997Date of Patent: February 15, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Kanji Meguro, Takeshi Fujita, Chitoshi Hatanaka, Satoru Ooi