Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/426)
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Patent number: 6281365Abstract: Organic platinum complexes active as anti-tumor agents in warm-blooded animals, and methods for synthesis of same, are described.Type: GrantFiled: May 26, 1989Date of Patent: August 28, 2001Assignee: American Cyanamid CompanyInventors: Ralph Grassing Child, Panayota Bitha, Joseph John Hlavka, Yang-I Lin
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Patent number: 6235778Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present 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, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 26, 1997Date of Patent: May 22, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6191292Abstract: The invention relates to precursors of the A-ring of vitamin D, of the formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrization of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.Type: GrantFiled: December 8, 1999Date of Patent: February 20, 2001Assignee: Laboratoire TheramexInventors: Jean-Claude Pascal, Maurits Vandewalle, Philippe Maillos, Pierre De Clercq
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Patent number: 6150532Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.Type: GrantFiled: December 11, 1998Date of Patent: November 21, 2000Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
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Patent number: 6124333Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6100263Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;and their salts, processes and intermediates for their preparation, and their use are described.Type: GrantFiled: June 16, 1999Date of Patent: August 8, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 6090852Abstract: Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.Type: GrantFiled: January 20, 1999Date of Patent: July 18, 2000Assignee: Pfizer IncInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6077954Abstract: Novel compounds having the formula: ##STR1## wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: August 1, 1996Date of Patent: June 20, 2000Assignee: ISIS Pharmaceuticals, Inc.Inventors: P. Dan Cook, Haoyun An
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6043282Abstract: Azinooxime ethers of the formula I ##STR1## (X=NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ; Y=O, NZ, where Z=H, alkyl; R.sup.1 =H, alkyl; R.sup.2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it being possible for the radicals R.sup.2 to be different if m=2; R.sup.3 =H, cyano, alkyl, haloalkyl, alkoxy, cycloalkyl; R.sup.4, R.sup.5, R.sup.6 =indepedently of one another H, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl), and their salts, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests.Type: GrantFiled: July 29, 1998Date of Patent: March 28, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Muller, Ruth Muller, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5994359Abstract: 2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3 (Ia), C(CONHCH.sub.3).dbd.NOCH.sub.3 (Ib), C(CONH.sub.2).dbd.NOCH.sub.3 (Ic), C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3 (Id) or C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3 (Ie);R.sup.2 is cyano, nitro, halogen, alkyl, haloalkyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, hydroxyl, halogen,alkyl, haloalkyl, alkoxyalkyl, alkoxy, haloalkoxy, alkylthio, cyclopropyl, alkenyl,unsubstituted or substituted aryloxyalkyl, benzyl or benzyloxy,R.sup.4 is hydrogen, cyano,unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and hetaryl;unsubstituted or substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, heterocyclyloxy, aryloxy and hetaryloxy;unsubstituted or substituted arylthio and hetarylthio;--Q--C(R.sup.5).dbd.N--Y.sup.1 --R.sup.6 or --Q--O--N.dbd.CR.sup.7 R.sup.8,R.sup.3 and R.sup.Type: GrantFiled: June 25, 1998Date of Patent: November 30, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Hubert Sauter, Reinhard Kirstgen, Herbert Bayer, Ruth Muller, Bernd Muller, Klaus Oberdorf, Wassilios Grammenos, Norbert Gotz, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5985334Abstract: A method for identifying anti-convulsant compounds is presented. The binding of test compounds with a receptor obtained from rat forebrain is determined. The receptor has a Kd of about 40 nM and a molecular weight of about 130 kD. Two pyran compounds that bind to the receptor are also disclosed.Type: GrantFiled: September 26, 1997Date of Patent: November 16, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Hugh Jonathan Herdon, Jeffrey Clifford Jerman, Wai Ngor Chan
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Patent number: 5968962Abstract: A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.Type: GrantFiled: August 13, 1996Date of Patent: October 19, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn
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Patent number: 5952316Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.Type: GrantFiled: August 14, 1997Date of Patent: September 14, 1999Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5932595Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.Type: GrantFiled: December 18, 1996Date of Patent: August 3, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
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Patent number: 5929088Abstract: Novel cyclic amino acids of formula (Ia) or (Ib) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders.Type: GrantFiled: May 18, 1998Date of Patent: July 27, 1999Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Justin S. Bryans, Clare O. Kneen, Giles Ratcliffe
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Patent number: 5908863Abstract: Compounds of formula I: ##STR1## wherein R.sub.a, R.sub.b, .PHI., B and R are as defined in the disclosure, have antagonistic activity on osteoclast hyper-reactivity.Type: GrantFiled: February 26, 1997Date of Patent: June 1, 1999Assignee: Dompe' S.p.A.Inventors: Marcello Allegretti, Marco Mantovanini, Gianfranco Caselli, Simonetta Fiorentino, Gaetano Clavenna, Carmelo A. Gandolfi
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Patent number: 5908581Abstract: A red fluorescent material includes a compound of the formula: ##STR1## wherein: R.sub.1, and R.sub.2 are individually alkyl of from 1 to 20 carbon atoms, aryl, carbocyclic and other heterocyclic systems; andR.sub.3, and R.sub.4 are individually alkyl of from 1 to 10 carbon atoms, and a branched or unbranched 5 or 6 member substituent ring connecting with R.sub.1, R.sub.2 respectively; andR.sub.5 is alkyl of from 2-20 carbon atoms; sterically hindered aryl and heteroaryl; andR.sub.6 is alkyl of from 1 to 10 carbon atoms, and a 5 or 6-member carbocyclic ring connecting with R.sub.5.Type: GrantFiled: April 7, 1997Date of Patent: June 1, 1999Assignee: Eastman Kodak CompanyInventors: Chin H. Chen, Kevin P. Klubek, Jianmin Shi
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Patent number: 5789440Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.Type: GrantFiled: October 12, 1994Date of Patent: August 4, 1998Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Elizabeth Lunney, Bradley Dean Tait
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Patent number: 5767151Abstract: The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammateory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: June 23, 1997Date of Patent: June 16, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5760006Abstract: The use of compounds of the following formula I: ##STR1## for treating psoriasis is disclosed.Type: GrantFiled: June 23, 1997Date of Patent: June 2, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Richard P. Shank, Claudia K. Derian
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Patent number: 5760073Abstract: The substituted 4H-pyrans are prepared by reacting either aldehydes or ylidene compounds with suitably substituted .beta.-diketones. The substituted 4H-pyrans according to the invention are suitable as active compounds in medicaments, in particular for the treatment of disorders of the central nervous system.Type: GrantFiled: August 7, 1996Date of Patent: June 2, 1998Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Bodo Junge, Frank Mauler, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry
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Patent number: 5739085Abstract: O-(Oximino)ethylcyclohexenone oxime ethers I ##STR1## (R.sup.1 and R.sup.2 =C.sub.1 -C.sub.6 -alkyl; R.sup.3 =unsubstituted or substituted phenyl, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.4 -alkenyl or C.sub.3 -C.sub.4 -alkynyl, which in each case can be substituted by halogen, C.sub.1 -C.sub.3 -alkyl, unsubstituted or substituted phenyl or unsubstituted or substituted phenoxy;R.sup.4 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, unsubstituted or substituted phenylthio-C.sub.1 -C.sub.6 -alkyl, N-(C.sub.1 -C.sub.4 -alkylsulfonyl)-N-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, unsubstituted or substituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: May 5, 1995Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
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Patent number: 5723633Abstract: A pyran derivative has a structure ofR.sup.2 R.sup.3 C.dbd.(C.sub.5 H.sub.2 R.sup.1 O)--(CH.dbd.CH).sub.n --C.sub.6 H.sub.2 R.sup.6 R.sup.7 --NR.sup.4 R.sup.5wherein n is 3 or 4; R.sup.1 is a proton, alkyl or phenyl group; each of R.sup.2 and R.sup.3 is independently a cyano, alkoxycarbonyl having an alkyl, acyl having an alkyl, aracyl having phenyl, sulfonyl, aryl, or aryloxy; each of R.sup.4 and R.sup.5 is an alkyl group; and each of R.sup.6 and R.sup.7 is a proton, provided that R.sup.4 and R.sup.5 are alkyl groups, and a pair of R.sup.4 and R.sup.6 as well as a pair of R.sup.5 and R.sup.7 can be bonded to each other to form a heterocycle.A photosensitive composition comprises a polymerizable compound, a polymerization initiator and a photosensitizer which is the pyran derivative. A photosensitive resin composition comprises a crosslinkable polymer, a crosslinking agent and the photosensitizer.Type: GrantFiled: December 20, 1995Date of Patent: March 3, 1998Assignee: Canon Kabushiki KaishaInventors: Shin Kobayashi, Susumu Matsumura, Naosato Taniguchi, Yoko Yoshinaga, Toshiyuki Sudo, Hideki Morishima, Tadashi Kaneko
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Patent number: 5723681Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers 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: June 23, 1997Date of Patent: March 3, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5708178Abstract: Novel acceptor-donor-acceptor and donor-acceptor-donor compounds for use in forming a thermally-stable electro-optic waveguide are disclosed. Also disclosed is a thermally stable waveguide material containing thermally stable acceptor-donor-acceptor or donor-acceptor-donor guest dipole compounds in a temperature-resistant polymer matrix. The waveguide has selected regions in which the net dipoles of the guest molecules are oriented, for electro-optic switching when an electric field is placed across these regions.Type: GrantFiled: September 20, 1996Date of Patent: January 13, 1998Assignee: Lockheed Martin CorporationInventors: Susan P. Ermer, Doris S. Y. Leung, Steven M. Lovejoy
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Patent number: 5705527Abstract: An amino acid compound of the formula: R.sup.1 NH--CH(R.sup.2)--COHN--A--ONO.sub.2, wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.7 alkanoyl group, a C.sub.1 -C.sub.6 alkoxycarbonyl group, a C.sub.6 -C.sub.10 arylcarbonyl group, a C.sub.7 -C.sub.13 aralkylcarbonyl group, a C.sub.7 -C.sub.13 aralkyloxycarbonyl group or a 5- or 6-membered aromatic heterocyclic carbonyl group; R.sup.2 represents a substituted C.sub.1 -C.sub.6 alkyl group; and A represents a C.sub.2 -C.sub.5 alkylene group; and pharmacologically acceptable salts thereof. The amino acid compound has an excellent vasodilator action for collateral vessels and is useful for treating angina pectoris.Type: GrantFiled: April 20, 1995Date of Patent: January 6, 1998Assignee: Sankyo Company, LimitedInventors: Sadao Ishihara, Fujio Saito, Takao Yoshioka, Hiroyuki Koike, Shigeki Miyake, Hiroshi Mizuno
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Patent number: 5672615Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: March 11, 1996Date of Patent: September 30, 1997Assignee: Novartis CorporationInventors: Lawrence J. MacPherson, David Thomas Parker
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Patent number: 5658942Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl or hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group; have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.Type: GrantFiled: March 7, 1995Date of Patent: August 19, 1997Assignee: Sankyo Company, LimitedInventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
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Patent number: 5648503Abstract: Compounds of the formula ##STR1## which have retinoid-like biological activity.Type: GrantFiled: May 31, 1996Date of Patent: July 15, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
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Patent number: 5646147Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: April 20, 1994Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5618775Abstract: Mixtures of optically active cyclohexenone oxime ethers having R- and S-configuration in the oxime ether moiety of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; ##STR2## X=C.sub.1-C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; m=0-3 or 1-4 where all X's are halogen;n=0-3 or 1-5 where all X's are halogen;R.sup.2 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkenyl, substituted or unsubstituted 5-membered saturated heterocyclic structure, substituted or unsubstituted 6- or 7-membered heterocyclic structure, substituted or unsubstituted 5-membered heteroaromatic structure, substituted or unsubstituted phenyl or pyridyl)and their agriculturally useful salts and esters with C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids.Type: GrantFiled: August 11, 1994Date of Patent: April 8, 1997Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Wolfgang Ladner, Helmut Walter, Karl-Otto Westphalen, Uwe Kardorff, Matthias Gerber
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Patent number: 5604229Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.Type: GrantFiled: June 17, 1994Date of Patent: February 18, 1997Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5585520Abstract: Preparation of O-substituted hydroxylammonium salts IR.sup.1 --CHX--O--NH.sub.2.HL (I)(L=halogen, hydrogensulfate; X=H, alkyl; R.sup.1 =unsubst. or subst. phenyl, thienyl, furanyl, pyrrolyl or --CR.sup.2 .dbd.CR.sup.3 R.sup.4 ; R.sup.2, R.sup.3, R.sup.4 =H, halogen or alkyl) by reaction of an acetone oxime O-allyl or --O--benzyl ether II ##STR1## with water and a mineral acid H--L with continuous removal of the acetone formed in this process, by carrying out the hydrolysis batchwise at 0.degree.-50.degree. C. and under a pressure of 10-500 mbar is described.The O-substituted hydroxylammonium salts I are intermediates for plant protection agents and pharmaceuticals.Type: GrantFiled: January 11, 1996Date of Patent: December 17, 1996Assignee: BASF AktiengesellschaftInventors: Ulrich Klein, Ernst Buschmann, Michael Keil, Norbert G otz, Albrecht Harreus
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Patent number: 5563114Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is alkyl,A is unsubstituted or substituted C.sub.3 -, C.sub.5 - or C.sub.6 -alkylene or C.sub.3 -, C.sub.5 - or C.sub.6 -alkenylene,X is NO.sub.2, CN, halogen, alkyl, alkoxy, phenoxy, alkylthio, haloalkyl, haloalkoxy, carboxyl, alkoxycarbonyl, unsubstituted or substituted benzyloxycarbonyl and/or unsubstituted or substituted phenyl,n is 0-3 or 1-5 where X is halogen,R.sup.Type: GrantFiled: March 24, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Norbert Meyer, Juergen Kast, Ulf Misslitz, Albrecht Harreus, Norbert Goetz, Bruno Wuerzer, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5554582Abstract: Cyclohexenone compounds of the formula ##STR1## where R.sup.1 is alkyl of 1 to 4 carbon atoms, alkenyl or alkynyl of 3 or 4 carbon atoms, haloalkenyl of 3 or 4 carbon atoms and 1 to 3 halogen substituents, or is thenyl which is unsubstituted or substituted by halo and/or alkyl, R.sup.2 is alkyl of 1 to 4 carbon atoms, and R.sup.3 is formyl, a radical of the general formula R.sup.4 XCHXR.sup.5, where X is oxygen or sulfur, and R.sup.4 and R.sup.5 are identical or different alkyl, or together denote alkylene of 1 to 4 carbon atoms and which is unsubstituted or substituted by alkyl, alkoxy, alkylthio, hydroxy, halogen, cyano or N,N-dialkylamino, have a good herbicidal action preferably on species from the grass family.Type: GrantFiled: November 30, 1992Date of Patent: September 10, 1996Assignee: BASF AktiengesellschaftInventors: Michael Keil, Ulrich Schirmer, Dieter Kolassa, Juergen Kast, Bruno Wuerzer, Norbert Meyer
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Patent number: 5552419Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: November 3, 1994Date of Patent: September 3, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5543425Abstract: This invention relates to a method of inhibiting platelet aggregation comprising administering compounds having the following formula ##STR1##Type: GrantFiled: October 28, 1994Date of Patent: August 6, 1996Assignee: G. D. Searle & Co.Inventors: Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
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Patent number: 5536734Abstract: Crop protection agents contain dihydropyrans of the formula ##STR1## wherein the variable substituents are defined in the specification.Type: GrantFiled: June 21, 1994Date of Patent: July 16, 1996Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Siegbert Brand, Hubert Sauter, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5514683Abstract: The compounds of the formula I ##STR1## and their pharmaceutical acceptable salts, which are defined herein, are ligands for cholecystokinin and/or gastrin receptors.Type: GrantFiled: August 9, 1994Date of Patent: May 7, 1996Assignee: James Black Foundation LimitedInventors: Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley, Ildiko M. Buck, Katherine I. M. Steel, Jonathan M. R. Davies, David J. Dunstone, Elaine A. Harper, Michael J. Pether, Michael J. Bodkin, Matthew J. Tozer, Martin L. Hudson
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Patent number: 5506242Abstract: The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I ##STR1## wherein Ar, R, R.sub.1 and R.sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.Type: GrantFiled: June 24, 1994Date of Patent: April 9, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker, Arco Y. Jeng
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Patent number: 5496792Abstract: Cyclohexenone oxime ethers I ##STR1## R.sup.1 =C.sub.1 -C.sub.6 -alkyl; W=unsubstituted or C.sub.1 -C.sub.3 -alkyl-substituted C.sub.2 -C.sub.4 -alkylene chain;X=NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; n=0-3 or 1-5 if all X's are halogen;R.sup.2 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkenyl, a substituted or unsubstituted 5-membered saturated heterocycle containing 1 or 2 oxygen and/or sulfur atoms, substituted or unsubstituted 6- or 7-membered heterocycle having 1 or 2 non-adjacent oxygen and/or sulfur atoms and which is saturated or mono- or diunsaturated, substituted or unsubstituted 5-membered heteroaromatic containing 1 or 2N atoms and one O or S atom, phenyl or pyridyl, both of which are unsubstituted or bear 1-3 halogen, NO.sub.Type: GrantFiled: August 11, 1994Date of Patent: March 5, 1996Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Kaspar Bott, Helmut Walter, Karl-Otto Westphalen, Uwe Kardorff, Matthias Gerber
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Patent number: 5492942Abstract: A pyran derivative has a structure ofR.sup.2 R.sup.3 C.dbd.(C.sub.5 H.sub.2 R.sup.1 O)--(CH.dbd.CH).sub.n --C.sub.6 H.sub.2 R.sup.6 R.sup.7 --NR.sup.4 R.sup.5wherein n is 3 or 4; R.sup.1 is a proton, alkyl or phenyl group; each of R.sup.2 and R.sup.3 is independently a cyano, alkoxycarbonyl having an alkyl, acyl having an alkyl, aracyl having phenyl, sulfonyl, aryl, or aryloxy; each of R.sup.4 and R.sup.5 is an alkyl group; and each of R.sup.6 and R.sup.7 is a proton, provided that R.sup.4 and R.sup.5 are alkyl groups, and a pair of R.sup.4 and R.sup.6 as well as a pair of R.sup.5 and R.sup.7 can be bonded to each other to form a heterocycle.A photosensitive composition comprises a polymerizable compound, a polymerization initiator and a photosensitizer which is the pyran derivative. A photosensitive resin composition comprises a crosslinkable polymer, a crosslinking agent and the photosensitizer.Type: GrantFiled: May 24, 1994Date of Patent: February 20, 1996Assignee: Canon Kabushiki KaishaInventors: Shin Kobayashi, Susumu Matsumura, Naosato Taniguchi, Yoko Yoshinaga, Toshiyuki Sudo, Hideki Morishima, Tadashi Kaneko
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Patent number: 5484786Abstract: Compounds of structure ##STR1## where W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.5 and R.sup.6 are independently selected from hydrogen and alkyl, or R.sup.5 and R.sup.6, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## L.sup.1 and L.sup.2 are independently selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is oxygen, >NR.sup.9 where R.sup.9 is hydrogen or alkyl, or ##STR4## where n=0, 1, or 2, and A is selected from ##STR5## inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.Type: GrantFiled: August 24, 1993Date of Patent: January 16, 1996Assignee: Abbott LaboratoriesInventors: Joseph F. Dellaria, Anwer Basha, Lawrence A. Black, Linda J. Chernesky, Wendy Lee
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Patent number: 5476935Abstract: Dye-donor element for use according to thermal dye transfer comprising least one dye corresponding to the general formula (I): ##STR1## wherein Z is --CN, --COOR.sup.1 or --CONR.sup.2 R.sup.3 ; R.sup.1 is --H, (cyclo)alkyl, or aryl; R.sup.2 and R.sup.3 is --H, (cyclo)alkyl, aryl, or R.sup.2 and R.sup.3 together represent the atoms necessary to complete a heterocyclic nucleus; R.sup.4 and R.sup.5 is --H, (cyclo)alkyl, aryl, a heterocyclic ring, SO.sub.2 R.sup.8, COR.sup.8, CSR.sup.8, POR.sup.8 R.sup.9, OR.sup.6, NR.sup.6 R.sup.7, SR.sup.6, or R.sup.4 and R.sup.5 together represent the atoms necessary to complete a aliphatic ring, a heterocyclic ring including a heterocyclic ring carrying a fused-on aliphatic or aromatic ring; R.sup.6 and R.sup.7 is (cyclo)alkyl, aryl, alkenyl, aralkyl, aryl, a heterocyclic group, or R.sup.6 and R.sup.7 together represent the atoms necessary to complete a 5- or 6-membered ring; R.sup.8 and R.sup.Type: GrantFiled: May 18, 1994Date of Patent: December 19, 1995Assignee: Agfa-Gevert, N.V.Inventors: Luc Vanmaele, Hans Junek, Renate Dworczak
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5472984Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: December 29, 1993Date of Patent: December 5, 1995Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5463081Abstract: The invention relates to novel intermediates for the preparation of a certain group of novel phenylsulfonylurea herbicides, which herbicides are particularly advantageous for use in crop protection. The novel intermediate compounds are of the formula II ##STR1## and of the formula VI, ##STR2## as defined in the specification and claims. The intermediate compounds may be used to prepare herbicidal and plant growth regulating compounds of the formula I or salts thereof: ##STR3## as defined in the specification. The herbicides so obtained are particularly suitable for selectively controlling weeds.Type: GrantFiled: September 21, 1993Date of Patent: October 31, 1995Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Klaus Bauer, Hermann Bieringer
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Patent number: 5455258Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.Type: GrantFiled: January 6, 1993Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: RE37035Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: October 7, 1997Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim KGInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht