Silicon Containing Patents (Class 546/14)
  • Patent number: 5700938
    Abstract: The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo?4,5-b!pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo?4,5-b!pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 23, 1997
    Assignees: Eisai Co., Ltd., Eisai Chemical Co., Ltd.
    Inventors: Yoshio Urawa, Ken Furukawa, Toshikazu Shimizu, Yoji Yamagishi, Tomio Tsurugi, Tomio Ichino
  • Patent number: 5688889
    Abstract: Process for conditioning textile materials in order to enable them to have, especially, a pleasant handle and a very low or even non-existent yellowing, characterized in that the textile materials are brought into contact with a composition comprising a polyorgano-siloxane having, per mole, at least one unit of general formula: ##EQU1## in which: R can represent a C.sub.1 -C.sub.4 alkyl radical;X can represent a hydrolysable radical;Z represents a residue containing (a) sterically hindered piperidyl group(s) of formulae: ##STR1## in which R.sup.1 is a divalent hydrocarbon radical, R'.sup.1 is a trivalent hydrocarbon radical, U and U' represent --O--, --NH-- or --N(alkyl)-, R.sup.2 can represent a C.sub.1 -C.sub.3 alkyl radical and R.sup.3 is H or R.sup.2,a and b are chosen from 0, 1 and 2,the sum a+b being not greater than 2.
    Type: Grant
    Filed: May 6, 1996
    Date of Patent: November 18, 1997
    Assignee: Rhone-Poulenc Chimie
    Inventors: Edith Canivenc, Jose-Luis Roca-Ortega, Andrew Van Der Spuy
  • Patent number: 5686608
    Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium as catalyst comprises adding to the reactiona) at least one water-soluble complexing ligand andb) sufficient water for the reaction mixture to form an aqueous phase.The reaction of the invention proceeds chemoselectively so that even electrophilic groups such as esters or nitriles do not have an adverse effect on the course of the reaction.The use according to the invention of a water-soluble complexing ligand in an aqueous phase enables polycyclic aromatic compounds to be prepared in very good yields and at the same time very high purity, in particular without contamination by the complexing ligands.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: November 11, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Steffen Haber, Javier Manero
  • Patent number: 5679818
    Abstract: The present invention is a compound having the formula:R.sup.1 --Ac.sup.1 --Ar.sup.1 --M--Ar.sup.2 --Ac.sup.2 --R.sup.2where R.sup.1 and R.sup.2 are independently selected from the group consing of hydrogen, unsubstituted alkyl groups, substituted alkyl groups, unsubstituted aryl groups, and substituted aryl groups, where Ac.sup.1 and Ac.sup.2 are independently selected alkynyl groups having at least 1 carbon-carbon triple bond, where Ar.sup.1 and Ar.sup.2 are independently selected substituted or unsubstituted aromatic diradicals, and where M has the structure ##STR1## where m is a positive integer, wherein x, p, y, r, n, and z are independently selected integers, where z.noteq.0 when n.noteq.0, and where R.sup.3 through R.sup.14 are independently selected from the group consisting of hydrogen, unsubstituted alkyl groups, substituted alkyl groups, unsubstituted aryl groups, and substituted aryl groups.
    Type: Grant
    Filed: July 26, 1996
    Date of Patent: October 21, 1997
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Daniel Bucca, Teddy M. Keller
  • Patent number: 5677455
    Abstract: Methyl (3R,6E)-3-?(tert-butyldimethylsilyl)oxy!-7-?2',6'-diisopropyl-4'-(4"-fluor ophenyl)-5'-(methoxymethyl)pyridin-3'-yl!-5-oxy-6-heptenoate or other 3-oxy-5-oxo-6-heptenoic acid derivative is prepared by the reaction of an aromatic aldehyde and an oxyglutaric acid derivative in an aliphatic alcohol containing a small amount of water in the presence of an alkali metal carbonate or hydrogen carbonate.
    Type: Grant
    Filed: September 6, 1995
    Date of Patent: October 14, 1997
    Assignee: Ube Industries, Ltd.
    Inventors: Katsumasa Harada, Akio Matsushita, Yasuhiro Kawachi, Hiroshi Sasaki
  • Patent number: 5677295
    Abstract: A compound of the structure ##STR1## wherein X--Y is C.dbd.NOR.sup.1 or CHNHOR.sup.2 ; R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO--, --(CH.sub.2).sub.m Ar, or --COR.sup.3 ;R.sup.3 is alkyl of 1-6 carbon atoms, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5, or --OR.sup.4 ;R.sup.4 and R.sup.5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring;Ar is an aryl or heteroaryl radical which may be optionally substituted; and m=0-6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: October 14, 1997
    Inventors: Amedeo A. Failli, Guy A. Schiehser, Oleg I. Bleyman
  • Patent number: 5670492
    Abstract: Provided are DC-89 derivatives represented by the formula: ##STR1## wherein X represents Cl or Br, R represents hydrogen or COR.sup.1, and W represents ##STR2## and pharmaceutically acceptable salts thereof. The compounds of the present invention have excellent anti-tumor activity and are useful as anti-tumor agents.
    Type: Grant
    Filed: November 28, 1995
    Date of Patent: September 23, 1997
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Nobuyoshi Amishiro, Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Akihiko Okamoto, Katsushige Gomi
  • Patent number: 5656206
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: August 12, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
  • Patent number: 5654319
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5650417
    Abstract: Substituted pyridines, their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## and to salts thereof in which 1, 2, 3 or 4 of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are an aliphatic, alicyclic or araliphatic radical bonded by a --O--CH.sub.2 -- or --O--CO--, and the remaining ones of these radicals are H, halogen or an aliphatic or aromatic radical, X is O, S or optionally substituted imino, Y is a bond or a bivalent radical and Z is an aromatic radical or optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and to their use as pesticides, in particular as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: July 22, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5648363
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 15, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5646161
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 8, 1997
    Assignee: Hoechst-Marion-Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5644059
    Abstract: 1,4-dihydropyridine derivatives and optically active 1,4-dihydropyridine derivatives with the following formula, having vasodilating activity based on calcium antagonism, and PAF antaognism, and methods of producing the same are disclosed: ##STR1## wherein (*) indicates a chiral center in the case of the optically active 1,4-dihydropyridine derivatives.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 1, 1997
    Assignee: Fujirebio Inc.
    Inventors: Hiroshi Ikawa, Akiyoshi Kadoiri, Yasuko Konagai, Tetsuaki Yamaura, Noriko Kase
  • Patent number: 5639764
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 17, 1997
    Assignee: Hoechst-Marion-Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5633378
    Abstract: Polyalkylpiperidine compounds of the formula I ##STR1## in which Y is the group ##STR2## are very effective stabilizers for organic materials.
    Type: Grant
    Filed: June 29, 1995
    Date of Patent: May 27, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Karl Gaa, Matthias Z ah, Josef Wiedemann
  • Patent number: 5629326
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 13, 1997
    Assignee: Hoechst-Marion-Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5629428
    Abstract: 3-Chloropyridines, process for their preparation, and their use in liquid-crystal mixturesA 3-chloropyridine of the formula (I) ##STR1## in which the symbols have the following meaning: R.sup.1 and R.sup.2, independently of one another, are, for example, H or straight-chain or branched alkyl, A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M.sup.1, M.sup.2, M.sup.3 and M.sup.4 are identical or different and are, for example, --O-- or --CO--O--, R.sup.3, R.sup.4, R.sup.6 and R.sup.7, independently of one another are, for example, H or straight-chain or branched alkyl, M.sup.5 is, for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.
    Type: Grant
    Filed: May 10, 1994
    Date of Patent: May 13, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hubert Schlosser, Dietmar Jungbauer, Javier Manero
  • Patent number: 5622958
    Abstract: A quinone imine enediyne possessing cytotoxic activity towards cancer cells having the general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, or OH or a linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or a linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or a linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or a linear or branched alkyl, etc; wherein R.sub.7 is H, OH or S--SR", or a linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl group; and wherein R, R' and R" are independently the same or different and are a linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl group.
    Type: Grant
    Filed: December 1, 1994
    Date of Patent: April 22, 1997
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Matthew D. Shair, Taeyoung Yoon, T.-C. Chou
  • Patent number: 5618931
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: April 8, 1997
    Assignee: Allergan
    Inventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5618943
    Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: April 8, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Richard L. Beard, Min Teng, Tae K. Song, Harold N. Wong, Roshantha A. Chandraratna
  • Patent number: 5616725
    Abstract: Pyrrolo[3,4-c]pyrroles of formula ##STR1## wherein D and E are each independently of the other a group of formula ##STR2## The symbols Q, R.sub.8, R.sub.9, R.sub.10, R.sub.11, X, Y, Z, m and n are as defined in claim 1.These pyrrolo[3,4-c]pyrroles are distinguished by outstanding solid state fluorescence in the UV range as well as by the ease with which they can be converted to pyrrolopyrrole pigments even in the substrate in which they are incorporated.
    Type: Grant
    Filed: October 11, 1995
    Date of Patent: April 1, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: John S. Zambounis, Zhimin Hao, Abul Iqbal
  • Patent number: 5612343
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5605915
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: February 25, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
  • Patent number: 5599820
    Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 4, 1997
    Assignees: The Research Foundation of State University of New York, Indena SpA Gruppo Inverni Della Beffa
    Inventors: Iwao Ojima, Ezio Bombardelli
  • Patent number: 5596100
    Abstract: A method is provided for the regioselective, palladium catalyzed carbo- or heteroannulation of internal alkynes by aryl iodides containing o-substituted side chains to yield aromatic carbocyclic and heterocyclic ring systems.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: January 21, 1997
    Assignee: Iowa State University Research Foundation, Inc.
    Inventor: Richard C. Larock
  • Patent number: 5595958
    Abstract: Herbicidal 3-substituted pyridine compounds and derivatives thereof of the formula: ##STR1## wherein Ar is a substituted or unsubstituted 5- or 6-membered heteroaryl group having 1, 2 or 3 ring nitrogen atoms with the remainder of the ring atoms being carbon; a substituted or unsubstituted 5-membered heteroaryl group having a ring heteroatom of oxygen or sulfur with the remainder of the ring atoms being carbon; or a substituted or unsubstituted 5-membered heteroaryl group having one ring nitrogen atom and either an oxygen or sulfur ring heteroatom with the remainder of the ring atoms being carbon. Herbicidal compositions containing such 3-substituted pyridine compounds and derivatives thereof and methods of controlling undesirable vegetation employing these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the disclosed 3-substituted pyridine derivatives.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: January 21, 1997
    Assignee: Zeneca Limited
    Inventors: Hsiao-Ling M. Chin, Nhan H. Nguyen, David B. Kanne, David L. Lee
  • Patent number: 5595981
    Abstract: Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: January 21, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Thomas E. Barta, Richard A. Mueller
  • Patent number: 5594011
    Abstract: In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: January 14, 1997
    Assignee: SIBIA Neurosciences, Inc.
    Inventors: Ian A. McDonald, Jeffrey P. Whitten, Nicholas D. Cosford
  • Patent number: 5591860
    Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: January 7, 1997
    Assignee: Abbott Laboratories
    Inventors: Dale J. Kempf, Daniel W. Norbeck, Hing L. Sham, Chen Zhao
  • Patent number: 5591854
    Abstract: A process of enantioselective synthesis of seven-membered carbocycles in the presence of di-rhodium(II) tetracarboxylate catalysts.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: January 7, 1997
    Assignee: Wake Forest University
    Inventor: Huw M. L. Davies
  • Patent number: 5583233
    Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: December 10, 1996
    Assignee: Abbott Laboratories
    Inventors: Dale J. Kempf, Daniel W. Norbeck, Hing L. Sham, Chen Zhao
  • Patent number: 5578726
    Abstract: Described is a new process for producing 7.beta.-substituted-4-aza-5.alpha.-androstan-3-ones and related compounds which are 5.alpha.-reductase inhibitors, consisting of reducing the corresponding androsteneone with lithium and liquid ammonia, contacting the product with an isomerizing agent, oxidizing the product to a seco acid and reacting that seco acid with an amine to cyclize to form 4-aza-5.alpha.-androstan-3-ones.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: November 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Gary H. Rasmusson
  • Patent number: 5578665
    Abstract: The present invention relates to novel piperidine compounds of the formula (I) ##STR1## in which A is e.g. a group of the formula ##STR2## where R.sub.4 is e.g. hydrogen or methyl, X.sub.3 is e.g. --O-- or --NH-- and R.sub.5 ' is e.g. ethylene, propylene or decamethylene, R.sub.1 is e.g. methyl, methoxy, ethoxy or OH, R.sub.2 and R.sub.3 are e.g. methyl, m+n is e.g. a number from 1 to 40, n varies e.g. from zero to 50% of the sum m+n, X.sub.1 is e.g. as defined for R.sub.1 or is a group (CH.sub.3).sub.3 SiO-- and X.sub.2 is e.g. hydrogen, methyl, ethyl, a group (CH.sub.3).sub.3 Si-- or a group ##STR3## and, when m+n is a number from 3 to 10, X.sub.1 and X.sub.2 together also form a direct bond. The compounds of the formula (I) are effective in stabilizing an organic material against thermal, oxidative and light-induced degradation.
    Type: Grant
    Filed: March 7, 1995
    Date of Patent: November 26, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Primo Carrozza, Valerio Borzatta
  • Patent number: 5574162
    Abstract: 1-Hydrocarbyloxy substituted hindered amine compounds which also contain a reactive functional group such as hydroxy, amino, oxirane or carboxyl can be chemically attached to selected polymer substrates by condensation reactions to give polymers containing a chemically-bonded, non-migrating stabilizer having excellent stabilization efficacy for protecting said polymer substrate from the adverse effects of actinic light.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: November 12, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: James P. Galbo, Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
  • Patent number: 5571914
    Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 5, 1996
    Assignee: Taiho Pharmaceutical Co. Ltd.
    Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
  • Patent number: 5563144
    Abstract: This invention relates to compounds having the formula R.sub.1 -(CH.sub.2).sub.n -Het wherein R.sub.1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; R.sub.3 is a hydrogen atom or a phenyl radical; R.sub.4 is a hydrogen or halogen atom or a residue Het; R.sub.5 is a carbonyl or sulfonyl radical; R.sub.6 is a radical Si(CH.sub.3).sub.2 or C(CH.sub.3).sub.2 ; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 8, 1996
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Dominique Damour, Richard Labaudiniere, Jean-luc Malleron, Serge Mignani
  • Patent number: 5563145
    Abstract: A compound of the structure ##STR1## wherein X-Y is C=NOR.sup.1 or CHNHOR.sup.2 ; R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO--, --(CH.sub.2).sub.m Ar, or --COR.sup.3 ;R.sup.3 is alkyl of 1-6 carbon atoms, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5, or -OR.sup.4 ;R.sup.4 and R.sup.5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring;Ar is an aryl or heteroaryl radical which may be optionally substituted; and m=0-6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
    Type: Grant
    Filed: December 7, 1994
    Date of Patent: October 8, 1996
    Assignee: American Home Products Corporation
    Inventors: Amedeo A. Failli, Guy A. Schiehser, Oleg I. Bleyman
  • Patent number: 5561232
    Abstract: Compounds of formulaA(B).sub.x, (I),whereinx is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores am distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: October 1, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
  • Patent number: 5561179
    Abstract: Compounds of the formula (I) ##STR1## in which m and n are numbers from 1 to 50; A is --O-- or >N--R.sub.6 where R.sub.6 is e.g. hydrogen or C.sub.1 -C.sub.18 alkyl; R.sub.1 and R.sub.4, which may be identical or different, are C.sub.1 -C.sub.18 alkyl, phenyl, C.sub.1 -C.sub.8 alkoxy, OH, ONa or OK; R.sub.2 is e.g. C.sub.2 -C.sub.12 alkylene; R.sub.3 is e.g. hydrogen or C.sub.1 -C.sub.8 alkyl; R.sub.5 is e.g. a group of the formula ##STR2## in which R.sub.9 is e.g. 2,2,6,6-tetramethyl-4-piperidyl; A' has one of the meanings of A; p is e.g. 1 and R.sub.10 is e.g. C.sub.2 -C.sub.18 alkylene; X.sub.1 has one of the meanings of R.sub.1 or is a group (R.sub.27).sub.3 SiO-- where R.sub.27 is C.sub.1 -C.sub.18 alkyl; X.sub.2 is hydrogen, Na, K, C.sub.1 -C.sub.8 alkyl or a group (R.sub.27).sub.3 Si-- with R.sub.27 as defined above and, when m+n is a number from 3 to 10, X.sub.1 and X.sub.
    Type: Grant
    Filed: November 21, 1995
    Date of Patent: October 1, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Valerio Borzatta, Primo Carrozza
  • Patent number: 5559236
    Abstract: The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo-[4,5-b]pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 24, 1996
    Assignees: Eisai Co., Ltd., Eisai Chemical Co., Ltd.
    Inventors: Yoshio Urawa, Ken Furukawa, Toshikazu Shimizu, Yoji Yamagishi, Tomio Tsurugi, Tomio Ichino
  • Patent number: 5559134
    Abstract: The invention relates to leukotriene-B.sub.4 antagonists of formula I ##STR1## in which n represents a whole number from 2 to 5,X represents a direct bond, 1 to 6 methylene units, an ortho-, meta- or para-substituted phenyl ring or a meta- or para-substituted pyridine ring,Y represents a bond to a hydrogen atom and simultaneously to a hydroxy group, a double-bound oxygen atom or --O--CH.sub.2 --CH.sub.2 --O--,R.sub.1 and R.sub.2 represent the radical OH, --O--(C.sub.1 -C.sub.4)--alkyl, O--(C.sub.3 -C.sub.6)--cycloalkyl, --O--(C.sub.6 -C.sub.10)--aryl, --O--(C.sub.7 -C.sub.12)--aralkyl, O--(CH.sub.2)--CO-- (C.sub.6 -C.sub.10)--aryl or the radical NHR.sub.3 with R.sub.3 meaning hydrogen, (C.sub.1 -C.sub.4)--alkyl, (C.sub.3 -C.sub.6)--cycloalkyl or (C.sub.7 -C.sub.12)--aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates.
    Type: Grant
    Filed: March 23, 1995
    Date of Patent: September 24, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Bernd Buchmann, Werner Skuballa, Josef Heindl, Wolfgang Fr ohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5554633
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.
    Type: Grant
    Filed: January 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Martin R. Teall
  • Patent number: 5554627
    Abstract: Compounds of formula (I), wherein Q.sup.1 represents an aryl group; the dotted line represents an optional covalent bond; one of X and Y represents H and the other represents hydroxy or C.sub.1-6 alkoxy, or X and Y together form a group .dbd.O or .dbd.NOR.sup.5 where R.sup.5 is H or C.sub.1-6 alkyl; Z represents O, S or NR.sup.2, where R.sup.2 is H or C.sub.1-6 alkyl; W represents a bond or a saturated or unsaturated hydrocarbon chain of 1, 2, 3, 4, 5 or 6 carbon atoms; R.sup.1 represents H or C.sub.1-6 alkyl. R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 represents an optionally substituted phenyl group; and R.sup.6 represents a specified amino group or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; and salts and prodrugs are tachykinin receptor antagonists.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Richard T. Lewis, Angus M. MacLeod, Kevin J. Merchant
  • Patent number: 5552409
    Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.
    Type: Grant
    Filed: March 31, 1994
    Date of Patent: September 3, 1996
    Assignee: Rohm and Haas Company
    Inventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
  • Patent number: 5550241
    Abstract: The present invention relates to novel adducts of cyclic carbonyl monomers with substituted olefins, which also are useful as solution viscosifiers.
    Type: Grant
    Filed: March 18, 1993
    Date of Patent: August 27, 1996
    Assignee: Exxon Research and Engineering Company
    Inventor: Stanley J. Brois
  • Patent number: 5550234
    Abstract: Polyalkylpiperidine compounds of the formula I ##STR1## in which Y is one of the groups ##STR2## are distinguished by very low volatility at elevated temperature and are very effective stabilizers for organic substances.
    Type: Grant
    Filed: June 29, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Karl Gaa, Matthias Z ah
  • Patent number: 5543523
    Abstract: Activated isoquinolines and naphthalenes are disclosed which are useful to prepare korupensamines, michellamines and analogs thereof.
    Type: Grant
    Filed: November 15, 1994
    Date of Patent: August 6, 1996
    Assignee: Regents of the University of Minnesota
    Inventor: Thomas R. Hoye
  • Patent number: 5541213
    Abstract: A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I): ##STR1## (wherein A represents an aromatic ring; R.sup.1 represents aryl or the like; R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like; and R.sup.7 and R.sup.8 each represent lower alkyl or the like) or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: June 10, 1994
    Date of Patent: July 30, 1996
    Assignee: Eisai Co., Ltd.
    Inventors: Masayuki Matsukura, Keizoh Satoh, Naoki Yoneda, Makoto Kaino, Kazutoshi Miyake, Yoshiharu Daiku, Naoya Kishi, Fusayo Yoshida, Kenichi Nomoto, Toshiaki Ogawa, Tadanobu Takamura, Koichi Nose, Mikio Tomimatsu, Masanori Mizuno, Shigeto Negi, Shigeru Souda
  • Patent number: 5541321
    Abstract: A process is disclosed for the preparation of a substituted diaminoalcohol of the formula: ##STR1##
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: July 30, 1996
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, John K. Pratt, Daniel W. Norbeck, Chen Zhao
  • Patent number: 5541320
    Abstract: A process is disclosed for the preparation of a substituted diaminoalcohol of the formula: ##STR1##
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: July 30, 1996
    Assignee: Abbot Laboratories
    Inventors: William R. Baker, John K. Pratt, Daniel W. Norbeck, Chen Zhao