Silicon Containing Patents (Class 546/14)
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Patent number: 5700938Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 23, 1997Assignees: Eisai Co., Ltd., Eisai Chemical Co., Ltd.Inventors: Yoshio Urawa, Ken Furukawa, Toshikazu Shimizu, Yoji Yamagishi, Tomio Tsurugi, Tomio Ichino
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Patent number: 5688889Abstract: 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: GrantFiled: May 6, 1996Date of Patent: November 18, 1997Assignee: Rhone-Poulenc ChimieInventors: Edith Canivenc, Jose-Luis Roca-Ortega, Andrew Van Der Spuy
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Patent number: 5686608Abstract: 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: GrantFiled: April 24, 1995Date of Patent: November 11, 1997Assignee: Hoechst AktiengesellschaftInventors: Steffen Haber, Javier Manero
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Patent number: 5679818Abstract: 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: GrantFiled: July 26, 1996Date of Patent: October 21, 1997Assignee: The United States of America as represented by the Secretary of the NavyInventors: Daniel Bucca, Teddy M. Keller
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Patent number: 5677455Abstract: 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: GrantFiled: September 6, 1995Date of Patent: October 14, 1997Assignee: Ube Industries, Ltd.Inventors: Katsumasa Harada, Akio Matsushita, Yasuhiro Kawachi, Hiroshi Sasaki
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Patent number: 5677295Abstract: 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: GrantFiled: May 30, 1996Date of Patent: October 14, 1997Inventors: Amedeo A. Failli, Guy A. Schiehser, Oleg I. Bleyman
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Patent number: 5670492Abstract: 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: GrantFiled: November 28, 1995Date of Patent: September 23, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Nobuyoshi Amishiro, Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Akihiko Okamoto, Katsushige Gomi
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Patent number: 5656206Abstract: 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: GrantFiled: June 14, 1995Date of Patent: August 12, 1997Assignee: Transitions Optical, Inc.Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
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Patent number: 5654319Abstract: 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: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5650417Abstract: 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: GrantFiled: September 12, 1994Date of Patent: July 22, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: 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
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Patent number: 5648363Abstract: 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: GrantFiled: June 6, 1995Date of Patent: July 15, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5646161Abstract: 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: GrantFiled: June 6, 1995Date of Patent: July 8, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5644059Abstract: 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: GrantFiled: June 2, 1995Date of Patent: July 1, 1997Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Akiyoshi Kadoiri, Yasuko Konagai, Tetsuaki Yamaura, Noriko Kase
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Patent number: 5639764Abstract: 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: GrantFiled: June 6, 1995Date of Patent: June 17, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5633378Abstract: Polyalkylpiperidine compounds of the formula I ##STR1## in which Y is the group ##STR2## are very effective stabilizers for organic materials.Type: GrantFiled: June 29, 1995Date of Patent: May 27, 1997Assignee: Hoechst AktiengesellschaftInventors: Karl Gaa, Matthias Z ah, Josef Wiedemann
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Patent number: 5629326Abstract: 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: GrantFiled: June 6, 1995Date of Patent: May 13, 1997Assignee: 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
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Patent number: 5629428Abstract: 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: GrantFiled: May 10, 1994Date of Patent: May 13, 1997Assignee: Hoechst AktiengesellschaftInventors: Hubert Schlosser, Dietmar Jungbauer, Javier Manero
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Patent number: 5622958Abstract: 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: GrantFiled: December 1, 1994Date of Patent: April 22, 1997Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Matthew D. Shair, Taeyoung Yoon, T.-C. Chou
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Patent number: 5618931Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification have retinoid-like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: April 8, 1997Assignee: AllerganInventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5618943Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification have retinoid-like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: April 8, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Alan T. Johnson, Richard L. Beard, Min Teng, Tae K. Song, Harold N. Wong, Roshantha A. Chandraratna
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Patent number: 5616725Abstract: 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: GrantFiled: October 11, 1995Date of Patent: April 1, 1997Assignee: Ciba-Geigy CorporationInventors: John S. Zambounis, Zhimin Hao, Abul Iqbal
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Patent number: 5612343Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5605915Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification.Type: GrantFiled: May 31, 1996Date of Patent: February 25, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
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Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment
Patent number: 5599820Abstract: 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: GrantFiled: June 5, 1995Date of Patent: February 4, 1997Assignees: The Research Foundation of State University of New York, Indena SpA Gruppo Inverni Della BeffaInventors: Iwao Ojima, Ezio Bombardelli -
Patent number: 5596100Abstract: 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: GrantFiled: April 4, 1995Date of Patent: January 21, 1997Assignee: Iowa State University Research Foundation, Inc.Inventor: Richard C. Larock
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Patent number: 5595958Abstract: 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: GrantFiled: May 2, 1994Date of Patent: January 21, 1997Assignee: Zeneca LimitedInventors: Hsiao-Ling M. Chin, Nhan H. Nguyen, David B. Kanne, David L. Lee
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Patent number: 5595981Abstract: 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: GrantFiled: March 6, 1995Date of Patent: January 21, 1997Assignee: G.D. Searle & Co.Inventors: Thomas E. Barta, Richard A. Mueller
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Patent number: 5594011Abstract: 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: GrantFiled: November 10, 1994Date of Patent: January 14, 1997Assignee: SIBIA Neurosciences, Inc.Inventors: Ian A. McDonald, Jeffrey P. Whitten, Nicholas D. Cosford
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Patent number: 5591860Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: April 4, 1995Date of Patent: January 7, 1997Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Hing L. Sham, Chen Zhao
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Patent number: 5591854Abstract: A process of enantioselective synthesis of seven-membered carbocycles in the presence of di-rhodium(II) tetracarboxylate catalysts.Type: GrantFiled: October 14, 1994Date of Patent: January 7, 1997Assignee: Wake Forest UniversityInventor: Huw M. L. Davies
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Patent number: 5583233Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: March 30, 1995Date of Patent: December 10, 1996Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Hing L. Sham, Chen Zhao
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Patent number: 5578726Abstract: 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: GrantFiled: November 10, 1994Date of Patent: November 26, 1996Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Gary H. Rasmusson
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Patent number: 5578665Abstract: 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: GrantFiled: March 7, 1995Date of Patent: November 26, 1996Assignee: Ciba-Geigy CorporationInventors: Primo Carrozza, Valerio Borzatta
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Patent number: 5574162Abstract: 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: GrantFiled: May 31, 1995Date of Patent: November 12, 1996Assignee: Ciba-Geigy CorporationInventors: James P. Galbo, Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
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Patent number: 5571914Abstract: 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: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
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Patent number: 5563144Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 8, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Dominique Damour, Richard Labaudiniere, Jean-luc Malleron, Serge Mignani
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Patent number: 5563145Abstract: 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: GrantFiled: December 7, 1994Date of Patent: October 8, 1996Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Guy A. Schiehser, Oleg I. Bleyman
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Patent number: 5561232Abstract: 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: GrantFiled: October 6, 1994Date of Patent: October 1, 1996Assignee: Ciba-Geigy CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 5561179Abstract: 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: GrantFiled: November 21, 1995Date of Patent: October 1, 1996Assignee: Ciba-Geigy CorporationInventors: Valerio Borzatta, Primo Carrozza
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Patent number: 5559236Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignees: Eisai Co., Ltd., Eisai Chemical Co., Ltd.Inventors: Yoshio Urawa, Ken Furukawa, Toshikazu Shimizu, Yoji Yamagishi, Tomio Tsurugi, Tomio Ichino
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Leukotriene-B.sub.4 antagonists, process for their production and their use as pharmaceutical agents
Patent number: 5559134Abstract: 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: GrantFiled: March 23, 1995Date of Patent: September 24, 1996Assignee: Schering AktiengesellschaftInventors: Bernd Buchmann, Werner Skuballa, Josef Heindl, Wolfgang Fr ohlich, Roland Ekerdt, Claudia Giesen -
Patent number: 5554633Abstract: 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: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5554627Abstract: 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: GrantFiled: April 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Richard T. Lewis, Angus M. MacLeod, Kevin J. Merchant
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Patent number: 5552409Abstract: 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: GrantFiled: March 31, 1994Date of Patent: September 3, 1996Assignee: Rohm and Haas CompanyInventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
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Patent number: 5550241Abstract: The present invention relates to novel adducts of cyclic carbonyl monomers with substituted olefins, which also are useful as solution viscosifiers.Type: GrantFiled: March 18, 1993Date of Patent: August 27, 1996Assignee: Exxon Research and Engineering CompanyInventor: Stanley J. Brois
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Patent number: 5550234Abstract: 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: GrantFiled: June 29, 1995Date of Patent: August 27, 1996Assignee: Hoechst AktiengesellschaftInventors: Karl Gaa, Matthias Z ah
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Patent number: 5543523Abstract: Activated isoquinolines and naphthalenes are disclosed which are useful to prepare korupensamines, michellamines and analogs thereof.Type: GrantFiled: November 15, 1994Date of Patent: August 6, 1996Assignee: Regents of the University of MinnesotaInventor: Thomas R. Hoye
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Propenoic acid derivatives diazole propenoic acid compounds which have useful pharmaceutical utility
Patent number: 5541213Abstract: 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: GrantFiled: June 10, 1994Date of Patent: July 30, 1996Assignee: 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: 5541321Abstract: A process is disclosed for the preparation of a substituted diaminoalcohol of the formula: ##STR1##Type: GrantFiled: March 30, 1995Date of Patent: July 30, 1996Assignee: Abbott LaboratoriesInventors: William R. Baker, John K. Pratt, Daniel W. Norbeck, Chen Zhao
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Patent number: 5541320Abstract: A process is disclosed for the preparation of a substituted diaminoalcohol of the formula: ##STR1##Type: GrantFiled: March 30, 1995Date of Patent: July 30, 1996Assignee: Abbot LaboratoriesInventors: William R. Baker, John K. Pratt, Daniel W. Norbeck, Chen Zhao