The Substituent Nitrogen Is Attached Indirectly To The Benzene Ring By Acyclic Nonionic Bonding Patents (Class 564/51)
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Patent number: 6063819Abstract: Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains.Type: GrantFiled: February 18, 1998Date of Patent: May 16, 2000Assignee: Cypros Pharmaceutical Corp.Inventors: Paul J. Marangos, Brian W. Sullivan, Torsten Wiemann, Anne M. Danks, Marina Sragovicz, Lewis R. Makings
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Patent number: 6057269Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.Type: GrantFiled: January 5, 1998Date of Patent: May 2, 2000Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
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Patent number: 6043284Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.Type: GrantFiled: February 5, 1998Date of Patent: March 28, 2000Assignee: Glaxo Wellcome Inc.Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
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Patent number: 6028223Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is ##STR2## pharmaceutical compositions thereof and methods of using such compounds and compositions as .alpha..sub.v .beta..sub.3 antagonists.Type: GrantFiled: August 27, 1996Date of Patent: February 22, 2000Assignee: G. D. Searle & Co.Inventors: Peter Gerrard Ruminski, Michael Clare, Paul Waddell Collins, Bipinchandra Nanubhai Desai, Richard John Lindmark, Joseph Gerace Rico, Thomas Edward Rogers, Mark Andrew Russell
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Patent number: 5998666Abstract: The invention concerns novel phenoxyethylamine derivatives having a high affinity for the 5-HT.sub.1A receptor, methods for preparing them, pharmaceutical compositions containing them and their use as medicine and particularly as inhibitors of gastric acid secretion or as antiemetic.Type: GrantFiled: March 11, 1999Date of Patent: December 7, 1999Assignee: Societe de Conseils de Recherches Et d'Applications ScientifiquesInventors: Dennis Bigg, Marie-Odile Galcera
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Patent number: 5892111Abstract: A cure-accelerator for an epoxy resin, which comprises a compound of the formula (I),R.sub.1 R.sub.2 NCONH--Ar--NECONR.sub.3 R.sub.4 (I)wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are C.sub.1 -C.sub.3 lower alkyl groups which may be the same or different, and Ar is a substituted tolylene group of the formula (II) ##STR1## (wherein R.sub.5 and R.sub.6 are C.sub.1 -C.sub.4 lower alkyl groups which may be the same or different) or a 1,5-naphthylene group.Type: GrantFiled: September 8, 1997Date of Patent: April 6, 1999Assignee: Hodogaya Chemical Co., Ltd.Inventor: Susumu Jinbo
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Patent number: 5872115Abstract: This invention is concerned with 2-ureido-benzamide compounds of the formula (1) ##STR1## in which R.sup.1 is H, halogen atom, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)dialkylamino and R.sup.2 is H, halogen atom, hydroxy, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.3 -C.sub.6) cycloalkylmethoxy, (C.sub.1 -C.sub.4) alkylthio, (C.sub.1 -C.sub.4) alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl or ##STR2## wherein j is an integer of from 0 to 2 and R.sup.3 and R.sup.4 are each independently H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkanoyl, (C.sub.1 -C.sub.4)alkylsulfonyl or (C.sub.1 -C.sub.4)alkylcarbamoyl, NR.sup.3 R.sup.4 can to form a pyrrolidine, piperidine, morpholine, imidazole or pyrazole ring;X is a (C.sub.3 -C.sub.15)alkyl, (C.sub.3 -C.sub.6) cycloalkyl, (C.sub.3 -C.sub.6) cycloalkylmethyl, .omega.-(C.sub.1 -C.sub.4) alkoxy-(C.sub.1 -C.sub.4) alkyl group or ##STR3## wherein k is an integer of from 1 to 4 and R.sup.5 and R.sup.Type: GrantFiled: December 30, 1996Date of Patent: February 16, 1999Assignees: Grelan Pharmaceutical Co. Ltd., Laboratoires Fournier S.C.A.Inventors: Jean Binet, Christian Guffroy, Hirotaka Kasai, Nagatoshi Wagatsuma
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Patent number: 5866611Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.Type: GrantFiled: May 19, 1994Date of Patent: February 2, 1999Assignee: Zeneca LimitedInventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5837873Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.Type: GrantFiled: March 24, 1995Date of Patent: November 17, 1998Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Lynn M. Codacovi, Steven J. Wittenberger
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Patent number: 5824705Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.Type: GrantFiled: July 29, 1994Date of Patent: October 20, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5753684Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: May 19, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5750573Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 5, 1995Date of Patent: May 12, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5744640Abstract: A fluorine rubber composition comprising a fluorine rubber and a polyfluoroalkyl group-containing block isocyanate compound represented by the following general formula:Rf(CH.sub.2)nXCONHRNHCOO(N.dbd.C--R.sup.2)mR.sup.1where Rf is a polyfluoroalkyl group having 4 to 20 carbon atoms; R is a divalent organic group; R.sup.1 is a lower alkyl group or phenyl group; R.sup.2 is a lower alkyl group; X is NH or O; n is an integer of 1 to 4 and m is 0 or 1, has a good vulcanization bond to metals without any substantial decrease in the rubber stretchability properly owned by the fluorine rubber.Type: GrantFiled: September 16, 1996Date of Patent: April 28, 1998Assignee: Nippon Mektron, LimitedInventors: Takashi Enokida, Akihiro Naraki, Eiichi Yamashita, Haruyoshi Tatsu
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Patent number: 5728874Abstract: The present invention relates to achiral polyurea oligomers, their uses and formulations as anti-HIV pharmaceuticals and to a process for the preparation of narrow mono- and polydispersed oligomers as an emodiment of the invention. The achiral oligomers are derived from repeating units of the monomer 4,4'-diamino-biphenyl-3,3'-disulfonic acid and are water soluble, have a rigid backbone, possess ordered anionic spacing and have a number average molecular weight of <20,000. The process relates to the synthesis of narrow poly- and mono-dipersed oligomers comprising the steps of: 1) restricting the crude olydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture; and/or 2) isolating the monodispersed anionic oligomer; and 3) optionally converting the narrow poly- or mono-dispersed anionic oligomer salt from Step 1 or 2 to a desired pharmaceutically-acceptable salt, especially a solim or potassium salt.Type: GrantFiled: December 27, 1993Date of Patent: March 17, 1998Assignees: Merrell Pharmaceuticals, Inc., The Dow Chemical Co.Inventors: Michael J. Mullins, Ray E. Drumright, Alan D. Cardin, Norton P. Peet
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Patent number: 5719320Abstract: A cure-accelerator for an epoxy resin, which comprises a compound of the formula (I),R.sub.1 R.sub.2 NCONH--Ar--NHCONR.sub.3 R.sub.4 (I)wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are C.sub.1 -C.sub.3 lower alkyl groups which may be the same or different, and Ar is a substituted tolylene group of the formula (II) ##STR1## wherein R.sub.5 and R.sub.6 are C.sub.1 -C.sub.4 lower alkyl groups which may be the same or different) or a 1,5-naphthylene group.Type: GrantFiled: April 8, 1996Date of Patent: February 17, 1998Assignee: Hodogaya Chemical Co., Ltd.Inventor: Susumu Jinbo
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Patent number: 5708004Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: January 13, 1998Assignee: Monsanto CompanyInventors: John J. Talley, Kathryn L. Reed
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Patent number: 5668136Abstract: A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.Type: GrantFiled: September 11, 1991Date of Patent: September 16, 1997Assignee: Eisai Co., Ltd.Inventors: Teiji Kimura, Nobuhisa Watanabe, Yasutaka Takase, Kenji Hayashi, Makoto Matsui, Hironori Ikuta, Youji Yamagishi, Kozo Akasaka, Hiroshi Tanaka, Issei Ohtsuka, Takao Saeki, Motoji Kogushi, Tohru Fujimori, Isao Saito
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Patent number: 5599984Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: September 29, 1994Date of Patent: February 4, 1997Assignee: The Picower Institute For Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5576335Abstract: Urea derivatives of formula (1) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: September 29, 1994Date of Patent: November 19, 1996Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Noriyoshi Sueda, Kazuhiko Yamada, Makoto Yanai, Katsutoshi Miura, Masato Horigome, Norio Oshida, Shigeru Hiramoto, Koichi Katasuyama, Fumihisa Nakata, Nobuhiro Kinoshita, Yoko Tsukada
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Patent number: 5576410Abstract: A diaminourea compound having the formula (I); ##STR1## wherein R.sub.1 and R.sub.2 are independently a straight or branched alkylene group having 2 to 8 carbon atoms, an alicyclic alkylene group having 6 to 15 carbon atoms, a phenylene group, a C.sub.1 -C.sub.4 alkyl-substituted phenylene group, a C.sub.1 -C.sub.4 mono- or di-alkylene substituted phenylene group, or a methanediphenylene group, and a production process thereof as well as a high heat resistant polyurethaneurea derived therefrom and a production process thereof.Type: GrantFiled: January 25, 1995Date of Patent: November 19, 1996Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Akihiko Yosizato, Satoshi Furubeppu
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Patent number: 5559153Abstract: Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing themThere are described benzoylguanidines of the formula I ##STR1## where R(1), R(3) or R(4) is --NR(6) C.dbd.X NR(7)R(8); X is oxygen, sulfur, R(6), R(7) and R(8) are H, (perfluoro)alk(en)yl, where R(7) and R(8) can also together be 4 or 5 methylene groups,the substituents R(1) to R(5) remaining in each case are H, Hal, (fluoro) alk(en)yl, CN, NO.sub.2, NR(16)R(17).Type: GrantFiled: August 11, 1994Date of Patent: September 24, 1996Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Hans-Jochen Lang, Heinz-Werner Kleemann, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5430059Abstract: A butenoic acid compound of the following formula: ##STR1## in which Z is O, S, vinylene or azomethyne, A is an alkylene group and J is phenyl group, is a useful in treating heart disease.Type: GrantFiled: December 20, 1993Date of Patent: July 4, 1995Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Toshiaki Ogawa, Hideyuki Adachi, Takanori Kawamura
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Patent number: 5414118Abstract: A diaminourea compound having the formula (I); ##STR1## wherein R.sub.1 and R.sub.2 are independently a straight or branched alkylene group having 2 to 8 carbon atoms, an alicyclic alkylene group having 6 to 15 carbon atoms, a phenylene group, a C.sub.1-C.sub.4 alkyl-substituted phenylene group, a C.sub.1-C.sub.4 mono- or di-alkylene substituted phenylene group, or a methanediphenylene group, and a production process thereof as well as a high heat resistant polyurethaneurea derived therefrom and a production process thereof.Type: GrantFiled: December 30, 1993Date of Patent: May 9, 1995Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Akihiko Yosizato, Satoshi Furubeppu
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Patent number: 5401426Abstract: Lactobionic acid amide compositions synthesized from lactobionic acid and a mixture of primary fatty amines, which contains at least 30 percent by weight of fatty amines having a chain length of 14 to 18 carbon atoms, and their use as softening, detergent, emulsifying, foam stabilizing and/or thickening components of detergents, rinsing or cleaning agents, softeners or cosmetic formulations.Type: GrantFiled: October 15, 1993Date of Patent: March 28, 1995Assignee: Solvay Deutschland GmbHInventors: Klaus-Guenter Gerling, Sabine Joisten, Kornelia Wendler, Claudia Schreer
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Patent number: 5389682Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: September 13, 1993Date of Patent: February 14, 1995Assignee: Warner-Lambert CompanyInventors: Bradley D. Tait, Michael W. Wilson
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Patent number: 5312820Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.Type: GrantFiled: July 17, 1992Date of Patent: May 17, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee, Steven M. Hutchins, Ralph A. Rivero
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Patent number: 5296591Abstract: The trifluoromethylketone derivatives (I) and pharmaceutically acceptable salts thereof have a human leukocyte elastase inhibiting activity and are useful as human leukocyte elastase inhibitors for treating or preventing degenerative diseases. The trifluoromethylketone derivatives (I) have the following formula: ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl which has one or two substituents selected from carboxy, esterified carboxy and di-C.sub.1-6 alkylcarbamoyl; phenyl(C.sub.1-6) alkyl, the phenyl moiety of which may have halogen or nitro or amino substituents and the alkyl moiety of which may have carboxy or esterified carboxy substituents; halo-phenyl; morpholino; or morpholino(C.sub.1-6) alkyl,R.sup.2 and R.sup.3 are each C.sub.1-6 alkyl,X is -- or --NH--, andY is ##STR2## and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 12, 1991Date of Patent: March 22, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Keiji Hemmi, Ichiro Shima, Keisuke Imai, Hirokazu Tanaka
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Patent number: 5276182Abstract: The preferred oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geomentry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of ARC.Type: GrantFiled: June 10, 1991Date of Patent: January 4, 1994Assignees: The Dow Chemical Company, Merrell Dow Pharmaceuticals Inc.Inventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
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Patent number: 5272144Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.Type: GrantFiled: June 13, 1991Date of Patent: December 21, 1993Assignee: Farmitalia Carlo Erba s.r.l.Inventors: Piero Melloni, Philippe Dostert, Arturo D. Torre, Alberto Bonsignori
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Patent number: 5254595Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.Type: GrantFiled: January 9, 1992Date of Patent: October 19, 1993Assignee: Elf SanofiInventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
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Patent number: 5221771Abstract: Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.Type: GrantFiled: July 15, 1992Date of Patent: June 22, 1993Assignee: Xoma CorporationInventors: Dayton T. Reardan, Dane A. Goff
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Patent number: 5220022Abstract: Disclosed are novel compounds of the formula ##STR1## wherein: R is ##STR2## where Ph is phenyl, or ##STR3## X is --NR.sub.5 R.sub.6 or --OR.sub.7 ; R.sub.1 and R.sub.2 are independently hydrogen, methyl, ethyl, cyclohexyl, ##STR4## butyl, or heptyl; R.sub.4 is o-phenylene or p-phenylene and R.sub.4 can be alkyl- halo- or alkoxy- substituted;R.sub.3 is hydrogen;R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, methyl, ethyl, tert-butyl, isobutyl, butyl, alkoxy, acyl, acylamino, aryl, amino, cyclohexyl, aminoalkyl and substituted or unsubstituted phenylamino;Y is sulfur and oxygen atom; and n is zero or 1; provided n=1 when Y is sulfur.Type: GrantFiled: January 28, 1991Date of Patent: June 15, 1993Assignee: International Paper Co.Inventors: Bruce M. Resnick, Allan J. Wexler
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Patent number: 5157099Abstract: Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl, groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.Type: GrantFiled: December 12, 1991Date of Patent: October 20, 1992Assignee: Xoma CorporationInventors: Dayton T. Reardan, Dane A. Goff
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Patent number: 5142095Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: August 17, 1989Date of Patent: August 25, 1992Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 5099030Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.Type: GrantFiled: June 27, 1991Date of Patent: March 24, 1992Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5090914Abstract: Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.Type: GrantFiled: August 24, 1990Date of Patent: February 25, 1992Assignee: Xoma CorporationInventors: Dayton T. Reardan, Dane A. Goff
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Patent number: 5066678Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof; wherein;R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-3 -alkyl group with the proviso that the sum total of carbon atom in R.sup.1 and R.sup.2 is not more than 4;X represents a direct bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene group and Y represents a direct bond or a C.sub.1-6 alkylene C.sub.2-6 alkenylene or C.sub.2-6 alknylene group with the proviso that the sum total of carbon atoms in X and Y is not more than 10;W represents a group ##STR2## wherein Z represents a group R.sup.3 (CH.sub.2).sub.q where q is 0, 1 or 2 and R.sup.3 is a group R.sup.4 CONH--, R.sup.4 NHCONH--, R.sup.4 R.sup.5 NSO.sub.2 NH--, R.sup.6 SO.sub.2 NH-- or --OH;R.sup.4 and R.sup.5 each represent a hydrogen atom or a C.sub.1-3 alkyl group;R.sup.6 represents a C.sub.1-3 alkyl group;R.sup.7 represents a chlorine atom or the group --CF.sub.Type: GrantFiled: April 23, 1990Date of Patent: November 19, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell, Charles Willbe, William L. Mitchell, Stephen Swanson, Brian D. Judkins
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5045565Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.Type: GrantFiled: September 8, 1989Date of Patent: September 3, 1991Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5030754Abstract: Hydroxy-terminated substituted diurea derivatives of hydroxy-terminated polyurea derivatives of secondary monoalkylamines and organic diisocyanates and hydroxy-terminated polyurea derivatives of secondary monalkylamines and prepolymers of organic diisocyanates with polyoxyalkylene polyols, such as hydroxy-terminated polyurea derivatives of secondary monoalkylamines and organic diisocyanates having the formula: ##STR1## wherein: R represents an aliphatic or an aromatic group containing from 6 to about 20 carbon atoms,R' represents H or an alkyl group containing 1 to 6 carbon atoms, andn is a positive integer having a value of 1 to 4.Type: GrantFiled: November 19, 1990Date of Patent: July 9, 1991Assignee: Texaco Chemical CompanyInventors: George P. Speranza, Jiang-Jen Lin
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Patent number: 5017618Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.Type: GrantFiled: September 18, 1989Date of Patent: May 21, 1991Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5001261Abstract: Cyclohexenone derivatives of the formula ##STR1## where R.sup.1, R.sup.2 R.sup.3, R.sup.4 and R.sup.5 have the meanings given in the disclosure, and their use for controlling unwanted plant growth.Type: GrantFiled: April 18, 1988Date of Patent: March 19, 1991Assignee: BASF AktiengesellschaftInventors: Michael Keil, Rainer Becker, Dieter Jahn, Norbert Goetz, Ulrich Schirmer, Bruno Wuerzer
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Patent number: 4997980Abstract: Disclosed are novel compounds of the formula: ##STR1## wherein: X=--NR.sub.5 R.sub.6, or --OR.sub.7 ;R.sub.1 and R.sub.2 are independently hydrogen, substituted or unsubstituted alkyl, haloalkyl, hydroxyalkyl alkoxyalkyl, alkylaminoalkyl or arylalkyl having up to 18 carbons, cycloalkyl; phenyl or naphthyl; alkylphenyl, cyanophenyl, halophenyl or alkoxyphenyl substituents;R.sub.3 is hydrogen, benzyl, alkoxybenzyl, halobenzyl or alkylbenzyl, provided that if neither R.sub.1 nor R.sub.2 is hydrogen, then R.sub.3 is hydrogen;R.sub.4 is a divalent aromatic group which is substituted or unsubstituted;R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen, alkyl, hydroxyalkyl, haloalkyl, alkoxyalkyl, alkylaminoalkyl, acylaminoalkyl, aminoalkyl or phenylalkyl having up to 12 carbons; a cycloalkyl substitutent; phenyl or naphthyl; an alkylphenyl, cyanophenyl, halophenyl or alkoxyphenyl substituent;Furthermore, either R.sub.1 and R.sub.3 or R.sub.1 and R.sub.Type: GrantFiled: April 17, 1989Date of Patent: March 5, 1991Assignee: Anitec Image CorporationInventors: Bruce M. Resnick, Allan J. Wexler
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Patent number: 4990668Abstract: Described is a process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of the formula ##STR1## wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl, or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, where R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.3 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5- to 7-membered heterocyclic group.The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.Type: GrantFiled: December 4, 1985Date of Patent: February 5, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Khuong H. X. Mai, Ghanshyam Patil, William L. Matier
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Patent number: 4943591Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.Type: GrantFiled: October 14, 1986Date of Patent: July 24, 1990Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4880840Type: GrantFiled: June 30, 1987Date of Patent: November 14, 1989Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Axel Ingendoh, Friedrich Berschauer, Anno de Jong, Martin Scheer
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Patent number: 4868210Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: March 30, 1988Date of Patent: September 19, 1989Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4849530Abstract: The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 6, 1988Date of Patent: July 18, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Gerhard Zol, Gerhard Pfarrhofer
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Patent number: 4822729Abstract: Cyan-forming color couplers according to the formula: ##STR1## wherein Z is hydrogen or a coupling off group, R.sup.1 is hydrogen, a halogen atom, alkyl, or alkoxy, R.sup.2 is hydrogen or alkyl, R.sub.3 is hydrogen, a halogen atom, alkyl, alkoxy, alkylsulphonyl, alkanamidosulphonyl, alkoxycarbonyl, alkanamidocarbonyl, alkanamido, alkylsulphonamido, or cyano, R.sup.4 is a substituent standing at the 3- or 6-position of the phenol and selected from hydrogen, a halogen atom, and alkyl, and n is 0 or 1. These couplers can be incorporated into (a) red-sensitized silver halide emulsion layer(s) of a photographic multilayer color element or in a non-light-sensitive colloid layer in water-permeable relationship with the red-sensitized emulsion layer(s).Type: GrantFiled: November 24, 1987Date of Patent: April 18, 1989Assignee: AGFA-Gevaert, N.V.Inventors: Marcel J. Monbaliu, Paul L. Van Meerbeeck