At Least Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 548/153)
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Publication number: 20020183369Abstract: This invention relates to compounds of Formula I 1Type: ApplicationFiled: April 5, 2002Publication date: December 5, 2002Inventor: Daisy Joe Du Bois
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Patent number: 6479527Abstract: A pharmaceutical composition comprising a compound of formula (I): or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1 and wherein A and B together form an optionally substituted 5-member aromatic ring which includes at least one heteroatom; R1 is an optionally substituted aryl or heteroaryl ring; R2 is selected from a range of organic groups including carboxy, and R3 is hydrogen, or a range of organic groups; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and these form a further aspect of the invention.Type: GrantFiled: July 26, 2000Date of Patent: November 12, 2002Assignee: AstraZeneca UK LimitedInventors: Andrew J. Barker, Alan W Faull, Jason G. Kettle
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Publication number: 20020156287Abstract: The present invention relates to new bromo- and chlorothiazolium salts of the formula (I) 1Type: ApplicationFiled: December 18, 2001Publication date: October 24, 2002Inventors: Joachim Rudolph, Ralf Wischnat
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Patent number: 6461747Abstract: Disclosed is a material for a light emitting device excellent in color purity, good in light emitting characteristics and excellent in stability, which consists of a compound represented by the following general formula (I): L&Parenopenst;A)m (I) wherein A represents a heterocyclic group in which two or more aromatic heterocycles are condensed; m represents an integer of 2 or more, and the heterocyclic groups represented by A may be the same or different; and L represents a connecting group.Type: GrantFiled: July 21, 2000Date of Patent: October 8, 2002Assignee: Fuji Photo Co., Ltd.Inventors: Hisashi Okada, Toshihiro Ise
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Publication number: 20020049215Abstract: Pyrazole-thiazole compounds that modulate and/or inhibit the activity of cyclin-dependent kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating cyclin-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: ApplicationFiled: August 8, 2001Publication date: April 25, 2002Inventors: Wesley Kwan Mung Chong, Rohit Kumar Duvadie
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Publication number: 20020045759Abstract: The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: ApplicationFiled: April 6, 2001Publication date: April 18, 2002Inventors: Craig A. Stump, Theresa M. Williams
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Patent number: 6127395Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: August 3, 1999Date of Patent: October 3, 2000Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 6096771Abstract: An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.Type: GrantFiled: February 3, 1999Date of Patent: August 1, 2000Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
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Patent number: 5998408Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 8, 1997Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5851425Abstract: Compounds of the general formula ##STR1## have a pronounced tendency to form liquid crystalline S (smectic) phases. Thus, optically inactive compounds of the formula I also have a tilted smectic phase, in particular an S.sub.C phase, in addition to a nematic phase. In contrast, many optically active compounds of the formula I additionally have, inter alia, a tilted smectic chiral phase, in particular a chiral S.sub.C phase, in addition to a cholesteric phase. The stated compounds are therefore particularly suitable as components and as dopants, respectively, for the preparation of a very wide range of liquid crystalline mixtures. The class of compounds comprising compounds of the general formula I offers a broad range of novel components and mixtures for optimization and modification of liquid crystalline mixtures.Type: GrantFiled: March 26, 1997Date of Patent: December 22, 1998Assignee: Rolic AGInventors: Richard Buchecker, Willy Friedrichsen, Jurg Funfschilling, Sandra Lupfert
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5733648Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: March 31, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5703093Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: May 31, 1995Date of Patent: December 30, 1997Assignee: Cytomed, Inc.Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
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Patent number: 5693460Abstract: This invention provides a silver halide photographic element comprising a silver halide emulsion in reactive association with a dioxide compound represented by the following formula: ##STR1## wherein b is C(O), C(S), C(Se), CH2 or (CH2)2; and R.sup.1 and R.sup.2 are independently H, or aliphatic, aromatic or heterocyclic groups, or R.sup.1 and R.sup.2 together represent the atoms necessary to form a five or six-membered ring or a multiple ring system. This invention further provides a method of making silver halide emulsions containing the dioxide compounds.Type: GrantFiled: June 24, 1996Date of Patent: December 2, 1997Assignee: Eastman Kodak CompanyInventor: Roger Lok
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Patent number: 5637724Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 5, 1995Date of Patent: June 10, 1997Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 5637725Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 5, 1995Date of Patent: June 10, 1997Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 5633371Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5591762Abstract: Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl.An exemplary compound is:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.Type: GrantFiled: June 1, 1995Date of Patent: January 7, 1997Assignee: Dr. Karl Thomae GmbHInventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
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Patent number: 5521213Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: August 29, 1994Date of Patent: May 28, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
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Patent number: 5434165Abstract: An aromatic amino-substituted compound represented by formula: ##STR1## wherein A represents CH, N, or N.fwdarw.O; R.sub.1 represents a nitro group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, or an acyl group; and R.sub.3 represents a group: ##STR2## wherein m represents 0 or 1; n represents an integer of from 0 to 3; R.sub.4 and R.sub.5 each represents a hydrogen atom or a lower alkyl group; R.sub.6 and R.sub.7 each represents a hydrogen atom or a straight chain or branched lower alkyl group; R.sub.4 and R.sub.6 may be joined together to form an alkylene chain forming a heterocyclic ring; R.sub.5 and R.sub.7 may be joined together to form an alkylene chain forming a heterocyclic ring and R.sub.6 and R.sub.Type: GrantFiled: November 13, 1992Date of Patent: July 18, 1995Assignee: Sanawa Kagaku Kenkyusho Company, Ltd.Inventors: Masayasu Kurono, Yutaka Baba, Tomoo Suzuki, Tsunemasa Suzuki, Kiyotaka Hirooka, Kiichi Sawai
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Patent number: 5350760Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: August 4, 1993Date of Patent: September 27, 1994Assignee: Merck Frosst Canada, Inc.Inventors: Mark LaBelle, Yibin Xiang, Claude Dufresne, Michel Belley
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Patent number: 5350857Abstract: This invention relates to improved imaging systems based on the formation of green-yellow colored coordination compounds of transition metals with certain ligands. The formation of colored coordination compounds can be employed to generate images and is important in the manufacture and use of pressure sensitive transfer papers for preparing carbonless copies. In particular, this invention relates to certain 2,5-bis(substituted aryl)thiazolo[5,4-d]thiazole compounds, and particularly to certain 2,5-bis(o-hydroxyaryl)thiazolo[5,4-d]thiazole compounds, to their coordination compounds with certain transition metals, and to their use in pressure sensitive carbonless copy paper systems. These compounds have been found to provide excellent green-yellow colors when used in pressure sensitive carbonless copy-papers wherein the image is formed by the reaction of a color-forming compound with transition metal salts such as those of nickel, cobalt, iron, copper, and similar materials.Type: GrantFiled: January 3, 1994Date of Patent: September 27, 1994Assignee: Minnesota Mining and Manufacturing CompanyInventor: Nusrallah Jubran
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Patent number: 5240938Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: August 13, 1991Date of Patent: August 31, 1993Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Thomas F. Walsh, Kenneth J. Fitch, Ralph A. Rivero, Daljit S. Dhanoa
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Patent number: 5194177Abstract: An optically active compound represented by the following formula (I): ##STR1## wherein R.sub.1 denotes a linear or branched alkyl group having 1-18 carbon atoms optionally including one or non-neighboring two or more methylene groups which can be replaced with --X-- or ##STR2## with the proviso that X denotes O or S and Y denotes halogen; R.sub.2 denotes a linear alkyl group having 4-8 carbon atoms: and C* denotes an optically active asymmetric carbon atom. The mesomorphic compound is effective for providing a ferroelectric liquid crystal composition showing improved response characteristics and also effective for suppressing occurrence of reverse domain.Type: GrantFiled: January 21, 1992Date of Patent: March 16, 1993Assignee: Canon Kabushiki KaishaInventors: Hiroyuki Nohira, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
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Patent number: 5182289Abstract: Heterobicyclic and heterocyclic intermediate compounds and their use in treating inflammation, hyperproliferative skin conditions such as psoriasis and allergy are disclosed.Type: GrantFiled: December 10, 1990Date of Patent: January 26, 1993Assignee: Schering CorporationInventors: Pauline C. Ting, Margaret H. Sherlock, Wing C. Tom, James J. Kaminski
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Patent number: 5179093Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.Type: GrantFiled: May 10, 1991Date of Patent: January 12, 1993Assignee: Schering CorporationInventors: Adriano Afonso, Stuart W. McCombie, Jay Weinstein
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Patent number: 5176739Abstract: Dicarboximides of the formulae Ia, Ib and Ic ##STR1## where X is oxygen or sulfur, R.sup.1 is hydrogen, halogen, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, haloalkoxy, haloalkylthio, alkylsulfonyl, haloalkylsulfonyl, phenyl, phenylalkyl, phenoxy or phenylthio, a 5-membered or 6-membered saturated or aromatic heterocyclic radical containing one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen, where the stated organic radicals may be further substituted, andR.sup.2 is hydrogen, hydroxyl, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, di-C.sub.1 -C.sub.Type: GrantFiled: June 21, 1991Date of Patent: January 5, 1993Assignee: BASF AktiengesellschaftInventors: Volker Maywald, Klaus Ditrich, Thomas Kuekenhoehner, Gerhard Hamprecht, Wolfgang Freund, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5153201Abstract: A novel condensed thiazole derivative of the formula [I]: ##STR1## wherein A is a single bond or CH.sub.2 ; R.sup.1 is hydrogen atom, or an optionally substituted aliphatic, carboxylic acyl or sulfonic acyl group; and R.sup.2 is hydrogen atom, or an optionally substituted aromatic cyclic or aliphatic group, or a salt thereof. The compound [I] is useful for medicines for preventing and treating various diseases such as cancer, arterial sclerosis, hepatopathy, cerebrovascular diseases, inflammatory and the like. A process of the compound of the formula [I] or a salt thereof and a pharmaceutical composition comprising the compound of the formula [I] or a pharmaceutically acceptable salt thereof as an active component are also disclosed.Type: GrantFiled: February 22, 1991Date of Patent: October 6, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Masahiro Suno, Go Kito
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Patent number: 4999359Abstract: A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 is C.sub.1-6 alkyl, or phenyl;R.sub.5 is hydrogen or together with R.sub.4 forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and `Het` is an optionally substituted single or fused ring heterocyclic group, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from oxygen, nitrogen and sulphur, with the proviso that when, simultaneously, R.sub.Type: GrantFiled: March 14, 1989Date of Patent: March 12, 1991Assignee: Dr. Lo Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Giuseppe Giardina
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Patent number: 4971975Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents R.sub.1 OOC-- in which R.sub.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl; R.sub.2 O-- in which R.sub.2 is C.sub.1-2 alkyl, C.sub.1-2 alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups;a group ##STR2## in which Y represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-2 alkyl group, Y being optionally C-substituted by a methyl group; or a group ##STR3## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.3 and the other is nitrogen or CR.sub.4 where R.sub.3 and R.sub.4 are independently selected from hydrogen and methyl; and each of p and q independently represents an integer of 2 to 4.Type: GrantFiled: April 15, 1988Date of Patent: November 20, 1990Assignee: Beecham Group plcInventors: Michael S. Hadley, Paul A. Wyman, Barry S. Orlek
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Patent number: 4923861Abstract: Novel 6-[2-[2-(substituted amino)-3-quinolinyl]-ethenyl and ethyl]tetrahydro-4-hydroxypyran-2-ones and/or oxides and the corresponding dihydroxy ring opened acids and esters are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are thus useful hypolipidemic and hypocholesterolemic agents.Type: GrantFiled: February 7, 1989Date of Patent: May 8, 1990Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
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Patent number: 4792606Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.Type: GrantFiled: July 16, 1987Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Hermann-Dieter Krall
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Patent number: 4764622Abstract: A light-collecting system, which contains a coumarin derivative of the formula ##STR1## in which T denotes O or NR.sub.4,R.sub.4 represents hydrogen, optionally substituted aryl, cycloalkyl or aralkyl,R.sub.1 denotes a carbocyclic or heterocyclic 5 or 6 membered ring bonded via a C.atom, or a 5 or 6 membered heterocyclic ring which is bonded via a N atom and is rotationally asymmetrical to an axis placed through the coumarin/N-heterocyclic bond, the 5 or 6 membered rings may carry non-ionic substituents and for an optionally substituted benzene ring or naphthalene ring to be fused to the said rings;X signifies ##STR2## or --OR.sub.2 ', R.sub.2 represents hydrogen, alkyl, cycloalkyl, aralkyl or aryl, hydrocarbon radicals may be substituted, andR.sub.3, in addition to having the definitions given for R.sub.2, also signifies a radical of the formulaeR.sub.6 --(X).sub.n --CO-- or R.sub.7 --(X).sub.n --SO.sub.2 --R.sub.6 and R.sub.Type: GrantFiled: October 17, 1986Date of Patent: August 16, 1988Assignee: Bayer AktiengesellschaftInventors: Uwe Claussen, Horst Harnisch
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Patent number: 4681949Abstract: Novel bis-aminopyridinium salts are useful as phase transfer catalysts in the preparation of aromatic ethers by the reaction of hydroxyaromatic compound alkali metal salts (e.g., bisphenol A disodium salt) with activated halo- or nitro-substituted aromatic compounds (e.g., 4-nitro-N-methylphthalimide). The bis-aminopyridinium salts may be prepared by the reaction of aminopyridines with bis-carbonium ion-generating compounds such as dibromoalkanes.Type: GrantFiled: April 30, 1986Date of Patent: July 21, 1987Assignee: General Electric CompanyInventor: Daniel J. Brunelle
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Patent number: 4632927Abstract: A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including cytoprotective, H.sub.2 -antagonist, anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.Type: GrantFiled: March 20, 1984Date of Patent: December 30, 1986Assignee: William H. Rorer, Inc.Inventors: Henry F. Campbell, Donald E. Kuhla, William L. Studt, Stuart A. Dodson
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Patent number: 4563474Abstract: Heterocyclically substituted nitriles of the formula I ##STR1## where X is SO.sub.2, CO, S, SO or CH.sub.2, A is an alkylene or alkenylene radical of not more than 6 carbon atoms, B is --CH.dbd.CH-- or S, and R.sup.1 and R.sup.2 are each hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, nitro or trifluoromethyl, and their preparation and use.The novel substances are useful for treating disorders.Type: GrantFiled: November 16, 1983Date of Patent: January 7, 1986Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, Gerd Steiner, Hans-Peter Hofmann, Claus-Dieter Muller, Hans-Jurgen Teschendorf
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Patent number: 4517183Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally briType: GrantFiled: May 17, 1983Date of Patent: May 14, 1985Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Wolfgang Kampe, Max Thiel, Uwe Bicker, Dietmar Boerner
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Patent number: 4497817Abstract: A novel 2-phenylimidazo[2,1-b]benzothiazole derivative shown by the following formula ##STR1## or a salt thereof which possesses an immunoregulatory action and is useful as an antiallergic agent, an antiasthmatic, and a suppressant of rejection at tissue transplantation and skin graft.Type: GrantFiled: April 26, 1983Date of Patent: February 5, 1985Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Murase, Toshiyasu Mase, Kenichi Tomioka
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Patent number: 4405632Abstract: Novel derivatives of bicyclic 2-iminothiazolidine oximes and methods of preparing same. This invention is also directed to an insecticidal composition comprising an acceptable carrier and an insecticidally effective amount of a compound of this invention, as well as to a method of controlling insects which comprises subjecting the insects to an insecticidally effective amount of a compound of this invention.Type: GrantFiled: June 27, 1980Date of Patent: September 20, 1983Assignee: Union Carbide CorporationInventors: Dean F. Bushey, Themistocles D. J. D'Silva
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Patent number: 4329476Abstract: Compounds of the formula: ##STR1## wherein R is alkyl, alkenyl or cycloalkyl optionally subsituted with chlorine, cycloalkylalkyl and (CH.sub.2).sub.n R'whereinn is 1-3 andR' is phenyl optionally substituted with CH.sub.3, CH.sub.3 O, NO.sub.2 or 1-2 halogens are useful to control a broad range of fungus diseases and insect and larval pests.Type: GrantFiled: April 21, 1980Date of Patent: May 11, 1982Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thomas S. Woods
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Patent number: 4329459Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.Type: GrantFiled: May 5, 1980Date of Patent: May 11, 1982Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4327221Abstract: Novel 2-substituted-3-hydroxythiazolo[2,3-b]thiazolium salts, the mesoionic didehydro derivatives thereof and related compounds and their use as modulators of the immune response are disclosed.Type: GrantFiled: October 15, 1980Date of Patent: April 27, 1982Assignee: American Home Products CorporationInventor: Peter H. L. Wei
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Patent number: 4316036Abstract: A benzopyranothiazole of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 independently represents hydrogen, alkyl of not more than 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or represents cycloalkyl, phenyl, benzyl, or phenyl or benzyl which is substituted by halogen, lower alkyl or lower alkoxy, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached represent a 5- or 6-membered heterocyclic radical or a N-carbazolyl radical, Q represents hydrogen, lower alkyl, benzyl or groups of the formulae (1a) or (1b) ##STR2## each of X, X.sub.1 and X.sub.2 represents hydrogen, halogen, lower alkyl or lower alkoxy, each of Y.sub.1, Y.sub.2, Y'.sub.1 and Y'.sub.Type: GrantFiled: September 11, 1978Date of Patent: February 16, 1982Assignee: Ciba-Geigy CorporationInventor: Jean C. Petitpierre
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Patent number: 4301280Abstract: There is described a process for preparing an enamine of formula (IX): ##STR1## where R.sup.2 is a carboxylic acid protecting group and R.sup.3 is the residue of a carboxylic acid derived acyl group and where R.sup.5 and R.sup.6 are the same or different C.sub.1-4 alkyl or C.sub.7-10 aralkyl groups; or taken together with the adjacent nitrogen atom form a heterocyclic ring containing from 4 to 8 carbon atoms and optionally a further heteroatom selected from oxygen and nitrogen; by reacting a compound of formula (XII): ##STR2## with an amine of formula HNR.sup.5 R.sup.6, the reactant of formula (XII) being prepared by reaction of an appropriate enol derivative with a phosphorus reagent. The enamines of formula (IX) are useful in the preparation of 3-hydroxycephalosporins.Type: GrantFiled: May 1, 1980Date of Patent: November 17, 1981Assignee: Lilly Industries LimitedInventors: John R. Corfield, Derek Johnson, Clifford G. Taylor
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Patent number: 4271305Abstract: Novel halogenating compounds, derived from triaryl phosphites and chlorine or bromine are employed to convert 7-acylamino-3-hydroxy-3-cephem compounds to 7-acylamino-3-halo-3-cephems and the corresponding C-7 imino halide cephem derivatives. The product 3-halo-3-cephems are antibiotic compounds or intermediates thereto.Type: GrantFiled: December 14, 1979Date of Patent: June 2, 1981Assignee: Eli Lilly and CompanyInventors: Lowell D. Hatfield, Larry C. Blaszczak, Jack W. Fisher
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Patent number: 4226986Abstract: Novel halogenating compounds, derived from triaryl phosphites and chlorine or bromine are employed to convert 7-acylamino-3-hydroxy-3-cephem compounds to 7-acylamino-3-halo-3-cephems and the corresponding C-7 imino halide cephem derivatives. The product 3-halo-3-cephems are antibiotic compounds or intermediates thereto.Type: GrantFiled: February 1, 1979Date of Patent: October 7, 1980Assignee: Eli Lilly and CompanyInventors: Lowell D. Hatfield, Larry C. Blaszczak, Jack W. Fisher
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Patent number: 4225498Abstract: N-substituted oligo-imides of the formula: ##STR1## in which D represents a divalent radical selected from the group comprising: ##STR2## in which m is 0 or 1, Y is hydrogen, chlorine or methyl, n is a positive integer of 5 or less, and R is an organic radical of valency n, containing up to 50 carbon atoms, are prepared by reacting an anhydride of the formula: ##STR3## with an amine of the formula:R----NH.sub.2).sub.n [III]in which formulae D, R and n are as above defined, said reaction being carried out in the presence of a catalyst system comprising a mixture of a compound (1) and a compound (2), (1) being a strong inorganic or organic oxygen-containing acid and (2) being an ammonium salt of such acid, said ammonium salt being di-, tri- or, preferably, tetra-substituted on the nitrogen atom by organic radicals.Type: GrantFiled: August 7, 1978Date of Patent: September 30, 1980Assignee: Rhone-Poulenc IndustriesInventors: Michel Baudouin, Jean Abblard
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Patent number: 4225497Abstract: N-substituted oligo-imides of the formula: ##STR1## in which D represents a divalent radical selected from the group comprising: ##STR2## in which m is 0 or 1, Y is hydrogen, chlorine or methyl, n is a positive integer of 5 or less, and R is an organic radical of valency n, containing up to 50 carbon atoms, are prepared by reacting an anhydride of the formula: ##STR3## with an amine of the formula:R--NH.sub.2).sub.n [III]in which formulae D, R, and n as above defined, said reaction being carried out in the presence of a catalyst system comprising a mixture of a compound (.alpha.) and a compound (.beta.), being a strong inorganic or organic oxygen-containing acid and (.beta.) being a salt of such acid with a cation selected from the group comprising pyridinium, quaternary phosphonium and tertiary sulfonium cations.Type: GrantFiled: January 31, 1979Date of Patent: September 30, 1980Assignee: Rhone-Poulenc IndustriesInventors: Michel Baudouin, Jean Abblard