At Least Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 548/153)
  • Publication number: 20020183369
    Abstract: This invention relates to compounds of Formula I 1
    Type: Application
    Filed: April 5, 2002
    Publication date: December 5, 2002
    Inventor: Daisy Joe Du Bois
  • Patent number: 6479527
    Abstract: 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: Grant
    Filed: July 26, 2000
    Date of Patent: November 12, 2002
    Assignee: AstraZeneca UK Limited
    Inventors: Andrew J. Barker, Alan W Faull, Jason G. Kettle
  • Publication number: 20020156287
    Abstract: The present invention relates to new bromo- and chlorothiazolium salts of the formula (I) 1
    Type: Application
    Filed: December 18, 2001
    Publication date: October 24, 2002
    Inventors: Joachim Rudolph, Ralf Wischnat
  • Patent number: 6461747
    Abstract: 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: Grant
    Filed: July 21, 2000
    Date of Patent: October 8, 2002
    Assignee: Fuji Photo Co., Ltd.
    Inventors: Hisashi Okada, Toshihiro Ise
  • Publication number: 20020049215
    Abstract: 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: Application
    Filed: August 8, 2001
    Publication date: April 25, 2002
    Inventors: Wesley Kwan Mung Chong, Rohit Kumar Duvadie
  • Publication number: 20020045759
    Abstract: 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: Application
    Filed: April 6, 2001
    Publication date: April 18, 2002
    Inventors: Craig A. Stump, Theresa M. Williams
  • Patent number: 6127395
    Abstract: 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: Grant
    Filed: August 3, 1999
    Date of Patent: October 3, 2000
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, Charles A. Blum
  • Patent number: 6096771
    Abstract: 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: Grant
    Filed: February 3, 1999
    Date of Patent: August 1, 2000
    Assignee: Sankyo Company, Limited
    Inventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
  • Patent number: 5998408
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5990145
    Abstract: 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: Grant
    Filed: December 22, 1997
    Date of Patent: November 23, 1999
    Assignees: 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
  • Patent number: 5851425
    Abstract: 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: Grant
    Filed: March 26, 1997
    Date of Patent: December 22, 1998
    Assignee: Rolic AG
    Inventors: Richard Buchecker, Willy Friedrichsen, Jurg Funfschilling, Sandra Lupfert
  • Patent number: 5824677
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: October 20, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
  • Patent number: 5733648
    Abstract: 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: Grant
    Filed: February 23, 1996
    Date of Patent: March 31, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5703093
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: December 30, 1997
    Assignee: Cytomed, Inc.
    Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
  • Patent number: 5693460
    Abstract: 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: Grant
    Filed: June 24, 1996
    Date of Patent: December 2, 1997
    Assignee: Eastman Kodak Company
    Inventor: Roger Lok
  • Patent number: 5637724
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: June 10, 1997
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, Charles A. Blum
  • Patent number: 5637725
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: June 10, 1997
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, Charles A. Blum
  • Patent number: 5633371
    Abstract: 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: Grant
    Filed: September 15, 1995
    Date of Patent: May 27, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
  • Patent number: 5591762
    Abstract: 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: Grant
    Filed: June 1, 1995
    Date of Patent: January 7, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5521213
    Abstract: 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: Grant
    Filed: August 29, 1994
    Date of Patent: May 28, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
  • Patent number: 5434165
    Abstract: 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: Grant
    Filed: November 13, 1992
    Date of Patent: July 18, 1995
    Assignee: Sanawa Kagaku Kenkyusho Company, Ltd.
    Inventors: Masayasu Kurono, Yutaka Baba, Tomoo Suzuki, Tsunemasa Suzuki, Kiyotaka Hirooka, Kiichi Sawai
  • Patent number: 5350760
    Abstract: 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: Grant
    Filed: August 4, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Mark LaBelle, Yibin Xiang, Claude Dufresne, Michel Belley
  • Patent number: 5350857
    Abstract: 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: Grant
    Filed: January 3, 1994
    Date of Patent: September 27, 1994
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Nusrallah Jubran
  • Patent number: 5240938
    Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: August 31, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Thomas F. Walsh, Kenneth J. Fitch, Ralph A. Rivero, Daljit S. Dhanoa
  • Patent number: 5194177
    Abstract: 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: Grant
    Filed: January 21, 1992
    Date of Patent: March 16, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Hiroyuki Nohira, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
  • Patent number: 5182289
    Abstract: Heterobicyclic and heterocyclic intermediate compounds and their use in treating inflammation, hyperproliferative skin conditions such as psoriasis and allergy are disclosed.
    Type: Grant
    Filed: December 10, 1990
    Date of Patent: January 26, 1993
    Assignee: Schering Corporation
    Inventors: Pauline C. Ting, Margaret H. Sherlock, Wing C. Tom, James J. Kaminski
  • Patent number: 5179093
    Abstract: 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: Grant
    Filed: May 10, 1991
    Date of Patent: January 12, 1993
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Stuart W. McCombie, Jay Weinstein
  • Patent number: 5176739
    Abstract: 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: Grant
    Filed: June 21, 1991
    Date of Patent: January 5, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Maywald, Klaus Ditrich, Thomas Kuekenhoehner, Gerhard Hamprecht, Wolfgang Freund, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5153201
    Abstract: 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: Grant
    Filed: February 22, 1991
    Date of Patent: October 6, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tetsuya Aono, Masahiro Suno, Go Kito
  • Patent number: 4999359
    Abstract: 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: Grant
    Filed: March 14, 1989
    Date of Patent: March 12, 1991
    Assignee: Dr. Lo Zambeletti S.p.A.
    Inventors: Vittorio Vecchietti, Giuseppe Giardina
  • Patent number: 4971975
    Abstract: 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: Grant
    Filed: April 15, 1988
    Date of Patent: November 20, 1990
    Assignee: Beecham Group plc
    Inventors: Michael S. Hadley, Paul A. Wyman, Barry S. Orlek
  • Patent number: 4923861
    Abstract: 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: Grant
    Filed: February 7, 1989
    Date of Patent: May 8, 1990
    Assignee: Warner-Lambert Company
    Inventors: Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 4792606
    Abstract: 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: Grant
    Filed: July 16, 1987
    Date of Patent: December 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Hermann-Dieter Krall
  • Patent number: 4764622
    Abstract: 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: Grant
    Filed: October 17, 1986
    Date of Patent: August 16, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Claussen, Horst Harnisch
  • Patent number: 4681949
    Abstract: 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: Grant
    Filed: April 30, 1986
    Date of Patent: July 21, 1987
    Assignee: General Electric Company
    Inventor: Daniel J. Brunelle
  • Patent number: 4632927
    Abstract: 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: Grant
    Filed: March 20, 1984
    Date of Patent: December 30, 1986
    Assignee: William H. Rorer, Inc.
    Inventors: Henry F. Campbell, Donald E. Kuhla, William L. Studt, Stuart A. Dodson
  • Patent number: 4563474
    Abstract: 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: Grant
    Filed: November 16, 1983
    Date of Patent: January 7, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Albrecht Franke, Gerd Steiner, Hans-Peter Hofmann, Claus-Dieter Muller, Hans-Jurgen Teschendorf
  • Patent number: 4517183
    Abstract: 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 bri
    Type: Grant
    Filed: May 17, 1983
    Date of Patent: May 14, 1985
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Wolfgang Kampe, Max Thiel, Uwe Bicker, Dietmar Boerner
  • Patent number: 4497817
    Abstract: 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: Grant
    Filed: April 26, 1983
    Date of Patent: February 5, 1985
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Murase, Toshiyasu Mase, Kenichi Tomioka
  • Patent number: 4405632
    Abstract: 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: Grant
    Filed: June 27, 1980
    Date of Patent: September 20, 1983
    Assignee: Union Carbide Corporation
    Inventors: Dean F. Bushey, Themistocles D. J. D'Silva
  • Patent number: 4329476
    Abstract: 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: Grant
    Filed: April 21, 1980
    Date of Patent: May 11, 1982
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Thomas S. Woods
  • Patent number: 4329459
    Abstract: 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: Grant
    Filed: May 5, 1980
    Date of Patent: May 11, 1982
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4327221
    Abstract: 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: Grant
    Filed: October 15, 1980
    Date of Patent: April 27, 1982
    Assignee: American Home Products Corporation
    Inventor: Peter H. L. Wei
  • Patent number: 4316036
    Abstract: 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: Grant
    Filed: September 11, 1978
    Date of Patent: February 16, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Jean C. Petitpierre
  • Patent number: 4301280
    Abstract: 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: Grant
    Filed: May 1, 1980
    Date of Patent: November 17, 1981
    Assignee: Lilly Industries Limited
    Inventors: John R. Corfield, Derek Johnson, Clifford G. Taylor
  • Patent number: 4271305
    Abstract: 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: Grant
    Filed: December 14, 1979
    Date of Patent: June 2, 1981
    Assignee: Eli Lilly and Company
    Inventors: Lowell D. Hatfield, Larry C. Blaszczak, Jack W. Fisher
  • Patent number: 4226986
    Abstract: 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: Grant
    Filed: February 1, 1979
    Date of Patent: October 7, 1980
    Assignee: Eli Lilly and Company
    Inventors: Lowell D. Hatfield, Larry C. Blaszczak, Jack W. Fisher
  • Patent number: 4225498
    Abstract: 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: Grant
    Filed: August 7, 1978
    Date of Patent: September 30, 1980
    Assignee: Rhone-Poulenc Industries
    Inventors: Michel Baudouin, Jean Abblard
  • Patent number: 4225497
    Abstract: 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: Grant
    Filed: January 31, 1979
    Date of Patent: September 30, 1980
    Assignee: Rhone-Poulenc Industries
    Inventors: Michel Baudouin, Jean Abblard