The Six-membered Hetero Ring And Another Ring Bonded Directly To The Same Carbon Patents (Class 546/333)
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Patent number: 6384228Abstract: The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.Type: GrantFiled: January 7, 2000Date of Patent: May 7, 2002Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Manabu Node, Daisaku Nakamura, Toshio Fujiwara, Shogo Ichihashi
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Patent number: 6380224Abstract: Amine and amide derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing amines and amides of formula A as the active ingredient are described. The amines and amides of formula A are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.Type: GrantFiled: July 27, 2000Date of Patent: April 30, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Scott L. Dax, James McNally, Mark Youngman
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Publication number: 20020010339Abstract: The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.Type: ApplicationFiled: January 7, 2000Publication date: January 24, 2002Inventors: MANABU NODE, DAISAKU NAKAMURA, TOSHIO FUJIWARA, SHOGO ICHIHASHI
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Patent number: 6166053Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.Type: GrantFiled: January 24, 2000Date of Patent: December 26, 2000Assignee: Cell Pathways, Inc.Inventors: Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
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Patent number: 6166006Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.Type: GrantFiled: December 17, 1998Date of Patent: December 26, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Patent number: 6147080Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The compounds are of the class of pyrido [1,2-c] pyrimidin-3-one or 1,2-dihydro-pyrido [1,2-c] pyrimidin-3-one derivatives, useful as inhibitors of p38. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: June 10, 1997Date of Patent: November 14, 2000Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, Edmund Martin Harrington
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Patent number: 6140354Abstract: .beta.-Aminotetralin derivatives of the formula: ##STR1## which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a .beta.-aminotetralin derivative as the active ingredient are described. The .beta.-aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.Type: GrantFiled: April 12, 1999Date of Patent: October 31, 2000Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Scott L. Dax, Timothy W. Lovenberg, James McNally, Allen B. Reitz, Mark A. Youngman
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Patent number: 6124332Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6124333Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6103743Abstract: Described herein are compounds having the general formula: ##STR1## Ar.sub.1 and Ar.sub.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sub.1 or Ar.sub.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sub.1 and Ar.sub.Type: GrantFiled: August 6, 1999Date of Patent: August 15, 2000Assignee: Allelix Neuroscience, Inc.Inventors: Stanley Charles Bell, Kathleen Da Silva, Allen Hopper, Methvin Isaac, Eric A. Meade, Vassil Ilya Ognyanov, Abdelmalik Slassi
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Patent number: 6066634Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.Type: GrantFiled: December 7, 1998Date of Patent: May 23, 2000Assignees: Cell Pathways, Inc., University of ArizonaInventors: Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
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Patent number: 6022899Abstract: There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange.Type: GrantFiled: January 9, 1998Date of Patent: February 8, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans-Jochen Lang, Udo Albus, Wolfgang Scholz
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Patent number: 6001854Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the following formulas I and II: ##STR1## or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 30, 1997Date of Patent: December 14, 1999Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 5945436Abstract: Compounds of of the formula ##STR1## wherein R is a C.sub.6 -C.sub.10 aryl group, optionally substituted with one or more halogen atoms, phenoxy, or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, or C.sub.1 -C.sub.6 haloalkyl; R.sup.1 is C.sub.3 -C.sub.6 cycloalkyl or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 haloalkenyl, C.sub.2 -C.sub.8 alkoxyalkyl or C.sub.1 -C.sub.6 haloalkyl; n is 1, 2 or 3; and R.sup.2 is CN, C(O)NH.sub.2 or C(S)NH.sub.2, or the physiologically acceptable salts thereof with organic and inorganic acids. These compounds are useful as fungicides.Type: GrantFiled: September 26, 1997Date of Patent: August 31, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./Cie.Inventors: Hoi Kiong Lai, Douglas Irving Relyea, Robert Allan Davis
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Patent number: 5925645Abstract: The 2-aryl-substituted pyridines are prepared by reacting pyridylaldehydes with organometallic compounds and then selectively reducing the products. The 2-aryl-substituted pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis.Type: GrantFiled: March 13, 1997Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Rolf Angerbauer, Arndt Brandes, Michael Logers, Matthias Muller-Gliemann, Hilmar Bischoff, Delf Schmidt, Stefan Wohlfeil
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5780488Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: March 26, 1997Date of Patent: July 14, 1998Assignee: Merck & Co., Inc.Inventors: Jeffrey Bergman, Christopher Dinsmore
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Patent number: 5741796Abstract: Compounds of the following general structure X-Y-Z-Aryl-A-B, for example, ##STR1## which inhibit osteoclast mediated bone resorption. Specifically, the compounds are useful for treating mammals suffering from a bone condition caused or mediated by increased bone resorption, who are in need of such therapy. The compounds may be administered in oral dosage forms such as tablets, capsules, e.g. sustained release capsules, powders, granules, and suspensions.Type: GrantFiled: September 26, 1996Date of Patent: April 21, 1998Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Mark E. Duggan, William F. Hoffman, Nathan C. Ihle
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Patent number: 5739340Abstract: The invention relates to indolizine derivatives of general formula: ##STR1## in which: X denotes an --S or --SO.sub.2 -- group,each of R.sub.1 and R.sub.2, which are identical or different, denotes hydrogen, the methyl or ethyl radical or a halogen atom,R.sub.3 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl radical,R.sub.4 denotes a precursor radical of a carboxyl group,R denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or phenyl radical, and their use as intermediates for the preparation of pharmaceutically active aminoalkoxybenzenesulphonylindolizine derivatives.Type: GrantFiled: April 2, 1997Date of Patent: April 14, 1998Assignee: Elf SanofiInventors: Jean Gubin, Michel Renard
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Patent number: 5723651Abstract: An economical process for producing .alpha.-L-aspartyldipeptide amide derivatives useful as sweeteners, by using amino protecting groups which can be removed by hydrolysis under acidic conditions, resulting in conversion of a .beta.-carboxyl acid ester to a carboxylic acid.Type: GrantFiled: December 28, 1995Date of Patent: March 3, 1998Assignee: Ajinomoto Co., Inc.Inventors: Toyoto Hijiya, Tadashi Takemoto, Ryoichiro Nakamura, Yusuki Amino, Naoko Sugiyama
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Patent number: 5719168Abstract: The present invention relates to compounds of formula (I) wherein R.sub.1 is selected from H and 3-chloro; R.sub.2 is selected from a phenyl group and a pyridyl group; R.sub.3 and R.sub.4 are selected independently of each other from H and methyl; R.sub.5 and R.sub.6 are selected independently of each other from H and a pyridyl-methyl group or both represent an ethyl group; n=0 or 1; R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are not simultaneously H when R.sub.2 is phenyl. The salts of the compounds have a pyridyl group with pharmaceutical acceptable acids are also disclosed.Type: GrantFiled: April 22, 1996Date of Patent: February 17, 1998Assignee: Laboratoire L. LafonInventor: Philippe Laurent
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Patent number: 5693659Abstract: Compounds of general formula (1) are described: ##STR1## wherein .dbd.W-- is (1) .dbd.C(Y)-- where Y is a halogen atom, or an alkyl or --XR.sup.a group where X is --O--, --S(O).sub.m -- ?where m is zero or an integer of value 1 or 2!, or --N(R.sup.b)-- ?where R.sup.b is a hydrogen atom or an optionally substituted alkyl group! and R.sup.a is a hydrogen atom or an optionally substituted alkyl group or, (2) .dbd.N--; L is a --XR, ?where R is an optionally substituted alkyl, alkenyl, cycloalkyl or cyloalkenyl group!, --C(R.sup.5).dbd.C(R.sup.1)(R.sup.2) or ?--CH(R.sup.5)!.sub.n CH(R.sup.1)(R.sup.2) group where R.sup.5 is a hydrogen or a fluorine atom or a methyl group, and R.sup.1 and R.sup.2, which may be the same or different, is each a hydrogen or fluorine atom or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, --CO.sub.2 R.sup.6, ?where R.sup.6 is a hydrogen atom or an optionally substituted alkyl, aralkyl, or aryl group!, --CONR.sup.7 R.sup.8 ?where R.sup.7 and R.sup.Type: GrantFiled: June 22, 1995Date of Patent: December 2, 1997Assignee: Celltech Therapeutics LimitedInventors: John Clifford Head, Graham John Warrellow, Rikki Peter Alexander
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Patent number: 5681961Abstract: The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH). They also have an effect on PGE.sub.2 production.Type: GrantFiled: March 21, 1995Date of Patent: October 28, 1997Assignee: Dr. Karl Thomae GmbHInventors: Armin Heckel, Josef Nickl, deceased, Rainer Soyka, Wolfgang Eisert, Thomas Muller, Johannes Weisenberger, Christopher Meade, Gojko Muacevic
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Patent number: 5672615Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: March 11, 1996Date of Patent: September 30, 1997Assignee: Novartis CorporationInventors: Lawrence J. MacPherson, David Thomas Parker
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Patent number: 5658908Abstract: Diarylmethylpiperazine compounds having utility as receptor-binding species, e.g., for mediating analgesia, and for combatting drug addiction, alcohol addiction, and drug overdose. The compounds may be administered orally, rectally, topically, nasally, ophthalmically, or parenterally (subcutaneously, intramuscularly, and intravenously), for veterinary and human use, and include delta receptor and mu receptor binding species.Type: GrantFiled: August 3, 1994Date of Patent: August 19, 1997Assignee: Delta Pharmaceuticals, Inc.Inventors: Kwen-Jen Chang, Grady Evan Boswell, Dulce Garrido Bubacz, Mark Allan Collins, Ann Otstot Davis, Robert Walton McNutt, Jr.
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Patent number: 5552418Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification,and a medicinal product containing said compound for treating a disorder of the melatoninergic system.Type: GrantFiled: May 23, 1995Date of Patent: September 3, 1996Assignee: Adir et CompagnieInventors: Patrick Depreux, Hamid Ait Mansour, Daniel Lesieur, Fran.cedilla.ois Lefoulon, Pierre Renard, G erard Adam, Philippe Delagrange
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Patent number: 5552419Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: November 3, 1994Date of Patent: September 3, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5482948Abstract: This invention relates to pyridyl derivatives of the formula ##STR1## wherein X, Y, A, n and R.sub.3 to R.sub.8 are defined hereinbelow, the enantiomers thereof, the cis- and trans-isomers thereof, which have antithrombotic pharmaceutical activity.Type: GrantFiled: July 5, 1994Date of Patent: January 9, 1996Assignee: Dr. Karl Thomae GmbHInventors: Rainer Soyka, Thomas Muller, Johannes Weisenberger
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Patent number: 5480998Abstract: An oxime derivative (I): ##STR1## that D ring and B bonding to D ring are (i)-(iv), wherein R.sup.1 is hydrogen, lower alkyl; R.sup.2 is hydrogen, alkyl, phenyl, cycloalkyl, monocyclic ring containing nitrogen, lower alkyl substituted by benzene ring or cycloalkyl, lower alkyl substituted by monocyclic ring containing nitrogen; R.sup.3 is alkyl, phenyl, cycloalkyl, monocyclic ring containing nitrogen, lower alkyl substituted by benzene ring or cycloalkyl, lower alkyl substituted by monocyclic ring containing nitrogen; e is 3-5, f is 1-3, p is 1-4, q is 1-2, r is 1-3; the position of the bond to D ring in (iii) and (iv) is a or b, and the ring in R.sup.2 and R.sup.3 may be substituted by lower alkyl, alkoxy, halogen, nitro, trihalomethyl; and salts thereof, possess an agonistic activity on PGl2 receptor, and therefore are useful for prevention and/or treatment of thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertension.Type: GrantFiled: March 17, 1994Date of Patent: January 2, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5472979Abstract: R.sub.1 and R.sub.2 form, with the carbon atoms to which they are attached, cyclopentane or cyclohexane,R.sub.3 represents hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or unsubstituted or substituted amino,R.sub.4 represents alkyl, unsubstituted or substituted phenyl, naphthyl, pyridyl or thienyl, X represents methylene or oxygen or sulfur,its enantiomers and its addition salts with a pharmaceutically acceptable base, and medicinal products containing the same are useful as anti-thrombotic.Type: GrantFiled: October 14, 1994Date of Patent: December 5, 1995Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Thierry Dubuffet, Olivier Muller, Michel Laubie, Tony Verbeuren, Serge Simonet, Jean-Jacques Descombes
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Patent number: 5426119Abstract: The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH). They also have an effect on PGE.sub.2 production.Type: GrantFiled: November 18, 1993Date of Patent: June 20, 1995Assignee: Dr. Karl Thomae GmbHInventors: Armin Heckel, Josef Nickl, deceased, Rainer Soyka, Wolfgang Eisert, Thomas Muller, Johannes Weisenberger, Christopher Meade, Gojko Muacevic
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Patent number: 5399575Abstract: Compounds of the formula I ##STR1## in which A signifies an alkylene radical with 1 to 3 carbon atoms or a group --CH.dbd.CH--, B an oxygen atom or a valency bond, m a whole number from 0 to 5, n the number 0 or 1, X a valency bond, an oxygen atom or a sulphur atom, Y a valency bond or a phenylene radical substituted, if desired, one or more times by C.sub.1 - to C.sub.6 -alkyl, C.sub.1 - to C.sub.6 -alkoxy, halogen, hydroxyl or aminocarbonyl, Z hydrogen, halogen, C.sub.1 - to C.sub.6 -alkyl or cyano and R a group CN, COOH, COOC.sub.1 - to C.sub.6 -alkyl, CONH-tetrazolyl, CON(OH)(C.sub.1 -C.sub.6 -alkyl) or 5-(1H)-tetrazolyl, as well as, for the case that Y represents a phenylene radical, also hydrogen, with the exception of the compound 4-[2-(4)-pyridinovinyl]-carboxymethoxybenzene, their physiologically compatible salts and processes for their preparation, as well as medicaments containing these compounds for the treatment of allergic diseases.Type: GrantFiled: June 14, 1993Date of Patent: March 21, 1995Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Wolfgang Kampe, Marcel Linssen, Otto-Henning Wilhelms
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Patent number: 5374724Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.Type: GrantFiled: November 2, 1992Date of Patent: December 20, 1994Assignee: Zeneca, LimitedInventors: Nigel Hall, Nigel Hughes, Prakash Patel
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Patent number: 5374641Abstract: Illustrative examples of the N-(3-pyridylalkyl)sulfonamide derivative are represented by the following formulae [II] and [III]: ##STR1## The derivatives are available for a thromboxane A.sub.2 production inhibitor, a thromboxane A.sub.2 antagonist, a prostaglandin H.sub.2 antagonist, an anti-thrombus agent, a thrombus-preventing agent and an anti-allergy agent.Type: GrantFiled: February 24, 1992Date of Patent: December 20, 1994Assignee: Terumo Kabushiki KaishaInventors: Hiroyuki Ohnishi, Masazumi Miyakoshi, Masashi Isozaki, Masayuki Fujitake, deceased, Naoya Mikami, Ryohei Yanoshita, Harue Akasofu, Katsuyoshi Sugizaki, Nobuyuki Nakata
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Patent number: 5308840Abstract: Aminophenol derivatives of the following formula (I) ##STR1## wherein X is hydrogen atom, lower alkyl or a protecting group for phenolic hydroxy, Y is hydrogen atom or lower alkyl, Z is hydrogen atom, lower alkyl, halogen atom or trifluoromethyl, A is hydrogen atom or lower alkyl, t is an integer of 1 to 5, l and m are respectively an integer of 2 to 4, E and W are nitrogen atoms, F is a direct bond or oxygen atom, P and Q are each hydrogen atom, halogen atom, lower alkyl or lower alkoxy, and R.sup.8 is hydrogen atom, hydroxy or a hydroxy-protecting group, and their pharmcologically acceptable salts. Since the aminophenol derivatives (I) of the present invention have excellent antioxidative action and antiinflammatory and antiallergic action in mammalian animals including human, they are extremely useful as pharmaceuticals such as an antiinflammatory or an antiallergic.Type: GrantFiled: April 6, 1992Date of Patent: May 3, 1994Assignee: Green Cross CorporationInventors: Naoki Sugiyama, Fumihiko Akaboshi, Haruko Yakumaru, Tomokazu Gotoh, Masanori Sugiura, Shigeki Kuwahara, Masahiko Kajii, Yoshiko Tanaka, Takao Kondoh, Chikara Fukaya
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Patent number: 5294626Abstract: The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH) They also have an effect on PGE.sub.2 production.Type: GrantFiled: May 14, 1990Date of Patent: March 15, 1994Assignee: Dr. Karl Thomas GmbHInventors: Armin Heckel, Josef Nickl, deceased, Rainer Soyka, Wolfgang Eisert, Thomas Muller, Johannes Weisenberger, Christopher Meade, Gojko Muacevic
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Patent number: 5231182Abstract: Methods of preparing bis-aryl amide and urea compounds of the general formula: ##STR1## wherein x is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor.Type: GrantFiled: October 4, 1991Date of Patent: July 27, 1993Assignee: American Cyanamid CompanyInventor: Allan Wissner
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Patent number: 5229404Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA re-uptake from the synaptic cleft.Type: GrantFiled: December 6, 1991Date of Patent: July 20, 1993Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
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Patent number: 5202331Abstract: A method for the therapeutic treatment of dysuria with alpha-phenyl-alpha-pyridylakanoic acid derivatives is disclosed.Type: GrantFiled: April 1, 1991Date of Patent: April 13, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventor: Masaaki Tomoi
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Patent number: 5196542Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.Type: GrantFiled: February 20, 1991Date of Patent: March 23, 1993Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
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Patent number: 5180832Abstract: Novel [[[(3-pyridinyl)methylen]amino]oxy]alkanoic acids and esters, compositions containing the same, and methods of treating clinical conditions related with the production of thromboxane A.sub.2, prostacyclin and/or prostaglandin s D.sub.2, E.sub.3 and F.sub.2.alpha..Type: GrantFiled: September 17, 1990Date of Patent: January 19, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Victor Sipido, Marc G. Venet
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Patent number: 5162329Abstract: .beta.-picoline derivatives of the formula ##STR1## where A is CR.sup.1 R.sup.2, R.sup.1 and R.sup.2 independently of each other are hydrogen, alkyl, alkenyl or alkynyl, or R.sup.1 and R.sup.2 together form a methylene chain,B is one of the groups CH.sub.2, CHOR.sup.3, CHalR.sup.4, C.dbd.O or C.dbd.N-O-R.sup.5, R.sup.3 being hydrogen, alkyl, haloalkyl, cycloalkyl, alkenyl, acyl, phenyl, benzyl or benzoyl, where the phenyl ring is substituted or unsubstituted, R.sup.4 being hydrogen, fluorine, chlorine, bromine or iodine, R.sup.5 being hydrogen, alkyl, haloalkyl, cycloalkyl, alkenyl, phenyl or benzyl, the phenyl ring being substituted or unsubstituted,Ar is a substituted or unsubstituted aryl radical,their N-oxides and plant-tolerated acid addition salts, and fungicides containing these compounds.Type: GrantFiled: May 23, 1991Date of Patent: November 10, 1992Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Bernhard Zipperer, Norbert Goetz, Michael Keil, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5155121Abstract: The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reaction of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkenecarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.Type: GrantFiled: August 2, 1991Date of Patent: October 13, 1992Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewohner, Ulrich E. Muller, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Patent number: 5134147Abstract: Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.Type: GrantFiled: October 21, 1991Date of Patent: July 28, 1992Assignee: Adir et CompagnieInventors: Jean L. Peglion, Francis Colpaert
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Patent number: 5118697Abstract: Novel cyclic beta-ketoamides which contain an aryl moiety having utility as blood cholesterol lowering agents rendering them useful in the treatment of atherosclerosis.Type: GrantFiled: March 6, 1991Date of Patent: June 2, 1992Assignee: Warner-Lambert CompanyInventors: Corinne E. Augelli-Szafran, Bharat K. Trivedi
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Patent number: 5118704Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are defined in the specification; R.sub.1 is selected from the group consisting of ##STR2## wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12, preferably 1 to 6, carbon atoms, and a is an integer of from zero to 3, for instance zero to 2; and pharmaceutically acceptable salts thereof; as dopaminergics.Type: GrantFiled: September 11, 1991Date of Patent: June 2, 1992Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
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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: 5023334Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.Type: GrantFiled: September 1, 1989Date of Patent: June 11, 1991Assignee: The Upjohn CompanyInventors: Douglas L. Rector, George A. Conder, Sylvester D. Folz
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Patent number: 4997842Abstract: The present invention relates to the + or - pirmenol stereoisomers and to selected metabolites of pirmenol or (+,-)-cis-.alpha.-[3-(2,6-dimethyl-1-piperidinyl))propyl]-.alpha.-phenyl-2 -pyridinemethanol which are active as antiarrhythmic agents. The pharmacological use of the metabolites that is the present invention is as antiarrhythmic agents. Pharmaceutical compositions comprising the metabolites are also within the scope of the invention.Type: GrantFiled: February 8, 1990Date of Patent: March 5, 1991Assignee: Warner-Lambert Co.Inventors: Timothy R. Hurley, Dino A. Sherwood, Peter W. K. Woo, Karl-Otto Vollmer, Egmont Schaller, Wolfgang Klemisch, Albrecht V. Hodenberg
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Patent number: 4980478Abstract: An improved process for producing a substituted vinyl pyridine compound of the general formula: ##STR1## wherein R.sup.1 is pyridyl group; R.sup.2 is an optionally substituted aromatic or heterocyclic group; R.sup.3 is a lower alkyl group, hydroxymethyl group, nitroxymethyl group, a nitrogen containing 5 membered ring-methyl group, an acetal-methyl group, a trialkylsilyloxymethyl group, an alkyl- or aryl-sulfonyloxymethyl group, an alkyl- or aryl-sulfonylaminocarbonyloxymethyl group, an acyloxymethyl group, an alkoxycarbonyloxymethyl group, a halogenomethyl group, an alkoxymethyl group, an aryl-oxymethyl group, cyano group, an optionally substituted carbamoyl group, an optionally substituted carbamoyloxymethyl group, an optionally substituted thiocarbamoyloxymethyl group, carboxyl group or an alkoxycarbonyl group; and n is an integer of 1 to 22, which comprises reacting a compound of the general formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, with a compound of the general formula:(C.sub.Type: GrantFiled: April 4, 1989Date of Patent: December 25, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Chitoshi Hatanaka, Sigel Nuwa, Satoru Oi