Ortho Fused Rings In Acid Moiety Patents (Class 560/10)
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Patent number: 5166377Abstract: The invention concerns novel 4-phenyl-1,3-dioxan-5-ylalkenoic acid derivatives of the formula I having cis relative stereochemistry at positions 4 and 5 of the dioxane ring and wherein Ra and Rb are variously hydrogen, alkyl, halogenoalkyl, alkenyl, and optionally substituted aryl or arylalkyl, Rc is hydroxy, alkoxy or alkanesulphonamido, n is 1 or 2, A is ethylene or vinylene, Y is (2-5C)polymethylene optionally substituted by alkyl, and benzene ring B is optionally substituted phenyl, or, when Rc is hydroxy, a salt thereof. The acid derivatives antagonize one or more of the actions of thromboxane A.sub.2 (TXA.sub.2) and are expected to be of value in those disease conditions in which TXA.sub.2 is involved. The invention also provides pharmaceutical compositions containing an acid derivative of formula I, and processes for their chemical production.Type: GrantFiled: February 9, 1988Date of Patent: November 24, 1992Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, Peter W. R. Caulkett
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Patent number: 5153227Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.Type: GrantFiled: February 6, 1989Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
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Patent number: 5153352Abstract: A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occuring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein R.sub.24 is the side chain of any of the naturally occuring amino acids, --CH.sub.1 SH, --Ch.sub.2 Cl, --Ch.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.Type: GrantFiled: August 20, 1990Date of Patent: October 6, 1992Assignee: Bristol-Myers Squibb CompanyInventors: Daniel W. Norbeck, Richard J. Pariza, Steven M. Hannick, Thomas J. Sowin
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Patent number: 5151544Abstract: Disclosed is a process for the synthesis of enantiomerically pure R and S isomers of 2,7-difluoro-4-methoxyspiro[9H-fluorene-9,4-imidazolidene]-2',5'-dione from 2,7-difluoro-4-methoxyfluorenone. Intermediate amino acid esters and urea esters and their preparation are also described.Type: GrantFiled: May 25, 1990Date of Patent: September 29, 1992Assignee: Alcon Laboratories, Inc.Inventors: Mark T. DuPriest, Raymond E. Conrow, Daniel Kuzmich
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Patent number: 5149859Abstract: A naphthalene derivative having the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or a non-toxic salt moiety; R.sup.2 and R.sup.3 independently represent a hydrogen atom or --OR.sup.4 where R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group;A represents a group: ##STR2## [where X.sup.1 and X.sup.2 represents an oxygen atom or N--OR.sup.5 (where R.sup.5 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], a group: ##STR3## [where Y.sup.1 and Y.sup.2 independently an oxygen atom or a group N--OR.sup.6 (where R.sup.6 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], or a group: ##STR4## (where n is 0 or 1); and B represents --(CH.sub.2).sub.m --wherein m is an integer of 1, to 8,--(CH.sub.2).sub.m.sbsb.1 --O--(CH.sub.2).sub.m.sbsb.2 --wherein m.sub.1 and m.sub.2 are independently 1 or 2, or ##STR5## wherein m.sub.3 is 0 or 1.Type: GrantFiled: September 14, 1990Date of Patent: September 22, 1992Assignee: Teijin LimitedInventors: Atsuo Hazato, Takumi Takeyasu, Koji Tomimori, Yoshinori Kato
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Patent number: 5145867Abstract: Naphthylalkylamino-substituted sulfamoylbenzoic acid derivatives, processes for the preparation thereof and the use thereof as medicines.Compounds I ##STR1## R(1) hydrogen, (C.sub.1 -C.sub.4)-alkyl and Na, K, NH.sub.4, Ca, Mg, R(2) and R(3) hydrogen, alkyl groups which can also be linked together in a ring,X oxygen, sulfur, SO, SO.sub.2, NR(6) [with R(6)=hydrogen-alkyl], CH.sub.2, CO, or a bond,R(4) phenyl, thienyl, which are unsubstituted or substitutedR(5) hydrogen, (C.sub.1 -C.sub.4)-alkyl,n 1, 2, 3 or 4,where the naphthyl system is unsubstituted or substituted like the phenyl radical of R(4),and where X and R(4) together can also be Cl are medicaments for treating sickle-cell anemia.Type: GrantFiled: April 6, 1990Date of Patent: September 8, 1992Assignee: Hoechst AktiengesellschaftInventors: John C. Ellory, Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Wulf Merkel
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Patent number: 5128479Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: January 29, 1990Date of Patent: July 7, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5124353Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.Type: GrantFiled: October 3, 1989Date of Patent: June 23, 1992Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey
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Patent number: 5118710Abstract: Acrylic esters of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or alkyl, X is S, SO or SO.sub.2, R.sup.3 is phenyl, naphthyl or phenanthrenyl, these radicals being unsubstituted or substituted, with the exception of compounds in which R.sup.3 is phenyl, 3-chlorophenyl, 4-chlorophenyl, 2,4-dichlorophenyl or methylphenyl, and fungicides containing these compounds.Type: GrantFiled: December 31, 1990Date of Patent: June 2, 1992Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Franz Schuetz, Bernd Wenderoth, Siegbert Brand, Bernd Mueller, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5112862Abstract: 3-Methoximinopropionic esters of the formula ##STR1## where the radicals R (m=1 to 5) are each hydrogen, halogen, cyano, nitro, alkyl, cycloalkyl, alkenyl, alkoxy, haloalkyl, haloalkoxy, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, unsubstituted or substituted benzyl or unsubstituted or substituted benzyloxy, or the group ##STR2## is naphthyl, and X is methyleneoxy, oxymethylene, ethylene, ethenylene, thiomethylene or oxygen, and fungicides containing these compounds.Type: GrantFiled: July 2, 1990Date of Patent: May 12, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Wenderoth, Hubert Sauter, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 5108489Abstract: Herbicidal disubstituted naphthalenes of the formula ##STR1## in which A represents optionally branched alkanediyl,R represents hydrogen or in each case optionally substituted alkyl or phenyl,R.sup.1 represents hydrogen, halogen, cyano or trifluoromethyl,R.sup.2 represents hydrogen or halogen,R.sup.3 represents halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio or trifluoromethylsulphonyl,R.sup.4 represents hydrogen or halogen,X represents nitrogen or the group C--R.sup.5, whereR.sup.5 represents hydrogen or halogen,Y represents oxygen or sulphur, andZ represents oxygen, the group N--(O).sub.n --R.sup.Type: GrantFiled: July 24, 1991Date of Patent: April 28, 1992Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5100917Abstract: The present invention relates to novel A-nor-steroid-3-carboxylic acid derivatives and to their use as inhibitors of mammalian 5.alpha.-reductase.Type: GrantFiled: September 11, 1990Date of Patent: March 31, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Philippe Bey, Thomas R. Blohm
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Patent number: 5087743Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: January 23, 1990Date of Patent: February 11, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5081282Abstract: Bicyclo prostaglandin analogues have been prepared.Type: GrantFiled: January 13, 1988Date of Patent: January 14, 1992Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5069819Abstract: The present invention relates to thioesters having the structural formula: ##STR1## wherein R.sup.x is selected from the group of formulae consisting of: ##STR2## R.sup.1, R.sup.2 and R.sup.3 are independently selected from the group of radicals consisting of hydrogen or methyl; R.sup.4 and R.sup.5 are independently selected from the group of radicals consisting of hydrogen, alkyls having 1 to 18 carbon atoms, aryls having 6 to 10 carbon atoms, aralkyls having 7 to 9 carbon atoms, and radicals of the formula: ##STR3## and R.sup.6 is selected from the group of radials consisting of alkyls having 1 to 24 carbon atoms, aryls having 6 to 12 carbon atoms and aralkyls having 7 to 12 carbon atoms.These thioesters are particularly useful as a synergist for conventional phenolic and amine antioxidants.Type: GrantFiled: September 10, 1990Date of Patent: December 3, 1991Assignee: The Goodyear Tire & Rubber CompanyInventors: Budd H. Sturm, Joseph A. Kuczkowski
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Patent number: 5068394Abstract: Herbicidal (hetero)aryloxynaphthalene derivatives of the formula ##STR1## in which X is N or --C--R.sup.5,R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are hydrogen or halogen or R.sup.1 may be cyano or trifluoromethyl,R.sup.3 is halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio or trifluoromethylsulphonyl,Y is optionally halogen-substituted alkanediyl or alkenediyl, andZ is CN or --CC--Z', whereZ' is halogen, hydroxyl, amine, alkoxy, or the like.Intermediates of the formula ##STR2## are also new.Type: GrantFiled: October 19, 1989Date of Patent: November 26, 1991Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5057537Abstract: Ortho-substituted 1-napthyl ethers of the formula ##STR1## where X is CH or N, Y is saturated or unsaturated alkylene and R is aryl, aryloxy, arylthio or arylalkoxy, the aromatic ring being substituted or unsubstituted, and fungicides containing these compounds.Type: GrantFiled: February 2, 1990Date of Patent: October 15, 1991Assignee: BASF AktiengesellschaftInventors: Bernd Wenderoth, Hubert Sauter, Albrecht Harreus, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5055451Abstract: Thiol protease inhibitors are disclosed having the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0 or 1;m is 0, 1 or 2;X is H or an N-protecting group;each Y is independently an optionally protected .alpha.-amino acid residue;R is an optionally protected .alpha.-amino acid side chain that is H or CH.sub.3 or that is bonded to the .alpha.-carbon atom to which it is attached by a methylene, methine or phenyl radical; andR' is optionally substituted aryl.Type: GrantFiled: December 7, 1987Date of Patent: October 8, 1991Assignee: Syntex Inc.Inventors: Alexander Krantz, Heinz W. Pauls, Roger A. Smith, Robin W. Spencer
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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: 5030653Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: October 23, 1990Date of Patent: July 9, 1991Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5030652Abstract: Indan derivatives of the formula: ##STR1## wherein R.sup.1 is substituted or unsubstituted phenyl, naphthyl or sulfur-containing heterocyclic group, and R.sup.2 is hydroxy-methyl or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or lower alkyl and R.sup.4 is cycloalkyl, lower alkoxycarbonyl-phenyl, carboxy-phenyl, nitrogen-containing heterocyclic group, lower alkyl, or lower alkyl having a substituent selected from lower alkoxycarbonyl, carboxy, lower alkoxycarbonyl-phenyl, carboxy-phenyl, lower alkoxycarbonyl-cycloalkyl and carboxy-cycloalkyl, or a pharmaceutically acceptable salt thereof, which are useful as a platelet aggregation-inhibiting agent and as an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis or embolism, coronary and cerebral vascular smooth muscle vellication, asthma, and the like, processes for the preparation thereof, and pharmaceutical composition containing said compound as an active ingredient.Type: GrantFiled: November 15, 1988Date of Patent: July 9, 1991Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Harumichi Kohno, Yasuhiko Sasaki, Katsuo Ikezawa, Akio Odawara
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Patent number: 5017583Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: February 23, 1988Date of Patent: May 21, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Joshua Rokach, Haydn R. Williams, Masatoshi Kakushima, Yvan Guindon
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Patent number: 5017610Abstract: A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 -- or ##STR2## (i) R.sup.1 and R.sup.2, which may be the same or different, each represent, (1) --H, (2) C1-16 alkyl or (3) the formula: --X-- .circle.A --(R.sup.4).sub.n wherein X is a single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by ##STR3## -- .circle.A -- is carbocyclic or heterocyclic ring, n is 1.about.5, R.sup.4 is (1) --H or C1-8 alkyl, (2) C1-14 alkoxy, (3) C1-6 alkylthio, (4) --OH, halogen, --NO.sub.2 or trihalomethyl, (5) the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, (6) tetrazole, (7) --SO.sub.3 H or --CH.sub.2 OH, (8) the formula: --SO.sub.2 NR.sup.41 R.sup.42 (9) the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R.sup.43 is --H, C1-4 alkyl or benzyl, (10) the formula: --CONR.sup.41 R.sup.42 (11) the formula: --COO--Z.sup.42 --COOR.sup.43 wherein Z.sup.42 is C1-4 alkylene, R.sup.Type: GrantFiled: June 12, 1989Date of Patent: May 21, 1991Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Yoshinobu Arai, Tadao Okegawa
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Patent number: 5015644Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.Type: GrantFiled: June 1, 1989Date of Patent: May 14, 1991Assignee: Warner-Lambert CompanyInventors: Bruce D. Roth, Bharat K. Trivedi
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Patent number: 5013861Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as intermediates in the preparation of pharmaceutically active products.Type: GrantFiled: October 6, 1986Date of Patent: May 7, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Eric M. Gordon
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Patent number: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5006542Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## where R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasopastic diseases.Type: GrantFiled: October 31, 1988Date of Patent: April 9, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Steven E. Hall, Philip D. Stein
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Patent number: 4996352Abstract: A process for preparing optically active naphtho[1,2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.- hydroxy-4-methoxybenzenepropanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin- 4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.Type: GrantFiled: June 29, 1989Date of Patent: February 26, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Erno Mohacsi
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Patent number: 4983628Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reaction substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: January 3, 1989Date of Patent: January 8, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Richard Frenette, Joshua Rokach, Masatoshi Kakushima, Robert N. Young
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Patent number: 4980372Abstract: A benzoylaminophenoxybutanoic acid derivative of general formula: ##STR1## [wherein R.sup.1 represents hydrogen atom or alkyl group of from 1 to 4 carbon atoms(s),A represents oxygen atom, sulfur atom or sulfinyl (SO) group, two R.sup.1 s represents methyl groups or chlorine atoms at the same time or cyclopentane, cyclohexane or benzene ring together with the carbon atoms of benzene ring each attaching,R.sup.2 represents a group of general formula: ##STR2## {wherein B represents oxygen atom, sulfur atom or a group of general formula:NR.sup.11 (wherein R.sup.11 represents hydrogen atom or alkyl group of from 1 to 4 carbon atom(s)),R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s) halogen atom, trifluoromethyl group or cyclobutylmethyl group,m represents 0 or 1,n represents an integer of from 1 to 5, andR.sup.9 and R.sup.Type: GrantFiled: May 6, 1988Date of Patent: December 25, 1990Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
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Patent number: 4976891Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted arly, aralkyl or hetelocycle; R.sub.3 is hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkeneylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.Type: GrantFiled: March 23, 1989Date of Patent: December 11, 1990Assignee: Shionogi & Co., Ltd.Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Sanji Hagishita, Kaoru Seno, Susumu Kamata
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Patent number: 4975444Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.Type: GrantFiled: August 25, 1989Date of Patent: December 4, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
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Patent number: 4975460Abstract: Novel indanoxyacetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a substituted or unsubstituted phenyl group, naphtyl group or a sulfur-containing heterocyclic group, R.sup.2 is hydroxy group or a protected hydroxy group, p is an integer of 2 or 3, and q is an integer of 0 or 1, and a salt thereof are disclosed.Said derivative (I) and a salt thereof are useful as a platelet aggregation-inhibiting agent and an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis, embolism, coronary and cerebral vascular smooth muscl vellication, asthma, and the like.Type: GrantFiled: February 17, 1989Date of Patent: December 4, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Harumichi Kohno, Yasuhiko Sasaki, Katsuo Ikezawa, Akio Odawara
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Patent number: 4971994Abstract: Novel N-phenyl-N-carbonylthioureas of the formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.10 alkyl, phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl or phenyl-C.sub.1 -C.sub.7 alkyl each of which is monohalogenated or polyhalogenated or interrupted once or more than once by oxygen and/or sulfur; C.sub.3 -C.sub.8 cycloalkyl; C hd 3-C.sub.8 cycloalkyl which is monosubstituted or polysubstituted by halogen or C.sub.1 -C.sub.5 alkyl; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 is C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, phenyl, phenyl-C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.8 cycloalkyl; C.sub.1 14 C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl each of which is monohalogenated or polyhalogenated or interrupted once or more than once by oxygen and/or sulfur; C.sub.3 -C.sub.8 cycloalkyl; phenyl or C.sub.3 -C.sub.8 cycloalkyl each of which is monosubstituted or polysubstituted by halogen or C.Type: GrantFiled: April 11, 1989Date of Patent: November 20, 1990Assignee: Ciba-Geigy CorporationInventors: Jozef Drabek, Manfred Boger, Josef Ehrenfreund
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4968809Abstract: New spirofluoreneisothiazolidinone dioxides and methods for their preparation are disclosed.Type: GrantFiled: November 4, 1988Date of Patent: November 6, 1990Inventor: Mark T. Dupriest
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Patent number: 4963587Abstract: There are disclosed are glycine derivative of the formula: ##STR1## (wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a carboxyl group which may be protected, Q represents a lower alkylene group and m represents 0 or 1) or a pharmacologically acceptable salt thereof and a process for preparing the same.Type: GrantFiled: December 5, 1989Date of Patent: October 16, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Yasuo Sekine, Yasuhiko Sasaki, Katsuo Ikezawa, Akio Odawara
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Patent number: 4962224Abstract: Disclosed herein are N-naphthoylglycines and methods of their preparation. The N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.Type: GrantFiled: August 22, 1989Date of Patent: October 9, 1990Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Kazimir Sestanj
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Patent number: 4960792Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.Type: GrantFiled: May 8, 1989Date of Patent: October 2, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James
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Patent number: 4959383Abstract: Phenylsulfone alkenoic acids and derivatives thereof are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR wherein R is hydrogen, alkali metal or lower alkyl or X is 5-tetrazolyl or ##STR2## wherein R' is lower alkyl or aryl; n is 2, 3 or 4 and m is 2, 3 or 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic disease.Type: GrantFiled: October 31, 1988Date of Patent: September 25, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Steven E. Hall
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Patent number: 4952235Abstract: (Hetero) aryloxynaphthalenes having substituents bonded via sulphur having herbicidal activity and of the formula ##STR1## in which m represents the number 0, 1 or 2,n represents the numbers 0 or 1,R.sup.1 represents hydrogen, halogen, cyano or trifluoromethyl,R.sup.2 represents hydrogen or halogen,R.sup.3 represents halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio or trifluoromethylsulphonyl,R.sup.4 represents hydrogen or halogen,X represents nitrogen or the group C--R.sup.5, whereinR.sup.5 represents hydrogen or halogen,Y represents oxygen or one of the groupings ##STR2## wherein R.sup.6 represents hydrogen, alkyl, --CO--Z or --SO.sub.2 --Z andZ represents hydrogen, halogen or an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkinyl, aryl or heteroaryl radical.Type: GrantFiled: June 22, 1989Date of Patent: August 28, 1990Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 4948810Abstract: Novel phenoxyacetic acid derivative of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, naphthyl group or a sulfur-containing 5-membered hetero-monocyclic group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or phenyl group, R.sup.5 is hydrogen atom or a lower alkyl group, R.sup.6 is carboxyl group, a protected carboxyl group, hydroxy group or a di(lower alkyl)-amino group, Ring A is a substituted or unsubstituted phenylene group, m is 0 or 1 and n is an integer 0 to 5, provided that, when m is 0,(1) at least either one of R.sup.1 to R.sup.4 is or/are a phenyl-lower alkyl group or phenyl group,(2) at least either one of R.sup.1 to R.sup.4 is or/are a lower alkyl group, and R.sup.6 is hydroxy group, or(3) all of R.sup.1 to R.sup.4 are hydrogen atom, and Ring A is a substituted phenylene group,or a pharmaceutically acceptable salt thereof are disclosed.Type: GrantFiled: February 6, 1989Date of Patent: August 14, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Takayuki Kawaguchi, Toyoharu Yamashita, Yasuhiko Sasaki, Tamotu Shimazaki
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Patent number: 4948809Abstract: The present invention provides sulphonylphenylalkylamines of the general formula: ##STR1## wherein R.sub.1 is an alkyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3-7 carbon atoms or an aralkyl, aralkenyl or aryl radical, the aryl moiety, in each case, being optionally substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, R.sub.2 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical or an aralkyl or aralkenyl radical, the aryl moiety, in each case, optionally being substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.Type: GrantFiled: December 5, 1988Date of Patent: August 14, 1990Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Hans-Peter Wolff, Karlheinz Stegmeier, Johannes Pill
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Patent number: 4939133Abstract: The present invention relates to novel N-substituted 2-hydroxybenzamide and N-substituted 2-hydroxy-.alpha.-oxo-benezene acetamide compounds pharmaceutical compositions, and methods of use for therefore for the treatment of diseases in which products having lipoxygenase enzyme activity contribute to the pathological condition. Selected novel intermediates are also the present invention.Type: GrantFiled: October 1, 1985Date of Patent: July 3, 1990Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn, Wiaczeslaw A. Cetenko, Jagadish C. Sircar, Charles F. Schwender, Elizabeth A. Johnson, Roderick J. Sorenson, Paul C. Unangst
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Patent number: 4937264Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: June 30, 1989Date of Patent: June 26, 1990Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee, Clarence S. Rooney
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Patent number: 4929754Abstract: The invention relates to new benzenesulphonamidoindanyl compounds useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.Type: GrantFiled: February 1, 1989Date of Patent: May 29, 1990Assignee: Dr. Karl Thomae GmbHInventors: Josef Nickl, Armin Heckel, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
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Patent number: 4929641Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.Type: GrantFiled: May 11, 1988Date of Patent: May 29, 1990Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
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Patent number: 4921632Abstract: Liquid Crystal compounds represented by the following formula are disclosed. ##STR1## wherein R and R' are independently selected from alkyl groups containing 1.about.20 carbon atoms; X is --O--, --O--CO--O-- or direct bond; A.sub.1 and A.sub.2 are independently cyclic groups (such as phenylene and biphenylene), said cyclic groups may be substituted with 1.about.4 fluorine, chlorine or bromine atoms, or 1 or 2 substituent groups selected from the group consisting of cyano, nitro and trifluoromethyl groups; Y is --CO--O--, --O--CO--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --N.dbd.N--, --CH.sub.2 S--, --SCH.sub.2 -- or direct bond; and * represents asymmetric atom providing optical activity.Type: GrantFiled: August 19, 1988Date of Patent: May 1, 1990Assignees: NEC Corporation, Sanyo Chemical Industries, Ltd.Inventors: Toyokazu Nakamura, Yuzi Kato, Shohei Naemura, Chizuka Tani, Masahiro Satoh, Kunikiyo Yoshio, Hiroshi Kishiki, Hiroshi Hoshino
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Patent number: 4916237Abstract: Intermediates useful for synthesis of cephalosporins are disclosed, which intermediates are concerned with 1,2,3-thiadiazole-4-thiolates and the preparation of such thiolates.Type: GrantFiled: August 26, 1988Date of Patent: April 10, 1990Assignee: American Cyanamid CompanyInventors: Ving J. Lee, William V. Curran