The Diazine Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/116)
-
Patent number: 5489503Abstract: Novel UV absorbers of the bis- or tris-2'-hydroxyphenyltriazine type and their use in photographic materials, inks or recording materials for ink-jet printing, and surface coatings are described which conform to the formula ##STR1## in which the radicals R.sub.1 and R.sub.9 are as defined in claim 1.Type: GrantFiled: December 6, 1994Date of Patent: February 6, 1996Assignee: Ciba-Geigy Corp.Inventor: Vien V. Toan
-
Patent number: 5482941Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable salts thereof whereinR.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or CONR.sup.5 R.sup.6 ;R.sup.2 is H or- C.sub.1 -C.sub.4 alkyl;R.sup.3 is C.sub.2 -C.sub.4 alkyl;R.sup.4 is H, C.sub.2 -C.sub.4 alkanoyl optionally substituted with NR.sup.7 R.sup.8, (hydroxy)C.sub.2 -C.sub.4 alkyl optionally substituted with NR.sup.7 R.sup.8, CH.dbd.CHCO.sub.2 R.sup.9, CH.dbd.CHCONR.sup.7 R.sup.8, CH.sub.2 CH.sub.2 CO.sub.2 R.sup.9, CH.sub.2 CH.sub.2 CONR.sup.7 R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, SO.sub.2 NH(CH.sub.2).sub.n NR.sup.7 R.sup.8 or imidazolyl;R.sup.5 and R.sup.6 are each independently H or C.sub.1 -C.sub.4 alkyl;R.sup.7 and R.sup.8 are each independently H or C.sub.1 -C.sub.4 alkyl, or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or 4-(NR.sup.10)-1-piperazinyl group wherein any of said groups is optionally substituted with CONR.sup.5 R.sup.6 ;R.sup.9 is H or C.sub.1 -C.sub.Type: GrantFiled: May 6, 1994Date of Patent: January 9, 1996Assignee: Pfizer Inc.Inventor: Nicholas K. Terrett
-
Patent number: 5482938Abstract: Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds are disclosed which are azabicyclo[2.2.2]oximes, azabicyclo[2.2.2]-amines, azabicyclo[3.2.1]oximes and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms.Type: GrantFiled: February 1, 1994Date of Patent: January 9, 1996Assignee: Warner-Lambert CompanyInventors: David J. Lauffer, Walter H. Moos, Michael R. Pavia, Haile Tecle, Anthony J. Thomas
-
Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 5466701Abstract: Compounds having the structural formula ##STR1## which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.Type: GrantFiled: June 22, 1994Date of Patent: November 14, 1995Assignee: Sterling Winthrop Inc.Inventors: Dennis J. Hlasta, James H. Ackerman, Albert J. Mura, Ranjit C. Desai
-
Patent number: 5426106Abstract: A class of 4-hydroxy-pyrrolo[1,2-b]pyridazin-2(1H)-one derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.Type: GrantFiled: March 16, 1993Date of Patent: June 20, 1995Assignee: Merck Sharp & Dohme LimitedInventors: Janusz J. Kulagowski, Paul D. Leeson
-
Patent number: 5403843Abstract: A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.Type: GrantFiled: August 7, 1992Date of Patent: April 4, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroshi Akimoto, Koichiro Ootsu, Fumio Itoh
-
Patent number: 5401745Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.Type: GrantFiled: March 19, 1993Date of Patent: March 28, 1995Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh, David L. Williams, Jr.
-
Patent number: 5385894Abstract: Novel disubstituted 6-aminoquinazolinones of the Formula (I), are useful as angiotensin II antagonists: ##STR1##Type: GrantFiled: April 4, 1994Date of Patent: January 31, 1995Assignee: Merck & Co., Inc.Inventors: Stephen E. de Laszlo, Tomasz W. Glinka, William J. Greenlee, Prasun K. Chakravarty, Arthur A. Patchett
-
Patent number: 5380719Abstract: Angiotensin II inhibition is exhibited by ##STR1## wherein: X is --CH.sub.2 -- or O;R is hydrogen, alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl;R.sup.1 and R.sup.2 are each independently O or absent;R.sup.3 is hydrogen, alkyl, alkenyl, alkoxy, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, halo, haloalkyl, or haloalkoxy;R.sup.4 is hydrogen, alkyl, alkenyl, alkoxy, aryl, cycloalkyl, aralkyl, cycloalkylalkyl, --R.sup.8 --OH, or --R.sup.8 CO.sub.2 R.sup.9 ;and the remaining symbols are as defined in the specification.Type: GrantFiled: April 28, 1992Date of Patent: January 10, 1995Assignee: E. R. Squibb & Sons, Inc.Inventor: Kyoung S. Kim
-
Patent number: 5378846Abstract: 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine derivatives having the formula (Formula I) ##STR1## and therapeutically acceptable acid addition salts thereof (Formula I.HX), wherein: R.sup.1 =hydrogen or acyl groups; and R.sup.2 =hydrogen or substituted aminomethyl groups. Said compounds and their acid addition salts have psychotropic activity, particularly anxiolytic activity.Type: GrantFiled: June 11, 1993Date of Patent: January 3, 1995Assignee: Russian-American Institute For New Drug DevelopmentInventors: Sergey B. Seredenin, Tatiana A. Voronina, Arkady M. Likhosherstov, Vitaly P. Peresada, Gennady M. Molodavkin, James A. Halikas
-
Patent number: 5369104Abstract: Novel compound represented by the formula: ##STR1## wherein X stands for a methine (i.e. the group --CH.dbd.) group or a nitrogen atom; R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, or, taken together, may form a 5- to 7-membered ring combined with the adjacent --C.dbd.C--; R.sup.4 and R.sup.5 respectively stands for a hydrogen atom or an optionally substituted lower alkyl group or, taken together, form a 3- to 7-membered homo- or heterocyclic ring combined with the adjacent carbon atom; A stands for an optionally substituted amino group; m and n denote 1 to 4, respectively, or salts thereof which has an antiallergic, antiinflammatory and anti-PAF activity and is useful as an antiasthmatic agent.Type: GrantFiled: December 28, 1992Date of Patent: November 29, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
-
Patent number: 5364831Abstract: Quinoxaline derivatives having the formula I ##STR1## wherein X represents a halogen atom; R represents ##STR2## --CH.dbd.CH--COOR.sup.2 (R.sup.2 represents a C.sub.1 -C.sub.4 alkyl group); --CN or --CH.sub.2 OH, and R.sup.1 represents ##STR3## --S--R.sup.3 (R.sup.3 represents a C.sub.1 -C.sub.4 alkyl or alkenyl group or phenyl or chlorophenyl group), --NH--R.sup.4 (R.sup.4 represents a C.sub.1 -C.sub.4 alkoxy carbonylalkyl group, hydroxy alkyl group, phenyl group; C.sub.1 -C.sub.4 alkoxy alkyl group or di C.sub.1 -C.sub.4 alkyl amino group), are remarkably effective as selective herbicides.Type: GrantFiled: August 6, 1980Date of Patent: November 15, 1994Assignee: Nissan Chemical Industries Ltd.Inventors: Yasukazu Ura, Gozyo Sakata, Kenzi Makino, Yasuo Kawamura, Yuzi Kawamura, Takasi Ikai, Tosihiko Oguti
-
Patent number: 5314889Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).Type: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
-
Patent number: 5308846Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.Type: GrantFiled: July 22, 1993Date of Patent: May 3, 1994Assignees: Merck & Co., Inc., E. I. Du Pont de Nemours and Co.Inventors: Eric E. Allen, Richard E. Olson
-
Patent number: 5296487Abstract: A compound of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, nitro, amino, protected amino, hydroxyamino, lower alkyl, hydroxy, protected hydroxy, sulfamoyl, carboxy, protected carboxy, mercapto, optionally substituted heterocyclic-carbonyl, optionally substituted heterocyclic-(lower)alkyl, lower alkylthio, hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.3 is aryl which may have suitable substituent(s), andA is lower alkylene,or pharmaceutically acceptable salts thereof.Type: GrantFiled: September 6, 1991Date of Patent: March 22, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Norihiko Shimazaki, Hitoshi Yamazaki, Takumi Yatabe, Hirokazu Tanaka, Yoshikuni Itoh, Masashi Hashimoto
-
Patent number: 5292734Abstract: This disclosure describes novel 2, 3, 6 substituted quinazolinones having the formula: ##STR1## wherein X, R, and R.sup.6 are described in the specification which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: April 23, 1993Date of Patent: March 8, 1994Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan
-
Patent number: 5283244Abstract: The present invention is a pyrazine derivative which has glutamate receptor antagonizing activity, represented by formula: ##STR1## wherein Z represents C or N, provided that two Zs are not N atoms at the same time; R.sup.1 represents: ##STR2## wherein ##STR3## represents ##STR4## R.sup.6 represents H or alkyl, and R.sup.7 and R.sup.8 represent each H, alkyl, nitro or phenyl, or alternatively R.sup.7 and R.sup.8 are combined together to represent butadienylene or 1,4-butylene; R.sup.2 and R.sup.3 represent each H, F, cyano, acyl, nitro, alkyl, morpholino or one of said species of R.sup.1 ; R.sup.4 and R.sup.5 represent each H, hydroxyl, alkyl, cycloalkyl, heterocycle, phenyl, or Y-substituted alkyl; Y represents hydroxyl, acyloxy, F-substituted methyl, cycloalkyl, tetrahydrofuryl, carboxyl, alkoxycarbonyl or ##STR5## R.sup.9 and R.sup.10 represent each H or alkyl, or alternatively R.sup.9 and R.sup.10 are combined together to represent a 5- or 6-membered cyclic group which may contain oxygen atom(s).Type: GrantFiled: May 3, 1993Date of Patent: February 1, 1994Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Shuichi Sakamoto, Junya Ohmori, Hirokazu Kubota, Masao Sasamata, Masamichi Okada, Kazuyuki Hidaka
-
Patent number: 5270466Abstract: There are provided substituted quinazoline compounds of formula I ##STR1## and their use for the prevention, control or amelioration of diseases caused by phytopathogenic fungi. Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infestations and diseases.Type: GrantFiled: June 11, 1992Date of Patent: December 14, 1993Assignee: American Cyanamid CompanyInventor: Gregory J. Haley
-
Patent number: 5264438Abstract: Compounds of the formula: ##STR1## are described wherein R.sup.1, R.sup.2, R.sup.3 and A are described in the claims. These compounds show significant dopamine receptor agonist activity.Type: GrantFiled: December 14, 1990Date of Patent: November 23, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Norihiko Shimazaki, Hitoshi Yamazaki, Takumi Yatabe, Hirokazu Tanaka, Yoshikuni Itoh, Masashi Hashimoto
-
Patent number: 5258380Abstract: (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.Type: GrantFiled: June 21, 1991Date of Patent: November 2, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Gaston S. M. Diels
-
Patent number: 5238942Abstract: Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists.Type: GrantFiled: April 16, 1992Date of Patent: August 24, 1993Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Dooseop Kim, Stephen E. de Laszlo, Tomasz W. Glinka
-
Patent number: 5202322Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the reninangiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.Type: GrantFiled: September 25, 1991Date of Patent: April 13, 1993Assignees: Merck & Co., Inc., E. I. du Pont de Nemours and CompanyInventors: Eric E. Allen, Richard E. Olson
-
Patent number: 5187276Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: November 28, 1990Date of Patent: February 16, 1993Assignee: Troponwerke GmbH & Co. KG.Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Thurman
-
Patent number: 5162325Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: May 7, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
-
Patent number: 5157035Abstract: Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.Type: GrantFiled: January 3, 1991Date of Patent: October 20, 1992Assignee: Janssen Pharmaceutica N. V.Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Joannes J. M. Willems, Marcel G. M. Luyckx
-
Patent number: 5141946Abstract: Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in whichA, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represnts a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.Type: GrantFiled: June 14, 1991Date of Patent: August 25, 1992Assignee: Meiji Seika Kabushiki KaishaInventors: Kiyoaki Katano, Tamako Tomomoto, Hiroko Ogino, Naoki Yamazaki, Fumiya Hirano, Yasukatsu Yuda, Fukio Konno, Motohiro Nishio, Tomoya Machinami, Seiji Shibahara, Takashi Tsuruoka, Shigeharu Inouye
-
Patent number: 5120845Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: July 24, 1991Date of Patent: June 9, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
-
Patent number: 5089043Abstract: A heterocyclic oxy-phenoxyacetic acid derivative of the formula: ##STR1## , or its salt, which is useful as a herbicide.Type: GrantFiled: November 6, 1990Date of Patent: February 18, 1992Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hayase, Kohei Matsumoto, Kazuo Kamei, Kinya Ide, Toshio Takahashi
-
Patent number: 5073558Abstract: Disclosed are an aminopyrimidine compound or an acid addition salt thereof represented by the formula: ##STR1## wherein R1, R2, R3, R4, R5 and Y have the same meanings defined in the specification;a process for preparing the compound and insecticide or bactericide containing the compound.Type: GrantFiled: October 26, 1989Date of Patent: December 17, 1991Assignee: Ube Industries, Ltd.Inventors: Tokio Obata, Katsutoshi Fujii, Isamu Narita, Shoji Shikita
-
Patent number: 5043337Abstract: Insecticidal pyrimidin-4-yl carbamates of the formula ##STR1## in which R.sup.1 represents alkoxy, alkylthio, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl or dialkylamino,R.sup.2 represents hydrogen or alkyl,R.sup.3 represents hydrogen, alkyl or alkoxy orR.sup.2 and R.sup.3 together represent a double-linked alkanediyl radical,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen or alkyl andA represents oxygen, sulphur or a radical ##STR2## where R.sup.6 represents alkyl.Type: GrantFiled: April 4, 1990Date of Patent: August 27, 1991Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Kurt Findeisen, Jurgen Hartwig, Benedikt Becker
-
Patent number: 5041548Abstract: Triethylene diamines are prepared in a high yield with an amine compound having a specific group as the starting material by bringing the same into contact with a catalyst formed of a crystalline metal silicate of which the molar ratio (SiO.sub.2 /M.sub.2 O.sub.3) of silicon dioxide (SiO.sub.2) to the oxide of a tervalent metal (M.sub.2 O.sub.3, M being the tervalent metal) is at least 12. Particularly high efficiency can be obtained by using a crystalline metal silicate crystallized in the presence of an organic crystallizing agent.Type: GrantFiled: June 17, 1987Date of Patent: August 20, 1991Assignee: Idemitsu Kosan Company LimitedInventors: Haruhito Sato, Masanori Tsuzuki
-
Patent number: 5008266Abstract: 4(3H)-Quinazolinone derivative of formula (I) are provided. ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, an aryl group, a substituted aryl group, or an aralkyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkylamino group, a phenyl group, a substituted phenyl group, or a 5- or 6-membered heterocyclic group containing one or more N, O or S as a hetero atom or atoms, said heterocyclic group optionally being substituted or fused with a benzene ring; n is 1 or 2; or R.sub.2 represents a geranyl group or a dipyridylmethyl group together with the group --(CH.sub.2).sub.n --; and X is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a halogen atom, and pharmaceutically acceptable acid addition salts thereof. They are useful as antiucler agents.Type: GrantFiled: July 26, 1989Date of Patent: April 16, 1991Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
-
Patent number: 4988809Abstract: The invention relates to substituted 2-pyrimidinyl-1- piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: February 21, 1990Date of Patent: January 29, 1991Assignee: Troponwerke GmbH & Co., KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, THomas Glaser, Teunis Schuurmann
-
Patent number: 4968797Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicalsX.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 30, 1987Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
-
Patent number: 4937343Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: September 22, 1988Date of Patent: June 26, 1990Assignee: Troponwerke GmbH & Co. KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
-
Patent number: 4923864Abstract: Simple amides and derivatives thereof useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.Type: GrantFiled: October 24, 1988Date of Patent: May 8, 1990Assignee: Pfizer Inc.Inventor: Robert L. Rosati
-
Patent number: 4923873Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: May 18, 1987Date of Patent: May 8, 1990Assignee: E. I. du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier
-
Patent number: 4921527Abstract: The invention relates to sulfonylurea compounds with a substituted or unsubstituted bicyclic nine-membered ring having one to five heteroatoms which are preemergent and/or postemergent herbicides or plant growth regulants.Type: GrantFiled: May 4, 1988Date of Patent: May 1, 1990Assignee: E. I. du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
-
Patent number: 4908056Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: February 17, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Chi-Ping Tseng
-
Patent number: 4894453Abstract: A compound of the formula ##STR1## wherein Q is --CO-- or --CH.sub.2 --, R is hydroxyl, lower alkoxy, halogen, --NH-lower alkylene-OH, --NH-lower alkylene-arylthio, --NH-lower alkylene-halogen, ##STR2## in which ##STR3## is dilower alkylamino, cycloalkylamino, morpholino, ##STR4## in which R.sub.9 is hydrogen, lower alkyl or aryl, R.sub.10 is hydrogen, lower alkyl, hydroxy-lower alkyl, hydroxy-lower alkoxy-lower alkyl or di(aryl)-lower alkyl, m is an integer from 4 to 6, n is 2 or 3, R.sub.1 is alkyl or aryl-lower alkyl, R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene, and R.sub.4 is hydrogen, lower alkyl or aryl, in which aryl is phenyl which is optionally substituted with a group selected from the group consisting of 1-3 halogen, nitro, lower alkyl and lower alkoxy, or a pharmaceutically acceptable salt thereof, inhibits blood platelet aggregation, has vasodilating activity and inhibits lipoperoxide generation.Type: GrantFiled: June 30, 1987Date of Patent: January 16, 1990Assignee: Toyo Jozo Kabushiki KaishaInventors: Masao Yaso, Yukio Suzuki, Kensuke Shibata, Daisuke Mochizuki, Eiichi Hayashi
-
Patent number: 4886800Abstract: The present invention comprises certain amide and ester derivatives of 4-substituted-cinnoline-3-carboxylic acids and 3-acyl-4-substituted-cinnoline derivatives, and their use as central nervous system (CNS) depressants.Type: GrantFiled: May 29, 1986Date of Patent: December 12, 1989Assignee: ICI Americas Inc.Inventor: James F. Resch
-
Patent number: 4877875Abstract: 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of 1-methyltetrazole-5-yl-thio, 1-imidazolyl, morpholino, ##STR2## in which R.sub.5 is hydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A and R.sub.1 are as defined above, R.sub.2 and R.sub.3 are each lower alkyl or together form tetramethylene, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.Type: GrantFiled: October 19, 1988Date of Patent: October 31, 1989Assignee: Toyo Jozo Kabushiki KaishaInventors: Masao Yaso, Yukio Suzuki, Kensuke Shibata, Eiichi Hayashi
-
Patent number: 4871387Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.Type: GrantFiled: December 4, 1986Date of Patent: October 3, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
-
Patent number: 4867783Abstract: This invention relates to certain sulfonylurea compounds having substituents ortho to the sulfonyl-urea linkage that includes a 3- or 4-membered carbocyclic ring, a saturated 5- or 6-membered carbocyclic ring of a heterocyclic ring which contains 1 hetero-atom selected from O, S and NR.sub.3, agriculturally suitable compositions thereof and a method of their use as herbicides or plant growth regulants.Type: GrantFiled: September 14, 1988Date of Patent: September 19, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: James V. Hay, Barry A. Wexler, Donna F. Zimmerman
-
Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
-
Patent number: 4837319Abstract: 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof.Type: GrantFiled: February 25, 1987Date of Patent: June 6, 1989Assignee: Toyo Jozo Kabushiki KaishaInventors: Masao Yaso, Yukio Suzuki, Kensuke Shibata, Eiichi Hayashi
-
Patent number: 4818756Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: March 10, 1986Date of Patent: April 4, 1989Assignee: Troponwerke GmbH & Co., KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
-
Patent number: 4802906Abstract: Ortho-Sulfonamide benzenesulfonylureas, such as N-cyclopropyl-N'-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,2-benzened isulfonamide, are useful as pre-emergent and post-emergent herbicides.Type: GrantFiled: December 23, 1985Date of Patent: February 7, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Donald J. Dumas
-
Patent number: RE34201Abstract: This invention pertains to novel substituted N/aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.Type: GrantFiled: April 14, 1992Date of Patent: March 23, 1993Assignee: Anaquest, Inc.Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer