The Diazine Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/116)
  • Patent number: 5489503
    Abstract: 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: Grant
    Filed: December 6, 1994
    Date of Patent: February 6, 1996
    Assignee: Ciba-Geigy Corp.
    Inventor: Vien V. Toan
  • Patent number: 5482941
    Abstract: 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: Grant
    Filed: May 6, 1994
    Date of Patent: January 9, 1996
    Assignee: Pfizer Inc.
    Inventor: Nicholas K. Terrett
  • Patent number: 5482938
    Abstract: 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: Grant
    Filed: February 1, 1994
    Date of Patent: January 9, 1996
    Assignee: Warner-Lambert Company
    Inventors: David J. Lauffer, Walter H. Moos, Michael R. Pavia, Haile Tecle, Anthony J. Thomas
  • Patent number: 5470975
    Abstract: 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: Grant
    Filed: January 11, 1994
    Date of Patent: November 28, 1995
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5466701
    Abstract: 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: Grant
    Filed: June 22, 1994
    Date of Patent: November 14, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Dennis J. Hlasta, James H. Ackerman, Albert J. Mura, Ranjit C. Desai
  • Patent number: 5426106
    Abstract: 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: Grant
    Filed: March 16, 1993
    Date of Patent: June 20, 1995
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Janusz J. Kulagowski, Paul D. Leeson
  • Patent number: 5403843
    Abstract: 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: Grant
    Filed: August 7, 1992
    Date of Patent: April 4, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroshi Akimoto, Koichiro Ootsu, Fumio Itoh
  • Patent number: 5401745
    Abstract: 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: Grant
    Filed: March 19, 1993
    Date of Patent: March 28, 1995
    Assignee: 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: 5385894
    Abstract: Novel disubstituted 6-aminoquinazolinones of the Formula (I), are useful as angiotensin II antagonists: ##STR1##
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: January 31, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Tomasz W. Glinka, William J. Greenlee, Prasun K. Chakravarty, Arthur A. Patchett
  • Patent number: 5380719
    Abstract: 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: Grant
    Filed: April 28, 1992
    Date of Patent: January 10, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Kyoung S. Kim
  • Patent number: 5378846
    Abstract: 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: Grant
    Filed: June 11, 1993
    Date of Patent: January 3, 1995
    Assignee: Russian-American Institute For New Drug Development
    Inventors: Sergey B. Seredenin, Tatiana A. Voronina, Arkady M. Likhosherstov, Vitaly P. Peresada, Gennady M. Molodavkin, James A. Halikas
  • Patent number: 5369104
    Abstract: 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: Grant
    Filed: December 28, 1992
    Date of Patent: November 29, 1994
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
  • Patent number: 5364831
    Abstract: 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: Grant
    Filed: August 6, 1980
    Date of Patent: November 15, 1994
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Yasukazu Ura, Gozyo Sakata, Kenzi Makino, Yasuo Kawamura, Yuzi Kawamura, Takasi Ikai, Tosihiko Oguti
  • Patent number: 5314889
    Abstract: 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: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5308846
    Abstract: 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: Grant
    Filed: July 22, 1993
    Date of Patent: May 3, 1994
    Assignees: Merck & Co., Inc., E. I. Du Pont de Nemours and Co.
    Inventors: Eric E. Allen, Richard E. Olson
  • Patent number: 5296487
    Abstract: 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: Grant
    Filed: September 6, 1991
    Date of Patent: March 22, 1994
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Norihiko Shimazaki, Hitoshi Yamazaki, Takumi Yatabe, Hirokazu Tanaka, Yoshikuni Itoh, Masashi Hashimoto
  • Patent number: 5292734
    Abstract: 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: Grant
    Filed: April 23, 1993
    Date of Patent: March 8, 1994
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan
  • Patent number: 5283244
    Abstract: 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: Grant
    Filed: May 3, 1993
    Date of Patent: February 1, 1994
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Shuichi Sakamoto, Junya Ohmori, Hirokazu Kubota, Masao Sasamata, Masamichi Okada, Kazuyuki Hidaka
  • Patent number: 5270466
    Abstract: 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: Grant
    Filed: June 11, 1992
    Date of Patent: December 14, 1993
    Assignee: American Cyanamid Company
    Inventor: Gregory J. Haley
  • Patent number: 5264438
    Abstract: 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: Grant
    Filed: December 14, 1990
    Date of Patent: November 23, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Norihiko Shimazaki, Hitoshi Yamazaki, Takumi Yatabe, Hirokazu Tanaka, Yoshikuni Itoh, Masashi Hashimoto
  • Patent number: 5258380
    Abstract: (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: November 2, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels
  • Patent number: 5238942
    Abstract: Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists.
    Type: Grant
    Filed: April 16, 1992
    Date of Patent: August 24, 1993
    Assignee: 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: 5202322
    Abstract: 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: Grant
    Filed: September 25, 1991
    Date of Patent: April 13, 1993
    Assignees: Merck & Co., Inc., E. I. du Pont de Nemours and Company
    Inventors: Eric E. Allen, Richard E. Olson
  • Patent number: 5187276
    Abstract: 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: Grant
    Filed: November 28, 1990
    Date of Patent: February 16, 1993
    Assignee: Troponwerke GmbH & Co. KG.
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Thurman
  • Patent number: 5162325
    Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.
    Type: Grant
    Filed: May 7, 1991
    Date of Patent: November 10, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
  • Patent number: 5157035
    Abstract: Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.
    Type: Grant
    Filed: January 3, 1991
    Date of Patent: October 20, 1992
    Assignee: Janssen Pharmaceutica N. V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Joannes J. M. Willems, Marcel G. M. Luyckx
  • Patent number: 5141946
    Abstract: 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: Grant
    Filed: June 14, 1991
    Date of Patent: August 25, 1992
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: 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: 5120845
    Abstract: 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: Grant
    Filed: July 24, 1991
    Date of Patent: June 9, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
  • Patent number: 5089043
    Abstract: A heterocyclic oxy-phenoxyacetic acid derivative of the formula: ##STR1## , or its salt, which is useful as a herbicide.
    Type: Grant
    Filed: November 6, 1990
    Date of Patent: February 18, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yoshio Hayase, Kohei Matsumoto, Kazuo Kamei, Kinya Ide, Toshio Takahashi
  • Patent number: 5073558
    Abstract: 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: Grant
    Filed: October 26, 1989
    Date of Patent: December 17, 1991
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Isamu Narita, Shoji Shikita
  • Patent number: 5043337
    Abstract: 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: Grant
    Filed: April 4, 1990
    Date of Patent: August 27, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Kurt Findeisen, Jurgen Hartwig, Benedikt Becker
  • Patent number: 5041548
    Abstract: 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: Grant
    Filed: June 17, 1987
    Date of Patent: August 20, 1991
    Assignee: Idemitsu Kosan Company Limited
    Inventors: Haruhito Sato, Masanori Tsuzuki
  • Patent number: 5008266
    Abstract: 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: Grant
    Filed: July 26, 1989
    Date of Patent: April 16, 1991
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
  • Patent number: 4988809
    Abstract: 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: Grant
    Filed: February 21, 1990
    Date of Patent: January 29, 1991
    Assignee: Troponwerke GmbH & Co., KG
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, THomas Glaser, Teunis Schuurmann
  • Patent number: 4968797
    Abstract: 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: Grant
    Filed: October 30, 1987
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
  • Patent number: 4937343
    Abstract: 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: Grant
    Filed: September 22, 1988
    Date of Patent: June 26, 1990
    Assignee: Troponwerke GmbH & Co. KG
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
  • Patent number: 4923864
    Abstract: Simple amides and derivatives thereof useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
    Type: Grant
    Filed: October 24, 1988
    Date of Patent: May 8, 1990
    Assignee: Pfizer Inc.
    Inventor: Robert L. Rosati
  • Patent number: 4923873
    Abstract: 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: Grant
    Filed: May 18, 1987
    Date of Patent: May 8, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: David M. Stout, William L. Matier
  • Patent number: 4921527
    Abstract: 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: Grant
    Filed: May 4, 1988
    Date of Patent: May 1, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4908056
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: March 13, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4894453
    Abstract: 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: Grant
    Filed: June 30, 1987
    Date of Patent: January 16, 1990
    Assignee: Toyo Jozo Kabushiki Kaisha
    Inventors: Masao Yaso, Yukio Suzuki, Kensuke Shibata, Daisuke Mochizuki, Eiichi Hayashi
  • Patent number: 4886800
    Abstract: 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: Grant
    Filed: May 29, 1986
    Date of Patent: December 12, 1989
    Assignee: ICI Americas Inc.
    Inventor: James F. Resch
  • Patent number: 4877875
    Abstract: 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: Grant
    Filed: October 19, 1988
    Date of Patent: October 31, 1989
    Assignee: Toyo Jozo Kabushiki Kaisha
    Inventors: Masao Yaso, Yukio Suzuki, Kensuke Shibata, Eiichi Hayashi
  • Patent number: 4871387
    Abstract: 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: Grant
    Filed: December 4, 1986
    Date of Patent: October 3, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
  • Patent number: 4867783
    Abstract: 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: Grant
    Filed: September 14, 1988
    Date of Patent: September 19, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: James V. Hay, Barry A. Wexler, Donna F. Zimmerman
  • Patent number: 4838925
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: September 25, 1987
    Date of Patent: June 13, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4837319
    Abstract: 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: Grant
    Filed: February 25, 1987
    Date of Patent: June 6, 1989
    Assignee: Toyo Jozo Kabushiki Kaisha
    Inventors: Masao Yaso, Yukio Suzuki, Kensuke Shibata, Eiichi Hayashi
  • Patent number: 4818756
    Abstract: 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: Grant
    Filed: March 10, 1986
    Date of Patent: April 4, 1989
    Assignee: Troponwerke GmbH & Co., KG
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
  • Patent number: 4802906
    Abstract: 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: Grant
    Filed: December 23, 1985
    Date of Patent: February 7, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Donald J. Dumas
  • Patent number: RE34201
    Abstract: 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: Grant
    Filed: April 14, 1992
    Date of Patent: March 23, 1993
    Assignee: Anaquest, Inc.
    Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer