Chalcogen Or Additional Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 548/196)
  • Patent number: 5292715
    Abstract: There is disclosed an iminothiazoline compound of the formula: ##STR1## wherein R.sup.1 is halogen, halo(lower)alkyl, halo(lower)alkoxy or halo(lower)alkylthio; R.sup.2 is methyl, ethyl, chlorine, bromine or iodine; R.sup.3 is lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, lower alkylamino, phenylamino or phenyl, all of which are optionally substituted with at least one substituent selected from halogen, lower alkyl, lower alkoxy, halo(lower)alkyl, lower cycloalkyl and lower cycloalkoxy; and R.sup.4 is hydrogen or halogen. Also disclosed are a process for producing this compound, a herbicidal composition comprising this compound as an active ingredient, and a method for controlling undesired weeds by use of this compound as a herbicide.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: March 8, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Ryo Sato, Tatsuhiro Hamada, Hideyuki Shibata
  • Patent number: 5281614
    Abstract: Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: January 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Prasun K. Chakravarty, Linda L. Chang, William J. Greenlee, Dooseop Kim, Nathan B. Mantlo, Arthur A. Patchett
  • Patent number: 5270317
    Abstract: The invention relates to N-substituted heterocyclic derivatives and its salts.These derivatives have the formula ##STR1## in which the substituents are as defined in the specification.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: December 14, 1993
    Assignee: Elf Sanofi
    Inventors: Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
  • Patent number: 5244863
    Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.
    Type: Grant
    Filed: October 1, 1991
    Date of Patent: September 14, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Tatsuhiro Hamada, Hideyuki Shibata, Ryo Sato
  • Patent number: 5240918
    Abstract: The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.
    Type: Grant
    Filed: March 24, 1992
    Date of Patent: August 31, 1993
    Assignee: EGIS Gyogyszergyar
    Inventors: Karoly Lempert, Gyula Hornyak, Jozsef Fetter, Antal Feller, Klara Gaso, Gabor Gigler, Laszlo Kapolnai, Lujza Petocz, Katalin Szemeredi, Marton Fekete
  • Patent number: 5221685
    Abstract: Disclosed are a thiazoline compound represented by the following formula (I): ##STR1## wherein R represents hydrogen atom or a lower alkyl group, X represents oxygen atom or sulfur atom, and Q represents Ar (where Ar represents a substituted or unsubstituted phenyl group or a substituted or unsubstituted naphthyl group) or ##STR2## (where Y represents a halogen atom, a lower alkyl group, a lower alkoxy group, a lower haloalkyl group, a lower haloalkoxy group, nitro group, acetyl group or cyano group and n represents an integer of 0 to 5),a process for preparing the same and a chemical for controlling noxious organisms containing the same as an active ingredient.
    Type: Grant
    Filed: January 30, 1992
    Date of Patent: June 22, 1993
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Yasuhisa Fukuda, Kiyoshi Tsutsumiuchi, Yoshinori Yamanaka
  • Patent number: 5177095
    Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Wallace Ashton, Kenneth J. Fitch, Thomas F. Walsh, Ralph A. Rivero, Daljit S. Dhanoa
  • Patent number: 5162360
    Abstract: The present invention provides N-substituted aryl-N'-heterocyclic substituted ureas and thioureas of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen, fluorine, chlorine, bromine, alkyl, alkoxy, substituted or unsubstituted benzoyl, substituted or unsubstituted phenyl, amino, substituted amino, or a monocyclic heterocyclic, or a carboxy group; and Het is a substituted monocyclic heterocyclic group containing two hetero atoms selected from nitrogen, oxygen or sulfur; which are useful in treating hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: June 24, 1991
    Date of Patent: November 10, 1992
    Assignee: Warner-Lambert Company
    Inventors: Mark W. Creswell, Andrew D. White
  • Patent number: 5099021
    Abstract: Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R.sub.1 and R.sub.2 independently of one another denote a hydrogen atom or an alkyl group, where R.sub.1 and R.sub.2 are not simultaneously hydrogen or R.sub.1 and R.sub.2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.
    Type: Grant
    Filed: October 30, 1990
    Date of Patent: March 24, 1992
    Assignee: Agrolinz Agrarchemikalien Gesellschaft m.b.H.
    Inventors: Rudolf H. Worther, Horst Korntner, Egmont Auer, Kurt Thonhofer
  • Patent number: 5086054
    Abstract: Novel arylcycloalkanepolyalkylamines useful as anti-psychotic, anti-ischemia, anti-stroke, anti-dementia and anti-convulsant agents. These arylcycloalkanepolyalkylamines are selective high-affinity ligands to the sigma binding-sites containing three basic units: arylcycloalkyl group, an amine group and an intermediate chain. Their preparation and use for treatment of psychoses, ischemia, stroke, dementia and convulsions are also disclosed.
    Type: Grant
    Filed: July 31, 1990
    Date of Patent: February 4, 1992
    Assignee: SRI International
    Inventor: Daniel W. Parish
  • Patent number: 5084571
    Abstract: There are disclosed substituted thiazole dye compounds represented by the following Formula (I):Formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a group capable of substitution onto a benzene ring, n is an integer of 1 to 4, x represents a substitutent capable of forming a hydrogen bond with the hydrogen of --CONH--, R.sub.2 represents an electron-attractive substituent, R.sub.3 represents a group capable of substitution onto a thiazole ring, and R.sub.4 represents an aromatic group or an unsaturated heterocyclic group that bonds to the nitrogen atom at a carbon atom having an unsaturated linkage.The dye compounds provide a cyan color which is good in hues and possesses fastness to light and heat.
    Type: Grant
    Filed: October 18, 1989
    Date of Patent: January 28, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Yasuhiro Shimada
  • Patent number: 5079369
    Abstract: The compound of the formula: ##STR1## wherein R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, and R.sup.6 is amino or protected amino, or its reactive derivative at the carboxy group effective for transforming the carboxy group into a reactive N-acylating group, or a salt thereof.
    Type: Grant
    Filed: June 23, 1989
    Date of Patent: January 7, 1992
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 5066666
    Abstract: compound of the formula: ##STR1## wherein A is the group of the formula:Ar.sup.1 --D--Ar.sup.2 --wherein Ar.sup.1 is a phenyl or thienyl group which may be optionally substituted with at least one of the same or different halogen atom; Ar.sup.2 is a phenylene or thienylene group which may be optionally substituted with at least one of the same or different halogen atom; D is a divalent radical selected from the group consisting of >.dbd.N.dbd.OR.sup.4 [wherein R.sup.4 is a hydrogen atom or lower alkyl group], >C.dbd.O, ##STR2## >CHOH, >NH radical, or single bond, wherein R.sup.5 is a lower alkoxy or a phenyl group which may be optionally substituted with at least one of the same or different halogen atom; E is a methine group or a nitrogen atom; F is a vinylene group or an oxygen atom, ##STR3## wherein R.sup.6 is a lower alkoxy group; R.sup.7 is a lower alkyl group; R.sup.
    Type: Grant
    Filed: January 26, 1990
    Date of Patent: November 19, 1991
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Yukinori Ozato, Nobuhiko Tamura, Hiroaki Masumori, Michihiro Yamamoto, Atsuyuki Kojima, Fumio Nishikaku, Yoshihiko Kimura
  • Patent number: 5053504
    Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.
    Type: Grant
    Filed: November 29, 1989
    Date of Patent: October 1, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
  • Patent number: 5043443
    Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.
    Type: Grant
    Filed: July 24, 1990
    Date of Patent: August 27, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
  • Patent number: 4987146
    Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.
    Type: Grant
    Filed: July 14, 1989
    Date of Patent: January 22, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
  • Patent number: 4948802
    Abstract: New guanidine carboxylic acid esters corresponding to the general formula I ##STR1## and a process for the preparation of these compounds are described. The compounds according to the invention are H.sub.2 -agonists optionally having an additional H.sub.1 -antagonistic component. They are distinguished by their improved oral activity. The use of the above-mentioned guanidine carboxylic acid esters and of pharmaceutical preparations containing these esters is also described.
    Type: Grant
    Filed: April 11, 1988
    Date of Patent: August 14, 1990
    Assignee: Heumann Pharma GmbH & Co.
    Inventors: Peter Morsdorf, Helmut Schickaneder, Volker Pfahlert, Heidrun Engler, Armin Buschauer, Walter Schunack
  • Patent number: 4933454
    Abstract: The invention concernes acylureidoaminothiazolyl derivatives possessing pharmacological activity and a method for preparing them.2-aminothiazolyl derivatives having an allyl radical with 1-4 carbon atoms are known in the pharmaceutical practice as immunomodulators, active against immune failure diseases.The aim of the invention is to synthesize new 2-aminothiazolyl derivatives possessing pharmacological activity and describe a new method for their preparation.
    Type: Grant
    Filed: April 20, 1989
    Date of Patent: June 12, 1990
    Assignee: Technologitchen Kombinat za Promishlena Mikrobologia
    Inventors: Tashka K. Atanassova, Anton I. Nakov, Lyudmila V. Petkova, Zoya T. Ivanova, Donka M. Mondeshka
  • Patent number: 4923886
    Abstract: Nitric acid esters of Thiazole carboxamides exhibiting vasodilating activities have been prepared.
    Type: Grant
    Filed: June 30, 1988
    Date of Patent: May 8, 1990
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka
  • Patent number: 4923998
    Abstract: 7-substituted 3-cephem or cepham compounds characterized by the grouping, in the 7-position thereof, of the formula:R'--A--CONH--where R' is thiadiazolyl or amino thiazolyl, and A is methylene carrying oxyiimino, or R' is haloacetyl and A may also be methylene, their preparation, and pharmaceutical uses.
    Type: Grant
    Filed: October 19, 1983
    Date of Patent: May 8, 1990
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Kiyoshi Tsuji, Toshiyuki Chiba
  • Patent number: 4914112
    Abstract: A compound of the formula: ##STR1## wherein A is the group of the formula:Ar.sup.1 --D--Ar.sup.2 --wherein Ar.sup.1 is a phenyl or thienyl group which may be optionally substituted with at least one of the same or different halogen atom; Ar.sup.2 is a phenylene or thienylene group which may be optionally substituted with at least one of the same or different halogen atom; D is a divalent radical selected from the group consisting of >C.dbd.N--OR.sup.4 [wherein R.sup.4 is a hydrogen atom or lower alkyl group], >C.dbd.O, ##STR2## >CHOH, >NH radical, or single bond, ##STR3## wherein R.sup.5 is a lower alkoxy or a phenyl group which may be optionally substituted with at least one of the same or different halogen atom; E is a methine group or a nitrogen atom; F is a vinylene group or an oxygen atom, ##STR4## wherein R.sup.6 is a lower alkoxy group; R.sup.7 is a lower alkyl group; R.sup.
    Type: Grant
    Filed: May 28, 1987
    Date of Patent: April 3, 1990
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Yukinori Ozato, Nobuhiko Tamura, Hiroaki Masumori, Michihiro Yamamoto, Atsuyuki Kojima, Fumio Nishikaku, Yoshihiko Kimura
  • Patent number: 4914097
    Abstract: Disclosed herein is an N-indanyl carboxamide derivative as a novel compound, represented by the following general formula (I): ##STR1## wherein A represents a group of the formula, ##STR2## (wherein X represents a halogen atom, a methyl group, or a trifluoromethyl group, Y represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group, a mercapto group, or a lower alkylthio group, R.sup.1 represents a methyl group or a trifluoromethyl group, and R.sup.2 and R.sup.3 independently represents a hydrogen atom or a methyl group), R represents a lower alkyl group, and n is an integer in the range of 1 to 6, and an agricultural/horticultural fungicide comprising said N-indanyl carboxamide derivative as an active ingredient.
    Type: Grant
    Filed: February 23, 1988
    Date of Patent: April 3, 1990
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Masatsugu Oda, Toshiro Sakaki, Naoko Sasaki, Hirofumi Tomita, Nobuyuki Nonaka
  • Patent number: 4904660
    Abstract: Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.
    Type: Grant
    Filed: February 25, 1988
    Date of Patent: February 27, 1990
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
  • Patent number: 4889953
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: December 26, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
  • Patent number: 4867780
    Abstract: Herbicidal compounds have the formula ##STR1## in which W is oxygen or sulfur; X is hydrogen, halogen, nitro, cyano, perhalomethyl, difluoromethyl, pentafluoroethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethylthio, difluoromethoxy, trifluoromethoxy, tetrafluoroethoxy, methylsulfonyl, trifluoromethylsulfonyl, phenoxy, pyridyloxy, halo-substituted-phenoxy or -pyridyloxy, trifluoromethyl-substituted-phenoxy or -pyridyloxy, C.sub.1 -C.sub.4 alkyloximinomethyl, benzyloximinomethyl, 1-(C.sub.1 -C.sub.4 alkyl)-oximinoethyl and 1-benzyloximinoethyl; Y is hydrogen, halogen, nitro, cyano, perhalomethyl, difluoromethyl, pentafluoroethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethylthio, trifluoromethoxy, tetrafluoroethoxy, methylsulfonyl and trifluoromethylsulfonyl; Z is hydrogen or fluoro if Y is hydrogen, or hydrogen if Y is other than hydrogen; R.sub.1 is hydrogen, methyl, ethyl or chloromethyl; A is oxygen, sulfur, ##STR2## in which R.sub.3 and R.sub.
    Type: Grant
    Filed: July 1, 1988
    Date of Patent: September 19, 1989
    Assignee: ICI Americas, Inc.
    Inventor: Frank X. Woolard
  • Patent number: 4863947
    Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.
    Type: Grant
    Filed: August 11, 1986
    Date of Patent: September 5, 1989
    Assignee: Rohm and Haas
    Inventor: Richard M. Jacobson
  • Patent number: 4851422
    Abstract: The compound represented by the formula: ##STR1## where R.sup.1 stands for amino or an organic residue bonded through nitrogen; R.sup.2 stands for carboxyl or a group derivable therefrom; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently stand for hydrogen or an organic residue, including the case where R.sup.5 or R.sup.6 forms a chemical bond or a ring with R.sup.7 or R.sup.8 ; X stands for hydrogen, methoxy or formylamino; or a salt thereof, produceable by the present method, exhibits excellent antimicrobial activity, and is utilized as antimicrobial agents.
    Type: Grant
    Filed: April 30, 1986
    Date of Patent: July 25, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Yasuhiko Kawano, Akira Morimoto, Kouichi Yoshioka
  • Patent number: 4826861
    Abstract: This invention relates to 2-aminothiazoles and to their process of manufacture. These compounds are endowed with potent antimicrobial and antifungic properties. They are useful in antibacterial and antifungal therapy.
    Type: Grant
    Filed: January 7, 1987
    Date of Patent: May 2, 1989
    Assignee: Albert Roland, S.A.
    Inventors: Moinet Gerard, Schaefer Michel
  • Patent number: 4798838
    Abstract: The present invention relates to novel phenoxy derivatives represented by the formula (I): ##STR1## wherein: A is an imidazolyl group, a pyridyl group, a pyridyloxy group, an oxo-substituted chromenyloxy group, a lower alkyl group, an amino group which may be substituted with a phenyl group or a lower alkyl group, or a carbamoyl group substituted with a cyclohexylamino group or an imidazolylalkyl group;B is a single bond, a thiazolyl group which may be substituted with a lower alkyl group, a group represented by the formula: --(CH.sub.2).sub.n --O--, --(CH.sub.2).sub.n CONH(CH.sub.2).sub.k -- or --(CH.sub.2).sub.n --N(R.sup.4)-- wherein k is 0 or an integer of 1 to 5, n is an integer of 1 to 6 and R.sup.4 is hydrogen or a lower alkyl group;m is 0 or an integer of 1 to 6;R.sup.1 is a hydroxyl group, an amino group or a lower alkoxy group;R.sup.2 and R.sup.3 which may be the same or different, represent a hydrogen atom or a lower alkyl group hereafter the same:and salts thereof.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: January 17, 1989
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Tadao Kojima, Shunji Kageyama, Minoru Okada, Isao Ohata, Noboru Sato
  • Patent number: 4742060
    Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: May 3, 1988
    Assignee: Nihon Tokushu Noyaku Seizo K. K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
  • Patent number: 4667040
    Abstract: This invention relates to a novel process for producing a 2-(2-aminothiazol-4-yl)glyoxylic acid derivative or a salt thereof which are useful in producing a cephalosporin antibiotic, and to intermediates for said derivative and salt and a process for producing the intermediates.
    Type: Grant
    Filed: July 9, 1985
    Date of Patent: May 19, 1987
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hiroshi Sadaki, Hiroyuki Imaizumi, Kenji Takeda, Takihiro Inaba, Ryuko Takeno, Seishi Morita, Tetsuya Kajita, Isamu Saikawa
  • Patent number: 4663341
    Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: May 5, 1987
    Assignee: Rohm and Haas Company
    Inventor: Richard M. Jacobson
  • Patent number: 4647557
    Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.
    Type: Grant
    Filed: December 23, 1983
    Date of Patent: March 3, 1987
    Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
  • Patent number: 4637902
    Abstract: A base precursor represented by the following general formula (A) or (B): ##STR1## wherein A.sub.1, A.sub.2, A.sub.5, A.sub.6, A.sub.7, and A.sub.8 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, a substituted aryl group, an acyl group, or a heterocyclic group, and A.sub.1 and A.sub.2 can combine to form a ring and two of A.sub.5, A.sub.6, A.sub.7, and A.sub.8 can combine to form a ring, A.sub.3 and A.sub.4 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, or an aralkyl group, and A.sub.3 and A.sub.4 can combine to form a ring or A.sub.3 and A.sub.4 can be a double bond forming an imino group from ##STR2## and X represents a nucleophilic group.
    Type: Grant
    Filed: March 14, 1984
    Date of Patent: January 20, 1987
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hiroyuki Hirai, Ken Kawata
  • Patent number: 4629734
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sub.1 -R.sub.6 are as defined in the specification;X is oxygen or sulphur; and the R.sub.6 NCXR.sub.5 and OCOH moieties are trans and, when one or the other of R.sub.1 and R.sub.2 is an amino group, pharmaceutically acceptable salts thereof, a process and intermediates for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.
    Type: Grant
    Filed: May 16, 1984
    Date of Patent: December 16, 1986
    Assignee: Beecham Group p.l.c.
    Inventor: Valerie A. Ashwood
  • Patent number: 4616025
    Abstract: New thiazolidine compounds of the formula (I) having anti-ulcer activity are disclosed: ##STR1## wherein Ar is a 2-furyl or a phenyl, naphthyl or pyridyl group optionally substituted by one or more C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, dihalomethyl, trihalomethyl, hydroxyl or nitro groups or by a group of the formula (II), ##STR2## wherein Y is nitrogen or CH;Z is cyano or carbamoyl if Y is nitrogen, and represents a nitro group if Y is CH.Also disclosed are several processes for preparing the new compounds as well as pharmaceutical compositions and method of treatment employing same.
    Type: Grant
    Filed: March 16, 1984
    Date of Patent: October 7, 1986
    Assignee: Richter Gedeon Vegyeszeti Gyar RT
    Inventors: Elemer Ezer, Kalman Harsanyi, Gyorgy Domany, Laszlo Szporny, Judit Matuz, Bela Hegedus, Katalin Pallagi, Istvan Szabadkai, Peter Tetenyi
  • Patent number: 4599426
    Abstract: The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5 or --HNCO--R.sup.5,R.sup.5 is aryl or heterocyclic, either of which may be substituted, andA is lower alkylene, or a salt thereof.
    Type: Grant
    Filed: September 13, 1983
    Date of Patent: July 8, 1986
    Assignee: Fujisawa Pharmaceutical Co.
    Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
  • Patent number: 4511574
    Abstract: The present invention provides new chemical compounds, N-(4-phenyl-2-thiazolyl)carbamate derivatives, a process for preparing the same and pharmaceutical compositions containing the carbamate derivatives. More particularly, the present invention provides N-(4-phenyl-2-thiazolyl)carbamate derivatives which have immuno-modulating activity and are thus effective against immunodiseases such as chronic rheumatoid arthritis and also useful against viral diseases or for the immunotherapy of cancers with low toxicity.
    Type: Grant
    Filed: September 8, 1982
    Date of Patent: April 16, 1985
    Assignee: Mitsui Toatsu Kagaku Kabushiki Kaisha
    Inventors: Isao Sakano, Tatsuro Yokoyama, Seitaro Kajiya, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Takuo Nakano, Akira Awaya
  • Patent number: 4500716
    Abstract: Highly active substantially pure Z-isomers of cephalosporins are produced by the following synthesis: ##STR1## in which R.sup.1, R.sup.4 and R.sup.5 ae various organic radicals,R.sup.2 is alkoxycarbonyl,Y is Cl, Br or --O--SO.sub.2 --R.sup.5, andX is a conventional cephalosporin substituent.Many of the intermediates are new, especially in pure Z-form.
    Type: Grant
    Filed: November 1, 1982
    Date of Patent: February 19, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventor: Gunther Kinast
  • Patent number: 4490393
    Abstract: The present invention provides thiazolyl derivatives as new chemical substance represented by the general formula: ##STR1## wherein R.sup.1 stands for a lower alkyl group or a substituted or unsubstituted phenyl group, R.sup.2 for a hydrogen atom, a lower alkyl, lower alkoxy or lower alkylthio group, and R.sup.3 for a pyridyl or iso-oxazolyl group or a grouping of the general formula: ##STR2## processes for preparing same and pharmaceutical compositions containing the thiazolyl derivatives. More particularly, the present invention provides new thiazolyl derivatives which possess immuno-modulating activity and are thus therapeutically effective against immunodiseases such as chronic rheumatoid arthritis and also useful against viral diseases or for the immunotherapy of cancers and possess properties desirous as medicines with a slight toxicity, processes for preparing same and pharmaceutical compositions containing the new substance.
    Type: Grant
    Filed: September 17, 1982
    Date of Patent: December 25, 1984
    Assignee: Mitsui Toatsu Kagaki Kabushiki Kaisha
    Inventors: Isao Sakano, Tatsuro Yokoyama, Seitaro Kajiya, Tamotsu Minami, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Takuo Nakano, Akira Awaya
  • Patent number: 4487937
    Abstract: Novel syn isomers of 7-amino-thiazolyl-acetamido-3-acetoxymethyl-cephalosporanic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --CONH.sub.2 and --COOR.sub.1 ', R.sub.1 ' is selected from the group consisting of alkyl of 1 to 3 carbon atoms, hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, R' and R" are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms with the ##STR2## group in the syn position with the proviso that when R.sub.1 is --COOR.sub.1 ' and R.sub.1 ' is hydrogen, A is hydrogen and when R.sub.1 is --COOR.sub.1 ' and R.sub.
    Type: Grant
    Filed: February 25, 1983
    Date of Patent: December 11, 1984
    Assignee: Roussel Uclaf
    Inventor: Ren/e/ Heymes
  • Patent number: 4479947
    Abstract: The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.
    Type: Grant
    Filed: June 7, 1982
    Date of Patent: October 30, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Burton G. Christensen
  • Patent number: 4473577
    Abstract: Disclosed are 2-thiazol derivatives having the general formula ##STR1## where R.sub.1 and R.sub.2 independently represent lower alkyl radicals having 1 to 4 carbon atoms and X represents a lower alkyl radical, a lower alkoxy radical, a lower alkoxycarbonyl radical, a halogenoalkoxy radical, a radical of the formula ##STR2## or a radical of the formula ##STR3## Also disclosed are a process for preparing the derivatives and pharmaceutical compositions having immunomodulatory activity which comprise the derivatives as the active ingredient.
    Type: Grant
    Filed: October 22, 1982
    Date of Patent: September 25, 1984
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Isao Sakano, Tatsuro Yokoyama, Kajiya Seitaro, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Takuo Nakano, Akira Awaya
  • Patent number: 4458077
    Abstract: Compounds of the formulaAr--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --ONHRwherein R is ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;X is O or CH.sub.2 ;m=0 or 1;n=2 or 3; andAr is a moiety selected from the group ##STR2## wherein R.sub.2 is hydrogen or lower alkyl, ##STR3## with the proviso that when Ar is ##STR4## and X is CH.sub.2, then R is other than ##STR5## and the pharmacologically acceptable salts thereof have H.sub.2 -antagonist activity and activity in decreasing gastric acid secretions.
    Type: Grant
    Filed: November 22, 1982
    Date of Patent: July 3, 1984
    Assignee: American Home Products Corporation
    Inventor: John R. Potoski
  • Patent number: 4427687
    Abstract: Carbamoyl-oxime compound of the formula ##STR1## wherein A, R.sup.3, R.sup.4 and R.sup.5 are as hereinafter set forth, a process for their preparation, pesticidal compositions containing one or more of these compounds as the active ingredient, methods of use of such compositions for the control of pests, particularly insects, mites, nematodes and molluscs, and intermediates for the production of such compounds are described.
    Type: Grant
    Filed: April 24, 1981
    Date of Patent: January 24, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph Luthy, Paul Winternitz
  • Patent number: 4426519
    Abstract: Novel syn isomers of 7-(2-amino-4-thiazolyl)-acetamido-cephalosporanic acid compounds of the formula ##STR1## wherein R is selected from the group consisting of --(CH.sub.2).sub.n --S--R.sub.2, --CHF.sub.2 and --(CH.sub.2).sub.n --S--CN, R.sub.2 is selected from the group consisting of optionally protonated ##STR2## n is an integer from 1 to 4, R.sub.1 is selected from the group consisting of hydrogen, chlorine, methoxy, alkyl and alkylthio of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms, azidomethyl, acetoxymethyl, carbamoyloxymethyl, ##STR3## and --CH.sub.2 --S--R', Alk is alkyl of 1 to 4 carbon atoms, R' is selected from the group consisting of an optionally substituted nitrogen containing heterocycle and an acyl of an aliphatic acid of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen and an easily cleavable ester and when R is --(CH.sub.2).sub.n --SR.sub.2, the COOA group may be the anion --COO-- and when R is --(CH.sub.2).sub.n --SCN or --CHF.sub.
    Type: Grant
    Filed: January 27, 1982
    Date of Patent: January 17, 1984
    Assignee: Roussel Uclaf
    Inventors: Michel Vignau, Rene Heymes
  • Patent number: 4419363
    Abstract: Novel 1-aryloxy-3-amidoamidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. Representative of the compounds disclosed is 1-(o-cyanophenoxy)-3-.beta.-(2-thenamidoacetamido)ethylaminopropan-2-ol.
    Type: Grant
    Filed: June 4, 1982
    Date of Patent: December 6, 1983
    Assignee: Imperial Chemical Industries PLC
    Inventor: Leslie H. Smith
  • Patent number: 4395544
    Abstract: The present invention relates to compounds obtained by condensing a compound of formula I, ##STR1## or a salt thereof, in which R is a primary, secondary or tertiary amino group,with a Vilsmeier reagent,and derivatives of such aldehydes.
    Type: Grant
    Filed: May 15, 1981
    Date of Patent: July 26, 1983
    Assignee: Sandoz Ltd.
    Inventor: Robert Egli
  • Patent number: 4386211
    Abstract: The invention relates to certain urea derivatives of the formula R.sub.1 CH.sub.2 S(CH.sub.2).sub.2 NHCONHR.sub.2 where R.sub.1 are certain furanyls, imidazoles and thiazolyls and R.sub.2 are certain imidazoles and thiazolyls. These compounds are H-2 histamine receptor inhibitors and therefore useful in the treatment of ulcers.
    Type: Grant
    Filed: August 25, 1981
    Date of Patent: May 31, 1983
    Assignee: G. D. Searle & Co.
    Inventors: Richard E. L. Henderson, Barnett S. Pitzele
  • Patent number: RE33125
    Type: Grant
    Filed: July 11, 1986
    Date of Patent: December 5, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas