Chalcogen Or Additional Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 548/196)
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Patent number: 5292715Abstract: 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: GrantFiled: August 28, 1992Date of Patent: March 8, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Ryo Sato, Tatsuhiro Hamada, Hideyuki Shibata
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Patent number: 5281614Abstract: Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists.Type: GrantFiled: November 2, 1992Date of Patent: January 25, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Prasun K. Chakravarty, Linda L. Chang, William J. Greenlee, Dooseop Kim, Nathan B. Mantlo, Arthur A. Patchett
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Patent number: 5270317Abstract: 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: GrantFiled: November 20, 1991Date of Patent: December 14, 1993Assignee: Elf SanofiInventors: Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
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Patent number: 5244863Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.Type: GrantFiled: October 1, 1991Date of Patent: September 14, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Tatsuhiro Hamada, Hideyuki Shibata, Ryo Sato
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Patent number: 5240918Abstract: 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: GrantFiled: March 24, 1992Date of Patent: August 31, 1993Assignee: EGIS GyogyszergyarInventors: Karoly Lempert, Gyula Hornyak, Jozsef Fetter, Antal Feller, Klara Gaso, Gabor Gigler, Laszlo Kapolnai, Lujza Petocz, Katalin Szemeredi, Marton Fekete
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Patent number: 5221685Abstract: 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: GrantFiled: January 30, 1992Date of Patent: June 22, 1993Assignee: Ube Industries, Ltd.Inventors: Tokio Obata, Katsutoshi Fujii, Yasuhisa Fukuda, Kiyoshi Tsutsumiuchi, Yoshinori Yamanaka
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Patent number: 5177095Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.Type: GrantFiled: August 13, 1991Date of Patent: January 5, 1993Assignee: 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
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Patent number: 5162360Abstract: 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: GrantFiled: June 24, 1991Date of Patent: November 10, 1992Assignee: Warner-Lambert CompanyInventors: Mark W. Creswell, Andrew D. White
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Patent number: 5099021Abstract: 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: GrantFiled: October 30, 1990Date of Patent: March 24, 1992Assignee: Agrolinz Agrarchemikalien Gesellschaft m.b.H.Inventors: Rudolf H. Worther, Horst Korntner, Egmont Auer, Kurt Thonhofer
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Patent number: 5086054Abstract: 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: GrantFiled: July 31, 1990Date of Patent: February 4, 1992Assignee: SRI InternationalInventor: Daniel W. Parish
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Patent number: 5084571Abstract: 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: GrantFiled: October 18, 1989Date of Patent: January 28, 1992Assignee: Fuji Photo Film Co., Ltd.Inventor: Yasuhiro Shimada
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Patent number: 5079369Abstract: 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: GrantFiled: June 23, 1989Date of Patent: January 7, 1992Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
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Patent number: 5066666Abstract: 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: GrantFiled: January 26, 1990Date of Patent: November 19, 1991Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Yukinori Ozato, Nobuhiko Tamura, Hiroaki Masumori, Michihiro Yamamoto, Atsuyuki Kojima, Fumio Nishikaku, Yoshihiko Kimura
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Patent number: 5053504Abstract: 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: GrantFiled: November 29, 1989Date of Patent: October 1, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
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Patent number: 5043443Abstract: 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: GrantFiled: July 24, 1990Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
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Patent number: 4987146Abstract: 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: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
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Patent number: 4948802Abstract: 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: GrantFiled: April 11, 1988Date of Patent: August 14, 1990Assignee: Heumann Pharma GmbH & Co.Inventors: Peter Morsdorf, Helmut Schickaneder, Volker Pfahlert, Heidrun Engler, Armin Buschauer, Walter Schunack
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Patent number: 4933454Abstract: 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: GrantFiled: April 20, 1989Date of Patent: June 12, 1990Assignee: Technologitchen Kombinat za Promishlena MikrobologiaInventors: Tashka K. Atanassova, Anton I. Nakov, Lyudmila V. Petkova, Zoya T. Ivanova, Donka M. Mondeshka
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Patent number: 4923886Abstract: Nitric acid esters of Thiazole carboxamides exhibiting vasodilating activities have been prepared.Type: GrantFiled: June 30, 1988Date of Patent: May 8, 1990Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka
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Patent number: 4923998Abstract: 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: GrantFiled: October 19, 1983Date of Patent: May 8, 1990Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Takao Takaya, Hisashi Takasugi, Kiyoshi Tsuji, Toshiyuki Chiba
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Patent number: 4914112Abstract: 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: GrantFiled: May 28, 1987Date of Patent: April 3, 1990Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Yukinori Ozato, Nobuhiko Tamura, Hiroaki Masumori, Michihiro Yamamoto, Atsuyuki Kojima, Fumio Nishikaku, Yoshihiko Kimura
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Patent number: 4914097Abstract: 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: GrantFiled: February 23, 1988Date of Patent: April 3, 1990Assignee: Mitsubishi Kasei CorporationInventors: Masatsugu Oda, Toshiro Sakaki, Naoko Sasaki, Hirofumi Tomita, Nobuyuki Nonaka
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Patent number: 4904660Abstract: 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: GrantFiled: February 25, 1988Date of Patent: February 27, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
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Patent number: 4889953Abstract: 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: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4867780Abstract: 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: GrantFiled: July 1, 1988Date of Patent: September 19, 1989Assignee: ICI Americas, Inc.Inventor: Frank X. Woolard
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Patent number: 4863947Abstract: 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: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
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Patent number: 4851422Abstract: 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: GrantFiled: April 30, 1986Date of Patent: July 25, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Yasuhiko Kawano, Akira Morimoto, Kouichi Yoshioka
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Patent number: 4826861Abstract: 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: GrantFiled: January 7, 1987Date of Patent: May 2, 1989Assignee: Albert Roland, S.A.Inventors: Moinet Gerard, Schaefer Michel
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Patent number: 4798838Abstract: 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: GrantFiled: September 30, 1986Date of Patent: January 17, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Tadao Kojima, Shunji Kageyama, Minoru Okada, Isao Ohata, Noboru Sato
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Patent number: 4742060Abstract: 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: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4667040Abstract: 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: GrantFiled: July 9, 1985Date of Patent: May 19, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Hiroshi Sadaki, Hiroyuki Imaizumi, Kenji Takeda, Takihiro Inaba, Ryuko Takeno, Seishi Morita, Tetsuya Kajita, Isamu Saikawa
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Patent number: 4663341Abstract: 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: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
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Patent number: 4647557Abstract: 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: GrantFiled: December 23, 1983Date of Patent: March 3, 1987Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
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Patent number: 4637902Abstract: 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: GrantFiled: March 14, 1984Date of Patent: January 20, 1987Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroyuki Hirai, Ken Kawata
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Patent number: 4629734Abstract: 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: GrantFiled: May 16, 1984Date of Patent: December 16, 1986Assignee: Beecham Group p.l.c.Inventor: Valerie A. Ashwood
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Patent number: 4616025Abstract: 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: GrantFiled: March 16, 1984Date of Patent: October 7, 1986Assignee: Richter Gedeon Vegyeszeti Gyar RTInventors: Elemer Ezer, Kalman Harsanyi, Gyorgy Domany, Laszlo Szporny, Judit Matuz, Bela Hegedus, Katalin Pallagi, Istvan Szabadkai, Peter Tetenyi
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Patent number: 4599426Abstract: 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: GrantFiled: September 13, 1983Date of Patent: July 8, 1986Assignee: Fujisawa Pharmaceutical Co.Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
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Patent number: 4511574Abstract: 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: GrantFiled: September 8, 1982Date of Patent: April 16, 1985Assignee: Mitsui Toatsu Kagaku Kabushiki KaishaInventors: Isao Sakano, Tatsuro Yokoyama, Seitaro Kajiya, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Takuo Nakano, Akira Awaya
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Patent number: 4500716Abstract: 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: GrantFiled: November 1, 1982Date of Patent: February 19, 1985Assignee: Bayer AktiengesellschaftInventor: Gunther Kinast
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Patent number: 4490393Abstract: 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: GrantFiled: September 17, 1982Date of Patent: December 25, 1984Assignee: Mitsui Toatsu Kagaki Kabushiki KaishaInventors: Isao Sakano, Tatsuro Yokoyama, Seitaro Kajiya, Tamotsu Minami, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Takuo Nakano, Akira Awaya
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Patent number: 4487937Abstract: 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: GrantFiled: February 25, 1983Date of Patent: December 11, 1984Assignee: Roussel UclafInventor: Ren/e/ Heymes
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Patent number: 4479947Abstract: 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: GrantFiled: June 7, 1982Date of Patent: October 30, 1984Assignee: Merck & Co., Inc.Inventor: Burton G. Christensen
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Patent number: 4473577Abstract: 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: GrantFiled: October 22, 1982Date of Patent: September 25, 1984Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Isao Sakano, Tatsuro Yokoyama, Kajiya Seitaro, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Takuo Nakano, Akira Awaya
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Patent number: 4458077Abstract: 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: GrantFiled: November 22, 1982Date of Patent: July 3, 1984Assignee: American Home Products CorporationInventor: John R. Potoski
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Patent number: 4427687Abstract: 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: GrantFiled: April 24, 1981Date of Patent: January 24, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Christoph Luthy, Paul Winternitz
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Patent number: 4426519Abstract: 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: GrantFiled: January 27, 1982Date of Patent: January 17, 1984Assignee: Roussel UclafInventors: Michel Vignau, Rene Heymes
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Patent number: 4419363Abstract: 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: GrantFiled: June 4, 1982Date of Patent: December 6, 1983Assignee: Imperial Chemical Industries PLCInventor: Leslie H. Smith
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Patent number: 4395544Abstract: 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: GrantFiled: May 15, 1981Date of Patent: July 26, 1983Assignee: Sandoz Ltd.Inventor: Robert Egli
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Patent number: 4386211Abstract: 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: GrantFiled: August 25, 1981Date of Patent: May 31, 1983Assignee: G. D. Searle & Co.Inventors: Richard E. L. Henderson, Barnett S. Pitzele
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas