The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
  • Patent number: 5059620
    Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: October 22, 1991
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • 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: 5030724
    Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof. R.sub.3 and R.sub.4 are the same or different and each is hydrogen or alkyl or R.sub.3 and R.sub.4 taken together with the nitrogen atoms to which they are attached form a 1,2-diazacyclobutane, 1,2-diazacyclopentane, 1,2-diazacyclohexane, or 1,2-diazacycloheptane ring.Y.sub.1 and Y.sub.2 are either hydrogen or OR.sub.11 but are not the same.R.sub.11 is hydrogen, alkanoyl of from one to ten carbon atoms, substituted alkanoyl of from two to ten carbon atoms, phenylcarbonyl, (substituted phenyl) carbonyl, heteroarylcarbonyl, phenylalkanoyl, (substituted phenyl) alkanoyl, or heteroarylalkanoyl.
    Type: Grant
    Filed: January 22, 1990
    Date of Patent: July 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joseph E. Sundeen, Robert Zahler, Stefan Jendrzejewski
  • Patent number: 5026710
    Abstract: Novel fungicidally active compounds of the formula ##STR1## in which R represents alkyl, cyanoalkyl or in each case optionally substituted alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl or phenylalkyl,R.sup.1 represents the --OR.sup.2 or --NR.sup.3 R.sup.4 groups, andR.sup.3 and R.sup.4 have special definitions.
    Type: Grant
    Filed: July 10, 1990
    Date of Patent: June 25, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Winfried Lunkenheimer, Wilhelm Brandes, Gerd Hassler
  • Patent number: 5017721
    Abstract: A new process for preparing oxalyl- and oxamyl-hydrazides which comprises contacting oxamide or diacetyloxamide with the corresponding hydrazine derivative of formulaR.sub.1 R.sub.2 N--NHR.sub.3wherein R.sub.1 represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, aryl, or aryl-alkyl group, R.sub.2 is a hydrogen atom or an optionally substituted alkyl group, or R.sub.1 and R.sub.2 taken together with the adjacent nitrogen atom represent a saturated heterocyclic ring, and R.sub.3 is a hydrogen atom or an optionally substituted alkyl group.
    Type: Grant
    Filed: April 21, 1989
    Date of Patent: May 21, 1991
    Assignee: Enichim ANIC S.p.A.
    Inventors: Giuseppe Messina, Loreno Lorenzoni, Paolo Calaresu, Giovanni M. Sechi
  • Patent number: 4996318
    Abstract: The amino-9,10-secosteroids ##STR1## of the present invention contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: February 26, 1991
    Assignee: The Upjohn Company
    Inventors: Martin Gall, Robert I. Higuchi
  • Patent number: 4996218
    Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.
    Type: Grant
    Filed: August 10, 1988
    Date of Patent: February 26, 1991
    Assignee: Glaxo Group Limited
    Inventor: Lawrence H. C. Lunts
  • 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: 4983619
    Abstract: Compounds of the following formula have pharmaceutical properties: ##STR1## in which X is R'(HO)C.dbd.C(CN)--, R.sup.1 (CO)--CH(CN)-- or ##STR2## R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-6 alkyl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halo-substituted C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkylthio, C.sub.2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R'R"N-- where R' and R" are each hydrogen or C.sub.1-4 alkyl or R'"CONH-- where R'" is C.sub.1-4 alkyl, or a group of the formula --CR.sup.7 R.sup.8 R.sup.9 in which R.sup.7, R.sup.8 and R.sup.9 are each C.sub.1-6 alkyl, halo-substituted C.sub.1-6 alkyl or optionally substituted phenyl, or R.sup.7 and R.sup.8, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R.sup.7, R.sup.8 and R.sup.
    Type: Grant
    Filed: January 11, 1990
    Date of Patent: January 8, 1991
    Assignee: Lilly Industries Limited
    Inventors: Peter T. Gallagher, Terence A. Hicks
  • Patent number: 4963548
    Abstract: Novel fungicidally active compounds of the formula ##STR1## in which R represents alkyl, cyanoalkyl or in each case optionally substituted alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl or phenylalkyl,R.sup.1 represents the --OR.sup.2 or --NR.sup.3 R.sup.4 groups, andR.sup.3 and R.sup.4 have special special definitions.
    Type: Grant
    Filed: May 27, 1988
    Date of Patent: October 16, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Winfried Lunkenheimer, Wilhelm Brandes, Gerd Hanssler
  • Patent number: 4962117
    Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, antiallergic, anti-inflammatory, and cytoprotective agents.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: October 9, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Joseph G. Atkinson
  • Patent number: 4956375
    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: November 29, 1989
    Date of Patent: September 11, 1990
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Masatsugu Oda, Toshiro Sakaki, Naoko Sasaki, Hirofumi Tomita, Nobuyuki Nonaka
  • Patent number: 4954518
    Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.
    Type: Grant
    Filed: October 7, 1988
    Date of Patent: September 4, 1990
    Assignee: Toyama Chemical Company, Ltd.
    Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
  • Patent number: 4948891
    Abstract: Compounds of the formula ##STR1## where Het is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors useful as anti-plasmin and anti-thrombin agents.
    Type: Grant
    Filed: August 9, 1989
    Date of Patent: August 14, 1990
    Assignee: Pfizer Inc.
    Inventors: Rodney C. Schnur, Anton F. J. Fliri
  • Patent number: 4946855
    Abstract: A compound of the formula: ##STR1## wherein the free valency of the groups A-, R- and --X--Y-- is attached to any of 2-, 4- and 5- positions of the thiazol ring, A is a C.sub.1-6 alkyl group, an aryl group which is unsubstituted or substituted with at least one substituent selected from the group consisting of hydroxy C.sub.1-6 alkoxy, aryl-(C.sub.1-6)alkoxy, halo-(C.sub.1-6)alkyl, halogen, and nitro,or 5- or 6-membered heterocyclic group containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus, these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from halogen,R is hydrogen or a C.sub.
    Type: Grant
    Filed: November 28, 1988
    Date of Patent: August 7, 1990
    Assignee: Sawai Pharmaceutical Co., Ltd.
    Inventors: Junji Yoshinaga, Takeshi Shogaki, Takao Kakita, Hiromi Ozeki, Yoshiko Kato
  • Patent number: 4942242
    Abstract: Thiazolyl phenoxy derivatives are provided as well as pharmaceutical compositions containing such derivatives. The compositions are useful for lowering lipid activity in a subject and accordingly useful for reducing cholesterol and triglycerides.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: July 17, 1990
    Inventors: Tadao Kojima, Shunji Kageyama, Minoru Okada, Isao Ohata, Noboru Sato
  • 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: 4925948
    Abstract: Compounds of the formula ##STR1## wherein r.sup.1 is amino or protected amino R.sup.2 is cycloalkenyl X is halogen and Y is carboxy or protected carboxy, or salts useful as intermediates for cephalosporin antibiotics.
    Type: Grant
    Filed: March 28, 1986
    Date of Patent: May 15, 1990
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Masayoshi Murata, Akiteru Yoshioka
  • 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: 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: 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: 4912224
    Abstract: An antibacterial 7beta-(carboxyalkenoyl)amino-3-cephem-4-carboxylic acid represented by the following formula: ##STR1## (wherein R is aryl or a heterocyclic group;R.sup.1 is hydrogen or halogen;R.sup.2 is a single bond, alkylene, or thiaalkylene;R.sup.3 is a hydrogen atom or carboxy modifying group;R.sup.4 is hydrogen or methoxy;R.sup.5 is hydrogen or a 3-substituent of cephalosporins;R.sup.6 is a hydrogen atom or carboxy modifying group; andX is oxygen, sulfur, or sulfinyl)a pharmaceutical composition containing the same, and a method for treating a bacterial infection with the same.
    Type: Grant
    Filed: December 9, 1987
    Date of Patent: March 27, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventor: Yoshio Hamashima
  • Patent number: 4910313
    Abstract: The present invention is related to new diselenobis benzoic acid amides of primary heterocyclic amines of the general formula I ##STR1## process for producing the same and process for treating certain diseases in human beings by administration of the same to the humans suffering from such diseases.
    Type: Grant
    Filed: August 6, 1987
    Date of Patent: March 20, 1990
    Assignee: Nattermann & CIE GmbH
    Inventors: Andre Welter, Axel Roemer, Sigurd Leyck, Michael J. Parnham
  • Patent number: 4904791
    Abstract: The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus.
    Type: Grant
    Filed: March 28, 1988
    Date of Patent: February 27, 1990
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Haruo Ohnishi, Hiroshi Kosuzume, Masahiro Mizota, Yasuo Suzuki, Ei Mochida
  • 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: 4902688
    Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1 and R.sub.2 have the meanings reported in the specification) and their preparation are described.The compounds of formula I have anti-allergic, anti-anaphylactic and anti-arthritic activity and are useful in pharmaceutical field.Compositions for pharmaceutical use containing a compound of formula I as active ingredient are described too.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: February 20, 1990
    Assignee: Zambon Group S.p.A.
    Inventors: Dario Chiarino, Gian Carlo Grancini, Viviana Frigeni, Angelo Carenzi
  • Patent number: 4886833
    Abstract: Novel fungicides of the formula ##STR1## in which R.sup.1 represents optionally substituted hydroxyalkyl, optionally substituted hydroxyalkoxyalkyl, optionally substituted heteroarylalkyl or optionally substituted heteroaryl, andR.sup.2 represents optionally substituted alkyl, optionally substituted alkenyl, or alkinyl.Intermediate therefor, wherein R.sup.2 is hydrogen or an alkali metal cation, are also new.
    Type: Grant
    Filed: August 24, 1987
    Date of Patent: December 12, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Klaus Jelich, Winfried Lunkenheimer, Wilhelm Brandes, Gerd Hanssler
  • Patent number: 4876261
    Abstract: A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower, alkyl or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt thereof.
    Type: Grant
    Filed: March 25, 1988
    Date of Patent: October 24, 1989
    Inventors: Akihiro Tanaka, Takashi Fujikura, Ryuji Tsuzuki, Masaki Yokota, Takeyuki Yatsu
  • Patent number: 4874864
    Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.
    Type: Grant
    Filed: May 24, 1988
    Date of Patent: October 17, 1989
    Assignee: Pfizer Inc.
    Inventors: Rodney C. Schnur, Anton F. J. Fliri
  • Patent number: 4873253
    Abstract: A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;Y represents ##STR4## or --OR.sup.3 wherein R.sup.1 R.sup.2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C.sub.1 -C.sub.4 alkylcarbonyl, (iii) C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or hydroxycarbonyl, (iv) C.sub.2 -C.sub.5 alkenyl which may be further substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (v) C.sub.1 -C.sub.
    Type: Grant
    Filed: March 30, 1987
    Date of Patent: October 10, 1989
    Assignees: Shosuke Okamoto, Showa Denko Kabushiki Kaisha
    Inventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Hiroshi Nojima, Takashi Shishikura
  • Patent number: 4871860
    Abstract: Intermediates for cephalosporins have been synthesized.
    Type: Grant
    Filed: May 31, 1984
    Date of Patent: October 3, 1989
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • 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: 4845105
    Abstract: A compound selected from the group consisting of optical isomers and racemates of 4-hydroxy-3-quinoline carboxylates of the formula ##STR1## wherein X is in the 5-, 6-, 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --SCF.sub.3 and --OCF.sub.3, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl and phenyl substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, A is either ##STR2## in which R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.
    Type: Grant
    Filed: March 24, 1987
    Date of Patent: July 4, 1989
    Assignee: Roussel Uclaf
    Inventors: Fran ois Clemence, Odile Le Martret, Fran oise Delevallee
  • Patent number: 4841062
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 is cyclo(lower)alkyl or lower alkynyl having 2 to 6 carbon atoms, andR.sup.6 is amino or protected amino, or the reactive derivative at the carboxy group, are disclosed as intermediates for the preparation of cephem and cepham compounds having antimicrobial activity.
    Type: Grant
    Filed: February 11, 1988
    Date of Patent: June 20, 1989
    Assignee: Fujisawa Pharmaceutical Company, Limited
    Inventors: Takao Takaya, Hisashi Takasugi, Kiyoshi Tsuji, Toshiyuki Chiba
  • 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: 4822888
    Abstract: A compound of the formula: ##STR1## wherein R.sup.2 is halo(lower)alkyl, andR.sup.6 is amino or protected amino, its reactive derivative at the carboxy group or its lower alkyl ester, is disclosed, having utility as an intermediate for producing cephems or cephams.
    Type: Grant
    Filed: February 19, 1986
    Date of Patent: April 18, 1989
    Assignee: Fujisawa Pharmaceutical Company, Limited
    Inventors: Takao Takaya, Hisashi Takasugi, Kiyosha Tsuji, Toshiyuki Chiba
  • Patent number: 4808210
    Abstract: A 5-pyrazolone of the formula ##STR1## wherein R is selected from the group consisting of mono- and polycyclic aromatic of 6 to 14 carbon atoms, heterocyclic optionally substituted with phenyl, ##STR2## and benzyl, all optionally substituted with at least one member of the group consisting of fluorine, chlorine, bromine, --CF.sub.3, optionally unsaturated alkyl of 1 to 8 carbon atoms and the radical OZ in which Z is an optionally unsaturated alkyl of 1 to 8 carbon atoms or an acyl of a carboxylic acid of 1 to 6 carbon atoms, A is selected from the group consisting of halogen, --CF.sub.3 and --CN, B and C are individually selected from the group consisting of hydrogen, halogen, --OH, --OR' and R' is optionally unsaturated alkyl of 1 to 8 carbon atoms, acyl of 1 to 6 carbon atoms, alkyl sulfonyl of 1 to 8 carbon atoms, aryl sulfonyl of 6 to 18 carbon atoms and benzyl optionally substituted with a member of the group consisting of fluorine, chlorine, bromine, --CF.sub.
    Type: Grant
    Filed: September 11, 1987
    Date of Patent: February 28, 1989
    Assignee: Roussel Uclaf
    Inventors: Jean Tessier, Pierre Girault
  • Patent number: 4794186
    Abstract: Novel thiazolylacetic acid derivative of the formula: ##STR1## wherein R.sup.1.sub.N H-- is amino or a protected amino group, R.sup.2 is hydrogen or lower alkyl, --COOR.sup.3 is carboxy or a protected carboxy group and n is an integer of 2 or 3, and processes for preparing the same. The compound (I) is useful as an intermediate in the synthesis of cephalosporins.
    Type: Grant
    Filed: December 13, 1984
    Date of Patent: December 27, 1988
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Toyonari Oine, Yoshihisa Yamada, Hiroshi Sugano
  • Patent number: 4791200
    Abstract: The present invention relates to novel 2-substituted-4-aryloxyalkylamine thiazoles as described herein. The thiazoles are useful as antisecretory agents.
    Type: Grant
    Filed: June 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, Maud Urbanski
  • Patent number: 4782158
    Abstract: The present invention involves certain thiazol-4-yl-acetic acid compounds which are valuable intermediates for the preparation of cephem antibiotics. Said intermediates have the following structure: ##STR1## wherein R.sup.1 is an amino or a protected amino group; R.sup.2 is a group of the formula 13 CONH--R.sup.5 or --NHCO--R.sup.5 wherein R.sup.5 is pyridyl, thiazolyl or an isoxazolyl ring having lower alkyl and halogen substituted phenyl substituents, and A is lower alkylene, or a non-toxic salt thereof.
    Type: Grant
    Filed: July 8, 1986
    Date of Patent: November 1, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
  • Patent number: 4782162
    Abstract: The new compounds of the formula ##STR1## in which Acyl is alkylcarbonyl optionally substituted by halogen or aryl, or arylcarbonyl, which is substituted by lower alkoxy, halogen or nitro,R.sup.1 is an alkyl or alkenyl radical, andR.sup.4 is an optionally substituted branched or straight-chain C.sub.1 -C.sub.6 -alkyl radical or a cycloalkyl radical,are produced by reacting a 2-halogenoacetylacrylic acid ester of the formula ##STR2## with an acylthiourea of the formula ##STR3## The reaction can be conducted in aqueous DMF, substantially pure Z-isomer selectively crystallizing out.
    Type: Grant
    Filed: June 9, 1986
    Date of Patent: November 1, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Boberg, Paul Naab, Samir Samaan
  • Patent number: 4782083
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: August 29, 1986
    Date of Patent: November 1, 1988
    Assignee: Beecham Group P.L.C.
    Inventors: Frederick Cassidy, Geoffrey Stemp, John M. Evans
  • Patent number: 4769062
    Abstract: Thiazolylamides of the formula ##STR1## where R.sup.1 if hydrogen or alkyl, R.sup.2 is alkyl, alkenyl, alkynyl or cycloalkyl, R.sup.3 is hydrogen, alkyl or halogen, X is halogen, alkoxy, haloalkoxy, alkyl, haloalkyl, cycloalkyl, alkylthio, nitro, cyano, unsubstituted or substituted phenyl or unsubstituted or substituted phenoxy, and n is 1, 2, 3 or 4, processes for their preparation, and their use for controlling undesirable plant growth.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: September 6, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Arno Lange, Bruno Wuerzer, Norbert Meyer
  • Patent number: 4766137
    Abstract: 4-(isoxazolyl)-thiazole-2-oxamic acids, esters and salts thereof; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiallergic and antianaphylactic activity and may be used in the pharmaceutical field.Compositions for pharmaceutical use containing said compounds as the active ingredients are also described.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: August 23, 1988
    Assignee: Zambon S.p.A.
    Inventors: Angelo Carenzi, Dario Chiarino, Davide Della Bella, Giancarlo Grancini
  • Patent number: 4766138
    Abstract: Use of 4-(isoxazolyl)-thiazole-2-oxamic acid derivatives; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiarthritic activity; compositions for pharmaceutical use containing said compounds as the active ingredients are also described.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: August 23, 1988
    Assignee: Zambon S.p.A.
    Inventors: Angelo Carenzi, Dario Chiarino, Davide Della Bella, Giancarlo Grancini
  • Patent number: 4755523
    Abstract: Abietamide derivatives of the formula I ##STR1## wherein X is NZ wherein Z is hydrogen, alkyl, unsubstituted or substituted phenyl or X is a sulphur atom; when X is NZ, V is nitrogen, W is , and R is hydrogen or alkyl and when X is a sulphur atom, V is , W is nitrogen, and R is hydrogen, alkyl, phenyl or --CH.sub.2 COOR'; wherein R' is hydrogen or alkyl and is a single or double bond, are useful for treating hyperlipemia and particularly for the prevention and therapy of arteriosclerosis.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: July 5, 1988
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Yoshiaki Yoshikuni, Shoichi Chokai, Yukio Fujita, Takayuki Ozaki
  • 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: 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