The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
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Patent number: 5523315Abstract: Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is various oxygen-bearing radicals; for example, HO--CH(R.sup.3)CH.sub.2 wherein R.sup.3 is, inter alia, hydrogen, lower alkyl, lower cycloalkyl or phenyl; or HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein each of R.sup.5 and R.sup.6 is lower alkyl, or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, cyclo-alkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.Type: GrantFiled: September 20, 1993Date of Patent: June 4, 1996Assignee: Bio-Mega/Boehringer Ingelheim Research Inc.Inventors: Paul C. Anderson, Teddy Halmos, Grace L. Jung, Marc-Andre Poupart, Bruno Simoneau
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Patent number: 5510478Abstract: The compound of the formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl, halo, perhaloalkyl, hydroxy, alkoxy, aryl or arylalkyl; n is an integer from 0-5; R is azabicyclo 2.2.2!octyl or azabicyclo 2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy, halo, or perhaloalkyl; N-(pyridyl)piperazinyl; N-(pyrimidinyl)piperazinyl; or 3-azabicyclo- 3.2.2!non-3-yl; X is oxygen or NH; n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.Type: GrantFiled: November 30, 1994Date of Patent: April 23, 1996Assignee: American Home Products CorporationInventor: Annmarie L. Sabb
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Patent number: 5508415Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.Type: GrantFiled: December 23, 1994Date of Patent: April 16, 1996Assignee: Sumitomo Chemical Company, LimitedInventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Tatsuhiro Hamada, Hideyuki Shibata, Ryo Sato
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Patent number: 5484933Abstract: There is disclosed a process for the production of a fluoroalkanecarboxamide derivative of the formula (I): ##STR1## wherein R.sup.1 is a halogen atom, an alkyl group substituted with at least one halogen atom or an alkoxyl group substituted with at least one halogen atom; R.sup.2 is a hydrogen atom or a halogen atom; and R.sup.3 is a methyl group, an ethyl group, a chlorine atom or a bromine atom; X and Y are the same or different and each of them represents a hydrogen atom, a chlorine atom, a fluorine atom or a trifluoromethyl group, with the proviso that X and Y do not simultaneously represent a hydrogen atom or a chlorine atom, which comprises the steps of:(a) reacting an iminothiazoline compound of the formula (II): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above, or a salt thereof with a fluoroolefin of the formula (III):XYC.dbd.CF.sub.Type: GrantFiled: July 29, 1994Date of Patent: January 16, 1996Assignee: Sumitomo Chemical Company, LimitedInventors: Sumio Nishida, Yuzuru Sanemitsu
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Patent number: 5478945Abstract: A thiazoline derivative represented by the formula: ##STR1## [wherein R.sup.1 is cyano, carbamoyl, thiocarbamoyl, morpholinothiocarbonyl, alkylthioimidoyl, amidino, substituted amidino or imidazolin-2-yl, R.sup.2 is alkyl or aralkyl, R.sup.3 is hydrogen or alkyl, R.sup.4 is hydroxyl, alkoxy, substituted alkoxy or amino, l is an integer of 1 to 5] and salts thereof have fibrinogen receptor antagonism and cell adhesion factor antagonism, and are useful as therapeutic agents for ischemic diseases and atherosclerosis diseases, and metastasis inhibitory agents of tumors.Type: GrantFiled: January 11, 1995Date of Patent: December 26, 1995Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Akira Manaka, Keiko Takahashi, Yutaka Kawashima, Katsuo Hatayama
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Patent number: 5463069Abstract: There is disclosed a process of producing a 2-iminothiazoline derivative of the general formula [II], characterized in that a thiourea derivative of the general formula [I] is treated with an acid. Also disclosed are a process of producing an N-substituted N-arylcyanamide derivative of the general formula [VI], characterized in that an N-arylcyanamide derivative of the general formula [IV] is reacted with an allyl halide derivative of the general formula [V] in an aprotic polar solvent in the presence of an iodide and an alkali metal carbonate; and a process of producing an N-substituted N-arylthiourea derivative of the general formula [VII], characterized in that an N-substituted N-arylcyanamide derivative of the general formula [VI] obtained as described above is further reacted with a chemical species which generates sulfide ion or hydrogensulfide ion.Type: GrantFiled: December 2, 1993Date of Patent: October 31, 1995Assignee: Sumitomo Chemical Company, LimitedInventors: Katuhisa Masumoto, Toshio Nagatomi, Akihiko Nakamura, Yoshimi Yamada
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Patent number: 5457205Abstract: Compounds of formula ##STR1## where the substituents are as defined herein, are disclosed, which compounds are useful in the treatment of diabetes and obesity, among other uses.Type: GrantFiled: March 12, 1993Date of Patent: October 10, 1995Assignee: Dr. Karl Thomae GmbHInventors: Manfred Reiffen, Rudolph Hurnaus, Robert Sauter, Wolfgang Grell, Eckhard Rupprecht
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5455348Abstract: The invention relates to cyclic imino derivatives of general formulaB--X.sub.5 --X.sub.4 --X.sub.3 --X.sub.2 --X.sub.1 --A--Y--E(I)whereinA, B, E, X.sub.2 to X.sub.5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.Type: GrantFiled: December 23, 1993Date of Patent: October 3, 1995Assignee: Karl ThomaeInventors: Volkhard Austel, Wolfgang Eisert, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Helmut Pieper, Johannes Weisenberger
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Patent number: 5449783Abstract: A novel diphenythiazole derivative represented by the following general formula (I): ##STR1## wherein m and n are each 1 or 2; R.sup.1 and R.sup.2 represent each a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylsulfenyl group, a nitro group, an amino group, a methanesulfonyloxy group or a halogen atom; A.sup.1 represents a lower alkanesulfonyl group, a halogenated lower alkanesulfonyl group, a substituted benzenesulfonyl group, a lower acyl group or a halogenated lower acyl group; and A.sup.2 represents a hydrogen atom, a lower alkanesulfonyl group, a halogenated lower alkanesulfonyl group or a lower alkyl group,and being efficacious as a drug having antiinflammatory, analgesic, antiallergic, uricosuric or platelet aggregation inhibiting effects.Type: GrantFiled: August 23, 1993Date of Patent: September 12, 1995Assignee: Hisamitsu Pharmaceutical Co., Inc.Inventors: Masaru Saita, Hisataka Inoue, Kouichi Ikesue, Noriyuki Fujimoto, Ikuo Shinohara, Taniguchi: Yasuaki, Yoshiki Deguchi, Hidenao Minami, Kanji Noda
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Patent number: 5447944Abstract: The present invention provides carbamoyl-2 -pyrrolidinone compounds useful as medicaments for improving cerebral functions and activating cerebral metabolism or protecting against anoxic brain damage.Type: GrantFiled: March 22, 1994Date of Patent: September 5, 1995Assignee: Taiho Pharmaceutical Company, LimitedInventors: Makoto Kajitani, Etsuo Hasegawa, Akihiro Kawaguchi, Junji Yamamoto, Katsuo Toide, Takaji Honna, Mitsugi Yasumoto, Nobuo Kasahara
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Patent number: 5426188Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.Type: GrantFiled: January 15, 1993Date of Patent: June 20, 1995Assignee: Sumitomo Chemical Company, LimitedInventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Tatsuhiro Hamada, Hideyuki Shibata, Ryo Sato
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Patent number: 5412117Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents =O, =S, =N-Z (Z represents a lower alkyl group, etc.), or =CHNO.sub.2 ; Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 each represent a hydrogen atom, a lower alkyl group, etc., are disclosed. The benzopyran derivatives exhibit K.sup.+ channel activating activities and are widely applicable as antiasthmatics, antiepileptics, and the like.Type: GrantFiled: January 26, 1993Date of Patent: May 2, 1995Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hiroyuki Nabata
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Patent number: 5393775Abstract: A compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and n are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same for treating a mammal afflicted with a disorder connected with peroxydation processes and biosynthesis of eicosanoids.Type: GrantFiled: September 7, 1993Date of Patent: February 28, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Jean-Paul Babingui, Sylvie Robert-Piessard, Pierre Renard, Daniel-henri Caignard, jean-Francois Renaud de la Faverle, Gerard Adam
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Patent number: 5389649Abstract: Oxathiane derivatives of formula ##STR1## in which R represents alkyl and A represents optionally substituted phenyl or a heteroaromatic group containing 1 or 2 nitrogen atoms optionally substituted by alkyl, alkoxy or halogen, and salts thereof possess pharmacological activity and are also useful in inhibiting head hair loss.Type: GrantFiled: July 20, 1992Date of Patent: February 14, 1995Assignee: Rhone-Poulenc Rorer LimitedInventors: Iain M. McLay, Roger J. A. Walsh
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Patent number: 5385942Abstract: A quinone derivative useful in the treatment of hepatic diseases defined by the general formula: ##STR1## where X and Y may be the same or different from each other and are each a hydroxyl group, a group represented by the formula --(--OCH.sub.2 --).sub.n --OR.sup.6, wherein n is 0 or 1 and R.sup.6 is a lower alkyl group, or an acyl group.Type: GrantFiled: March 1, 1993Date of Patent: January 31, 1995Assignee: Eisai Co., Ltd.Inventors: Shinya Abe, Yasushi Okamoto, Katsuya Tagami, Shigeki Hibi, Junichi Nagakawa, Kazuo Hirota, Ieharu Hishinuma, Kaname Miyamoto, Takashi Yamanaka, Hiromitsu Yokohama, Tsutomu Yoshimura, Tohru Horie, Yasunori Akita, Koichi Katayama, Isao Yamatsu
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Patent number: 5369116Abstract: Disclosed are a polyfluorinated thiazoline compound represented by the following formula (I): ##STR1## wherein Q represents a phenyl group; a phenyl group substituted by a halogen atom, a halo-lower alkyl group, a nitro group, a cyano group, a formyl group, a lower alkoxycarbonyl group or a benzoyl group; a pyridyl group; or a pyridyl group substituted by a halogen atom, a halo-lower alkyl group, a nitro group, a cyano group, a formyl group, a lower alkoxycarbonyl group or a benzoyl group; andR represents a hydrogen atom, a lower alkyl group or an acetyl group,and a chemical for controlling noxious organisms containing the same as an active ingredient.Type: GrantFiled: July 2, 1993Date of Patent: November 29, 1994Assignee: Ube Industries, Ltd.Inventors: Tokio Obata, Katsutoshi Fujii, Yasuhisa Fukuda, Kiyashi Tsutsumiuchi, Yoshinori Yamanaka
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Patent number: 5358957Abstract: Compounds of the formula ##STR1## wherein A is a substituted or unsubstituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical that is bonded by way of a carbon atom to X; each of R.sub.1 and R.sub.2, independently of the other, is hydrogen or C.sub.1 -C.sub.6 alkyl; X is NR.sub.3, 0 or S; and R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: September 2, 1993Date of Patent: October 25, 1994Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna
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Patent number: 5350736Abstract: 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 lower alkyl, chlorine; bromine or iodine; R.sup.3 is (lower alkyl)carbonyl, (lower cycloalkyl)carbonyl, (lower cycloalkoxy)carbonyl, (lower alkoxy)carbonyl or (lower alkyl)sulfonyl, all of which are optionally substituted with at least one substituent selected from halogen, lower alkyl, lower alkoxy, lower cycloalkyl and lower cycloalkoxy; and R.sup.4 is 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 21, 1992Date of Patent: September 27, 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: 5340832Abstract: A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms, R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.Type: GrantFiled: August 17, 1993Date of Patent: August 23, 1994Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5336776Abstract: Thiazole intermediates for Cephalosporing are prepared.Type: GrantFiled: October 16, 1991Date of Patent: August 9, 1994Assignee: Roussel UCLAFInventors: Rene Heymes, Andrr Lutz
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Patent number: 5324837Abstract: 3,4-Diaryl-4,5-dihydro-1H-pyrazole compounds having a selected 5- or 6-membered aromatic heterocyclic moiety in the 4-position and an optionally substituted phenyl moiety in the 3-position, such as 4,5-dihydro-3-(4-fluorophenyl)-4-(5-trifluoromethyl-2-pyridinyl)-1H-pyrazo le were prepared as intermediates in the preparation of insecticidal 3,4,N-triaryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds. The 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds can be prepared from appropriate 1,2-diarylethanone compounds by successive treatments with N,N,N',N'-tetramethyldiaminomethane in dichloromethane in the presence of acetic anhydride (to form a Mannich adduct) and hydrazine in the presence of a catalytic amount of trifluoroacetic acid.Type: GrantFiled: August 17, 1992Date of Patent: June 28, 1994Assignee: DowElancoInventors: James M. Renga, Kevin L. McLaren, James T. Pechacek, Michael J. Ricks, Yulan C. Tong
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Patent number: 5314889Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).Type: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
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Patent number: 5314891Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 -- which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio or imino;Ar is optionally substituted phenylene;R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety;R.sup.5 is hydrogen or (1-4C)alkyl; andR.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: September 10, 1992Date of Patent: May 24, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, Keith Oldham, David Waterson
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Patent number: 5312926Abstract: Indonaphthol thermal transfer dyes have the formula ##STR1## where X is nitrogen or the radical CH,R.sup.1 and R.sup.2 are each independently of the other C.sub.1 -C.sub.6 -alkyl, which may be substituted, C.sub.1 -C.sub.6 -monooxaalkyl or -dioxaalkyl or allyl,R.sup.3 and R.sup.4 are each independently of the other hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkanoylamino, andR.sup.5 is five-membered hetaryl which is not benzofused and has two or more hetero atoms,with the proviso that R.sup.1 and R.sup.2 are not both unsubstituted C.sub.1 -C.sub.6 -alkyl at one and the same time.Type: GrantFiled: March 29, 1991Date of Patent: May 17, 1994Assignee: BASF AktiengesellschaftInventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
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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: 5258357Abstract: Carboxamides of the formulae Ia to Ic ##STR1## where X is oxygen or sulfur;R.sup.1 is hydrogen or substituted or unsubstituted cycloalkyl or alkyl;R.sup.2 is hydroxy, alkoxy, cyanoalkyl, substituted or unsubstituted alkenyl, alkynyl, phenyl or naphthyl, a substituted or unsubstituted 5- to 6-membered heterocyclic structure or one of the groups stated for R.sup.1, orR.sup.1 and R.sup.2 together are a 4- to 7-membered chain which contains, in addition to methylene groups, one of the following groups as ring member: oxygen, sulfur, N-methyl or carbonyl;R.sup.3 and R.sup.4 are each nitro, cyano, halogen, substituted or unsubstituted amino, alkoxy, alkylthio, a substituted or unsubstituted 5- to 6 -membered heterocyclic structure, substituted or unsubstituted alkenyl, alkynyl, phenyl, phenoxy or phenylthio, or one of the groups stated for R.sup.1 ;R.sup.5 is formyl, 4,5-dihydrooxazol-2-yl or COYR.sup.6 (Y=O,S);R.sup.Type: GrantFiled: September 21, 1992Date of Patent: November 2, 1993Assignee: BASF AktiengesellschaftInventors: Peter Muenster, Gerd Steiner, Wolfgang Freund, Bruno Wuerzer, Karl-Otto Westphalen
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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: 5231109Abstract: 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.Intermediates therefor, wherein R.sup.2 is hydrogen or an alkali metal cation, are also new.Type: GrantFiled: June 8, 1989Date of Patent: July 27, 1993Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Klaus Jellch, Winfried Lunkenhelmer, Wilhelm Brandes, Gerd Hanssler
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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: 5215989Abstract: Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members, X and Y are bridging groups, Q is a nitrogen containing heterocycle, R.sup.2 and R.sup.3 are H, substituted or unsubtituted C.sub.1-3 alkyl, C.sub.1-3 alkoxy, N(R).sub.2, halogen, CF.sub.3 or R.sup.5 and R.sup.1 is H or an aryl group.Type: GrantFiled: July 15, 1991Date of Patent: June 1, 1993Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
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Patent number: 5210239Abstract: A quinone derivative useful in the treatment of hepatic diseases defined by the general formula: ##STR1## where R1 is selected from the group consisting of alkyl, alkenly, alkynyl or heterocycle, R2 is a substituted nitrogen containing radical wherein the substituents on said nitrogen are selected from the group consisting of hydrogen, substituted or unsubstituted lower alkyl or heterocycles, and where said nitrogen may be a ring heteroatom, and R3, R4 and R5, may be the same or different and each are hydrogen, lower alkyl or lower alkoxy groups.Type: GrantFiled: August 31, 1990Date of Patent: May 11, 1993Assignee: Eisai Co., Ltd.Inventors: Shinya Abe, Yasushi Okamoto, Katsuya Tagami, Shigeki Hibi, Junichi Nagakawa, Kazuo Hirota, Ieharu Hishinuma, Kaname Miyamoto, Takashi Yamanaka, Hiromitsu Yokohama, Tsutomu Yoshimura, Tohru Horie, Yasunori Akita, Koichi Katayama, Isao Yamatsu
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Patent number: 5204468Abstract: This invention provides the single species (-)-(S)-4-(3,4-dihydroxyphenyl)-7, 8-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride hydrate, which is useful as a nephrovascular dilator.Type: GrantFiled: July 25, 1991Date of Patent: April 20, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Akihiro Tanaka, Takashi Fujikura, Ryuji Tsuzuki, Masaki Yokota, Takeyuki Yatsu
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Patent number: 5202340Abstract: The compounds of the formula: ##STR1## (wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is carbocyclic or heterocyclic ring, unsubstituted or substituted by R.sup.3 s; R.sup.3 is halogen, trihalomethyl, hydroxy, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfornyl, cyano, nitro, or group of the formula: --C.sub.6 H.sub.4 --R.sup.4, --NR.sup.5 R.sup.6, --CO--R.sup.7, --COOR.sup.8, --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6 or --NHCO--R.sup.7, in which R.sup.4 is hydrogen, halogen, trihalomethyl, hydroxy, alkyl or alkoxy, R.sup.5 and R.sup.6 are each hydrogen or alkyl, R.sup.7 is alkyl or phenyl substituted by R.sup.4 and R.sup.8 is hydrogen or alkyl; Z is hydrogen or group of the formula: --COR.sup.9, ##STR2## in which R.sup.9 is alkyl or phenyl substituted by R.sup.10, in which R.sup.10 is hydrogen, halogen, trihalomethyl, alkyl or alkoxy, R.sup.11 and R.sup.12 are each hydrogen, alkyl or phenyl substituted by R.sup.10, or R.sup.11 and R.sup.Type: GrantFiled: April 2, 1991Date of Patent: April 13, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
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Patent number: 5192781Abstract: The present invention relates to the derivatives of formula (I): ##STR1## and their addition salts, and to their use in therapeutics, especially for the treatment of cardiovascular diseases and in particular for the treatment of hypertension and cardiac insufficiency.Type: GrantFiled: July 11, 1991Date of Patent: March 9, 1993Assignee: Laboratoires UPSAInventors: Nicole Bru-Magniez, Michele Launay, Jean-Marie Teulon
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Patent number: 5189049Abstract: Compounds of formula ##STR1## in which R.sub.1 represents H, an alkyl or a substituted alkyl, R.sub.2 represents H or alkyl and R.sub.3 represents an optionally substituted cycloalkyl or an optionally substituted aromatic group, which can be a phenyl or a heterocyclic group comprising one or more hetero-atoms chosen from O, S and N, or R.sub.2 and R.sub.3 considered together represent the group ##STR2## which is optionally substituted on the phenyl ring, and Z represents a heterocycle comprising one or more heteroatoms chosen from O, S and N, fused with an aromatic ring which can comprise a hetero-atom and can be substituted, the said heterocycle being optionally substituted on N, when it comprises such an atom, by an alkyl or a substituted alkyl group, and the salts of these compounds with acids or bases.Use of these compounds as medicaments.No figure.Type: GrantFiled: December 5, 1990Date of Patent: February 23, 1993Assignee: SanofiInventors: Daniel Frehel, Danielle Gully, Gerard Valette, Jean-Pierre Bras
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Patent number: 5179207Abstract: Provided are certain substituted 2-aminothiazoles and 2-aminothiophenes which are useful as red colorants and as intermediates in the synthesis of bathochromic azo dyes. These compounds are prepared by reacting 2-aminothiophenes or 2-aminothiazoles, which contain a primary amino group, with 2-chloro-3-negatively-substituted maleimides. These compounds can be diazotized and coupled with azo components, for example, anilines, 1,2,3,4-tetrahydroquinolines, 2,3-dihydroindoles, and 3,4-dihydro-2H-1,4-benzoxazines to form bathochromic blue-cyan azo dyes.Type: GrantFiled: August 19, 1991Date of Patent: January 12, 1993Assignee: Eastman Kodak CompanyInventors: James J. Krutak, Max A. Weaver
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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: 5175182Abstract: The invention relates to acryloyl substituted pyrrole derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, --CN, --NO.sub.2, C.sub.1 -C.sub.4 alkyl, or a group ##STR2## R.sub.3 is hydrogen, halogen, --CN, or --NO.sub.2 ; each R.sub.4 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;A is a bond, a group ##STR3## or a group --NH--Het--CO--, wherein Het is a saturated or unsaturated pentatomic or hexatomic heteromonocyclic ring; andB is a group ##STR4## in which m is 1, 2 or 3 and each R.sub.5 is, independently, a C.sub.1 -C.sub.4 alkyl group, and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents.Type: GrantFiled: November 5, 1990Date of Patent: December 29, 1992Assignee: Farmitalia Carlo Erba SrlInventors: Nicola Mongelli, Giovanni Biasoli, Laura Capolongo, Gabriella Pezzoni
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Patent number: 5166161Abstract: 3-Oxo-4-acyl or carbamyl-bicyclic aromatic and heterocyclic compounds as inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergy and antiinflammatory agents.Type: GrantFiled: January 22, 1991Date of Patent: November 24, 1992Assignee: Pfizer Inc.Inventors: Toshihide Kokura, Kazunari Nakao, Fumitaka Ito, Masami Nakane
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Patent number: 5158950Abstract: 2-(1,3-Dithiol-2-ylidene)-2-[N-(substituted) carbamoly] acetate esters and salts thereof, having potent therapeutic or prophylactic effect for hepatic disorder, are provided. Processes for their preparation and intermediates in their preparation also are disclosed.Type: GrantFiled: May 23, 1990Date of Patent: October 27, 1992Assignee: Yuhan Corporation, Ltd.Inventors: Choong S. Kim, Jeong S. Chae, Young R. Choi, Jong W. Lee, Joung K. Yoo
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Patent number: 5158943Abstract: A sulfur-containing hetrocyclic compound of the formula (I) ##STR1## wherein the ring A is an optionally substituted benzene ring, R is a hydrogen atom or an optionally substituted hydrocarbon residue, B is a carboxyl group which may be esterified or amidated, X is --CH(OH)-- or --CO--, and n is an integer of 0, 1 or 2, or its salt, which is useful in the prevention or treatment of osteoporosis.Type: GrantFiled: May 23, 1991Date of Patent: October 27, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Iwao Yamazaki
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Patent number: 5155106Abstract: A cysteamine derivative represented by general formula (I): ##STR1## wherein R.sub.1 represents a straight-chain or a branched alkyl radical having 1 to 6 carbon atoms, R.sub.2 represents hydrogen atom or n-propyl radical, and X represents a radical selected from the group consisting of radicals containing cysteamine moiety (N S) represented by formula (II): ##STR2## formula (III): ##STR3## formula (IV): ##STR4## formula (V): ##STR5## or formula (VI): ##STR6## wherein R.sub.2 represents hydrogen atom or a straight-chain or a branched alkyl group having 1 to 10 carbon atoms is provided.The cysteamine derivative is effective as an antirheumatic agent.Type: GrantFiled: July 20, 1990Date of Patent: October 13, 1992Assignee: Terumo Kabushiki KaishaInventors: Masaki Shimizu, Shingo Koyama, Hiromasa Kohama, Ryoichi Nanba, Kazuhito Inoue
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Patent number: 5149872Abstract: 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: GrantFiled: February 14, 1991Date of Patent: September 22, 1992Assignee: Enichem Anic S.p.A.Inventors: Giuseppe Messina, Loreno Lorenzoni, Paolo Calaresu, Giovanni M. Sechi
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Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 5103013Abstract: 2-(1,3-Dithietan-2-ylidene)-2-[N-(subsittuted)carbamoyl]acetate esters and 2-(1,3-dithiolan-2-ylidene)-2-[N-(substituted) carbamoyl]acetate esters, having potent therapeutic and prophylactic effect for hepatic disorders, are provided.Type: GrantFiled: October 23, 1989Date of Patent: April 7, 1992Assignee: Yuhan Corporation, Ltd.Inventors: Choong S. Kim, Jeong S. Chae, Ho Seong Yoo, Jong W. Lee, Jae G. Park, Jeong W. Lee
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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: 5071841Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.Type: GrantFiled: December 28, 1989Date of Patent: December 10, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki