The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
  • Patent number: 5523315
    Abstract: 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: Grant
    Filed: September 20, 1993
    Date of Patent: June 4, 1996
    Assignee: Bio-Mega/Boehringer Ingelheim Research Inc.
    Inventors: Paul C. Anderson, Teddy Halmos, Grace L. Jung, Marc-Andre Poupart, Bruno Simoneau
  • Patent number: 5510478
    Abstract: 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: Grant
    Filed: November 30, 1994
    Date of Patent: April 23, 1996
    Assignee: American Home Products Corporation
    Inventor: Annmarie L. Sabb
  • Patent number: 5508415
    Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: April 16, 1996
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Tatsuhiro Hamada, Hideyuki Shibata, Ryo Sato
  • Patent number: 5484933
    Abstract: 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: Grant
    Filed: July 29, 1994
    Date of Patent: January 16, 1996
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sumio Nishida, Yuzuru Sanemitsu
  • Patent number: 5478945
    Abstract: 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: Grant
    Filed: January 11, 1995
    Date of Patent: December 26, 1995
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Akira Manaka, Keiko Takahashi, Yutaka Kawashima, Katsuo Hatayama
  • Patent number: 5463069
    Abstract: 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: Grant
    Filed: December 2, 1993
    Date of Patent: October 31, 1995
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Katuhisa Masumoto, Toshio Nagatomi, Akihiko Nakamura, Yoshimi Yamada
  • Patent number: 5457205
    Abstract: 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: Grant
    Filed: March 12, 1993
    Date of Patent: October 10, 1995
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Manfred Reiffen, Rudolph Hurnaus, Robert Sauter, Wolfgang Grell, Eckhard Rupprecht
  • Patent number: 5457122
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: October 10, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5455348
    Abstract: 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: Grant
    Filed: December 23, 1993
    Date of Patent: October 3, 1995
    Assignee: Karl Thomae
    Inventors: Volkhard Austel, Wolfgang Eisert, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Helmut Pieper, Johannes Weisenberger
  • Patent number: 5449783
    Abstract: 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: Grant
    Filed: August 23, 1993
    Date of Patent: September 12, 1995
    Assignee: Hisamitsu Pharmaceutical Co., Inc.
    Inventors: Masaru Saita, Hisataka Inoue, Kouichi Ikesue, Noriyuki Fujimoto, Ikuo Shinohara, Taniguchi: Yasuaki, Yoshiki Deguchi, Hidenao Minami, Kanji Noda
  • Patent number: 5447944
    Abstract: 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: Grant
    Filed: March 22, 1994
    Date of Patent: September 5, 1995
    Assignee: Taiho Pharmaceutical Company, Limited
    Inventors: Makoto Kajitani, Etsuo Hasegawa, Akihiro Kawaguchi, Junji Yamamoto, Katsuo Toide, Takaji Honna, Mitsugi Yasumoto, Nobuo Kasahara
  • Patent number: 5426188
    Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.
    Type: Grant
    Filed: January 15, 1993
    Date of Patent: June 20, 1995
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Tatsuhiro Hamada, Hideyuki Shibata, Ryo Sato
  • Patent number: 5412117
    Abstract: 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: Grant
    Filed: January 26, 1993
    Date of Patent: May 2, 1995
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroshi Koga, Hiroyuki Nabata
  • Patent number: 5393775
    Abstract: 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: Grant
    Filed: September 7, 1993
    Date of Patent: February 28, 1995
    Assignee: Adir et Compagnie
    Inventors: Guillaume Le Baut, Jean-Paul Babingui, Sylvie Robert-Piessard, Pierre Renard, Daniel-henri Caignard, jean-Francois Renaud de la Faverle, Gerard Adam
  • Patent number: 5389649
    Abstract: 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: Grant
    Filed: July 20, 1992
    Date of Patent: February 14, 1995
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Iain M. McLay, Roger J. A. Walsh
  • Patent number: 5385942
    Abstract: 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: Grant
    Filed: March 1, 1993
    Date of Patent: January 31, 1995
    Assignee: 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
  • Patent number: 5369116
    Abstract: 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: Grant
    Filed: July 2, 1993
    Date of Patent: November 29, 1994
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Yasuhisa Fukuda, Kiyashi Tsutsumiuchi, Yoshinori Yamanaka
  • Patent number: 5358957
    Abstract: 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: Grant
    Filed: September 2, 1993
    Date of Patent: October 25, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna
  • Patent number: 5350736
    Abstract: There is disclosed an iminothiazoline compound of the formula: ##STR1## wherein R.sup.1 is halogen, halo(lower)alkyl, halo(lower)alkoxy or halo(lower)alkylthio; R.sup.2 is 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: Grant
    Filed: August 21, 1992
    Date of Patent: September 27, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Ryo Sato, Tatsuhiro Hamada, Hideyuki Shibata
  • Patent number: 5340832
    Abstract: 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: Grant
    Filed: August 17, 1993
    Date of Patent: August 23, 1994
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
  • Patent number: 5336776
    Abstract: Thiazole intermediates for Cephalosporing are prepared.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: August 9, 1994
    Assignee: Roussel UCLAF
    Inventors: Rene Heymes, Andrr Lutz
  • Patent number: 5324837
    Abstract: 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: Grant
    Filed: August 17, 1992
    Date of Patent: June 28, 1994
    Assignee: DowElanco
    Inventors: James M. Renga, Kevin L. McLaren, James T. Pechacek, Michael J. Ricks, Yulan C. Tong
  • Patent number: 5314889
    Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5314891
    Abstract: 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: Grant
    Filed: September 10, 1992
    Date of Patent: May 24, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Philip N. Edwards, Keith Oldham, David Waterson
  • Patent number: 5312926
    Abstract: 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: Grant
    Filed: March 29, 1991
    Date of Patent: May 17, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
  • Patent number: 5292715
    Abstract: There is disclosed an iminothiazoline compound of the formula: ##STR1## wherein R.sup.1 is halogen, halo(lower)alkyl, halo(lower)alkoxy or halo(lower)alkylthio; R.sup.2 is methyl, ethyl, chlorine, bromine or iodine; R.sup.3 is lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, lower alkylamino, phenylamino or phenyl, all of which are optionally substituted with at least one substituent selected from halogen, lower alkyl, lower alkoxy, halo(lower)alkyl, lower cycloalkyl and lower cycloalkoxy; and R.sup.4 is hydrogen or halogen. Also disclosed are a process for producing this compound, a herbicidal composition comprising this compound as an active ingredient, and a method for controlling undesired weeds by use of this compound as a herbicide.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: March 8, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Ryo Sato, Tatsuhiro Hamada, Hideyuki Shibata
  • Patent number: 5258357
    Abstract: 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: Grant
    Filed: September 21, 1992
    Date of Patent: November 2, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Muenster, Gerd Steiner, Wolfgang Freund, Bruno Wuerzer, Karl-Otto Westphalen
  • Patent number: 5244863
    Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.
    Type: Grant
    Filed: October 1, 1991
    Date of Patent: September 14, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinichi Kawamura, Keiichi Izumi, Junichi Sato, Yuzuru Sanemitsu, Tatsuhiro Hamada, Hideyuki Shibata, Ryo Sato
  • Patent number: 5240918
    Abstract: The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.
    Type: Grant
    Filed: March 24, 1992
    Date of Patent: August 31, 1993
    Assignee: EGIS Gyogyszergyar
    Inventors: Karoly Lempert, Gyula Hornyak, Jozsef Fetter, Antal Feller, Klara Gaso, Gabor Gigler, Laszlo Kapolnai, Lujza Petocz, Katalin Szemeredi, Marton Fekete
  • Patent number: 5231109
    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.Intermediates therefor, wherein R.sup.2 is hydrogen or an alkali metal cation, are also new.
    Type: Grant
    Filed: June 8, 1989
    Date of Patent: July 27, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Klaus Jellch, Winfried Lunkenhelmer, Wilhelm Brandes, Gerd Hanssler
  • Patent number: 5221685
    Abstract: Disclosed are a thiazoline compound represented by the following formula (I): ##STR1## wherein R represents hydrogen atom or a lower alkyl group, X represents oxygen atom or sulfur atom, and Q represents Ar (where Ar represents a substituted or unsubstituted phenyl group or a substituted or unsubstituted naphthyl group) or ##STR2## (where Y represents a halogen atom, a lower alkyl group, a lower alkoxy group, a lower haloalkyl group, a lower haloalkoxy group, nitro group, acetyl group or cyano group and n represents an integer of 0 to 5),a process for preparing the same and a chemical for controlling noxious organisms containing the same as an active ingredient.
    Type: Grant
    Filed: January 30, 1992
    Date of Patent: June 22, 1993
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Yasuhisa Fukuda, Kiyoshi Tsutsumiuchi, Yoshinori Yamanaka
  • Patent number: 5215989
    Abstract: 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: Grant
    Filed: July 15, 1991
    Date of Patent: June 1, 1993
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
  • Patent number: 5210239
    Abstract: 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: Grant
    Filed: August 31, 1990
    Date of Patent: May 11, 1993
    Assignee: 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
  • Patent number: 5204468
    Abstract: 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: Grant
    Filed: July 25, 1991
    Date of Patent: April 20, 1993
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Akihiro Tanaka, Takashi Fujikura, Ryuji Tsuzuki, Masaki Yokota, Takeyuki Yatsu
  • Patent number: 5202340
    Abstract: 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: Grant
    Filed: April 2, 1991
    Date of Patent: April 13, 1993
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
  • Patent number: 5192781
    Abstract: 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: Grant
    Filed: July 11, 1991
    Date of Patent: March 9, 1993
    Assignee: Laboratoires UPSA
    Inventors: Nicole Bru-Magniez, Michele Launay, Jean-Marie Teulon
  • Patent number: 5189049
    Abstract: 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: Grant
    Filed: December 5, 1990
    Date of Patent: February 23, 1993
    Assignee: Sanofi
    Inventors: Daniel Frehel, Danielle Gully, Gerard Valette, Jean-Pierre Bras
  • Patent number: 5179207
    Abstract: 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: Grant
    Filed: August 19, 1991
    Date of Patent: January 12, 1993
    Assignee: Eastman Kodak Company
    Inventors: James J. Krutak, Max A. Weaver
  • Patent number: 5177095
    Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Wallace Ashton, Kenneth J. Fitch, Thomas F. Walsh, Ralph A. Rivero, Daljit S. Dhanoa
  • Patent number: 5175182
    Abstract: 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: Grant
    Filed: November 5, 1990
    Date of Patent: December 29, 1992
    Assignee: Farmitalia Carlo Erba Srl
    Inventors: Nicola Mongelli, Giovanni Biasoli, Laura Capolongo, Gabriella Pezzoni
  • Patent number: 5166161
    Abstract: 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: Grant
    Filed: January 22, 1991
    Date of Patent: November 24, 1992
    Assignee: Pfizer Inc.
    Inventors: Toshihide Kokura, Kazunari Nakao, Fumitaka Ito, Masami Nakane
  • Patent number: 5158950
    Abstract: 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: Grant
    Filed: May 23, 1990
    Date of Patent: October 27, 1992
    Assignee: Yuhan Corporation, Ltd.
    Inventors: Choong S. Kim, Jeong S. Chae, Young R. Choi, Jong W. Lee, Joung K. Yoo
  • Patent number: 5158943
    Abstract: 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: Grant
    Filed: May 23, 1991
    Date of Patent: October 27, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Iwao Yamazaki
  • Patent number: 5155106
    Abstract: 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: Grant
    Filed: July 20, 1990
    Date of Patent: October 13, 1992
    Assignee: Terumo Kabushiki Kaisha
    Inventors: Masaki Shimizu, Shingo Koyama, Hiromasa Kohama, Ryoichi Nanba, Kazuhito Inoue
  • Patent number: 5149872
    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: February 14, 1991
    Date of Patent: September 22, 1992
    Assignee: Enichem Anic S.p.A.
    Inventors: Giuseppe Messina, Loreno Lorenzoni, Paolo Calaresu, Giovanni M. Sechi
  • Patent number: 5112868
    Abstract: 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: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
  • Patent number: 5103013
    Abstract: 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: Grant
    Filed: October 23, 1989
    Date of Patent: April 7, 1992
    Assignee: Yuhan Corporation, Ltd.
    Inventors: Choong S. Kim, Jeong S. Chae, Ho Seong Yoo, Jong W. Lee, Jae G. Park, Jeong W. Lee
  • Patent number: 5084571
    Abstract: There are disclosed substituted thiazole dye compounds represented by the following Formula (I):Formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a group capable of substitution onto a benzene ring, n is an integer of 1 to 4, x represents a substitutent capable of forming a hydrogen bond with the hydrogen of --CONH--, R.sub.2 represents an electron-attractive substituent, R.sub.3 represents a group capable of substitution onto a thiazole ring, and R.sub.4 represents an aromatic group or an unsaturated heterocyclic group that bonds to the nitrogen atom at a carbon atom having an unsaturated linkage.The dye compounds provide a cyan color which is good in hues and possesses fastness to light and heat.
    Type: Grant
    Filed: October 18, 1989
    Date of Patent: January 28, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Yasuhiro Shimada
  • Patent number: 5079369
    Abstract: The compound of the formula: ##STR1## wherein R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, and R.sup.6 is amino or protected amino, or its reactive derivative at the carboxy group effective for transforming the carboxy group into a reactive N-acylating group, or a salt thereof.
    Type: Grant
    Filed: June 23, 1989
    Date of Patent: January 7, 1992
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 5071841
    Abstract: 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: Grant
    Filed: December 28, 1989
    Date of Patent: December 10, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki