Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
-
Patent number: 5534481Abstract: The present invention provides an indazolesulfonylurea derivative represented by the general formula: ##STR1## [wherein R.sup.1 is a hydrogen atom or an alkyl group, etc., R.sup.2 and R.sup.3 are the same or different and represent a hydrogen atom, a halogen atom, an alkyl group, the formula --COR.sup.4 (wherein R.sup.4 represents an alkoxy group, etc.), an alkoxy group, a haloalkoxy group or a cyano group, etc., X is an oxygen atom or a sulfur atom, Y is a hydrogen atom or an alkyl group, etc., A and B are the same or different and represent a halogen atom, an alkoxy group or an alkyl group, etc., and Z represents a nitrogen atom or a methine group], as well as a herbicide containing it as an active ingredient and an intermediate for its production.The compound of the present invention exhibits excellent herbicidal effects over a wide range from the preemergence stage to the growing stage of various weeds which are problematic in agricultural fields.Type: GrantFiled: January 30, 1995Date of Patent: July 9, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Chiharu Suzuki, Katsumi Masuda, Masatoshi Tamaru, Masahito Inamori, Nobuo Takefuji, Katsutada Yanagisawa, Yasunori Ogawa
-
Patent number: 5527763Abstract: A herbicide containing a pyrimidine or triazine derivative of the formula (I): ##STR1## [wherein A is a furan ring, a pyrimidine ring, a 1,2,4-triazine ring or the like which may suitably be substituted, R is a hydroxyl group or a lower alkoxy group, each of R.sup.1 and R.sup.2 which may be the same or different, is a halogen atom, a lower alkyl group or a lower alkoxy group, W is an oxygen atom or a sulfur atom, and Z is nitrogen or a methine group] and its salt, as an active ingredient, is presented. The pyrimidine or triazine derivative of the present invention has excellent herbicidal effects against noxious weeds in paddy fields, upland fields and non-agricultural fields.Type: GrantFiled: December 8, 1993Date of Patent: June 18, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masahiro Miyazaki, Masafumi Matsuzawa, Takumi Yoshimura, Kuniaki Shimizu, Shigehiko Tachikawa
-
Patent number: 5525724Abstract: A process for the preparation of chloropyrimidines of the formula ##STR1## in which the substituents may be alkyl, cycloalkyl, aryl or radicals containing heteroatoms, but in which at least one of the substituents R.sup.1 to R.sup.4 must be Cl, which involves:reacting a hydroxy-pyrimidine or its tautomeric keto form with phosphoryl chloride in the presence of an amine or amine hydrochloride;recovering phosphoryl chloride after the reaction by adding phosphorus pentachloride and distilling the phosphoryl chloride; andseparating the chloropyrimidine from the amine hydrochloride by addition of a solvent which will dissolve the chloropyrimidine but not the amine hydrochloride and removing the amine hydrochloride.Type: GrantFiled: February 27, 1995Date of Patent: June 11, 1996Assignee: Huels AktiengesellschaftInventor: Artur Hunds
-
Patent number: 5525604Abstract: A 4-aminopyrimidine of the formula (I): ##STR1## wherein A is a bond, C1-4 alkylene or C1-4 oxyalkylene;Y is a bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenylene or phenyl(C1-4)alkylene;Z is a bond or vinylene;R1 is 4-15 membered heterocyclic ring containing one or two nitrogen atom;R2 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one or two of oxygen or one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) C1-4 alkoxy,(iv) hydroxy(C1-4 alkoxy) or(v) hydroxy;R3 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one oxygen, one sulfur, or one nitrogen and one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) formula:CH2.dbd.CH(X)--whereinX is halogen.(iv) hydrogen.l is 1 or 2.and some compounds are excluded.and acid addition salts thereof, salts thereof; have inhibitory effect on cGMP-PDE, or additionally on TXA2 synthetase.Type: GrantFiled: August 24, 1994Date of Patent: June 11, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Sung J. Lee, Yoshitaka Konishi, Orest T. Macina, Kigen Kondo, Dingwei T. Yu, Tamara A. Miskowski
-
Patent number: 5518994Abstract: Disclosed are a herbicide and a plant growth regulator comprising a 2-arylaminopyrimidinone derivative represented by the formula (1): ##STR1## (wherein Q represents various kinds of aromatic ring or heterocyclic ring).This compound can be used safely to main crops and shows high herbicidal effect to many weeds with a low dosage, and also shows plant growth regulating effect.Type: GrantFiled: December 6, 1994Date of Patent: May 21, 1996Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasuo Kawamura, Jun Satow, Kenzo Fukuda, Eiichi Oya, Kaoru Itoh, Hiroshi Kita, Hisashi Nakata, Tsutomu Nawamaki, Seiichi Fujii, Shigeomi Watanabe, Kimihiro Ishikawa, Yoichi Ito
-
Patent number: 5519024Abstract: A composition comprises a 1,7-disubstituted-4-oxo-3-quinolinecarboxylic acid or 1,7-disubstituted-4-oxo-3-naphthyridinecarboxylic acid derivative which is useful as a prophylactic and/or therapeutic agent for peripheral arterial obstruction, acute myocardial infarction, an antitumor agent, and as a prophylactic and/or therapeutic agent for osteoporosis.Type: GrantFiled: March 8, 1994Date of Patent: May 21, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Masahira Nakamura, Hideto Fukushi
-
Patent number: 5500406Abstract: The present invention provides novel iminosulfonylurea derivatives which are useful as herbicides with excellent activity and selectivity. These derivatives can be used to protect rice, wheat, corn, soybean, cotton and sugar beet from weeds.Type: GrantFiled: April 15, 1994Date of Patent: March 19, 1996Assignee: Nissan Chemical Industries Ltd.Inventors: Kenzi Makino, Shigeaki Akiyama, Hideaki Suzuki, Takeshi Nagaoka, Toshio Niki, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe, Kimihiro Ishikawa
-
Patent number: 5496942Abstract: A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):Het--X.sup.2 --H (IIIa)wherein Het and X.sup.2 are as defined above, with a carboxylic acid represented by Formula (II): ##STR2## or a reactive derivative thereof.Type: GrantFiled: February 14, 1994Date of Patent: March 5, 1996Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Mitsuaki Ohta, Tokuo Koide, Takeshi Suzuki, Akira Matsuhisa, Keiji Miyata, Junya Ohmori, Isao Yanagisawa
-
Patent number: 5494886Abstract: R*--O--CO--NR.sup.3 A,where R.sup.3 stands for phenyl or alkyl.The compounds of formula (II) can be obtained from the corresponding sulphochlorides.Type: GrantFiled: November 10, 1994Date of Patent: February 27, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinz Kehne, Lothar Willms, Oswald Ort, Klaus Bauer, Hermann Bieringer
-
Patent number: 5491234Abstract: 2,4-diaminopyrimidine derivatives as potentiators of chemotherapeutic agents in the treatment of cancer.Type: GrantFiled: October 14, 1993Date of Patent: February 13, 1996Assignee: Pfizer Inc.Inventors: Jotham W. Coe, Anton F. J. Fliri, Takushi Kaneko, Eric R. Larson
-
Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
-
Patent number: 5461026Abstract: The present invention relates to novel pyridinesulfonylurea derivatives, having a herbicidal activity, which is described in the following structure of general formula (I) ##STR1## wherein, Q is Q-1, Q-2, Q-3 or Q-4 as follows; ##STR2## E is single bond or CH.sub.2 R.sup.2 is C.sub.1 -C.sub.6 alkyl substituted with 1 to 3 halogens;R.sup.1, R.sup.3, W and A are defined in the claims; and these may be an agriculturally suitable salt.Type: GrantFiled: November 29, 1993Date of Patent: October 24, 1995Assignee: Korea Research Institute of Chemical TechnologyInventors: Dae-Whang Kim, Hae Sung Chang, Jae Wook Ryu, In Ho Jo
-
Patent number: 5440040Abstract: The present invention is directed to compounds of formula (I), ##STR1## wherein R.sup.1 is OH, NH.sub.2 ; R.sup.2 is a heteroaromatic or aromatic substituent; R.sup.3 is H, OH, F, OCH.sub.3 ; R.sup.4 is H, F, OH or an ether or ester residue thereof, OCH.sub.3, CN, C.dbd.CH, N.sub.3 ; R.sup.5 is OH or an ether or ester residue thereof including mono, di- and triphosphate esters (.alpha.), wherein n is 0 or 1 and M is hydrogen or a pharmaceutically acceptable counterion such as sodium, potassium, ammonium or alkylammonium; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising said compounds can be used for therapeutic treatment of virus infections. The present invention is also directed to compounds of formula (I'), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, as intermediates.Type: GrantFiled: January 18, 1991Date of Patent: August 8, 1995Assignee: Medivir ABInventor: Salo Gronowitz
-
Patent number: 5439874Abstract: The invention relates to novel substituted bicyclo[3.1.0]hexanes of the formula ##STR1## in which R.sup.1 represents, e. g., hydroxyl or alkoxy,R.sup.2 to R.sup.8 represent, e. g., hydrogen or alkyl,R.sup.9 and R.sup.10 represent, e.g., methyl or methoxy,X represents, e.g., oxygen,Y represents, e.g., oxygen or sulphur andZ represents, e.g., CH or N,as well as salts of the free acid (R.sup.1 =OH) and their further functional derivatives, and furthermore to processes and novel intermediates for their preparation, and to their use as herbicides.In addition, a novel process is described for preparing certain 2-keto-bicyclo[3.1.0]hexanes, which are required as intermediates, starting from correspondingly substituted .alpha.,.beta.-unsaturated carbonyl compounds (of the methacrolein type) and .beta.-keto acid esters (of the acetoacetic acid ester type).Type: GrantFiled: July 21, 1993Date of Patent: August 8, 1995Assignee: Bayer AktiengesellschaftInventors: Mark W. Drewes, Rolf Kirsten, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
-
Patent number: 5426110Abstract: The present invention provides novel pyrimidinyl-glutamic acid derivatives and intermediates thereto. Further provided are methods for inhibiting dihydrofolate reductase in mammals and for treating susceptible neoplasms in mammals, particularly humans.Type: GrantFiled: October 6, 1993Date of Patent: June 20, 1995Assignee: Eli Lilly and CompanyInventors: Lynn S. Gossett, Chuan Shih
-
Patent number: 5403814Abstract: N-pyridinesulfonyl-N'-pyrimidinyl- and -triazinyl-ureas of formula I ##STR1## wherein R.sub.1 is hydrogen or fluorine;or R.sub.1 together with R.sub.3 is a C.sub.2 -C.sub.4 alkylene chain;R.sub.3 is hydrogen, fluorine or C.sub.1 -C.sub.3 alkyl;R.sub.2 is hydrogen, fluorine or C.sub.1 -C.sub.3 alkyl;R.sub.4 is hydrogen, fluorine, chlorine or C.sub.1 -C.sub.3 alkyl;R.sub.5 is hydrogen, fluorine, chlorine, C.sub.1 -C.sub.3 alkyl, or C.sub.1 -C.sub.3 alkyl substituted by fluorine or chlorine;R.sub.a is hydrogen or halogen, or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio radical each of which may be unsubstituted or mono- or poly-substituted by halogen;R.sub.b is hydrogen or a C.sub.1 -C.sub.4 alkyl radical;X is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkyl mono- to tri-substituted by halogen, C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkoxy mono- to tri-substituted by halogen;Y is halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkyl mono- to tri-substituted by halogen, C.Type: GrantFiled: April 7, 1994Date of Patent: April 4, 1995Assignee: Ciba-Geigy CorporationInventor: Werner Fory
-
Patent number: 5397781Abstract: The present invention relates to novel 5-(.omega.-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.Type: GrantFiled: February 11, 1993Date of Patent: March 14, 1995Assignee: Mochida Pharmaceutical Company, LimitedInventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
-
Patent number: 5393733Abstract: This invention relates to herbicidal pyridinesulfonylureas which are highly active as preemergence and postemergence herbicides.Type: GrantFiled: April 27, 1993Date of Patent: February 28, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventor: Paul H. Liang
-
Patent number: 5385880Abstract: Herbicidal composition containing a compound having the following formula or its salt: ##STR1## wherein W is an oxygen atom, a sulfur atom, a NH group or a group of the formula, >NC(O)B;Z is a methine group or a nitrogen group;X is a phenyl group which may be substituted or a group having the formula: ##STR2## and n is an integer of from 1 to 3.Type: GrantFiled: September 17, 1992Date of Patent: January 31, 1995Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masahiro Miyazaki, Masafumi Matsuzawa, Keiji Toriyabe, Michiya Hirata
-
Patent number: 5373012Abstract: A 5-fluoro-minoxidil compound and compositions are disclosed which are useful in the treatment of hair growth and cardiovascular disorders. The 5-fluoro-minoxidil compounds have been shown to have increased transdermal transport than minoxidil and therefore can be used in decreased amounts to achieve the same pharmacological efficacy of minoxidil.Type: GrantFiled: May 10, 1993Date of Patent: December 13, 1994Assignee: The Upjohn CompanyInventor: Heinrich J. Schostarez
-
Patent number: 5371062Abstract: The present invention relates to new substituted azines, of the general formula (I) ##STR1## in which n, Q.sup.1, Q.sup.2, Q.sup.3, R.sup.1, R.sup.2, R.sup.3, X, Y and Z have the meanings given in the description, to a plurality of processes for their preparation, and to their use as herbicides.Type: GrantFiled: April 1, 1993Date of Patent: December 6, 1994Assignee: Bayer AktiengesellschaftInventors: Roland Andreee, Mark W. Drewes, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
-
Patent number: 5359080Abstract: There is disclosed an acylacetamide-type yellow coupler having an acyl group represented by formula (I) and a silver halide color photographic material containing same. ##STR1## wherein R.sub.1 represents a monovalent group, Q represents a group of non-metallic atoms required to form together with the C a substituted or unsubstituted 3- to 5-membered cyclic hydrocarbon group or a substituted or unsubstituted 3- to 5-membered heterocyclic group having in the group at least one hetero atom selected from a group consisting of N, 0, S, and P, provided that R.sub.1 is not a hydrogen atom and does not bond to Q to form a ring.Type: GrantFiled: February 12, 1993Date of Patent: October 25, 1994Assignee: Fuji Photo Film Co., Ltd.Inventors: Yoshio Shimura, Hidetoshi Kobayashi, Yasuhiro Yoshioka
-
Patent number: 5358945Abstract: The present invention relates to pyrimidine compounds represented by the formula ##STR1## (wherein X is a substituted or a cyclic amino group and Y is a substituted amino group or a substituted carbonyl group) or their pharmaceutically acceptable salts, and a therapeutic agent for neurological diseases comprising the compounds.These compounds are useful for treatment of various disorders in nervous systems since they are effective on growth of neurons and promotion of the formation and elongation of neutrites.Type: GrantFiled: March 30, 1992Date of Patent: October 25, 1994Assignees: Mitsui Petrochemical Industries, Ltd., Mitsui Pharmaceuticals, Inc.Inventors: Akira Mizuchi, Ken Ikeda, Yuichiro Kokubun, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Noriaki Kihara
-
Patent number: 5356862Abstract: The invention relates to herbicidal sulfonylurea compounds, agriculturally suitable compositions thereof and a method for their use as general or selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: July 22, 1992Date of Patent: October 18, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventor: William T. Zimmerman
-
Patent number: 5342823Abstract: N-Arylsulfonyl-N'-pyrimidinyl-and N'-triazinylureas of formula I ##STR1## wherein Q is ##STR2## R is hydrogen or methyl; R.sub.1 is hydrogen, fluoro, chloro, C.sub.1 -C.sub.4 alkyl or methoxy;R.sub.2 is hydrogen, fluoro or chloro;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are each independently of one another hydrogen or C.sub.1-C.sub.4 alkyl;R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are each independently of one another hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.13, R.sub.14, R.sub.15, R.sub.16 and R.sub.17 are each independently of one another hydrogen or C.sub.1 -C.sub.4 alkyl;Z is methyl or 2-pyridyl;E is methine or nitrogen;X is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkylthio,C.sub.2 -C.sub.5 alkoxyalkyl, C.sub.2 -C.sub.5 alkoxyalkoxy, C.sub.2 -C.sub.5 alkylthioalkyl or cyclopropyl;Y is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.Type: GrantFiled: February 17, 1993Date of Patent: August 30, 1994Assignee: Ciba-Geigy CorporationInventors: Rainer Kuhlmeyer, Werner Topfl, Werner Fory
-
Patent number: 5332833Abstract: The .beta.-oxo-.beta.-benzenepropanethioamide derivative of the present invention has potassium channel opening action and is useful for treatment of hypertension, asthma, hypersensitive colon syndrome, and enteritis through pharmacological actions including blood vessel dilation, bronchial tract dilation, relaxation of gastrointestinal tract smooth muscle, and the like. The present invention also includes a pharmaceutical composition containing, as the active ingredient, the compound of the present invention and a method for producing the same.Type: GrantFiled: December 23, 1992Date of Patent: July 26, 1994Assignee: Mitsubishi Kasei CorporationInventors: Tetsuo Sekiya, Mikio Tsutsui, Tetsuro Shimpuku, Tatsuo Nagano, Junko Hayashi, Asami Seino
-
Patent number: 5324710Abstract: Compounds of the formula I or their salts ##STR1## in which R.sup.1 to R.sup.6, W, X, a and b are as defined in claim 1 and L is a heterocyclic or isocyclic aromatic radical having 5 to 6 ring atoms, which can be condensed with an aromatic or non-aromatic 5- or 6-membered ring, where the radical can be unsubstituted or substituted, and a, b and c independently of one another are 0 or 1, are suitable as herbicides, plant growth regulators and fungicides. They can be prepared by the processes defined herein, it being possible in some cases to use novel intermediates.Type: GrantFiled: April 21, 1992Date of Patent: June 28, 1994Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
-
Patent number: 5317021Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.Type: GrantFiled: November 4, 1992Date of Patent: May 31, 1994Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
-
Patent number: 5304555Abstract: This invention provides novel pyrimidines or their pharmaceutically acceptable salts thereof and process for preparation thereof. The novel compounds are useful for neurological diseases of the peripheral and central nervous systems of animals.Type: GrantFiled: October 19, 1990Date of Patent: April 19, 1994Assignees: Mitsui Petrochemical Industries, Ltd., Mitsui Pharmaceuticals, Inc.Inventors: Akira Awaya, Kazutoshi Horikomi, Tadayuki Sasaki, Hisashi Kobayashi, Akira Mizuchi, Takuo Nakano, Ikuo Tomino, Shintaro Araki, Mitsuyuki Takesue, Koji Kato, Keiichi Yokoyama
-
Patent number: 5300510Abstract: The present invention relates to minoxidil aceturate corresponding to the formula I ##STR1## The invention also encompasses the process for preparing minoxidil aceturate, as well as its use as an active principle in dermato-cosmetic compositions, especially in hair-care compositions intended for the treatment of alopecia.Type: GrantFiled: January 29, 1993Date of Patent: April 5, 1994Assignee: NorchimInventors: Jean-Pierre Allaigre, Jacques Desbois
-
Patent number: 5292744Abstract: The invention relates to the use of certain 1-[2-pyri(mi)dyl]-5-hydroxy-pyrazoles which are characterized by formula (I) given in the description, as microbicides for the protection of industrial materials, and to certain novel 1-[2-pyri(mi)dyl]-5-hydroxy-pyrazoles which are characterised by formula (II) given in the description.Type: GrantFiled: August 12, 1992Date of Patent: March 8, 1994Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Michael Schwamborn, Peter Wachtler, Monika Frie, Georg-Wilhelm Ludwig, Wilfried Paulus, Hans-Georg Schmitt
-
Patent number: 5292740Abstract: The novel sulfonamides of formula I, ##STR1## in which the symbols R.sup.1 -R.sup.9, R.sup.a, R.sup.b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.Type: GrantFiled: June 9, 1992Date of Patent: March 8, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Kaspar Burri, Martine Clozel, Walter Fischli, Georges Hirth, Bernd-Michael Loffler, Werner Neidhart, Henri Ramuz
-
Patent number: 5284945Abstract: The process according to the invention for the preparation of herbicidal pyridylsulfonylureas of the formula (I) ##STR1## in which R.sup.1 to R.sup.5 and X are as defined in claim 1 comprises the reaction of the zwitterion (II) with the amino heterocycle (III) ##STR2## The novel zwitterionic 1,1,3-trioxo-1,2,4-thiadiazolo[4,5-a]pyridines can be obtained according to the invention by the reaction of phosgene with compounds IV, or the reaction of phosgene with compounds V ##STR3## in the presence of an alkyl isocyanate.Type: GrantFiled: February 26, 1993Date of Patent: February 8, 1994Assignee: Hoechst AktiengesellschaftInventor: Heinz Kehne
-
Patent number: 5280009Abstract: Pyrimidine derivatives of the Formula Ia or Ib ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen or alkyl;A is a substituted or unsubstituted bi- or tricyclic carbo- or heterocyclic radical which may contain one or several double bonds;R.sup.5 is H or alkyl;X is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or haloalkylthio; and addition salts thereof with organic or inorganic acids and the use of said pyrimidine derivative to control undesirable plant growth.Type: GrantFiled: July 16, 1992Date of Patent: January 18, 1994Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Klaus Ditrich, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
-
Patent number: 5262416Abstract: Insecticidal and fungicidal substituted 2-[6-(pyrimidinyl)-indol-1-yl]-acrylic esters of the formula ##STR1## in which R.sup.1 represents alkyl, or represents optionally substituted aralkyl,R.sup.2 represents dialkylamino, alkoxy or alkylthio, or represents in each case optionally substituted aralkyloxy or arylalkylthio,R.sup.3 and R.sup.4 in each case independently of one another represent hydrogen, cyano, halogen or alkyl,R.sup.5, R.sup.6 and R.sup.8 represent hydrogen or other radicals, andR.sup.7 represents optionally substituted pyrimidinyl. The corresponding acetic acid esters are also active.Type: GrantFiled: September 23, 1992Date of Patent: November 16, 1993Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Alexander Klausener, Dieter Berg, Ulrike Wachendorff-Neumann, Christoph Erdelen, Gerd Hanssler, Wilhelm Brandes, Stefan Dutzmann
-
Patent number: 5260293Abstract: The present invention provides pyrazines, pyridazines or pyrimidines, or salts or prodrugs thereof, substituted on one of the ring carbon atoms thereof with a non-aromatic azacyclic or azabicyclic ring system; and independently substituted on each of the other ring carbon atoms with a substituent of low lipophilicity or a hydrocarbon substituent; which compounds stimulate central muscarinic acetylcholine receptors and therefore are useful in the treatment of neurological and mental illnesses.Type: GrantFiled: October 10, 1991Date of Patent: November 9, 1993Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Leslie J. Street, John Saunders
-
Patent number: 5250517Abstract: Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.Type: GrantFiled: May 4, 1992Date of Patent: October 5, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albrecht Edenhofer, Eva-Maria Gutknecht, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
-
Patent number: 5223505Abstract: This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.Type: GrantFiled: April 20, 1990Date of Patent: June 29, 1993Assignee: Imperial Chemical Industries PlcInventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
-
Patent number: 5221315Abstract: N-Pyridinesulfonyl-N'-pyrimidinyl- and -triazinylureas of the formula I ##STR1## in which R.sub.1 and R.sub.2 independently of one another are hydrogen, C.sub.1 -C.sub.8 alkyl or C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.8 alkyl or C.sub.3 -C.sub.8 cycloalkyl substituted by halogen; C.sub.1 -C.sub.8 alkyl or C.sub.3 -C.sub.8 cycloalkyl substituted by --NR.sub.5 R.sub.6, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkyl-S(O).sub.n --; C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl substituted by C.sub.2 -C.sub.4 alkenyl, C.sub.5 -C.sub.6 cycloalkenyl, C.sub.2 -C.sub.6 alkynyl or C.sub.4 -C.sub.8 alkadienyl; or C.sub.2 -C.sub.4 alkenyl, C.sub.5 -C.sub.6 cycloalkenyl and C.sub.4 -C.sub.8 alkadienyl substituted by halogen; or R.sub.1 and R.sub.2 together are a 4-5-membered C.sub.4 -C.sub.10 alkylene chain which can be interrupted by oxygen, sulfur or N--R.sub.7 ; R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 - C.sub.4 alkylthio; C.sub.1 -C.sub.4 alkyl, C.sub.Type: GrantFiled: May 24, 1991Date of Patent: June 22, 1993Assignee: Ciba-Geigy CorporationInventors: Werner Fory, Rolf Schurter
-
Patent number: 5221316Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: February 19, 1992Date of Patent: June 22, 1993Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
-
Patent number: 5213608Abstract: Herbicidal substituted sulphonylamidinohydrazones of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted aryl, aralkyl or heteroaryl,R.sup.2 represents hydrogen, or represents in each case optionally substituted alkyl, aryl or aralkyl,R.sup.3 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkadienyl, alkinyl, (hetero)aryl, aralkyl, aralkenyl, alkoxy, alkoxycarbonyl or dialkylamino, or together with R.sup.2 represents optionally substituted alkanediyl,R.sup.4 represents hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X represents nitrogen or a --CH group,Y represents nitrogen or a --CR.sup.5 group whereR.sup.5 represents hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl, andZ represents nitrogen or a --CR.sup.6 group whereR.sup.Type: GrantFiled: July 16, 1992Date of Patent: May 25, 1993Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Ernst R. F. Gesing, Rolf Kirsten, Joachim Kluth, Reinhard Lantzsch, Klaus-Helmut Muller, Theodor Pfister, Hans-Jochem Riebel, Frank Rosenfeldt, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
-
Patent number: 5209770Abstract: This invention relates to herbicidal pyridinesulfonylureas which are highly active as preemergence and postemergence herbicides.Type: GrantFiled: December 13, 1991Date of Patent: May 11, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventor: Paul H. Liang
-
Patent number: 5166206Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.Type: GrantFiled: March 27, 1991Date of Patent: November 24, 1992Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
-
Patent number: 5153324Abstract: A process for preparing herbicidal sulfonylureas which comprises mixing a sulfonylisocyanate and a heterocyclic amine in the absence of a solvent.Type: GrantFiled: December 26, 1991Date of Patent: October 6, 1992Assignee: E. I. du Pont de Nemours and CompanyInventor: Teddy H. Grindstaff
-
Patent number: 5149357Abstract: Compound of the formula ##STR1## in which A is O, S, or NR.sup.3 ; G is CH or N; R and R.sup.1 are independently alkyl, alkoxy, haloalkoxy or alkylamino; R.sup.2 is phenyl, substituted phenyl, alkyl, cycloalkyl, haloalkyl or --CH.sub.2 [(R.sup.4)C(R.sup.5).sub.n --Z; R.sup.3 and R.sup.7 are, independently, hydrogen, alkyl, --C(O)NH.sub.2 or --C(O)alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, or halogen; R.sup.6 is halogen, alkyl, alkoxy, haloalkoxy, NO.sub.2, amino, alkyl substituted amino, or acyl substituted amino; n is 0 to 5; Z is cyano, amino, alkylamino, dialkylamino, --NHCO.sub.2 alkyl, alkoxy, alkylthio, alkylsulfonyl, alkenyl, alkynyl, phenyl or substituted phenyl; and Q is hydrogen, halogen, alkyl, alkoxy, haloalkoxy, nitro, amino, haloalkyl, alkythio, alkylsulfonyl, phenyl, substituted phenyl or phenoxy; or a 5 or 6 membered aromatic heterocycle having the formula ##STR2## in which "m" is 0 or 1; A' is O, S, or NR.sup.Type: GrantFiled: June 19, 1990Date of Patent: September 22, 1992Assignee: FMC CorporationInventors: John A. Dixson, Natesan Murugesan, Keith D. Barnes
-
Patent number: 5147876Abstract: 2,6-di-, 2,4,6-, 2,5,6-tri- or 2,4,5,6-tetra-substituted pyrimidines, and 2,6-di-substituted pyridines. These compounds are useful for treatment of neurological diseases.Type: GrantFiled: December 29, 1989Date of Patent: September 15, 1992Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Akira Mizuchi, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Mitsuyuki Takesue, Noriaki Kihara
-
Patent number: 5145967Abstract: The present invention is directed to a method for preparing a 4-alkoxyalkyl-4-phenylaminopiperidine compound which comprises the steps of (a) reacting an N-substituted-4-piperidone compound with an aniline compound to form a Schiff base compound, (b) reacting the Schiff base compound with an anionic reagent having an anion stabilizing group to form an amine compound, and (c) reducing the amine compound in step (b) with a reducing agent to displace the anion stabilizing group.The anionic reagent in step (b) above has the general formula:X--CYM--Zwherein X is an anion stabilizing group, Y is hydrogen or lower-alkyl, Z is lower-alkoxy or phenylmethoxy, M is an alkali or alkaline earth metal, and C is a carbon atom.Type: GrantFiled: November 2, 1990Date of Patent: September 8, 1992Assignee: Anaquest, Inc.Inventors: Bor-Sheng Lin, H. Kenneth Spencer, Joseph W. Scheblein
-
Patent number: 5141941Abstract: Disclosed are a compound of the formula (I) or an acid addition salt thereof: ##STR1## wherein Q represents R.sup.1 , R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n and z are defined as in the specification, preparation method thereof and fungicides containing the same.Type: GrantFiled: November 15, 1989Date of Patent: August 25, 1992Assignee: Ube Industries, Ltd.Inventors: Katsutoshi Fujii, Toshinobu Tanaka, Yasuhisa Fukuda
-
Patent number: 5136080Abstract: A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.Type: GrantFiled: June 5, 1990Date of Patent: August 4, 1992Assignee: Burroughs Wellcome Co.Inventors: Alistair A. Miller, Malcolm S. Nobbs, Richard M. Hyde, Michael John
-
Patent number: 5129941Abstract: Sulfonylureas of the formula ##STR1## where A is a bond or a C.sub.1 -C.sub.10 -hydrocarbon radical,R.sup.1 is an optionally unsaturated hydrocarbon radical which is optionally substituted by halogen, optionally unsaturated alkoxy, alkylthio, alkylsulfonyl or alkylsulfinyl, cycloalkyl, optionally substituted phenyl or a heterocycle, or is optionally substituted phenyl, NRR' with R and R' being alkyl, alkoxy or alkylene (cyclic with N),Y is S, SO or SO.sub.2,R.sup.1 is optionally unsaturated alkoxy which is optionally substituted, or is cycloalkoxy, cycloalkenyloxy, cyclopropylmethyloxy, epoxypropyloxy, furfuryloxy, tetrahydrofurfuryloxy or optionally substituted phenoxyalkoxy or phenoxy,R.sup.3 is alkyl which is optionally unsaturated, or is alkoxy,R.sup.4 is optionally substituted pyrimidinyl, pyrimidinylmethyl, pyrimidinyl with a fused-on cyclopentane, oxolane, oxolene, oxane, pyridine or pyrazine ring or purinyl or triazolyl, andZ is O or S,have herbicidal and/or plant-growth-regulatory properties.Type: GrantFiled: July 17, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Heinz-Josef Loher, Lothar Willms, Michael Frey, Klaus Bauer, Hermann Bierigner