Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Patent number: 5527916Abstract: A process for the separation of at least one isomer from a mixture of isomers of a tetrahydropyran-2-one, having at least two chiral centers which comprises selective reaction of at least one isomer with a reagent catalyzed by a hydrolase enzyme whereby at least one isomer is preferentially converted into a distinct chemical species from the other isomers so that it is susceptible of separation by an appropriate chemical or physical separation process in which the tetrahydropyran-2-one is of Formula (1): ##STR1## wherein: Z is --H or a protecting group susceptible of reaction with the reagent under the influence of the enzyme; andY is formyl or protected formyl.Type: GrantFiled: August 1, 1994Date of Patent: June 18, 1996Assignee: Zeneca LimitedInventors: Andrew J. Blacker, John Crosby, John A. L. Herbert
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Patent number: 5523410Abstract: The present invention relates to synthetic intermediates useful for preparing amino acid derivatives possessing renin-inhibitory activity, and to processes for preparing the amino acid derivatives using the synthetic intermediates.Type: GrantFiled: January 3, 1995Date of Patent: June 4, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kooji Kagara, Nobutaka Kawai, Koji Machiya, Tetsuo Furutera, Takashi Nakamura, Hiroki Omori
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Patent number: 5521317Abstract: There is disclosed a process for the preparation of an indanylamine compound of general formula ##STR1## wherein R.sup.1 represents an optionally substituted alkyl group, and R.sup.2, R.sup.3 and R.sup.4 independently represent a hydrogen atom or an optionally substituted alkyl group, the process including the steps of hydrogenating a compound of general formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described above and R.sup.5 and R.sup.6 independently represent a halogen atom, a hydroxyl, nitro or cyano group, or an optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylcarboxy or alkylamino group provided that R.sup.5 and R.sup.6 represent different atoms or groups, and subsequent rearrangement and derivatization of the product thereof. Compounds of general formula I may be used to prepare preferred stereoisomers of fungicidal N-indanyl carboxamide compounds.Type: GrantFiled: October 12, 1994Date of Patent: May 28, 1996Assignee: American Cyanamid Co.Inventor: Paul H. Briner
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Patent number: 5516913Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: May 12, 1995Date of Patent: May 14, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5510530Abstract: The invention relates to new optically active sulphur-containing amino acid derivatives, a process for their preparation, their polymerization to give optically active polymers and the use of these optically active polymers as adsorbents for chromatographic separation of racemates into enantiomers.Type: GrantFiled: May 11, 1994Date of Patent: April 23, 1996Assignee: Bayer AktiengesellschaftInventors: Michael Grosse-Bley, Bruno Bomer, Rolf Grosser, Dieter Arlt, Walter Lange
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Patent number: 5508450Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.Type: GrantFiled: September 30, 1994Date of Patent: April 16, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5506237Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the carbon and nitrogen atoms to which it is attached, a heterocycle,B represents, with the nitrogen atom to which it is attached, a heterocycle,n is equal to 1, 2, 3 or 4,R represents phenyl substituted by at least one halogen or alkyl, hydroxyl, alkoxy, trifluoromethyl, nitro, amino, cyano, carboxyl or alkoxycarbonyl, benzyl, thienyl or pyridyl. The compounds may be used as medicaments.Type: GrantFiled: March 23, 1994Date of Patent: April 9, 1996Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Bernard Protevin, Georges Remond, Jean Lepagnol, Veronique Heidet
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Patent number: 5506190Abstract: The present invention relates to 3,4,5,6-tetrahydrophthalamide derivatives and 3,4,5,6-tetrahydroisophthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof.More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetrahydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): ##STR1## These tetrahydrophthalamide derivatives and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment.Type: GrantFiled: September 19, 1994Date of Patent: April 9, 1996Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co. Ltd.Inventors: Kenji Hirai, Tomoko Matsukawa, Tomoyuki Yano, Emiko Ejiri, Kiyomi Aizawa, Koichi Shikakura, Tomoko Yoshii, Sadayuki Ugai, Osamu Yamada, Shigeki Kishi
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Patent number: 5504057Abstract: Dialkyl-1-H-3-(2,4-dimethylphenyl)-pyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents alkyl which is optionally substituted by halogen andB represents C.sub.2 -C.sub.10 -alkyl orA and B together with the carbon atom to which they are bonded represent an unsubstituted cycle,G represents hydrogen (a) or the groups ##STR2## E represents a metal ion equivalent or an ammonium ion, L and M represent oxygen and/or sulphur. These compounds possess herbicidal and pesticidal activity.Type: GrantFiled: February 22, 1994Date of Patent: April 2, 1996Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Patent number: 5495023Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: May 3, 1994Date of Patent: February 27, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5480897Abstract: The use of nicotinic anilide derivatives of the general formula ##STR1## where the substituents have the following meanings: R.sup.1 halogen, methyl, trifluoromethyl, methoxy, methylthio, methylsulfinyl, methylsulfonylR.sup.2 unsubstituted or halogen-substituted alkyl, unsubstituted or halogen-substituted alkenyl, alkynyl, unsubstituted or halogen-substituted alkoxy, unsubstituted or halogen-substituted alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxyfor combating Botrytis, and nicotinic anilides of the formula I.Type: GrantFiled: March 21, 1994Date of Patent: January 2, 1996Assignee: BASF AktiengesellschaftInventors: Karl Eicken, Norbert Goetz, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz, Harald Rang
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Patent number: 5481005Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.Type: GrantFiled: November 28, 1994Date of Patent: January 2, 1996Assignee: SanofiInventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
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Patent number: 5474999Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.Type: GrantFiled: October 26, 1994Date of Patent: December 12, 1995Assignee: Imperial Chemical Industries PLCInventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5475113Abstract: Compounds of the formula ##STR1## as herein defined, have retinoid-like activity and are substantially non-teratogenic and non-irritating to the skin.Type: GrantFiled: June 15, 1994Date of Patent: December 12, 1995Assignee: Allergan, Inc.Inventor: Roshantha A. Chandraratna
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Patent number: 5466708Abstract: Novel compounds of the formula ##STR1## wherein Q, R.sup.1 and R.sup.2 are described herein, are disclosed along with pharmaceutical compositions, methods of use, and process for producing compounds of formula I which starts from the corresponding .beta.-hydroxycarboxylic acids.Type: GrantFiled: September 19, 1994Date of Patent: November 14, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
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Patent number: 5459131Abstract: Renin inhibiting compounds of the formula: ##STR1## wherein A is a moiety selected from those of the formula: ##STR2## where Z is O, S, SO, or SO.sub.2, P is 1 or 2 and X is --O-- or --S--; and analogs thereof which inhibit the substrate-cleaving acting of renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.Type: GrantFiled: March 15, 1991Date of Patent: October 17, 1995Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Charles F. Howell
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Patent number: 5458814Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds having certain substituents at the number 5 and 6 carbon atoms of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: December 9, 1993Date of Patent: October 17, 1995Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, Barry Van Gemert, David B. Knowles
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Patent number: 5451678Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)-, --N(acyl)- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: September 29, 1993Date of Patent: September 19, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5432189Abstract: Bis-aryl amide and urea compounds of the general formula: ##STR1## wherein X is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor. Pharmaceutical compositions containing the compounds and methods of treating platelet activating factor associated conditions are also included.Type: GrantFiled: May 24, 1994Date of Patent: July 11, 1995Assignee: American Cyanamid CompanyInventor: Allan Wissner
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Patent number: 5432175Abstract: Pyridine and pyridine N-oxide derivatives of diaryl methyl piperidines or piperazines and pharmaceutically acceptable salts thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Pharmaceutical compositions containing and methods of using the compounds are also described.Type: GrantFiled: April 1, 1993Date of Patent: July 11, 1995Assignee: Schering CorporationInventors: John J. Piwinski, Jesse Wong, Michael J. Green, Vera Seidl, Richard Friary
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Patent number: 5426118Abstract: Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.7 are hydrogen, lower alkyl of 1-6 carbons, or halogen;Y is phenyl, pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl;A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.14, CR.sub.14 (OR.sub.12).sub.2, or CR.sub.14 OR.sub.13 O, where R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.Type: GrantFiled: December 30, 1993Date of Patent: June 20, 1995Assignee: Allergan, Inc.Inventors: Roshantha A. Chandraratna, Richard L. Beard
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Thiazolidinyl-terminated non-peptidyl .alpha.-succinamidoacyl aminodiols as anti-hypertensive agents
Patent number: 5418249Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a thiazolidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: January 25, 1994Date of Patent: May 23, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran -
Patent number: 5411974Abstract: Heterocyclic compounds of the general formula: ##STR1## wherein, Z represents methylene group or sulfur atom, R represents a general formula:G--E--D--B--A--.Type: GrantFiled: June 27, 1994Date of Patent: May 2, 1995Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5411976Abstract: New thiazolidine derivatives of the general formula: ##STR1## wherein X stands for a proline or thioproline residue and R for --CH.sub.2 OH or --CHO, a process for preparing the same which comprises reacting N-benzyloxycarbonyl-L-proline or --L-thioproline with L-thioprolinol and, if necessary, oxidizing the resultant N-benzyloxycarbonyl-L-prolyl-L-thioprolinol or --L-thioprolyl-L-thioprolinol to the corresponding thioprolinal compound, and an anti-amnestic composition containing at least one of the thiazolidine derivatives together with a conventional excipient. The new thiazolidine derivatives are extremely strong in anti-amnestic activity when compared with known similar anti-amnestic agents.Type: GrantFiled: December 19, 1991Date of Patent: May 2, 1995Assignee: Kabushiki Kaisha Yakult NonshaInventors: Kunio Kado, Toshizo Shiga
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Patent number: 5407950Abstract: Arylalkanoylamine derivatives having excellent prolyl endopeptidase inhibitory action and resistances to hypoxia and amnesia which are represented by the following general formula (I): ##STR1## wherein A represents an indanyl, indenyl, 1,2,3,4-tetrahydronaphthalenyl or benzofuranyl group; m represents an integer of 0 to 5; Z represents a hydroxymethyl, formyl, nitrile, hydroxyiminomethyl, semicarbazonomethyl or dialkoxymethyl group; X and Y may be the same or different, and individually represent a methylene group or sulfur atom, wherein compounds defined by the following substituents are excluded: A represents an indanyl, indenyl, or 1,2,3,4-tetrahydronaphthalenyl group; X and Y each represent a methylene group; and Z represents a hydroxymethyl or formyl group. Also disclosed is a pharmaceutical composition and method for improving mneme, cerebral circulation and cerebral metabolism comprising the arylalkanoylamine derivatives as the effective ingredient.Type: GrantFiled: December 7, 1992Date of Patent: April 18, 1995Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Akihiro Okubo, Hiroyasu Nishioka, Heihachiro Arai, Yoshiaki Tanaka, Hisayoshi Kato, Naoki Nakata
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Patent number: 5401760Abstract: Heterocyclic compounds of the general formula: ##STR1## R represents a general formula:G--E--D--B--A--G represents a carbocyclic or heterocyclic ring which is unsubstituted or substituted, L represents a group of general formula:--CO--COR.sup.2--CO--CH.sub.2 --COR.sup.2--CO--CF.sub.2 --COR.sup.2--CO--CO--NR.sup.5 R.sup.6or--CO--CH.sub.2 --CO--NR.sup.5 R.sup.6and non-toxic salt or hydrate thereof possess an inhibitory activity on propyl endopeptidase, and therefore usefull for prevention and/or treatment of amnesia.Type: GrantFiled: January 22, 1993Date of Patent: March 28, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5393766Abstract: Thiazolyl-5-carbonamide derivatives of formula I ##STR1## wherein R.sub.3 is furanyl or thienyl and R.sub.1 and R.sub.2 are as defined herein, have valuable microbicidal activity. They can be used in the form of compositions for controlling or preventing plant diseases.Type: GrantFiled: January 25, 1993Date of Patent: February 28, 1995Assignee: Ciba-Geigy CorporationInventor: Adolf Hubele
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Patent number: 5385902Abstract: Antimicrobial compounds of the formula ##STR1## wherein A is selected from the group consisting of alkyl; phenyl; alkoxy; phenoxy; benzyloxy; monoalkylamino; dialkylamino; cyclic amino, anilino; heterocyclic; amino substituted with heterocyclic ring, methods of making and using said compounds, and compositions comprising said compounds are disclosed.Type: GrantFiled: September 1, 1993Date of Patent: January 31, 1995Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5385922Abstract: Thiazolidine derivatives containing at least one organic nitrate ester group have cardiovascular activity.Type: GrantFiled: March 4, 1993Date of Patent: January 31, 1995Assignee: Cedona Pharmaceuticals B.V.Inventors: Jan Bron, Geert J. Sterk, Hendrik Timmerman, Jan. F. Van Der Werf
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Patent number: 5354867Abstract: Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.Type: GrantFiled: April 15, 1993Date of Patent: October 11, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: David J. Carini, John Jonas V. Duncia, Pancras C. Wong
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Patent number: 5350759Abstract: Bis-aryl amide and urea compounds of the general formula: ##STR1## wherein X is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor. Pharmaceutical compositions containing the compounds and methods of treating platelet activating factor associated conditions are also included.Type: GrantFiled: April 5, 1993Date of Patent: September 27, 1994Inventor: Allan Wissner
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Patent number: 5347042Abstract: The invention relates to new optically active sulphur-containing amino acid derivatives, a process for their preparation, their polymerisation to give optically active polymers and the use of these optically active polymers as adsorbents for chromatographic separation of racemates into enantiomers.Type: GrantFiled: June 11, 1992Date of Patent: September 13, 1994Assignee: Bayer AktiengesellschaftInventors: Michael Grosse-Bley, Bruno Bomer, Rolf Grosser, Dieter Arlt, Walter Lange
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Patent number: 5324723Abstract: 1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system.Type: GrantFiled: July 1, 1993Date of Patent: June 28, 1994Assignee: Merck Sharpe & Dohme Ltd.Inventors: Raymond Baker, John Saunders, Roger J. Snow, Graham A. Showell
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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: 5312831Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 12, 1993Date of Patent: May 17, 1994Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5290799Abstract: 7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula ##STR1## wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or ##STR2## wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is ##STR3## then Y cannot be O, and when Z is --CH.dbd.CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO.sub.2 H, CO.sub.2 lower alkyl, CH.sub.2 OH, CO.sub.2 alkali metal, CONHSOR.sup.3, CONHR.sup.3a or --CH.sub.2 -5-tetrazolyl, X is O, S or NH; and where R.sup.1, R.sup.2, R.sup.3 and R.sup.3a are as defined herein.Type: GrantFiled: September 19, 1990Date of Patent: March 1, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Raj N. Misra, Philip M. Sher, Philip D. Stein, Steven E. Hall, David Floyd, Joel C. Barrish
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Patent number: 5286881Abstract: A benzodifuranone compounds of the formula, ##STR1## wherein R.sup.1 and R.sup.2 are each independently a naphthyl group or an unsubstituted or substituted phenyl group, which is useful for dyeing or printing hydrophobic fiber materials, is prepared in high purity and high yield by allowing benzofuran compounds of the formula, ##STR2## wherein R.sup.1 is as defined above, to react with acetonitrile compounds of the formula, ##STR3## wherein R.sup.2 is as defined above, and then carrying out an oxidation reaction to give the benzodifuranone compound.Type: GrantFiled: September 30, 1992Date of Patent: February 15, 1994Assignee: Sumitomo Chemical Company LimitedInventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
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Patent number: 5283362Abstract: Process for the preparation of very pure ureas of the formula phenyl--(NH--CO--NR.sub.1 R.sub.2).sub.n in which phenyl represents an unsubstituted or substituted phenyl or phenylene group and R.sub.1 and R.sub.2 are either identical and each represent an alkyl group, or are different, in which case R.sub.1 represents a hydrogen atom and R.sub.2 represents an alkyl or phenyl group, or R.sub.1 and R.sub.2, together with the nitrogen atom, represent an aliphatic heterocyclic ring and n is the number 1 or 2, by reacting a phenylurea of the formula phenyl--(NH--CO--NH.sub.2).sub.n with an amine of the formula NR.sub.1 R.sub.2 H at temperatures from 100 to 200.degree. C. in a diluent which is inert under the reaction conditions, the reaction being interrupted before by-products are formed, and the urea which is formed being removed from the starting compounds, and the unreacted starting compounds being returned to the process if appropriate.Type: GrantFiled: July 31, 1992Date of Patent: February 1, 1994Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Kurt A. Hackl, Heinz Falk
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Patent number: 5272268Abstract: A following dipeptide derivative of the following formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloaklyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.Type: GrantFiled: November 10, 1992Date of Patent: December 21, 1993Assignee: Shionogi & Co., Ltd.Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
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Patent number: 5264577Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.Type: GrantFiled: April 22, 1992Date of Patent: November 23, 1993Assignee: Warner-Lambert CompanyInventors: Vladimir Beylin, Huai G. Chen, Om P. Goel, Mark E. Marlatt, John G. Topliss
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Patent number: 5256632Abstract: Herbicidal sulphonylated carboxamides of the formulaR.sup.1 --CO--NH--SO.sub.2 --(A).sub.n --R.sup.2 (I)in whichn represents the numbers 0 or 1,A represents oxygen, iminio (NH) or methylene (CH.sub.2),R.sup.1 represents a five-membered heteroaryl radical which contains 1 or 2 nitrogen atoms and additionally one oxygen or sulphur atom in the ring and which is optionally substituted by halogen or by alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or phenyl which are in each case optionally substituted, andR.sup.2 represents aryl or heteroaryl which are in each case optionally substituted,or salts thereof, with the exclusion of the compound 2-dimethylamino-N-(4-methyl-phenylsulphonyl)-5-thiazole carboxamide.Type: GrantFiled: June 18, 1992Date of Patent: October 26, 1993Assignee: Bayer AktiengesellschaftInventors: Hilmar Wolf, Rolf Kirsten, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5254575Abstract: The invention concerns a 4-aryl-thiazole or imidazole derivative having the formula I ##STR1## wherein X is 0 or NOH,Y is S or NR.sub.3,Ar is a group selected from phenyl, naphthyl, tetrahydronaphthyl, and biphenyl,R is one to four substituents independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower thioalkyl, cycloalkyl, halogen, CF.sub.3, NO.sub.2, and O-ALK-NR.sub.1 R.sub.2, in which ALK is a saturated aliphatic hydrocarbon group having 2-6 carbon atoms, and R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl, or form, together with the nitrogen atom to which they are bonded, a heterocyclic ring, andR.sub.3 is hydrogen or a lower alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that 4-(4-chlorophenyl)-thiazole-2-carboxamide is excluded.Type: GrantFiled: March 25, 1992Date of Patent: October 19, 1993Assignee: AKZO N.V.Inventors: John H. Pick, Robert T. Logan
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Patent number: 5250501Abstract: A compound of formula (I): ##STR1## or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X.sup.1 and X.sup.2 are independently oxygen or sulphur, R.sup.1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C.sub.2 -C.sub.4 alkylene group which is optionally interposed by an oxygen atom, a group ##STR2## or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and R.sup.b is alkyl or alkoxy; provided that when X, X.sup.1 and X.sup.2 are oxygen R.sup.1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.Type: GrantFiled: January 10, 1992Date of Patent: October 5, 1993Assignees: Imperial Chemical Industries PLC, ICI Americas, Inc.Inventors: John E. D. Barton, David Cartwright, John M. Cox, Glynn Mitchell, Charles G. Carter, David L. Lee, Francis H. Walker, Frank X. Woolard
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Patent number: 5244867Abstract: Oxazole- and thiazolecarboxamides of the formulae Ia and Ib ##STR1## where the substituents have the following meanings: X oxygen or sulfur;R.sup.2 formyl, 4,5-dihydrooxazol-2-yl or --COYR.sup.5 ;Y oxygen or sulfur; andR.sup.4 is methyl and herbicidal agents containing compounds of the formulae Ia or Ib as active ingredients.Type: GrantFiled: December 26, 1991Date of Patent: September 14, 1993Assignee: BASF AktiengesellschaftInventors: Klaus Ditrich, Volker Maywald, Gerhard Hamprecht, Albrecht Harreus, Bruno Wuerzer, Karl-Otto Westphalen
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Patent number: 5231182Abstract: Methods of preparing bis-aryl amide and urea compounds of the general formula: ##STR1## wherein x is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor.Type: GrantFiled: October 4, 1991Date of Patent: July 27, 1993Assignee: American Cyanamid CompanyInventor: Allan Wissner
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Patent number: 5229386Abstract: The invention relates to new thiazole compounds, of antithrombotic, vasodilating, antiallergic, antiinflammatory and 5-lipoxygenase inhibitory activity, of the formula: ##STR1##Type: GrantFiled: March 10, 1992Date of Patent: July 20, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hisashi Takasugi, Shigetaka Nishino, Akito Tanaka
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Patent number: 5228898Abstract: This invention relates to substituted bicycloheptadione derivatives with high herbicidal activity which are represented by general formula (I) ##STR1## (where R.sup.1 is a lower alkyl group, a phenyl group which may be substituted, an aralkyl group which may be substituted, or a heterocyclic group which may be substituted;R.sup.2 is, same or different, a halogen, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an alkyl group, an alkoxyalkyl group, or an alkoxylcarbonyl group, and n is 0 to 4;R.sup.3 and R.sup.4 are, same or different, hydrogen or a lower alkyl group).Type: GrantFiled: February 3, 1992Date of Patent: July 20, 1993Assignee: Nippon Soda Co., Ltd.Inventors: Akiyoshi Ueda, Shigemi Suga, Hiroyuki Adachi, Toshio Aihara, Kazuyuki Tomida, Hideki Yamagishi, Hideo Hosaka
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Patent number: 5225425Abstract: Bis-aryl amide and urea compounds of the general formula: ##STR1## wherein X is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor. Pharmaceutical compositions containing the compounds and methods of treating platelet activating factor associated conditions are also included.Type: GrantFiled: April 14, 1992Date of Patent: July 6, 1993Assignee: American Cyanamid CompanyInventor: Allan Wissner
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Patent number: 5223489Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl optionally substituted aryl; or amino optionally substituted; andR.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted;R.sup.3 is hydrogen or lower alkyl; andR.sup.Type: GrantFiled: January 30, 1992Date of Patent: June 29, 1993Assignee: Ujisawa Pharmaceutical Co., Ltd.Inventors: Keiji Hemmi, Masahiro Neya, Hiroshi Marusawa, Keisuke Imai, Natsuko Kayakiri, Masashi Hashimoto
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Patent number: 5214045Abstract: Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.Type: GrantFiled: July 11, 1990Date of Patent: May 25, 1993Assignee: Richter Gedeon Vegyeszeti Gyar RTInventors: Tamas Fodor, Janos Fischer, Laszlo Dobay, Elemer Ezer, Judit Matuz, Laszlo Szporny, Gyorgy Hajos