Patents Examined by Catherine Scalzo
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Patent number: 5288724Abstract: There are disclosed novel ergoline derivatives of 2-propinylamine of the general formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group,X represents a hydrogen or a halogen atom,Z represents a carbonyl or methylene group andC.sub.9 C.sub.10 represents a single or a double bond, diastereomeric forms, racemates and acid addition salts thereof.There are also described a process for the manufacture of the compounds of the general formula I and a pharmaceutical composition containing the same.The compounds of the general formula I can be used in the pharmaceutical industry as active substances for the manufacture of medicaments used in the treatment of hypertension, migraine, anxiety states, depressions, obesity etc.Type: GrantFiled: June 22, 1992Date of Patent: February 22, 1994Assignee: LEK, tovarna farmacevtskihInventors: Rudolf Rucman, Breda Bole-Vunduk, Magdalena Ocvirk, Bogomila Lavric, Igor Krisch
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Patent number: 5284953Abstract: A diastereomer salt of optically active quinolinemevalonic acid of the formula ((-)I.Type: GrantFiled: June 23, 1992Date of Patent: February 8, 1994Assignee: Nissan Chemical Industries Ltd.Inventors: Yoshio Ohara, Mikio Suzuki, Yoshinobu Yanagawa, Hiroshi Iwasaki, Nobuhide Miyachi
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Patent number: 5283330Abstract: The present invention is directed to the compound 1,2-benzo-8-(D,L alanyl)-3-phenoxazone nitrate and to the method for preparing this compound.Type: GrantFiled: September 11, 1992Date of Patent: February 1, 1994Inventor: Kantilal G. Bhansali
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Patent number: 5273972Abstract: This invention provides novel 2-substituted-3-quinuclidinyl arylcarboxamides and arylthiocarboxamides and corresponding arylcarboxylates which have utility as therapeutic agents which exhibit gastric prokinetic, antiemetic, anxiolytic and 5-HT (serotonin) antagonist effects in warm blooded animals.Illustrative of an invention compound is 5-chloro-2-methoxy-4-(methylamino)-N-[2-(1-piperidinylmethyl)-1-azabicyclo [2.2.2]oct-3-yl]benzamide: ##STR1## or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 26, 1992Date of Patent: December 28, 1993Assignee: A. H. Robins Company, IncorporatedInventors: Gunnar E. Jagdmann, Harry R. Munson, Jr.
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Patent number: 5273994Abstract: The invention relates to the derivatives of general formula (I): ##STR1## in which: Z represents an oxygen atom or a sulfur atom,R.sub.1 represents a hydrogen atom or an alkyl group,R.sub.2 represents a hydrogen atom or an alkyl group,1.ltoreq.n.ltoreq.6,R.sub.3 represents a nitrile group, an optionally substituted amino group or any one of the groups described in the description, andmedicinal products containing the same.Type: GrantFiled: October 9, 1992Date of Patent: December 28, 1993Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Beatrice Guardiola
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Patent number: 5264453Abstract: This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts thereof of the structure ##STR1## where R.sup.1, R.sup.2, and R.sup.3 are as defined herein. These compounds are for pharmaceutical use in treating thrombotic diseases, asthma or nephritis.Type: GrantFiled: February 28, 1992Date of Patent: November 23, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Akihiko Sawada, Hirokazu Tanaka, Masashi Hashimoto
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Patent number: 5264452Abstract: A benzofurancarboxamide of the formula: ##STR1## where: X is hydrogen or methoxy,R.sup.1 is a radical of the formula: ##STR2## wherein R.sup.3 to R.sub.5 are each, independently of one another, hydrogen or C.sub.1-6 alkyl, R.sup.6 is a branched or unbranched C.sub.1-6 alkyl, or benzyl which may be methyl- or halogen-substituted on the nucleus, and is a single or double bond.Type: GrantFiled: June 25, 1992Date of Patent: November 23, 1993Assignee: BASF AktiengesellschaftInventors: Rainer Schlecker, Hans-Juergen Teschendorf, Liliane Unger
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Patent number: 5260303Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: March 7, 1991Date of Patent: November 9, 1993Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
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Patent number: 5258392Abstract: The invention relates to a 3-quinuclidine derivative having the formula I ##STR1## wherein X is O or S, and R represents one to five substituents independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower aralkyloxy, lower alkanoyloxy, halogen, NO.sub.2, CF.sub.3, CN, NR.sub.1 R.sub.2, and COR.sub.3, in which R.sub.1 and R.sub.2 are independently selected from hydrogen, lower alkyl, and lower alkanoyl, and R.sub.3 is selected from OH, lower alkyl, lower alkoxy, and NR.sub.4 R.sub.5, wherein R.sub.4 and R.sub.5 are independently hydrogen or lower alkyl; or pharmaceutically acceptable salts thereof.Type: GrantFiled: January 31, 1992Date of Patent: November 2, 1993Assignee: Akzo N.V.Inventors: Johannes H. Wieringa, Sjoerd F. van Aelst, Ralf Plate
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Patent number: 5256334Abstract: Novel radiopaque materials and a method for their preparation are described. The radiopaque materials comprise composites of polymers and heavy metal-containing organic compounds, which heavy metal containing compounds have the following formula: ##STR1## wherein X is a heavy metThis invention was made with Government support under research Grant No. NIH-1-RO1-DEO6179001A1 awarded by the National Institutes of Health. The Government has certain rights in this invention.Type: GrantFiled: February 28, 1992Date of Patent: October 26, 1993Assignee: The Research Foundation of the State University of New YorkInventors: Johannes Smid, Yadollah Delaviz, Israel Cabasso
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Patent number: 5256799Abstract: A novel method for the synthesis of 6-hydroxyindolines and new fluorescent dyes produced therefrom, which dyes are ring-constrained indoline-based rhodamine class dyes. These dyes have absorption and emission spectra which make them particularly useful in certain dye laser applications.Type: GrantFiled: July 14, 1992Date of Patent: October 26, 1993Assignee: The United States of Americas as represented by the United States Department of EnergyInventors: George F. Field, Peter R. Hammond
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Patent number: 5252578Abstract: The invention relates to the derivatives of general formula (I): ##STR1## in which: Z represents an oxygen atom or a sulfur atom,R.sub.1 represents a hydrogen atom or an alkyl group,R.sub.2 represents a hydrogen atom or an alkyl group,1.ltoreq.n.ltoreq.6,R.sub.3 represents a nitrile group, an optionally substituted amino group or any one of the groups described in the description, and medicinal products.Type: GrantFiled: March 29, 1991Date of Patent: October 12, 1993Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Beatrice Guardiola
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Patent number: 5244904Abstract: This invention is directed to a indole derivative represented by the general formula (1) ##STR1## wherein R.sub.1 stands for alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, cycloalkenylalkyl of 5 to 7 carbon atoms, aralkyl of 7 to 14 carbon atoms, trans-alkenyl of 4 to 5 carbon atoms, allyl, furanyl-2-ylalkyl of 1 to 5 carbon atoms, thienyl-2-ylalkyl of 1 to 5 carbon atoms, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, alkanoyl of 1 to 5 carbon atoms, aralkylcarbonyl of 7 to 14 carbon atoms, 2-furoyl, thiophene-2-carbonyl, cycloalkylcarbonyl of 4 to 7 carbon atoms, alkenylcarbonyl of 3 to 8 carbon atoms, or anisoyl, R.sub.2 for a hydrogen atoms, alkyl of 1 to 3 carbon atoms, benzyl, or alkanoyl of 1 to 5 carbon atoms, R.sub.3 for a hydrogen atoms, a fluorine atom, a chlorine atom, a bromine atom, nitro, or alkyl of 1 to 5 carbon atoms, R.sub.4 for a hydrogen atom, alkyl of 1 to 5 carbon atoms, benzyl, or phenyl, and R.sub.Type: GrantFiled: January 29, 1992Date of Patent: September 14, 1993Assignee: Toray Industries, Inc.Inventors: Hiroshi Nagase, Akira Mizusuna, Yoshihiro Onoda, Koji Kawai, Shu Matsumoto, Takashi Endo
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Patent number: 5242929Abstract: Derivatives of 1-phenyl-3-azabicycloalkylimidazolidin-2-ones are provided of general formula (1) ##STR1## in which inter alia R represents a group ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof. which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addition agents and analgesic.Type: GrantFiled: February 28, 1992Date of Patent: September 7, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Franco Heidempergher, Nicola Carfagna, Ruggero Fariello
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Patent number: 5238947Abstract: The present invention are novel compounds of the formula: ##STR1## wherein R is OH, NH.sub.2, OW, or H; X is H, F, Cl, Br, I, OH, OW, NO.sub.2 or NH.sub.2 ; Y is H, F, Cl, I, or Br; W is C(O)Z or a C.sub.1 to C.sub.12 alkyl group; Z is an aliphatic or aromatic group of from C.sub.1 to C.sub.12 ; X and Y can both vary within the molecule; and if R is H, at least one of X or Y is not H. In a preferred embodiment, R is OH or NH.sub.2. The most preferred compound is (4-hydroxy-3-N-phenylacetylamino-2,6-piperidinedione), in which R is OH, X is H and Y is H. These compounds have cytostatic activity and insert stereochemically into DNA.Type: GrantFiled: May 21, 1991Date of Patent: August 24, 1993Assignees: University of Georgia Research Foundation, Inc., Stereochemical Genetics, Inc.Inventors: Lawrence B. Hendry, Chung K. Chu, Virendra B. Mahesh
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Patent number: 5237066Abstract: Enantiomer of absolute configuration S of formula: ##STR1## where: X=O or S; andAr denotes a:* phenyl ring substituted with one, two or three C.sub.1 -C.sub.4 alkoxy groups;* phenyl ring substituted at the 2-position with a OCH.sub.3 group and at the 5-position with a halogen atom or a lower alkylcarbonyl group;* phenyl ring substituted at the 2-position with OCH.sub.3, at the 4-position with NH.sub.2 or alkylcarbonyl-NH and at the 5-position with a halogen;* 3-fluoro-2-methoxyphenyl group;* 5-pyrimidinyl group substituted at the 2-position with NH.sub.2 and in the 4-position with alkoxy or phenyloxy.These compounds are useful as medicinal products having activity in respect of gastric movements and antiemetic activity.Type: GrantFiled: September 17, 1991Date of Patent: August 17, 1993Assignee: Delande S.A.Inventors: Nicole A. M. Dorme, Alain J. L. Renaud, Michel Langlois
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Patent number: 5231100Abstract: Compounds of formula I: ##STR1## in which: R represents: --OH or --OR', wherein R' represents C.sub.1 -C.sub.6 alkyl,R.sub.1.sup.a and R.sub.1.sup.b, which may be identical or different, represent hydrogen or C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted by a hydroxyl, an amino, a N'-alkylamino or a N',N'-dialkylamino group, such N'-alkyl groups containing 1-4 carbon atoms,n is 2-5 andR.sub.2 represents hydrogen, or straight chain C.sub.1 -C.sub.4 alkyl, in the form of a free base or a pharmaceutically acceptable acid addition salt are useful in antineoplastic treatment and prophylaxis, especially of leukemias.Type: GrantFiled: September 16, 1991Date of Patent: July 27, 1993Assignee: British Technology Group LimitedInventors: Wieslaw M. Cholody, Jerzy K. Konopa
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Patent number: 5229408Abstract: The invention concerns a 1,2-dihydro-3H-indazol-3-one derivative of formula I ##STR1## wherein R.sup.a is hydrogen, halogeno, hydroxy, cyano, trifluoromethyl, (1-6C)alkyl or (1-6C)alkoxy;R.sup.b is hydrogen or (1-6C)alkyl;R.sup.c is hydrogen, (1-8C)alkyl or (3-8C)alkenyl; andY is (1-8C)alkyl, (3-8C)alkenyl or (3-8C)alkynyl, or Y is a group of the formula --A--Q in which A is (1-6C)alkylene or (3-6C)alkenylene, and Q is phenyl or naphthyl, which may optionally bear one or two substituents;or a pharmaceutically-acceptable salt thereof;or a 1-(1-4C)alkoxycarbonyl derivative thereof.The invention also concerns processes for the manufacture of an indazol-3-one of the formula I and pharmaceutical compositions containing said indazol-3-one. Also included in the invention is a method of treating various inflammatory or allergic diseases using an indazol-3-one of the formula I.Type: GrantFiled: May 8, 1991Date of Patent: July 20, 1993Assignees: ICI PHARMA, Imperial Chemical Industries PLCInventor: Pierre A. R. Bruneau
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Patent number: 5227386Abstract: 3-(3-Indolyl)quinuclidines for the formula IInd--R Iin whichInd is a 3-indolyl group which is unsubstituted or monosubstituted to tetrasubstituted by C.sub.1-4 -alkyl, trifluoromethyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, fluorine, chlorine, hydroxyl, hydroxymethyl, C.sub.6-10 -aryloxy, C.sub.7-11 -aralkyloxy, C.sub.1-5 -acyloxy, C.sub.6-10 -aroyloxy, C.sub.1-4 -alkylsulfonyloxy, C.sub.6-10 -arylsulfonyloxy, carboxyl, C.sub.1-4 -alkoxycarbonyl and/or methylenedioxy andR is 3-quinuclidinyl or 2,3-dehydro-3-quinuclidinyl,and their physiologically acceptable salts can be used as psychopharmaceuticals.Type: GrantFiled: March 22, 1991Date of Patent: July 13, 1993Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Henning Bottcher, Christoph Seyfried, Klaus-Otto Minck, Hans-Peter Wolf
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Patent number: 5227383Abstract: New analogs of sampangine and cleistopholine, compositions and methods of preparation thereof, method of treating fungal and mycobacterial infections. The compounds have the general formula: ##STR1## where the R.sub.1, R.sub.2, and R.sub.5 groups are defined herein.Type: GrantFiled: June 14, 1991Date of Patent: July 13, 1993Assignee: The University of MississippiInventors: Alice M. Clark, Charles D. Hufford, Shihchih Liu, Babajide O. Oguntimein, John R. Peterson, Jordan K. Zjawiony