Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 514/294)
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Benzo[c]quinolizine derivatives, their preparation and use as 5&agr;-reductases inhibitors
Patent number: 6552034Abstract: The present invention refers to benzo[c]quinolizine derivatives of general formula (I) their pharmaceutically acceptable salts or esters, processes for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: June 25, 2001Date of Patent: April 22, 2003Assignee: Applied Research Systems ARS Holding N.V.Inventors: Antonio Guarna, Mario Serio -
Patent number: 6552035Abstract: This invention relates to a composition for inducing smoking cessation comprising as active ingredient alkaloids from Radix ipecauanhae. In smoking cessation program using the composition, the considerable number of volunteers participated in the program became nausea and thus ultimately to have no craving for smoking.Type: GrantFiled: September 13, 2001Date of Patent: April 22, 2003Assignee: Hwa-Mok ParkInventors: Hwa-Mok Park, Byung-Zun Ahn
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Patent number: 6525049Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 22, 2001Date of Patent: February 25, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Valerie A. Vaillancourt, Sandra Staley, Audris Huang, Richard Allen Nugent, Ke Chen, Sajiv K. Nair, James A. Nieman, Joseph Walter Strohbach
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Patent number: 6514986Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.Type: GrantFiled: March 9, 2001Date of Patent: February 4, 2003Assignee: Wockhardt LimitedInventors: Noel J. de Souza, Shivkumar Agarwal, Mahesh V. Patel, Satish B. Bhawsar, Rupinder K. Beri, Ravindra D. Yeole, Nitin Shetty
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Patent number: 6514912Abstract: Disclosed are compositions of benzo(c)quinolizine derivatives and methods for promoting plant and seed growth. The compounds are benzo[c]quinolizine derivatives which exert an inhibiting effect on the 5-alpha-reductase enzymes. The compounds selectively affect the growth of plants, improving morphogenesis and development of commercially useful plants while acting as herbicides to inhibit weed development.Type: GrantFiled: January 10, 2000Date of Patent: February 4, 2003Assignee: Applied Research Systems ARS Holding N.V.Inventors: Antonio Guarna, Mario Serio
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Publication number: 20020165227Abstract: The present invention relates to optically pure 8-(substituted piperidino)-benzo[i,j]quinolizines, their isomers, derivatives, salts, pseudopolymorphs, polymorphs prodrugs and hydrates thereof, to processes for their preparation, and to pharmaceutical compositions comprising 8-(substituted piperidino)-benzo[i,j]quinolizines their isomers, derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof. These compounds and compositions possess potent activity in treating local and systemic infections, particularly infections caused by sensitive and resistant Gram-positive organism infections, Gram-negative organism infections, mycobacterial infections and nosocomial pathogens, and particularly those belonging to the staphylococcus, streptococcus and enterococcus groups. Methods for treating the diseases and disorders arising from the foregoing infections in humans and animals are described by administering the compounds of the invention to said humans and animals.Type: ApplicationFiled: May 7, 2001Publication date: November 7, 2002Applicant: WOCKHARDT RESEARCH CENTERInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Shiv Kumar Agarwal, Shirkant V. Gupte, Dilip J. Upadhyay, Satish B. Bhawsar, Mohammad A. Jafri
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Publication number: 20020160997Abstract: The present invention is a chemical compound of formula (I) 1Type: ApplicationFiled: December 14, 2001Publication date: October 31, 2002Inventors: Jonathan Mark Bentley, Michael John Bickerdike, Paul Hebeisen, Guy Anthony Kennett, Sean Lightowler, Patrizio Mattei, Jacques Mizrahi, Timothy James Morley, Jean-Marc Plancher, Hans Richter, Stephan Roever, Sven Taylor, Steven Paul Vickers
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Patent number: 6468998Abstract: The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition containing a compound of the formula (I), an optically active compound thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive. The compound of the present invention has a serotonin 2 receptor antagonistic action along with a platelet aggregation suppressive action, a peripheral circulation improving action and a lacrimation promoting action. Therefore, the compound of the present invention can be a useful medicine showing effect against thrombotic embolism, dry eye and the like.Type: GrantFiled: May 1, 2001Date of Patent: October 22, 2002Assignee: Mitsubishi Pharma CorporationInventors: Takanobu Kuroita, Masakazu Fujio, Haruto Nakagawa
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Patent number: 6455032Abstract: Compositions and a method of protecting skin from either UV-induced immunosuppression or from UV-induced skin damage using a composition containing an extract of soy or clover, and/or the isoflavone compounds genistein, biochanin, dihydro-diadzein, formonentin, dihydro-geneistein, 2-dehydro-O-desmethyl-angolensin, tetrahydro-daidzein, equol, dehydro-equol, O-desmethyl-angolensin, or 6-hydroxy-O-desmethyl-angolensin.Type: GrantFiled: June 23, 2000Date of Patent: September 24, 2002Assignee: Novogen Research Pty. Ltd.Inventors: Graham Edmund Kelly, Alan James Husband
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Patent number: 6448258Abstract: The present invention provides for methods for the treatment of fibromyalgia syndrome or chronic fatigue syndrome by the administration of heterocyclic amine-type compounds or a salt of any said compound.Type: GrantFiled: April 17, 2001Date of Patent: September 10, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Robert Clyde Marshall, David W. Robertson, Thomas M. Ashley
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Patent number: 6444812Abstract: This invention concerns intermediates in the preparation of compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyType: GrantFiled: November 29, 2000Date of Patent: September 3, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Marc Gaston Venet, Patrick René Angibaud, Yannick Aimé Eddy Ligny, Virginie Sophie Poncelet, Gerard Charles Sanz
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Patent number: 6440458Abstract: Providing an oral formulation of a macrolide compound where the dissolution of the macrolide compound is under sustained release; and a sustained-release formulation containing a composition in solid solution, where the macrolide compound is present at an amorphous state in a solid base.Type: GrantFiled: November 5, 1999Date of Patent: August 27, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazunari Yamashita, Eiji Hashimoto, Yukihiro Nomura, Fumio Shimojo, Shigeki Tamura, Takeo Hirose, Satoshi Ueda, Takashi Saitoh, Rinta Ibuki, Toshio Ideno
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Patent number: 6436954Abstract: Benzo[b]quinolizidine and benzo[f]indolizidine derivatives are provided which are useful for the treatment of Alzheimer's disease, senile dementia or other conditions characterized by memory loss. Pharmaceutical compositions containing these compounds, and methods for their use, are also provided.Type: GrantFiled: March 14, 2001Date of Patent: August 20, 2002Assignees: American Biogenetic Sciences, Inc., University College DublinInventors: Jacob Szmuszkovicz, Ciaran Regan
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Patent number: 6433175Abstract: A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesityType: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, Jonathan Richard Anthony Roffey, Richard John Hamlyn, Suneel Gaur, Matthew Alexander James Duncton, James Edward Paul Davidson, Michael John Bickerdike, Ian Anthony Cliffe, Howard Langham Mansell
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Patent number: 6417220Abstract: A prophylactic and/or therapeutic method for treating a disease caused by mitochondrial functional abnormality, or a disease with mitochondrial functional abnormality, including: administering a prophylactically and/or therapeutically effective amount to a patient in need of such treatment of a medicament including as an active ingredient a substance having a stabilizing effect on mitochondrial membrane by suppressing or eliminating depolarization of mitochondrial membranes which is caused by elevation of intracellular calcium ion concentration, wherein the stabilizing effect on mitochondrial membrane is an action of suppressing or eliminating depolarization of mitochondrial membranes, wherein the depolarization of mitochondrial membranes is caused by elevation of intracellular calcium ion concentration. The disease may be ischemic diseases, toxic diseases, or degenerative diseases. The medicament may be 2-oxo-1-pyrrolidinylacetic acid 2,6-dimethylanilide which acts as a benzodiazepine receptor antagonist.Type: GrantFiled: May 26, 1999Date of Patent: July 9, 2002Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Mitsunobu Yoshii, Shigeo Watabe
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Publication number: 20020061908Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.Type: ApplicationFiled: March 9, 2001Publication date: May 23, 2002Applicant: WOCKHARDT LTDInventors: Noel J. de Souza, Shivkumar Agarwal, Mahesh V. Patel, Satish B. Bhawsar, Rupinder K. Beri, Ravindra D. Yeole, Nitin Shetty, Habil F. Khorakiwala
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Publication number: 20020049206Abstract: The treatment of addictive disorders, psychoactive substance use disorders, intoxication disorders, inhalation disorders, alcohol addiction, tobacco addiction, and nicotine addiction using a heterocyclic amine, a phenylazacycloalkane, a cabergoline, or an aromatic bicyclic amine active agent, or a pharmaceutically acceptable derivative or salt of any said active agent is described herein.Type: ApplicationFiled: August 14, 2001Publication date: April 25, 2002Inventors: Richard W. Anderson, Sylvia S. McBrinn, David W. Robertson, Robert C. Marshall
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Patent number: 6376507Abstract: The present invention relates to a method of treating or preventing a disorder selected from stroke, epilepsy, head trauma, spinal cord trauma, ischemic neuronal damage such as cerebral ischemic damage from stroke or vascular occlusion (e.g., during open heart surgery), excitotoxic neuronal damage (e.g., in stroke or epilepsy) and amyotrophic lateral sclerosis in mammals, including humans, using an NK-1 antagonist. It also relates to a method of treating or preventing such disorders in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, pyrrolidine derivatives, azanorbornane derivatives, ethylene diamine derivatives and related compounds that are substance P receptor antagonists.Type: GrantFiled: June 18, 1998Date of Patent: April 23, 2002Assignee: Pfizer Inc.Inventors: Robert B. Nelson, John A. Lowe, III
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Patent number: 6346537Abstract: To provide a pharmaceutical composition comprising a water-insoluble active substance, surfactant(s) and solid carrier(s), which is improved in dissolution and oral absorption characteristics.Type: GrantFiled: June 4, 1999Date of Patent: February 12, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takehisa Hata, Yuji Tokunaga, Fumio Shimojo, Sumihisa Kimura, Takeo Hirose, Satoshi Ueda
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Publication number: 20010036943Abstract: Pharmaceutical compositions are disclosed for the treatment of acute, chronic and/or neuropathic pain. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an analgesic agent and a pharmaceutically acceptable carrier. The analgesic agent is selected from opioid analgesics, NMDA antagonists, substance P antagonists, COX 1 and COX 2 inhibitors , tricyclic antidepressants (TCA), selective serotonin reuptake inhibitors (SSRI), capsaicin receptor agonists, anesthetic agents, benzodiazepines, skeletal muscle relaxants, migraine therapeutic agents, anti-convulsants, anti-hypertensives, anti-arrythmics, antihistamines, steroids, caffeine, and botulinum toxin. The method of using these compounds and a method of treating acute, chronic and/or neuropathic pain and migraine in a mammal including a human is also disclosed.Type: ApplicationFiled: December 18, 2000Publication date: November 1, 2001Inventors: Jotham W. Coe, Steven B. Sands, Edmund P. Harrigan, Brian T. O'Neill, Eric J. Watsky
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Benzo[c]quinolizine derivatives, their preparation and use as 5&agr;-reductases inhibitors
Patent number: 6303622Abstract: The present invention refers to benzo[c]quinolizine derivatives of general formula (I) their pharmaceutically acceptable salts or esters, processes for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: July 29, 1998Date of Patent: October 16, 2001Assignee: Applied Research Systems ARS Holding N.V.Inventors: Antonio Guarna, Mario Serio -
Patent number: 6242450Abstract: This invention provides 5-HT1f antagonists of Formula I: where AR1, AR2, R, and R′ are as defined in the specification.Type: GrantFiled: June 17, 1999Date of Patent: June 5, 2001Assignee: Eli Lilly and CompanyInventors: Daniel James Koch, Lee Alan Phebus, Vincent Patrick Rocco, Tammy Joy Sajdyk
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Patent number: 6211189Abstract: There are provided novel compounds of formula (I) wherein A represents an aromatic carbocyclic ring or a 5- or 6-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S; X represents —(CH2)n— wherein n represents zero or 1; and R1, R2 and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and tautomers thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: May 31, 2000Date of Patent: April 3, 2001Assignee: AstraZeneca UK LimitedInventors: Peter Hamley, Austen Pimm, Alan Tinker
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Patent number: 6197781Abstract: A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.Type: GrantFiled: August 13, 1999Date of Patent: March 6, 2001Assignee: Novartis AGInventors: Patrice Guitard, Barbara Haeberlin, Rainer Link, Friedrich Richter
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Patent number: 6187786Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyanoType: GrantFiled: December 20, 1999Date of Patent: February 13, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Marc Gaston Venet, Patrick René Angibaud, Yannick Aimé Eddy Ligny, Virginie Sophie Poncelet, Gerard Charles Sanz
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Patent number: 6133283Abstract: To provide novel compounds relating to retinoid which can substitute for retinoic acid used for preventing and treating several diseases and having antagonism against retinoid. Heterocyclic compounds represented by the general formula (1-I) or physiologically acceptable salts thereof:Z--(CR.sup.3 .dbd.CR.sup.2).sub.n --COOR.sup.1-- (1-I)Compounds represented by the general formula (2-I) or physiologically acceptable salts thereof: ##STR1## The compounds according to the present invention exhibit extremely high ability to bind RARs and are effective for treating various kind of diseases such as abnormality in cornification and rheumatoid arthritis.Type: GrantFiled: January 26, 1999Date of Patent: October 17, 2000Assignee: Eisai Co., Ltd.Inventors: Shigeki Hibi, Kouichi Kikuchi, Hiroyuki Yoshimura, Mitsuo Nagai, Katsuya Tagami, Shinya Abe, Ieharu Hishinuma, Junichi Nagakawa, Norimasa Miyamoto, Takayuki Hida, Aichi Ogasawara, Seiko Higashi, Kenji Tai, Takashi Yamanaka, Makoto Asada
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Patent number: 6114370Abstract: This invention relates to a pharmaceutical amnesic sedation composition for administering to a subject comprising an effective of: (i) a benzodiazepine derivative, (ii) a phenanthrene derivative, and (iii) an anticholinergic agent. This invention also relates to a method of administering to a subject a pharmaceutical amnesic sedation composition comprising: (a) preparing a pharmaceutical amnesic sedation composition of this invention, and (b) administering to a subject a therapeutically effective amount of the composition that sedates the subject.Type: GrantFiled: September 28, 1999Date of Patent: September 5, 2000Inventor: William H. Wall, Jr.
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Patent number: 6103736Abstract: Compounds of the formula: ##STR1## which are useful as anti-ulcer agent are provided.Type: GrantFiled: June 29, 1999Date of Patent: August 15, 2000Assignee: Shinnippon Pharmaceutical Inc.Inventors: Hironori Tanaka, Kazuyoshi Fukuzumi, Takeshi Togawa, Kimiko Banno, Toshihisa Ushiro, Masaaki Morii, Takafumi Nakatani
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Patent number: 6093724Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: August 16, 1999Date of Patent: July 25, 2000Assignee: UCB, S.A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 6080754Abstract: The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.Type: GrantFiled: June 1, 1998Date of Patent: June 27, 2000Assignee: Novo Nordisk A/SInventors: Anker Steen Jorgensen, Poul Jacobsen, Lise Brown Christiansen, Paul Stanley Bury, Anders Kanstrup
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Patent number: 6075036Abstract: The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.Type: GrantFiled: June 1, 1998Date of Patent: June 13, 2000Assignees: Novo Nordisk, Karo Bio ABInventors: Anker Steen Jorgensen, Poul Jacobsen, Lise Brown Christiansen, Paul Stanley Bury, Anders Kanstrup
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Patent number: 6013653Abstract: A process for producing pyridiondole derivatives represented by general formula (III) or their salts (wherein R.sup.1 represents hydrogen, lower alkyl or lower alkenyl; R.sup.2 represents hydrogen, lower alkyl or halogeno; and R.sup.3 represents optionally substituted imidazolyl), which comprises reacting a compound represented by general formula (I) or its salt (wherein R.sup.1 and R.sup.2 are each as defined above) with a compound represented by general formula (II) or its salt (wherein R.sup.3.sub.a represents optionally substituted imidazolyl having an imino protecting group; and X represents halogeno), followed by a reaction for eliminating the imino protecting group); and a process for producing optically active pyridoindole derivatives represented by general formula (IV) or their salts: which comprises reacting a racemic mixture of the pyridoindole derivative represent by formula (III) or its salt with (1R)-(-)-10-camphorsulfonic acid.Type: GrantFiled: April 21, 1998Date of Patent: January 11, 2000Assignee: Fujisawa Pharmaceuticals Co., Ltd.Inventors: Kooji Kagara, Nobutaka Kawai, Takashi Nakamura, Shigeru Ieda, Koji Machiya, Atsushi Ohigashi
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Patent number: 5998409Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: June 2, 1995Date of Patent: December 7, 1999Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5990122Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.Type: GrantFiled: January 7, 1998Date of Patent: November 23, 1999Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Thomas Schenke, Thomas Jaetsch, Stephan Bartel, Klaus Dieter Bremm, Rainer Endermann, Karl Georg Metzger
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Patent number: 5990121Abstract: The present invention relates to the new use of 1,2-bridged 1,4-dihydropyridines which are known in some cases, of the general formula (I) ##STR1## in which R.sup.1 to R.sup.4 and a have the meaning indicated in the description, processes for their preparation and their use as medicaments, as selective potassium channel modulators, in particular for the treatment of the central nervous system.Type: GrantFiled: December 8, 1995Date of Patent: November 23, 1999Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Bodo Junge, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry, Henning Sommermeyer
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Patent number: 5981752Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 represents halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, cycloalkyl, or cycloalkyloxy; R.sup.2 represents hydrogen or halogen; R.sup.3 represents hydrogen, alkyl, or cycloalkyl; and the dotted line represents a single or double carbon--carbon bond]; and salts thereof have valuable fungicidal activities which make them of considerable value in agriculture and horticulture.Type: GrantFiled: April 9, 1998Date of Patent: November 9, 1999Assignee: Sankyo Company, LimitedInventors: Hideo Takeshiba, Chiaki Imai
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Patent number: 5965575Abstract: New N-arylpiperidine compounds of formula: ##STR1## wherein: A, m, R, E, n and Ar are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same are useful in the treatment of disorders involving the serotininergic system.Type: GrantFiled: March 27, 1998Date of Patent: October 12, 1999Assignee: Adir Et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert, Valerie Audinot
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Patent number: 5955470Abstract: This invention relates to novel amide derivatives of certain 2,6-methano-2H-quinolizine-type compounds, to the intermediates and processes for their preparation, to their ability to antagonize the effects of serotonin at the 5HT.sub.3 receptors, and to their end-use application in the treatment of chemotherapeutically-induced nausea and vomiting, as anti-anxiety agents, in the symptomatic treatment of pain associated with migraine, as anti-arrhythmic agents, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses of the type manifested in patients suffering from schizophrenia, and mania, in the treatment of glaucoma, for stimulating gastric motility, to combat drug abuse, to treat sleep apnea and to treat irritable bowel syndrome.Type: GrantFiled: October 29, 1998Date of Patent: September 21, 1999Assignee: Merrell Pharmaceuticals, Inc.Inventor: Maurice W. Gittos
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Patent number: 5952339Abstract: A pharmaceutical composition incorporating a nicotinic antagonist is provided. The composition is an effective amount of a compound of the formula: wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; A, A' and A" are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z" is hydrogen or a substituent other than hydrogen; Y is C.dbd.O, C(OH)R' or C--A, where R' is hydrogen or lower alkyl.Type: GrantFiled: April 2, 1998Date of Patent: September 14, 1999Inventors: Merouane Bencherif, Patrick Michael Lippiello
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Patent number: 5939427Abstract: A lotion comprising a tricyclic compound, typically 17-allyl-1,14-dihydroxy-12-?2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l!-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo ?22.3.1.0.sup.4,9 !octacos-18-ene-2,3,10,16-tetraone, or a pharmaceutically acceptable salt thereof, a solubilizing and/or absorption-promoting agent, a liquid medium, and optionally an emulsifier and/or a viscosity increasing agent. The lotion is stable, excellent in absorption and has less irritation against the skin and sustained release. Also, the lotion is effective for the treatment and/or prophylaxis of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.Type: GrantFiled: January 5, 1998Date of Patent: August 17, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Akira Kagayama, Sachiyo Tanimoto, Saburo Murata, Takehisa Hata
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Patent number: 5935970Abstract: The imidazo?1,5-a!quinolines (I) are useful in treating neurological diseases/conditions or chronic neurodegenerative diseases/conditions.Type: GrantFiled: June 3, 1996Date of Patent: August 10, 1999Assignee: Pharmacia & Upjohn CompanyInventor: Donald B. Carter
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Patent number: 5910501Abstract: This invention relates to the manufacture of certain esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines and their use as medicaments in the treatment of cognitive disorders.Type: GrantFiled: August 26, 1997Date of Patent: June 8, 1999Assignee: Merrell Pharmaceuticals Inc.Inventors: Maurice W. Gittos, Marcel Hibert
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Patent number: 5854256Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.Type: GrantFiled: March 21, 1997Date of Patent: December 29, 1998Assignee: Pfizer Inc.Inventor: John Adams Lowe, III
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Patent number: 5852014Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: June 2, 1995Date of Patent: December 22, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5840903Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro;m is 1 or 2;X is O or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.Type: GrantFiled: July 27, 1992Date of Patent: November 24, 1998Assignee: G. D. Searle & Co.Inventors: Daniel Lee Flynn, Robert L. Shone
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Patent number: 5807883Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 24, 1996Date of Patent: September 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Masataka Hikota, Toshiro Shikano, Masaaki Nagasaki
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Patent number: 5792774Abstract: A compound of formula (I) ##STR1## or a pharmaceutically-acceptable salt, solvate or hydrate thereof.Type: GrantFiled: February 21, 1997Date of Patent: August 11, 1998Assignee: Chiroscience LimitedInventors: Alan Findlay Haughan, Steven Colin Beasley, John Gary Montana, Robert John Watson
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Patent number: 5780481Abstract: The invention is a method for inhibiting activation of the human A3 adenosine receptor with adenosine, by treating the receptor a compound of the formula ##STR1## to treat asthma.Type: GrantFiled: August 8, 1996Date of Patent: July 14, 1998Assignee: Merck & Co., Inc.Inventors: Marlene A. Jacobson, Richard Norton, Prasun K. Chakravarty
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Patent number: 5770597Abstract: The present invention relates to quinoline derivatives substituted in the 7-position by a trans-2,8-diazabicyclo?4.3.0!nonan-8-yl group having a broad antibacterial spectrum and to processes for preparing the same.Type: GrantFiled: October 11, 1995Date of Patent: June 23, 1998Assignees: Korea Research Institute of Chemical Technology, Smithkline Beecham P.L.C.Inventors: Wan Joo Kim, Tae Ho Park, Moon Hwan Kim, Bong Jin Kim, Neil D. Pearson
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Patent number: 5750535Abstract: The present invention relates to a method treating or preventing disorders caused by a spiral urease-positive gram-negative bacterium such as Helicobacter pylori in mammals, including humans, using compounds that are substance P receptor antagonists and, specifically, using certain quinuclidine derivatives, piperidine derivatives, pyrrolidine derivatives, azanorbornane derivatives, ethylene diamine derivatives and related compounds.Type: GrantFiled: August 29, 1995Date of Patent: May 12, 1998Assignee: Pfizer Inc.Inventor: Joanna Clancy