Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 546/197)
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Patent number: 6153625Abstract: A compound selected from those of formula (I): ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen, halogen, alkyl, alkenyl, alkynyl, hydroxy, alkoxy, trihaloalkyl, or any pair may form a heterocycle,R.sub.5 represents hydrogen, alkyl, or arylalkyl,R.sub.6 represents hydrogen, halogen, alkyl, hydroxy, alkoxy, or trihaloalkyl,A, together with the carbons of the phenyl, represents a heterocycle,their isomers and addition pharmaceutically-acceptable acid or base salts thereof, and medicinal products containing the same which are useful in the treatment of pathologies in which 5HT.sub.1B receptors are involved.Type: GrantFiled: August 13, 1999Date of Patent: November 28, 2000Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Adrian Newman-Tancredi
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Patent number: 6153611Abstract: Novel non-dopaminergic antiischemic compounds have Formula I: ##STR1## wherein R=R.sub.1 and is independently H, C.sub.1-4 alky C.sub.1-4 alkoxy, C.sub.1-4 trihaloalkyl or halogen, or R and R.sub.1 may be taken together to form an --O(CH.sub.2).sub.m O-- (m=1 or 2);X=a 3-indolyl, phenyl, naphthalenyl or 2-benzothiazolyl residue;n=0, 1, 2 or 3; ##STR2## R.sub.2 =R.sub.3 and is independently H or C.sub.1-4 alkyl; and R.sub.4 =phenyl, 2-thienyl, 2-quinolinyl, 4-pyridinyl or substituted phenyl.Type: GrantFiled: June 25, 1993Date of Patent: November 28, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, John D. Catt
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Patent number: 6150527Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains.Type: GrantFiled: February 28, 1997Date of Patent: November 21, 2000Assignee: Ariad Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Patent number: 6149841Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: December 17, 1999Date of Patent: November 21, 2000Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Patent number: 6140321Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.Type: GrantFiled: December 30, 1996Date of Patent: October 31, 2000Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
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Patent number: 6136825Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; g is 0, 1, 2, 3 or 4; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents an aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress and spasticity ##STR1##Type: GrantFiled: June 16, 1999Date of Patent: October 24, 2000Assignee: Knoll AktiengesellschaftInventors: Neil Wishart, Alan Martin Birch
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Patent number: 6133288Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2000Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 6133289Abstract: Invented are methods of treatment using novel forms of paroxetine hydrochloride anhydrate.Type: GrantFiled: September 2, 1997Date of Patent: October 17, 2000Assignee: SmithKline Beecham CorporationInventors: Neal Ward, Victor Witold Jacewicz
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Patent number: 6133456Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formulaM.sup.1 --L--M.sup.2where M.sup.1 and M.sup.2 are independently moieties of the formula: ##STR1## in which B.sup.1, B.sup.2, B.sup.3, R.sup.1, R.sup.2, n, W, X and Y are as defined.Type: GrantFiled: February 28, 1997Date of Patent: October 17, 2000Assignee: ARIAD Gene Therapeutics, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Patent number: 6130234Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.Type: GrantFiled: December 20, 1996Date of Patent: October 10, 2000Assignees: Warner-Lambert Company, Cocensys, IncorporatedInventors: Christopher F. Bigge, Jonathan Wright, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F. W. Keana
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Patent number: 6124330Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: April 29, 1999Date of Patent: September 26, 2000Assignee: Janssen-Cilag S.A.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Patent number: 6124321Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: October 24, 1997Date of Patent: September 26, 2000Assignee: Pfizer IncInventors: Yuhpyng Liang Chen, Arthur Adam Nagel
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Patent number: 6114354Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neuragenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: August 17, 1999Date of Patent: September 5, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
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Patent number: 6107310Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; G.sub.1 --G.sub.2 --G.sub.3 are absent or form a heteroaromatic chain; g is 0,1,2,3 or 4; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO. HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mrellitus, hyperglvcaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: June 16, 1998Date of Patent: August 22, 2000Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, Paul Anthony Bradley, Julie Carolyn Gill
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Patent number: 6096761Abstract: The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-6 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R.sup.5 -, Alk-X--R.sup.6, -Alk-Y--C(.dbd.O)--R.sup.8, or -Alk-Y--C(.dbd.O)--NR.sup.10 R.sup.11 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R.sup.6 is hydrogen, C.sub.Type: GrantFiled: August 11, 1998Date of Patent: August 1, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul Rene Marie Bosmans, John Christopher Love, Michel Anna Jozef Decleyn, Henri Elisabeth Frans D'Haen
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Patent number: 6083943Abstract: A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.Type: GrantFiled: March 19, 1999Date of Patent: July 4, 2000Assignee: Pfizer IncInventors: Masaya Ikunaka, Yuji Shishido, Masami Nakane
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Patent number: 6080759Abstract: "Paroxetine hydrochloride (I) anhydrate free of bound propan-2-ol, and various forms thereof, are useful in the treatment of depression and other disorders for which administration of selective serotonin reuptake inhibitors are indicated.Type: GrantFiled: September 2, 1997Date of Patent: June 27, 2000Assignee: SmithKline Beecham CorporationInventors: Neal Ward, Victor Witold Jacewicz
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Patent number: 6066650Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.Type: GrantFiled: July 21, 1997Date of Patent: May 23, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino, John E. Lawson, Henry M. Holava, Richard A. Partyka
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Patent number: 6063927Abstract: Piperidine compounds, processes for preparing them, pharmaceutical compositions comprising them and their use in therapy are disclosed.Type: GrantFiled: April 23, 1999Date of Patent: May 16, 2000Assignee: SmithKline Beecham plcInventors: Andrew Simon Craig, Alan David Jones, Deirdre O'Keeffe, Neal Ward
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Patent number: 6063795Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: G.D. Searle & CompanyInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6060487Abstract: A compound of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X--Y, A, Z and Z' are as defined in the description, in the form of the cis or trans isomers each in racemic or optically active form, and acid addition salts thereof, and medicinal products containing the same are useful in the treatment of diseases of the central nervous system or of manifestations of pain.Type: GrantFiled: March 22, 1999Date of Patent: May 9, 2000Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Adrian Newman-Tancredi, Anne Dekeyne
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Patent number: 6057441Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.Type: GrantFiled: October 6, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Patent number: 6054585Abstract: The present invention relates to a process of making high purity piperine for nutritional and nutraceutical application. This process recovers piperine from piperine-containing oleoresin by using isourea, urea or a urea derivative to remove organic matter other than piperine from the oleoresin. Preferrably, the process recovers piperine from oleoresin of fruit of piper nigrum or piper longum. More preferably, the process recovers piperine from oleoresin of fruit of piper nigrum, i.e. black pepper.Type: GrantFiled: December 23, 1998Date of Patent: April 25, 2000Assignee: Sabinsa CorporationInventors: Muhammed Majeed, Vladimir Badmaev
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Patent number: 6037352Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.Type: GrantFiled: November 19, 1998Date of Patent: March 14, 2000Assignee: Schering CorporationInventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
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Patent number: 6022495Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, nenzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: July 10, 1998Date of Patent: February 8, 2000Assignee: Transitions Optical, Inc.Inventor: Anil Kumar
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Patent number: 6008223Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: January 20, 1998Date of Patent: December 28, 1999Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Scott C. Miller
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Patent number: 5998440Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: May 8, 1998Date of Patent: December 7, 1999Assignee: Merck Sharpe & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Angus Murray MacLeod, Monique Bodil Van Niel
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Patent number: 5985864Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.Type: GrantFiled: June 6, 1997Date of Patent: November 16, 1999Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka, Yukio Narabu
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Patent number: 5977111Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.Type: GrantFiled: June 21, 1996Date of Patent: November 2, 1999Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 5973155Abstract: The process consists of reacting (-)trans-N-p-fluorophenyl)-3-[[3,4-(methylenedioxy)phenoxy]methyl]-piperid ine acetate with 2-chloro- or 2-bromo-4'-fluoroacetophenone. The resulting compound can be isolated as a pharmaceutically acceptable addition salt by reaction with the corresponding acid.Type: GrantFiled: October 27, 1997Date of Patent: October 26, 1999Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Santiago Gubert, Aurelio Sacristan, Jose A. Ortiz
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Patent number: 5968954Abstract: New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are as defined in the description, in the form of a racemic mixture and in the form of optical isomers, and physiologically-tolerable acid addition salts thereof. The products of the invention are useful as medicaments and exhibit selective binding affinity for the 5HT.sub.1B receptors.Type: GrantFiled: February 26, 1998Date of Patent: October 19, 1999Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert
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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: 5962689Abstract: This invention relates to new stereoselective processes for preparing 3-substituted-4-aryl piperidines and methods for controlling the absolute stereochemistry at the C-3 and C-4 positions of the piperidine ring. Compounds of this type are key intermediates in the preparation of paroxetine, femoxetine, and other medicaments.Type: GrantFiled: August 19, 1997Date of Patent: October 5, 1999Assignee: Brantford Chemicals Inc.Inventors: K. S. Keshava Murthy, Allan W. Rey
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Patent number: 5958927Abstract: A compound of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X-Y, A, Z and Z' are as defined in the description, in the form of the cis or trans isomers each in racemic or optically active form, and acid addition salts thereof, and medicinal products containing the same are useful in the treatment of diseases of the central nervous system or of manifestations of pain.Type: GrantFiled: October 2, 1998Date of Patent: September 28, 1999Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Adrian Newman-Tancredi, Anne Dekeyne
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Patent number: 5955520Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and having certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12 or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans and spiro(indoline)type compounds, are also described.Type: GrantFiled: June 17, 1996Date of Patent: September 21, 1999Assignee: PPG Industries, Inc.Inventors: Harry G. Heller, Julian R. Levell
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Patent number: 5952349Abstract: 1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, --O--, --SO.sub.0-2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 --C.sub.6 alkyl)--, --C(C.sub.1 --C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --; R is C.sub.3 --C.sub.6 cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl; R.sup.1 is H, --CN, --CF.sub.3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, --COR.sup.15, --COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or --CON(R.sup.13).sub.2 ; R.sup.2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; and R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.13, R.sup.15 and R.sup.Type: GrantFiled: July 8, 1997Date of Patent: September 14, 1999Assignee: Schering CorporationInventors: Theodros Asberom, Derek B. Lowe, Michael J. Green
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Patent number: 5952352Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: October 1, 1997Date of Patent: September 14, 1999Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Henrik Sune Andersen, Rolf Hohlweg, Tine Krogh J.o slashed.rgenen, Peter Madsen, Zdenek Polivka, Alexandra Silhankova, Karel Sindelar
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5922733Abstract: Novel heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders are disclosed.Type: GrantFiled: June 30, 1997Date of Patent: July 13, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Ian Thomson Forbes, Graham Elgin Jones, Francis David King, Peter Ham, David Thomas Davies, Angela Moghe
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Patent number: 5919797Abstract: Halogenated naphthyl methoxy piperidines having a strong affinity for the serotonin transporter are disclosed. Those compounds can be labeled with positron-emitting and/or gamma emitting halogen isotopes by a late step synthesis that maximizes the useable lifeterm of the label. The labeled compounds are useful for localizing serotonin transporter sites by positron emission tomography and/or single photon emission computed tomography.Type: GrantFiled: April 24, 1997Date of Patent: July 6, 1999Assignee: Emory UniversityInventors: Mark M. Goodman, Bahjat Faraj
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Patent number: 5919806Abstract: Disclosed are cardiotonic medicines containing, as the active ingredient, at least one of compounds of formula (I) and their pharmacologically acceptable salts when they form salts. ##STR1## wherein X.sup.1 and X.sup.2 do not exist or represents an oxygen atom; A represents OH or a C.sub.1 -C.sub.4 acyloxy group; B represents a hydrogen atom or may form a chemical bond along with A; X is an oxygen atom, nitrogen, sulfur, etc.; R.sup.1 and R.sup.2 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc.; R.sup.3 and R.sup.4 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc., or they may together form a 1,4-butylene or 1,5-pentylene group. The compounds have a strong activity of reinforcing the contraction of cardiac muscles and a strong activity of reducing the rate of heart beats. As they are not toxic, they are useful as cardiotonic medicines.Type: GrantFiled: September 29, 1995Date of Patent: July 6, 1999Assignee: Nissan Chemical Industries, Ltd.Inventors: Kiyotomo Seto, Hiroo Matsumoto, Yoshimasa Kamikawaji, Kazuhiko Ohrai, Toru Yamashita, Yukinori Masuda
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Patent number: 5916902Abstract: This invention relates to a process for preparing the compound having the formula ##STR1## which comprises i) heating the compound of formula ##STR2## wherein R.sup.3 is R.sup.4 or benzyl and R.sup.4 is R.sup.5 C(.dbd.O), R.sup.5 C(.dbd.O) or R.sup.5 SO.sub.2 wherein R.sup.5 is (C.sub.1 -C.sub.6)alkyl or (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.6)alkyl;at an elevated temperature in the presence of a base with the proviso that when R.sup.3 in the resultant product is R.sup.4 said product is ii) further treated with an aqueous mineral acid at an elevated temperature followed by iii) treatment of the product of ii) with a) a benzylating agent in the presence of a base or b) benzaldohyde in the presence of a reducing agent and an acid.Type: GrantFiled: April 16, 1997Date of Patent: June 29, 1999Assignee: Pfizer Inc.Inventors: Keith M. Devries, Anabella Villalobos
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Patent number: 5900423Abstract: "Paroxetine hydrochloride (I) anhydrate ##STR1## free of bound propan-2-ol, and various forms thereof, are useful in the treatment of depression and other disorders for which administration of selective serotonin reuptake inhibitors are indicated.Type: GrantFiled: September 2, 1997Date of Patent: May 4, 1999Assignee: SmithKline Beecham CorporationInventors: Neal Ward, Victor Witold Jacewicz
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Patent number: 5892046Abstract: The present invention relates to trifluoromethylpyridone-based methine and azamethine dyes of the formula I ##STR1## a process for their thermal transfer, a process for dyeing or printing synthetic materials and their use.Type: GrantFiled: April 24, 1997Date of Patent: April 6, 1999Assignee: BASF AktiengesellschaftInventors: Clemens Grund, Helmut Reichelt, Andreas Johann Schmidt, Stefan Beckmann
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Patent number: 5886011Abstract: Piperidine derivatives represented by general formula (I) ##STR1## or pharmaceutically acceptable acid addition salts thereof: wherein n represents an integer of 0 or 1; X represents CH.sub.2, O or CH--CH.sub.3 ; R represents hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, substituted aminosulfonyl or nitro; R.sub.1 and R.sub.2 may be the same or different and each represents hydrogen or lower alkyl, are disclosed. The piperidine derivatives have an antagonism on Substance P and is useful as a preventive or remedy for asthma, vomiting, etc.Type: GrantFiled: September 26, 1997Date of Patent: March 23, 1999Assignee: Hisamitsu Pharmaceutical Co., Inc.Inventors: Yoshihiro Tanoue, Koichi Beppu, Akira Okayama, Osami Sakamoto
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Patent number: 5874447Abstract: The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: ##STR1## wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group optionally substituted by C.sub.1-4 alkyl, alkylthio, alkoxy, halogen, nitro, acylamino, methylsulfonyl or methylenedioxy, or represents tetrahydronaphthyl,R.sup.1 represents hydrogen, trifluoro (C.sub.1-4) alkyl, alkyl or alkynyl,X represents hydrogen, alkyl having 1-4 carbon atoms, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio or aralkoxy,R.sup.2 represents:a C1-C10 alkyl group,a phenyl group optionally substituted by one or more of the following groups:a C1-C10 alkyl group,a halogen group,a nitro group,hydroxy group,and/or an alkoxy group.Type: GrantFiled: June 10, 1997Date of Patent: February 23, 1999Assignee: Synthon B. V.Inventors: Franciscus Bernardus Gemma Benneker, Frans Van Dalen, Jacobus Maria Lemmens, Theodorus Hendricus Antonium Peters, Frantisek Picha
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Patent number: 5872132Abstract: "Paroxetine hydrochloride (I) anhydrate ##STR1## free of bound propan-2-ol, and various forms thereof, are useful in the treatment of depression and other disorders for which administration of selective serotonin reuptake inhibitors are indicated.Type: GrantFiled: October 18, 1996Date of Patent: February 16, 1999Assignee: SmithKline Beecham CorporationInventors: Neal Ward, Victor Witold Jacewicz
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Patent number: 5869520Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: January 8, 1997Date of Patent: February 9, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5866589Abstract: Anti-AIDS compounds of formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are as defined in the specification and R.sub.8 is alkyl of substituted alkyl.Type: GrantFiled: June 9, 1997Date of Patent: February 2, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Donna L. Romero, Richard C. Thomas, Paul D. May, Toni-Jo Poel
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Patent number: 5861429Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is methyl, ethyl, isopropyl or sec-butyl; X is carbonyl or methylene; Z is .dbd.C.dbd.(R.sup.2).sub.2 or .dbd.C.dbd.(CH.sub.2).sub.m, in which R.sup.2 is alkyl, and m is integer of from 2 to 5); n is 0 or 1; R.sup.3 is nitro, amino, alkylamino, dialkylamino, alkoxy, alkoxyalkoxy, or a group (iii), (iv), (v), (vi), (vii), (viii) or (ix): ##STR2## , wherein: R.sup.4 represents: alkyl; substituted alkyl; cycloalkyl having from 3 to 6 carbon atoms; substituted cycloalkyl; alkenyl; alkynyl; carbocyclic aryl; or heterocyclic; R.sup.5 is hydrogen atom or alkyl; R.sup.6 represents: hydrogen; alkyl; or cycloalkyl; R.sup.7 represents: alkyl; cycloalkyl; carbocyclic aryl; or aralkyl; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, are fuised to form heterocyclic ring; Y is oxygen or sulfur; r is 1, 2 or 3; Q is methylene or carbonyl; R.sup.8 is: alkyl or carbocyclic aryl; R.sup.Type: GrantFiled: September 30, 1996Date of Patent: January 19, 1999Assignee: Sankyo Company, LimitedInventors: Kazuo Sato, Akio Saito, Toshimitsu Toyama