Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
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Publication number: 20020103191Abstract: Dibenzofluorene derivatives having a formula selected from the group consisting of 1Type: ApplicationFiled: January 14, 2002Publication date: August 1, 2002Applicant: Board of Regents, The University of Texas SystemInventors: Frederick F. Becker, Bimal K. Banik
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Patent number: 6426347Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1-C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, alkylthio, hydroxy, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.Type: GrantFiled: December 13, 2000Date of Patent: July 30, 2002Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Xi Chen
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Patent number: 6423717Abstract: Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed.Type: GrantFiled: August 21, 2000Date of Patent: July 23, 2002Assignee: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Francis David King, Paul Adrian Wyman
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Patent number: 6410530Abstract: New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.Type: GrantFiled: August 31, 2000Date of Patent: June 25, 2002Assignee: AstraZeneca ABInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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Patent number: 6407113Abstract: A medicament for treating or preventing diastolic dysfunction, comprising 2-(1-piperazinyl)-5-methylbenzenesulfonic acid derivative or its salt, or hydrate or solvate thereof as an active ingredient.Type: GrantFiled: October 4, 2001Date of Patent: June 18, 2002Assignee: Mitsubishi Chemical CorporationInventors: Hisashi Kawasumi, Yuji Abe, Naoya Satoh, Yoshimi Kitada
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Patent number: 6403651Abstract: Method for mediating the effects of light on melatonin rhythmicity in mammals and a method of mediating circadian rhythms, effected by the administration of a compound or compounds effective at a 5-HT2c serotonin receptor site. By administration of selected doses of the 5-HT2c receptor active compound it is possible to advance or delay circadian rhythms as measured by the rate of melatonin production or moderation of core body temperature rhythms.Type: GrantFiled: March 6, 2000Date of Patent: June 11, 2002Assignee: Luminis Pty LimitedInventor: David Kennaway
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Publication number: 20020068736Abstract: Novel intermediates of Formula IV wherein the substituents are as defined in the specification and a process for preparing the same.Type: ApplicationFiled: June 29, 2001Publication date: June 6, 2002Inventors: Dominique Lesuisse, Jean-Georges Teutsch
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Patent number: 6395739Abstract: The present invention is directed to an N-phenyl-N′-phenylpropylpiperazine derivative represented by formula (1): (wherein R1 represents a lower alkyl group; R2 represents a lower alkoxy group; and R3 represents a cyano group, a carboxyl group, or an indolecarbonyl group); a medicament; and to a process for producing the derivative. The compound of the present invention is endowed with potent &agr;1-adrenoceptor blocking activity, and thus is useful for the prevention or treatment of hypertension, congestive heart failure, myocardinal ischemia, arrhythmia, angina pectoris, and urinary obstruction and pollakiuria caused by benign prostatic hyperplasia.Type: GrantFiled: December 29, 2000Date of Patent: May 28, 2002Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Hiroki Sato, Eiichi Nagano, Jun Chikazawa, Mineo Takei, Raita Higashino
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Patent number: 6387906Abstract: The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 7, 2000Date of Patent: May 14, 2002Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
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Publication number: 20020052378Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: 1Type: ApplicationFiled: January 5, 2001Publication date: May 2, 2002Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Publication number: 20020052383Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: July 6, 2001Publication date: May 2, 2002Inventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
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Patent number: 6380199Abstract: A method of treating ADHD comprising administering a 5-HT6 receptor antagonist according to formula (A) hereinbelow: wherein: P is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur; A is a single bond, a C1-6alkylene or a C1-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more halogen atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, nitro, amino, C1-6alkylamino or diC1-6alkylamino, cyano or R1 is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur; n is 0, 1, 2, 3, 4, 5 or 6, R2 is hydrogen, C1-6 alkyl or aryl C1-6 alkyl; R3 is a group R5 or together with R5 forms a group (CH2)2O or (CH2)3O or R3 is linked to R2 to form a group (CH2)2 or (CH2)3; R4 is &mdashType: GrantFiled: April 17, 2001Date of Patent: April 30, 2002Assignee: SmithKline Beechan p.l.c.Inventors: Charles Alan Reavill, Carol Routledge
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Patent number: 6376494Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionallyType: GrantFiled: November 28, 2000Date of Patent: April 23, 2002Assignee: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Yvette L. Palmer, Edward J. Podlesny
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Patent number: 6376495Abstract: Piperazine derivatives of formula (I) wherein Z, X, n, Ar and i have the meanings defined herein are usefull in the treatment of pathologies associated with insulin-resistance syndrome.Type: GrantFiled: January 29, 2001Date of Patent: April 23, 2002Assignee: Merck Patent GesellschaftInventors: Gérard Moinet, Dominique Marais, Didier Mesangeau, Liliane Doare, Micheline Kergoat
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Publication number: 20020045618Abstract: The present invention relates to novel heteroaryl diazacycloalkane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: August 23, 2001Publication date: April 18, 2002Inventors: Simon Feldbaek Nielsen, Dan Peters, Elsebet Ostergaard Nielsen, Gunnar M. Olsen
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Publication number: 20020035113Abstract: A piperidine, tetrahydropyridine or piperazine derivative having formula (I), 1Type: ApplicationFiled: July 9, 2001Publication date: March 21, 2002Applicant: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Christian Krog-Jensen, Berith Bjornholm
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Patent number: 6358515Abstract: A hydroquinone compound is represented by the following formula or a pharmacologically acceptable salt thereof with W, R, R1-4, and B1-2 defined herein.Type: GrantFiled: July 30, 1999Date of Patent: March 19, 2002Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Hidetoshi Nakao, Kazuhiko Ito, Takahiro Sakaue, Sachiko Inoue, Masahito Iemura
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Patent number: 6358958Abstract: A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.Type: GrantFiled: January 3, 2001Date of Patent: March 19, 2002Assignee: Eli Lilly and CompanyInventors: Daniel Timothy Kohlman, Yao-Chang Xu
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Publication number: 20020028822Abstract: A medicament for treating or preventing diastolic dysfunction, comprising 2-(1-piperazinyl)-5-methylbenzenesulfonic acid derivative or its salt, or hydrate or solvate thereof as an active ingredient.Type: ApplicationFiled: October 4, 2001Publication date: March 7, 2002Inventors: Hisashi Kawasumi, Yuji Abe, Naoya Satoh, Yoshimi Kitada
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Publication number: 20020022630Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: August 29, 2001Publication date: February 21, 2002Applicant: Neurogen CorporationInventors: Xiaoyan Zhang, Jennifer Tran, He Zhao, Andrew Thurkauf
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Patent number: 6344458Abstract: Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, migraine, obesity, cognitive disorders, and neurodegenerative diseases.Type: GrantFiled: December 13, 1999Date of Patent: February 5, 2002Assignee: American Home Products CorporationInventors: Michael G. Kelly, Yvette L. Palmer
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Patent number: 6344456Abstract: The invention concerns compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein. Said compounds are useful in therapy as antithrombotic agents.Type: GrantFiled: January 10, 2001Date of Patent: February 5, 2002Assignee: Laboratoire L. LafonInventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
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Patent number: 6344466Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.Type: GrantFiled: February 28, 2001Date of Patent: February 5, 2002Assignee: 3-Dimensional Pharmaceuticals Inc.Inventors: Richard M. Soll, Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Publication number: 20020013324Abstract: Compounds of the Formula (I) 1Type: ApplicationFiled: August 23, 2001Publication date: January 31, 2002Applicant: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Edward J. Podlesny
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Publication number: 20020002164Abstract: Substituted heterocycles of the general structural formula: 1Type: ApplicationFiled: April 17, 2001Publication date: January 3, 2002Applicant: Merck & Co., Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: 6335337Abstract: Novel compounds which are inhibitors of the binding of fibrinogen to the Gp iib/iiia platelet receptors, and which can be used therapeutically as antithrombotic agents.Type: GrantFiled: January 9, 2001Date of Patent: January 1, 2002Assignee: Laboratoire L. LafonInventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
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Publication number: 20010051623Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I 1Type: ApplicationFiled: July 10, 2001Publication date: December 13, 2001Inventors: Stefan Berg, Svante Ross, Seth-Olov Thorberg
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Publication number: 20010051626Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I 1Type: ApplicationFiled: July 10, 2001Publication date: December 13, 2001Inventors: Stefan Berg, Mats Linderberg, Svante Ross, Seth-Olov Thorberg, Bengt Ulff
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Publication number: 20010047001Abstract: Novel compounds of the general formula: 1Type: ApplicationFiled: February 22, 2001Publication date: November 29, 2001Inventors: Vaibhav Varkhedkar, Venkata P. Palle, Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn
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Patent number: 6323229Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.Type: GrantFiled: April 14, 1999Date of Patent: November 27, 2001Assignee: Pfizer INCInventor: Harry R. Howard
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Patent number: 6316450Abstract: The invention relates to novel compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.Type: GrantFiled: January 10, 2000Date of Patent: November 13, 2001Assignee: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Stephen Frederick Moss
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Patent number: 6313118Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salType: GrantFiled: October 21, 1998Date of Patent: November 6, 2001Assignee: Astra AktiebolagInventors: Stefan Berg, Mats Linderberg, Svante Ross, Seth-Olov Thorberg, Bengt Ulff
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Patent number: 6306859Abstract: Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.Type: GrantFiled: March 1, 2000Date of Patent: October 23, 2001Assignee: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Edward J. Podlesny
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Publication number: 20010029258Abstract: Compounds of the formula 1Type: ApplicationFiled: March 26, 2001Publication date: October 11, 2001Inventor: Terrance P. Snutch
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Patent number: 6297247Abstract: Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes using the compounds.Type: GrantFiled: June 22, 2000Date of Patent: October 2, 2001Assignee: Warner-Lambert CompanyInventors: Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
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Patent number: 6294539Abstract: Novel compositions comprising heterocyclic hydroxamic acid derivatives of the general formula: These compounds are useful in the treatment of diseases and conditions in which matrix metalloproteinases are involved, such as cancer, arthritis, tumor metastasis and multiple sclerosis (MS).Type: GrantFiled: January 19, 2000Date of Patent: September 25, 2001Assignee: Advanced Syntech, LLCInventors: Boliang Lou, Adnan M. M. Mjalli
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Patent number: 6291465Abstract: The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy halogen, amino, —N(R6)2 or trifluoromethyl; R1 is hydrogen lower alkoxy or halogen, R and R1 may be together —CH═CH—CH═CH—; R2 is halogen, lower alkyl or trifluoromethyl; R3 is hydrogen or lower alkyl; R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl; R5 is hydrogen, nitro, amino or —N(R6)2; R6 is hydrogen or lower alkyl, X is —C(O)N(R6)—, —(CH2)nO—, (CH2)nN(R6)—, —N(R6)C(O)— or —N(R6)(CH2)n—; and n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.Type: GrantFiled: February 25, 2000Date of Patent: September 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Patent number: 6284761Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: R1, R2, R3 R4 and R5, R6, R7, and R8 represent organic and/or inorganic substituents as defined herein, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: January 6, 2000Date of Patent: September 4, 2001Assignee: Neurogen CorporationInventors: Xiaoyan Zhang, Jennifer Tran, He Zhao, Andrew Thurkauf
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Patent number: 6281214Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.Type: GrantFiled: October 5, 1998Date of Patent: August 28, 2001Assignee: Eisai Co., LtdInventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
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Patent number: 6281215Abstract: New 4-(1-piperazinyl)benzoic acid derivatives of the formula (I) are described. Also described is methods for making these compounds and their use as therapeutic agents. In particular, the compounds find use in the treatment of diabetes.Type: GrantFiled: October 20, 1999Date of Patent: August 28, 2001Assignee: Merck Patent GmbHInventors: Gérard Moinet, Gérard Botton, Liliane Doare, Micheline Kergoat, Didier Messangeau
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Publication number: 20010016207Abstract: Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof 1Type: ApplicationFiled: February 7, 2001Publication date: August 23, 2001Inventor: Martin Missbach
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Publication number: 20010011093Abstract: The invention relates to new arylglycinamide derivatives of general formula I 1Type: ApplicationFiled: January 3, 2001Publication date: August 2, 2001Inventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Publication number: 20010009915Abstract: Compound of formula (I): 1Type: ApplicationFiled: January 18, 2001Publication date: July 26, 2001Inventors: Gilbert Lavielle, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Jean-Jacques Descombes
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Patent number: 6258813Abstract: Piperazine derivatives of the formula I in which R1 and R2 have the meanings given in claim 1 are dopamine ligands with a selectivity for the D4 receptor and are suitable for the treatment and prophylaxis of states of anxiety, depression, schizophrenia, obsessions, Parkinson's disease, tardive dyskinesia, nausea and disorders of the gastro-intestinal tract.Type: GrantFiled: March 9, 1999Date of Patent: July 10, 2001Assignee: Merck Patent Gesellschaft mitInventors: Michael Arlt, Henning Bottcher, Gerd Bartoszyk, Christoph Seyfried
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Patent number: 6251909Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula wherein p is 2 or 3 and X denotes oxygen, N(CH2)nR6 or CR7R8, and R3, R4, R5, R6, R7, R8, Ar and n have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin)-antagonists.Type: GrantFiled: February 18, 2000Date of Patent: June 26, 2001Assignee: Boehringer Ingelheim KGInventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Publication number: 20010003749Abstract: A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.Type: ApplicationFiled: January 3, 2001Publication date: June 14, 2001Inventors: Alexander Glenn Godfrey, Daniel Timothy Kohlman, John Cunningham O'Toole, Yao-Chang Xu, Tony Yantao Zhang
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Patent number: 6245767Abstract: A monohydrate of an aminobenzenesulfonic acid derivative represented by the following formula (I), for example, 2-(1-piperazinyl)-5-methylbenzenesulfonic acid, is substantially free from weight change due to moisture absorption and can be weighed accurately in manufacturing a pharmaceutical composition for the treatment of heart diseases comprising said monohydrate.Type: GrantFiled: September 24, 1999Date of Patent: June 12, 2001Assignee: Mitsubishi Chemical CorporationInventors: Chika Yamazaki, Tadao Sato, Tatsuo Nagano
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Patent number: 6239135Abstract: A series of aryl piperazine compounds of the formula: or the pharmaceutically acceptable salts thereof, are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.Type: GrantFiled: December 9, 1998Date of Patent: May 29, 2001Assignee: Eli Lilly and CompanyInventors: Daniel Timothy Kohlman, Yao-Chang Xu
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Patent number: 6232314Abstract: Arylalkylpiperazine compounds (1) wherein B is aryl or optionally substituted aryl; R1 is hydroxy; R2 and R3 are the same or different and are independently selected from hydrogen or C1-3 alkyl; m is 0, 1 or 2; D is a linking chain of atoms which may be optionally substituted and which contains from 1 to 8 atoms in the chain; E is a phenolic antioxidant group or a corresponding amino derivative thereof wherein the phenolic hydroxyl is replaced by amino, are disclosed. The compounds have both free radical scavenging activity and block excitatory amino acid activity. Some compounds of the present invention also display an affinity for voltage-sensitive sodium channels.Type: GrantFiled: March 18, 1999Date of Patent: May 15, 2001Assignee: Monash UniversityInventors: Bevyn Jarrott, Philip Mark Beart, William Roy Jackson, Vijaya Bhaskar Kenche, Alan Duncan Robertson, Maree Patricia Collis
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Patent number: 6221868Abstract: Remedies/preventives (therapeutic or preventive agents) against frequent urination (pollakiuria)/urinary incontinence which contain as an active ingredient compound having a tropone structure or pharmacologically acceptable salt thereof and a novel compound having the tropone structure. The compounds having a tropone structure and having the above pharmacological effects are those represented by, for example, general (1): wherein R1 and R2 represent each a hydrogen atom, lower alkyl group, etc., R3 represents —OR or —NR2; R4, R5 and R12 represents each a hydrogen atom or a lower alkyl group, X represents a nitrogen atom or CH, Z represents —CHAr2, an unsubstituted or substituted phenyl, etc. m is 1 or 2. These compounds are novel ones excluding those wherein Z is —CHAr2.Type: GrantFiled: December 20, 1999Date of Patent: April 24, 2001Assignee: Nippon Kayaku Kabushiki KaishaInventors: Ichiro Koga, Kazuhisa Narita, Atsushi Okada