Chalcogen And A Carbocyclic Ring Bonded Directly At 4-position Patents (Class 546/217)
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Publication number: 20040266751Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: June 16, 2004Publication date: December 30, 2004Inventor: Bryan W. King
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Patent number: 6821965Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseaseType: GrantFiled: February 2, 2001Date of Patent: November 23, 2004Assignee: AsterZeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6806378Abstract: The present invention provides a catalyst system and a process for the preparation of a nonracemic chiral alcohol by hydrogenation of a ketone using the catalyst system, wherein the catalyst system comprises ruthenium, a nonracemic chiral diphosphine ligand, an amino-thioether ligand, and a base.Type: GrantFiled: May 21, 2002Date of Patent: October 19, 2004Assignee: DSM N.V.Inventors: Charles E. Tucker, Qiongzhong Jiang
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Patent number: 6794511Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: December 1, 2000Date of Patent: September 21, 2004Assignee: G. D. SearleInventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo, Clara I. Villamil
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Publication number: 20040180929Abstract: The present invention provides compounds having formula (I): 1Type: ApplicationFiled: March 4, 2004Publication date: September 16, 2004Inventors: Kyungjin Kim, Emily Aijun Liu, Steven Gregory Mischke
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Patent number: 6753336Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.Type: GrantFiled: March 11, 2003Date of Patent: June 22, 2004Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
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Patent number: 6743921Abstract: The present invention provides a process for the preparation of a nonracemic diastereomer of 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol by hydrogenation of a corresponding nonracemic 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanone using a catalyst system comprising ruthenium, a nonracemic diphosphine ligand, a bidentate amine ligand selected from amino-thioethers and achiral diamines, and a base.Type: GrantFiled: January 24, 2002Date of Patent: June 1, 2004Assignees: DSM Catalytica Pharmaceuticals, Inc., Pfizer, Inc.Inventors: Charles E. Tucker, Qiongzhong Jiang
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Publication number: 20040063759Abstract: A compound of the formula 1Type: ApplicationFiled: July 8, 2003Publication date: April 1, 2004Applicant: Pfizer Inc.Inventors: Laura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Christopher S. Poss
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Patent number: 6710060Abstract: The present invention relates to a compound represented by the following formula (I) or a salt thereof, or a pharmaceutical composition containing the compound as an effective ingredient: (wherein A represents, for example, phenyl group substituted with R1 and R2 or unsubstituted thienyl group; R1 and R2 each independently represent, for example, hydrogen atom, halogen atom or lower alkoxycarbonyl group; R3 represents, for example, hydrogen atom; R4 represents, for example, lower alkyl group; R5 represents, for example, lower alkoxy group; R6 represents, for example, hydrogen atom; R7 and R8 each represent, for example, hydrogen atom, respectively; X represents, for example, a single bond; Y represents, for example, methylene group or benzylidene group substituted with R1; and Z represents, for example, methylene group.Type: GrantFiled: October 4, 2001Date of Patent: March 23, 2004Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ichiro Yamamoto, Manabu Itoh, Fumiaki Yamasaki, Yutaka Miyazaki, Shinichi Ogawa
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Publication number: 20040010139Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) 1Type: ApplicationFiled: March 18, 2003Publication date: January 15, 2004Inventors: William A. Nugent, Tai Yue
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Patent number: 6664273Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: November 25, 2002Date of Patent: December 16, 2003Assignee: Schering CorporationInventors: Duane A. Burnett, Wen-Lian Wu
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Publication number: 20030212108Abstract: A novel crystal form of ,&agr;-dimethyl-4-{1-hydroxy-4-{4-(hydroxydiphenylmethyl)-1-piperidinyl}butyl}benzeneacetic acid hydrochloride, processes for its preparation and its pharmaceutical use are disclosed.Type: ApplicationFiled: June 6, 2003Publication date: November 13, 2003Inventors: Julian Anthony Davies, James E. Gano
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Patent number: 6645986Abstract: The present invention is directed to a process for the preparation of the mesylate trihydrate of the (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol compound having the formula (I): The present invention is also further comprises a process for enantiomeric resolution and isolation of the (D)-(−)-tartrate salt of the compound of the formula (I).Type: GrantFiled: April 23, 2001Date of Patent: November 11, 2003Assignee: Pfizer Products, Inc.Inventors: Stanley Walter Walinsky, Terry Gene Sinay, Jr., Joseph Philip Rainville
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Patent number: 6642256Abstract: Described are piperidines of Formula I and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.Type: GrantFiled: November 30, 2001Date of Patent: November 4, 2003Assignee: Warner-Lambert Company LLCInventors: Brian Edward Kornberg, Russell Andrew Lewthwaite, David Manning, Sham Shridhar Nikam, Ian Leslie Scott
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Patent number: 6638950Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 20, 2001Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
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Publication number: 20030153764Abstract: The present invention provides a process for preparing N-protected-4-substituted piperidines of formula (I) wherein Pg represents a suitable nitrogen protecting group; X represents a heterocycle, substituted heterocycle, substituted alkenyl or substituted aryl wherein the substituted heterocycle, substituted alkenyl or substituted aryl are substituted with from 1 to 3 suitable activating groups; and R1, R2, R3, R4, R5, R6, R7, and R8 each independently represent an alkyl, alkenyl, cycloalkyl, aryl, substituted aryl, heterocycle, or substituted heterocycle, comprising treating a compound of formula (II) wherein the substituents are defined as above, with triethylsilane and trifluoroacetic acid.Type: ApplicationFiled: May 28, 2002Publication date: August 14, 2003Inventors: Alexander Glenn Godfrey, Steven Wayne Pedersen
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Publication number: 20030144521Abstract: The present invention provides a process for the preparation of a nonracemic diastereomer of 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol by hydrogenation of a corresponding nonracemic 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanone using a catalyst system comprising ruthenium, a nonracemic diphosphine ligand, a bidentate amine ligand selected from amino-thioethers and achiral diamines, and a base.Type: ApplicationFiled: January 24, 2002Publication date: July 31, 2003Applicant: DSM CATALYTICA PHARMACEUTICALS, INC.Inventors: Charles E. Tucker, Qiongzhong Jiang
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Patent number: 6570018Abstract: The present invention is directed to a novel process for the preparation of the mesylate trihydrate of the compound of formula (I), (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol: The present invention is further directed to a process for the preparation of a (2S)-(+)-compound of formula (II): wherein R1 is a protecting group. In addition, the present invention relates to intermediates useful in said processes.Type: GrantFiled: April 23, 2001Date of Patent: May 27, 2003Assignee: Pfizer IncInventors: Stanley Walter Walinsky, Terry Gene Sinay, Jr., Joseph Philip Rainville
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Patent number: 6559166Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.Type: GrantFiled: September 27, 2001Date of Patent: May 6, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
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Patent number: 6555541Abstract: The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: July 10, 2000Date of Patent: April 29, 2003Assignee: Astrazeneca UK LimitedInventors: Mark Furber, Timothy J Luker, Michael P Mortimore, Philip Thorne, Premji Meghani
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Patent number: 6538002Abstract: The present in to s directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: June 8, 2000Date of Patent: March 25, 2003Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates
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Patent number: 6525069Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 21, 2000Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
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Patent number: 6518286Abstract: The invention provides compounds of general formula (I) wherein: R1 represents optionally substituted, C1-C12 alkyl or optionally substituted 3- to 10-membered saturated or unsaturated ring system comprising up to two ring carbon atoms that form carbonyl groups and comprising up to 4 ring heteroatoms independently selected from nitrogen, oxygen and sulfur; m is 0-1; Q represents OCH2, C1-C4 alkylene or C2-C4 alkenylene; T represents C(O)NH, or when m is 0, T may additionally represent a bond or NH, or when m is 1 and Q represents C1-C4 alkylene, T may additionally represent NH; n is 1-4; each R2 and R3 independently represents H or C1-C4 alkyl; V represents N, and W represents N or CH; X represents O, C(O), CH(OH), SO2, NH or N(C1-C6 alkyl), provided that when W represents N, then X represents either C(O) or SO2 and when W represents CH, then X is other than SO2; R4 represents optionally substituted phenyl; R5 and R6 each independently represent H, C1-C6 alkyl or hydroxyC1-C6 alkyl, or R5 and R6 together withType: GrantFiled: June 1, 2000Date of Patent: February 11, 2003Assignee: AstraZeneca ABInventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas McInally, Bryan Roberts, Stephen Thom
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Publication number: 20030027812Abstract: The present invention relates to lactam derivatives of the formula 1Type: ApplicationFiled: August 15, 2002Publication date: February 6, 2003Applicant: Pfizer Inc.Inventor: Harry R. Howard
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Publication number: 20020193600Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1Type: ApplicationFiled: April 24, 2002Publication date: December 19, 2002Inventors: Daniel R. Henton, Frederick J. McCarty, Susan I. Tripp, Jill E. DeWitt
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Patent number: 6476054Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: October 17, 2000Date of Patent: November 5, 2002Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates, Dooseop Kim, Shankaran Kothandaraman, Liping Wang
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Patent number: 6455549Abstract: A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.Type: GrantFiled: March 20, 1998Date of Patent: September 24, 2002Assignee: Suntory LimitedInventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura
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Patent number: 6448270Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using the 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as cerebral ischemia, central nervous system trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headaches, convulsions, aminoglycoside antibiotics-induced hearing loss, chronic pain, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, urinary incontinence and neurodegenerative disorders such as lathyrism, Alzheimers' 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: June 13, 2000Date of Patent: September 10, 2002Assignees: 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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Publication number: 20020123492Abstract: The present invention relates beta-amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: September 5, 2002Inventors: David Lauffer, Michael Mullican
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Patent number: 6444686Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: December 17, 1999Date of Patent: September 3, 2002Assignee: Brsitol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6437136Abstract: Disclosed is a method for producing (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterized in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-piperidine-hydrobromide and reacted with 1,3,5-trimethoxybenzol to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring.Type: GrantFiled: April 27, 2001Date of Patent: August 20, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Breipohl, Jürgen Michalowsky
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Patent number: 6432985Abstract: The invention relates to a compound of the formula its R,R-, S,S-enantiomers and racemic mixtures thereof and to their pharmaceutically acceptable acid addition salts. The compound of formula I and its R,R- and S,S-enantiomers may be used as medicaments for the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.Type: GrantFiled: March 19, 2001Date of Patent: August 13, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
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Publication number: 20020091117Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: November 6, 2001Publication date: July 11, 2002Applicant: Pfizer Inc.Inventor: Harry Ralph Howard
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Patent number: 6362203Abstract: Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1 and R2 are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3 represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4 and R5 each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9 or —OCOR10 (in which R6, R9 and R10 each independently represents a hydrogen atom, a lower alkyl group, or the like, R7 and R8 are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.Type: GrantFiled: October 30, 2000Date of Patent: March 26, 2002Assignee: SSP Co., LTDInventors: Kinichi Mogi, Yoshihiko Kanamaru, Noriyuki Kawamoto, Teruo Komoto, Norimitsu Umehara, Susumu Sato, Tetsuo Oka
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Publication number: 20020016465Abstract: The present invention is directed to a process for the preparation of the mesylate trihydrate of the (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy4-phenylpiperidin-1-yl)-1-propanol compound having the formula (I): 1Type: ApplicationFiled: April 23, 2001Publication date: February 7, 2002Inventors: Stanley Walter Walinsky, Terry Gene Sinay, Joseph Philip Rainville
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Publication number: 20020016466Abstract: The present invention is directed to a novel process for the preparation of the mesylate trihydrate of the compound of formula (I), (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol: 1Type: ApplicationFiled: April 23, 2001Publication date: February 7, 2002Inventors: Stanley Walter Walinsky, Terry Gene Sinay, Joseph Philip Rainville
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Patent number: 6271383Abstract: The present invention relates to antibiotic compounds and in particular to antibiotic compounds containing an oxazolidinone ring. This invention further relates to processes for their preparation, to intermediates useful in their preparation, to their use as therapeutic agents and to pharmaceutical compositions containing them.Type: GrantFiled: July 30, 1999Date of Patent: August 7, 2001Assignee: Zeneca LimitedInventor: Michael Barry Gravestock
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Publication number: 20010011092Abstract: Novel compounds of the formula 1Type: ApplicationFiled: January 25, 2001Publication date: August 2, 2001Inventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 6225473Abstract: Disclosed is a method for producing (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterised in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-pyridine-hydrobromide and reacted with 1,3,5-trimethoxyphenyl to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring.Type: GrantFiled: July 21, 2000Date of Patent: May 1, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Breipohl, Jürgen Michalowsky
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Patent number: 6180648Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, and Y have any of the meanings defined in the specification; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula I, to a mammal in need of such treatment.Type: GrantFiled: April 7, 1998Date of Patent: January 30, 2001Assignee: Biostream Therapeutics, Inc.Inventors: Alan P. Kozikowski, Gian Luca Araldi
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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: 6090824Abstract: 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 Substance P and NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: November 14, 1996Date of Patent: July 18, 2000Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Bruce T. Dembofsky
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Patent number: 6063926Abstract: Compounds within the genus represented by the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein: T is substituted phenyl or substituted pyridyl; ##STR2## R.sup.4 is methyl or ethyl; and Z is substituted piperidinyl.Type: GrantFiled: November 18, 1998Date of Patent: May 16, 2000Assignee: Schering CorporationInventors: Gregory A. Reichard, Cheryl A. Alaimo, Neng-Yang Shih, Pauline C. Ting, Nicholas I. Carruthers, Brian J. Lavey
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Patent number: 6048876Abstract: A medicine having the following basic structure, for the alleviation or treatment of symptoms derived from ischemic diseases and seizures, epilepsy, and migraine, having a powerful action in suppressing cytotoxic Ca.sup.2+ overload and free from side-effects: ##STR1## wherein Z.dbd.C, CH, or N, X.dbd.O or CH.sub.2, E and Y.dbd.H, OH, a halogen, alkoxy, alkyl, or a halogen-substituted alkyl.Type: GrantFiled: September 23, 1996Date of Patent: April 11, 2000Assignee: Suntory LimitedInventors: Hirokazu Annoura, Mayumi Uesugi, Shinsuke Matsuki, Atsuko Fukunaga, Toshio Tatsuoka, Shigeki Tamura, Norio Inomata
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Patent number: 6046213Abstract: This invention relates to compounds of formula (I), or pharmaceutically acceptable acid addition salts thereof, wherein: (a) R.sup.2 and R.sup.5 are taken separately and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, (C.sub.1 -C.sub.6) alkyl, halo, CF.sub.3, OH or OR.sup.7 and R.sup.5 is methyl or ethyl; or (b) R.sup.2 and R.sup.5 are taken together, forming a chroman-4-ol ring, and R.sup.1, R.sup.3 and R.sup.4 are each independently hydrogen, (C.sub.1 -C.sub.6) alkyl, halo, CF.sub.3, OH or OR.sup.7 ; and R.sup.6 is a substituted piperidinyl, pyrrolidinyl or 8-azabicyclo(3.2.1)octanyl derivative; provided that (a) when R.sup.2 and R.sup.5 are taken separately, at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is not hydrogen; and (b) when R.sup.2 and R.sup.5 are taken together, at least one of R.sup.1, R.sup.3 and R.sup.Type: GrantFiled: February 13, 1997Date of Patent: April 4, 2000Assignee: Pfizer Inc.Inventors: Bertrand L. Chenard, Todd W. Butler
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Patent number: 6017933Abstract: Mannich bases of conjugated styryl ketones have been developed which are effective as cytotoxicity and anticancer agents, and which also have antifungal activity. Preferred compounds are those of the formula ##STR1## where R.sub.1 is Cl, CH.sub.3 or OCH.sub.3 and R.sub.2 is H or Cl. A compound of particular interest is (3-[3-(4-chlorophenyl)-2-propenoyl]-4-[2-(4-chlorophenyl)vinylene]-1-ethyl -4-piperidinol hydrochloride.Type: GrantFiled: January 28, 1999Date of Patent: January 25, 2000Assignees: University of Saskatchewan Technologies Inc., Wayne State UniversityInventors: Jonathan R. Dimmock, Elias K. Manavathu
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Patent number: 6008233Abstract: The invention relates to the trihydrate of the mesylate salt of (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propano l, pharmaceutical compositions containing said compound and methods of treating disorders of the central nervous system by administering said compound.Type: GrantFiled: May 7, 1998Date of Patent: December 28, 1999Assignee: Pfizer IncInventors: Marta M. Andino, Terry G. Sinay, Eugene F. Fiese
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Patent number: 5998444Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 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: November 26, 1997Date of Patent: December 7, 1999Assignee: Zeneca Ltd.Inventor: Keith Russell
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Patent number: 5981539Abstract: The present invention discloses compounds of the formula ##STR1## any of its enantiomers or any mixture thereof, or a pharmaceutically-acceptable addition salt thereof, wherein X, Ar, R, R.sup.1, R.sup.2, n are as defined herein.Type: GrantFiled: May 29, 1998Date of Patent: November 9, 1999Assignee: Neurosearch A/SInventors: Oskar Axelsson, Dan Peters, Nielsen Elsebet stergaard, Palle Christophersen
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Patent number: 5932735Abstract: Selected derivatives of 1-oxyl-2,2,6,6-tetramethyl-4-hydroxypiperidine are surprisingly effective as inhibitors to prevent the premature polymerization of acrylic and methacrylic acids, their esters, their amides, vinyl acetate and acrylonitrile in the presence of water. Some of these derivatives are new compounds.Type: GrantFiled: June 10, 1998Date of Patent: August 3, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Glen T. Cunkle, Matthew E. Gande, Raymond Seltzer, Thomas F. Thompson