Ring Sulfur In The Polycyclo Ring System Patents (Class 546/202)
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Patent number: 6420415Abstract: Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.Type: GrantFiled: March 20, 2001Date of Patent: July 16, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Patent number: 6417199Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are a-substituted with ether, thioether amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: September 29, 1995Date of Patent: July 9, 2002Assignee: Eli Lilly and CompanyInventor: Brian S. Muehl
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Publication number: 20020087001Abstract: The present invention relates to certain novel substituted piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of psychotic disorders.Type: ApplicationFiled: January 11, 2002Publication date: July 4, 2002Inventors: Duncan Robertson Rae, David Robert Jaap
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Patent number: 6407121Abstract: The present invention provides an arylpiperidine derivative of the formula (I) or a pharmaceutically acceptable salt thereof, which has antipsychotic effect: wherein D is a carbon atom or a nitrogen atom, E is a CH group or a nitrogen atom, G is an oxygen atom, a sulfur atom, a nitrogen atom or an NH group, Y1 is a hydrogen atom or a halogen atom, n is an integer of 1 to 4, and R1 is a group represented by any of the formulas (i) to (iv) defined in the specification.Type: GrantFiled: September 13, 2000Date of Patent: June 18, 2002Assignees: Nihon Nohyaku Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Masashi Nagamine, Makoto Gotoh, Masanori Yoshida, Atsuro Nakazato, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa
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Patent number: 6403614Abstract: This invention provides novel benzothiophene compounds of formula I: which are useful for the inhibition of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further. relates to pharmaceutical formulations of compounds of formula I.Type: GrantFiled: September 30, 1998Date of Patent: June 11, 2002Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Mark Gregory Stocksdale
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Publication number: 20020068739Abstract: The present invention relates to the compounds of formula (I) in which X, R1, R2 and R3 are as defined in claim 1. These compounds are cholesteryl acyl transferase (ACAT) inhibitors.Type: ApplicationFiled: November 1, 2001Publication date: June 6, 2002Applicant: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Diedier Festal, Jean Yves Nioche, Guy Augert, Jacques Deserprit
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Patent number: 6399778Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.Type: GrantFiled: June 6, 1995Date of Patent: June 4, 2002Assignee: Eli Lilly and CompanyInventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
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Patent number: 6399634Abstract: The present invention provides method of treating endometriosis using novel benzothiophene compounds of formula I wherein R is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R1 is —H, —OH, —O(C1-C4 alkyl),, —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl) chloro or bromo; R2 is —H or —OH; n is 2 or 3; and R3 and R4 each are independently C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 19, 1995Date of Patent: June 4, 2002Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, George J. Cullinan, Jeffrey A. Dodge, Kennan J. Fahey, Charles D. Jones
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Patent number: 6395755Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)3, CO(CH2)4, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; R6 is and pharmaceutically acceptable salts thereof; useful in treating estrogen deficient pathology.Type: GrantFiled: March 10, 1995Date of Patent: May 28, 2002Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Jeffrey A. Dodge
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Patent number: 6391891Abstract: The invention relates to compounds which are ligands for 5HT1, of formula (I) Wherein L, Q, Ra, Rb and Ry are as defined in the specification, processes for their preparation and their pharmaceutical composition as well as their use in the treatment of anxiety and depression.Type: GrantFiled: January 26, 2000Date of Patent: May 21, 2002Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman, Sean Thomas Flynn
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Patent number: 6391890Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, R1, R2 and m 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 neurogenic 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: March 27, 2000Date of Patent: May 21, 2002Assignee: Novo Nordisk A/SInventors: Tine Krogh Jørgensen, Knud Erik Andersen, Rolf Hohlweg, Uffe Bang Olsen, Erik Fischer, Zdenek Polivka, Kaler Sindelar
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Patent number: 6391901Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: May 21, 2002Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Alan D Palkowitz, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Patent number: 6387512Abstract: A photochromic grey coloring 2H-naphtho[1,2-b]pyran of formula (1) wherein R1 is selected from mono-, di- or poly-substituted aryl groups, mono-, di- or poly-substituted naphthyl groups and mono-, di- or poly-substituted heteroaryl groups, wherein at least one substituent is a nitrogen containing group, including amino, C1-C20 and C6-C20 alkylamino, C1-C20 and C6-C20 dialkylamino, C2-C20 dialkenylamino, C2-C20 or C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, tetra (C1-C10 linear or branched alkyl) guanidino and cyclic-amino groups and at least one of R7 and R9, which may be the same or different, is selected from C1-C20 N alkylamino C1-C20 N-alkylamido, C1-C20 N,N-dialkylamido, amido, nitro, amino, C1-C20 alkylamino, C1-C20 dialkylamino, C2-C20 dialkenylamino, C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, or cyclicamino groups.Type: GrantFiled: March 16, 2001Date of Patent: May 14, 2002Assignee: James Robinson LimitedInventors: David Allan Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
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Patent number: 6380220Abstract: Piperidineketocarboxylic acid derivatives of the general formula I and their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given in the description, preparation of these compounds and their use as drugs.Type: GrantFiled: April 15, 1999Date of Patent: April 30, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Jürgen Delzer
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Patent number: 6369074Abstract: The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formulae Ia and Ib are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: October 1, 1999Date of Patent: April 9, 2002Assignee: Pfizer Inc.Inventors: Harry R. Howard, Brian T O'Neill
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Patent number: 6358980Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Patent number: 6359138Abstract: The present invention relates to 4-hydroxy-piperidine derivatives of the general formula wherein X denotes —O—, —NH—, —CH2—, —CH═, —CHOH—, —CO—, —S—, —SO— or —SO2—; R1-R4 are, independently from each other, hydrogen, hydroxy, lower-alkyl-sulfonylamino, 1- or 2-imidazolyl or acetamido; R5-R8 are, independently from each other, hydrogen, hydroxy, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or trifluoromethyloxy; a and b may be a double bond, provided that when “a” is a double bond, “b” cannot be a double bond; n is 0-2; m is 1-3; p is 0 or 1 and to pharmaceutically acceptable addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers, which can be used in mediating processes underlying development of CNS including learning and memory formation and function.Type: GrantFiled: November 24, 1997Date of Patent: March 19, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Büttelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, René Wyler
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Patent number: 6355804Abstract: A process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them, which comprises the step of reacting a 2-oxazoline compound with a piperidine derivative in the presence of an acid is provided. This process is an industrially excellent process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them.Type: GrantFiled: December 29, 2000Date of Patent: March 12, 2002Assignee: Ajinomoto Co., Inc.Inventors: Isao Arai, Takashi Yamamoto, Hirokazu Naora
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Patent number: 6353010Abstract: Compounds of the formula (i) have therapeutic utility via inhibition of TNF or phosphodiesterase.Type: GrantFiled: October 21, 1999Date of Patent: March 5, 2002Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, John Gary Montana
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Patent number: 6350884Abstract: This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.Type: GrantFiled: September 30, 1997Date of Patent: February 26, 2002Assignee: Eli Lilly and CompanyInventors: Charles David Jones, Alan David Palkowitz, Kenneth Jeff Thrasher
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Publication number: 20020019533Abstract: The present invention relates to a novel serotonin antagonist and an anti-platelet agent, more particularly, a serotonin antagonist and an anti-platelet agent which potently and specifically inhibit the serotonin 2 receptor with low adverse side effect.Type: ApplicationFiled: February 8, 1999Publication date: February 14, 2002Inventors: SHINGO MAKINO, HARUMI ARISAKA, HIROSHI YAMAMOTO, MASATAKA SHOJI, RYOTA YOSHIMOTO
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Publication number: 20020016298Abstract: Compounds according to the formula: 1Type: ApplicationFiled: December 21, 2000Publication date: February 7, 2002Inventors: Bruce A. Hay, Anthony P. Ricketts, Bridget M. Cole
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Patent number: 6323206Abstract: Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1998Date of Patent: November 27, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
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Patent number: 6316470Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, 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: June 29, 2000Date of Patent: November 13, 2001Assignee: Neurogen CorporationInventors: Renata Xavier Kover, Silva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Patent number: 6303593Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f 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-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Christopher Forbes, Shouwu Miao, William H. Parsons, Kathleen Rupprecht, Frank Kayser
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Patent number: 6303633Abstract: Compounds of the formula wherein ring A, ring B, ring D, R2, R3, R4, R5, R6, R11, R12, R13, 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: November 11, 1999Date of Patent: October 16, 2001Assignee: Pfizer IncInventors: Yuhpyng L. Chen, Arthur A. Nagel
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Patent number: 6303620Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: May 6, 1999Date of Patent: October 16, 2001Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Michael Ankersen
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Patent number: 6291484Abstract: This invention provides novel benzothiophene compounds of the formula I: which are useful for the treatment of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.Type: GrantFiled: January 13, 2000Date of Patent: September 18, 2001Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Jeffrey Alan Dodge
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Patent number: 6288105Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: February 3, 2000Date of Patent: September 11, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Matthew J Fisher, Richard W Harper, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Patent number: 6288234Abstract: Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.Type: GrantFiled: June 4, 1999Date of Patent: September 11, 2001Assignee: Advanced Medicine, Inc.Inventor: John H. Griffin
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Patent number: 6288085Abstract: The present invention relates to certain novel piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of psychotic disorders.Type: GrantFiled: June 17, 1999Date of Patent: September 11, 2001Assignee: Akzo Nobel N.V.Inventors: Duncan Robertson Rae, Samuel George Gibson
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Patent number: 6284756Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: September 4, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Richard W Harper, Todd J Kohn, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Michael R Wiley, Minsheng Zhang
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Patent number: 6284775Abstract: There are disclosed compounds of the formula, where n is 0, 1 or 2; A is where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; K is N or CH; m is 1 or 2; k is 1 or 2; R1 and R2 are independently hydrogen, loweralkyl, or aryl except that when R1 is or aryl, R2 is hydrogen, or alternatively R1+R2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R3 and R4 are independently hydrogen or loweralkyl, or alternatively R3+R4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl sigType: GrantFiled: June 17, 1998Date of Patent: September 4, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Nicholas Joseph Hrib, John Gerard Jurcak
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Patent number: 6281228Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof, or prodrug esters thereof, A is where Z is N or CH, or where Z is or CH2 when is a single bond; and wherein L1, R, R1, R3, R3′, R3a, R3b, R4, R4′, R5, R5a, X, are as defined herein.Type: GrantFiled: June 14, 1999Date of Patent: August 28, 2001Assignee: Bristol-Myers Squibb CompanyInventor: Joseph A. Tino
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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: 6265575Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.Type: GrantFiled: August 5, 1999Date of Patent: July 24, 2001Assignee: Eli Lilly and CompanyInventors: Kenneth Jeff Thrasher, Kenneth Lee Hauser, Alan David Palkowitz
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Patent number: 6258826Abstract: Formulations and applications thereof are described which are useful for the inhibition of various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of structure I represented by the following structure in combination with compounds of formula II represented by the following structure where X, Y, R, R′, R6, R7 and R8 are as defined herein.Type: GrantFiled: September 1, 1999Date of Patent: July 10, 2001Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Brian Stephen Muehl, Kenneth Jeff Thrasher
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Patent number: 6251921Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.Type: GrantFiled: May 14, 1999Date of Patent: June 26, 2001Assignee: Eli Lilly and CompanyInventors: Jolie Anne Bastian, Nickolay Yuri Chirgadze, Michael Lyle Denney, Matthew Joseph Fisher, Robert James Foglesong, Richard Waltz Harper, Mary George Johnson, Valentine Joseph Klimkowski, Todd Jonathan Kohn, Ho-Shen Lin, Michael Patrick Lynch, Jefferson Ray McCowan, Alan David Palkowitz, Michael Enrico Richett, Daniel Jon Sall, Gerald Floyd Smith, Kumiko Takeuchi, Jennifer Marie Tinsley, Minsheng Zhang
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Patent number: 6242605Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is 0 or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturatedType: GrantFiled: December 10, 1999Date of Patent: June 5, 2001Assignee: American Home Products CorporationInventors: Panolil Raveendranath, Joseph Zeldis, Galina Vid, John R. Potoski, Jianxin Ren, Silvio Iera
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Patent number: 6231786Abstract: In the fluorinated azoles of the formula (I) R1(—A1)a—T—(A2—)b(M—A3—)cR2 (I) the symbols and indices have -the following meanings: T is undirected and is 4-fluorothiazole-2,5-diyl, 5-fluorothiazole-2,4-diyl, 4-fluorooxazole-2,5-diyl, 5-fluorooxazole-2,4-diyl or 4-fluoroisoxazole-2,5-diyl; R1 and R2 are identical or different and are hydrogen or a straight-chain or branched C1-20-alkyl or C2-20-alkenyl radical (with or without asymmetrical carbon atoms); A1, A2 and A3 are identical or different and are, for example, phenylene-1,4-diyl or cyclohexane-1,4-diyl; M is undirected and is —OC(═O)—, —OCH2—, —CH2CH2—, —OC(═O)CH2CH2—, —OCH2CH2CH2—, —C≡C—, —CH2CH2CH2CH2— or a single bond; a, b and c, independently of one another, are 0 or 1, with the proviso that the sum a+b+c is 1 or 2.Type: GrantFiled: January 18, 2000Date of Patent: May 15, 2001Assignee: Clariant GmbHInventors: Rainer Wingen, Barbara Hornung, Ayako Ogawa, Wolfgang Schmidt
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Patent number: 6214827Abstract: Novel compounds of Formula are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: June 23, 1998Date of Patent: April 10, 2001Assignee: Schering CorporationInventors: Adriano Afonso, John J. Baldwin, Ronald J. Doll, Ge Li, Alan K. Mallams, F. George Njoroge, Dinanath F. Rane, John C. Reader, Randall R. Rossman
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Patent number: 6207683Abstract: Disclosed are N-substituted hydroxyalkyl or carboxyalkyloxyalkyl analogs of 9- and/or 10-oxo-4Hbenzo[4,5]cycloheptal[1,2-b]thiophene compounds, or 9-OH and/or 10-OH-substituted analogs thereof, which possess antihistaminic and antiasthmatic properties with reduced sedative side effects. The optically active isomers and pharmaceutically acceptable salts thereof are also described. The compounds were also found to prevent smooth muscle hyperreactivity.Type: GrantFiled: October 29, 1999Date of Patent: March 27, 2001Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
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Patent number: 6207834Abstract: A process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them, which comprises the step of reacting a 2-oxazoline compound with a piperidine derivative in the presence of an acid is provided. This process is an industrially excellent process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them.Type: GrantFiled: October 12, 1999Date of Patent: March 27, 2001Assignee: Ajinomoto Co., Inc.Inventors: Isao Arai, Takashi Yamamoto, Hirokazu Naora
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Patent number: 6184221Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal illnesses.Type: GrantFiled: August 4, 1998Date of Patent: February 6, 2001Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann, Joachim Brendel
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Patent number: 6166006Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.Type: GrantFiled: December 17, 1998Date of Patent: December 26, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Patent number: 6156787Abstract: The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## where A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O),R.sup.1, OR.sup.1 or NR.sup.1 R.sup.6 ;R.sup.1 is hydrogen; C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl each of which is optionally substituted by amino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxy, C.sub.1-6 alkylaminocarbonyl, one, two or three hydroxy groups, one, two or three halogen atoms or a four, five or six-membered saturated heterocyclic ring containing a nitrogen atom and optionally either an oxygen atom or a further nitrogen atom which ring is optionally substituted by C.sub.1-4 alkyl on the further nitrogen atom; aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro, cyano, C.sub.Type: GrantFiled: April 22, 1999Date of Patent: December 5, 2000Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Mark Stuart Chambers
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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: 6150355Abstract: A phenylpiperidine derivative or pharmaceutical acceptable salt thereof represented by formula (I): ##STR1## wherein X represents CH or N; Y--Z represents CH.sub.2 --O, CH.sub.2 --S, CH.sub.2 --CH.sub.2, CH.dbd.CH or CONR.sup.5 (wherein R.sup.5 represents hydrogen or lower alkyl); R.sup.1 represents hydrogen, lower alkyl, halogen, lower alkoxy or trifluoromethyl; and R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen, lower alkyl or QR.sup.6 (wherein Q represents a single bond or lower alkylene, and R.sup.6 represents hydroxy, lower alkoxyalkoxy, lower alkoxy, lower alkylthio, nitro, halogen, lower alkanoyloxy, lower alkoxycarbonyl, lower alkanoyl or carboxyl).The present invention provides novel phenylpiperidine derivatives useful as analgesics.Type: GrantFiled: March 13, 1998Date of Patent: November 21, 2000Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Hirokazu Koshimura, Shigeru Aono, Shunji Ichikawa, Shigeto Kitamura
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Patent number: 6147092Abstract: The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen,--CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl),or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogenR.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ;R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen;n is 0-4; and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: April 19, 1999Date of Patent: November 14, 2000Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Raymond Francis Kauffman
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Patent number: 6143744Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 5, 1999Date of Patent: November 7, 2000Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker