The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/368)
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Patent number: 6589953Abstract: The invention concerns novel indole piperazine derivatives of formula (I). It also concerns a method for preparing said compounds and their use as therapeutically active substances, in particular for treating or preventing diseases related to the disfunction of 5-HT1-like receptors.Type: GrantFiled: July 11, 2001Date of Patent: July 8, 2003Assignee: Pierre Fabre MedicamentInventors: Michel Perez, Serge Halazy
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Publication number: 20030119849Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, -Z represents —C, ═C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy,and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors.Type: ApplicationFiled: October 15, 2002Publication date: June 26, 2003Inventors: Roelof W. Feenstra, Johannes A.M. van der Heijden, Cornelis G. Kruse, Stephen K. Long, Gustaaf J.M. van Scharrenburg
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Publication number: 20030114448Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: May 28, 2002Publication date: June 19, 2003Applicant: Millennium Pharmaceuticals, Inc.Inventors: Penglie Zhang, Bing-Yan Zhu, Wenrong Huang, Robert M. Scarborough
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Patent number: 6573264Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: October 23, 2000Date of Patent: June 3, 2003Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Prabha N. Ibrahim, Kevin Shenk, Elfatih Elzein, Venkata Palle
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Patent number: 6569882Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: February 19, 2002Date of Patent: May 27, 2003Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Patent number: 6566363Abstract: Pyrazole-thiazole compounds that modulate and/or inhibit the activity of cyclin-dependent kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating cyclin-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: August 8, 2001Date of Patent: May 20, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Wesley Kwan Mung Chong, Rohit Kumar Duvadie
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Publication number: 20030083336Abstract: The present invention relates to a novel class of substituted phenylpiperazinyl derivatives having the formula 1Type: ApplicationFiled: June 25, 2002Publication date: May 1, 2003Applicant: H. Lundbeck A/SInventors: Thomas Ruhland, Jan Kehler, Kim Andersen, Benny Bang-Andersen, Mario Rottlander
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Patent number: 6545151Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31 (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: January 16, 2001Date of Patent: April 8, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6541471Abstract: A compound of formula (I): wherein: G represents a group such as: wherein R1 and R2 independently represent a hydrogen atom or an alkyl, cycloalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl or heteroarylalkyl group, or, R1 and R2 together with the nitrogen atom form a heterocycloalkyl group, R3 represents a hydrogen atom or an alkyl or optionally substituted phenyl group, Ra represents a hydroxy group, a linear or branched (C1-C6)alkoxy group or an amino group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, m is an integer of from 0 to 1 inclusive, n and q are integers of from 0 to 6 inclusive, p and r are integers of from 1 to 6 inclusive, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base; and medicinal products containing the same which are useful as a TXA2 receptType: GrantFiled: July 12, 2002Date of Patent: April 1, 2003Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Thierry Dubuffet, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Christine Vayssettes-Courchay
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Patent number: 6537995Abstract: A method is provided for treating or preventing a disorder or condition selected from hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant personality disorder, premature ejaculation, eating disorders, obesity, cluster headache, migraine, pain, obsessive-compulsive disorder, panic disorder, endocrine disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, premenstrual syndrome, fibromyalgia syndrome, stress incontinence, chronic paroxysmal hemicrania and headache in a mammal, comprising administering to a mammal in need of such treatment or prevention an amount of a compound of the formula (I) or the pharmaceutically acceptable salt thereof; wherein X, Y, Z, R2 and R3 are as defined herein.Type: GrantFiled: May 22, 2001Date of Patent: March 25, 2003Assignee: Pfizer Inc.Inventor: Harry R. Howard
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Patent number: 6534506Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: April 6, 2001Date of Patent: March 18, 2003Assignee: Merck & Co., Inc.Inventors: Diem N. Nguyen, Craig A. Stump, Theresa M. Williams
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Publication number: 20020198217Abstract: Compounds of the formula: 1Type: ApplicationFiled: April 24, 2002Publication date: December 26, 2002Applicant: WyethInventors: Megan Tran, Gary P. Stack
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Publication number: 20020169314Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: ApplicationFiled: December 6, 2001Publication date: November 14, 2002Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Patent number: 6469011Abstract: Compound of formula (I): which is useful as a TXA2 and 5-HT2 receptor antagonist and pharmaceutical compositions containing the same.Type: GrantFiled: January 18, 2001Date of Patent: October 22, 2002Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Jean-Jacques Descombes
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Publication number: 20020151552Abstract: The compounds of the formulas described herein, wherein X, R0, R1, R2, n and m have the meanings given in the specification, are useful as active ingredients in pharmaceutical compositions. The invention relates to the use of said compounds as a medicament and for the manufacture of a medicament for the treatment of erectile dysfunction.Type: ApplicationFiled: December 17, 2001Publication date: October 17, 2002Inventor: Adnan Badwan
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Patent number: 6448244Abstract: The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof; as antifungals; their processes for preparation, composition containing them and their use as a medicine.Type: GrantFiled: November 9, 2000Date of Patent: September 10, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken
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Publication number: 20020115670Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: November 1, 2001Publication date: August 22, 2002Applicant: American Home Products CorporationInventors: Michael Gerard Kelly, Derek Cecil Cole
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Patent number: 6432958Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R1 and R2 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, alkylthio, hydroxy, (un)substituted amino, cyano, nitro, sulfonamide, trifluoromethyl or trifluoromethoxy; R3, R4, R5, R6, and R8 are independently hydrogen or alkyl; and X is sulfur, oxygen or NR7 where R8 is defined herein; m is an integer chosen from 0, 1 or 2; and Ar is an aryl or heteroaryl group as further 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: August 29, 2001Date of Patent: August 13, 2002Assignee: Neurogen CorporationInventor: Xiao Shu He
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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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Publication number: 20020094989Abstract: Pyrrolidine compounds of Formula I: 1Type: ApplicationFiled: October 10, 2001Publication date: July 18, 2002Inventors: Jeffrey J. Hale, Christopher L. Lynch, Charles G. Caldwell, Christopher A. Willoughby, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Amy Gentry, Malcolm MacCoss, Zenon D. Konteatis
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Patent number: 6399777Abstract: The esylate, mesylate, and tartrate salts of ziprasidone exhibit excellent solubilities in cyclodextrins.Type: GrantFiled: May 7, 2001Date of Patent: June 4, 2002Assignee: Pfizer Inc.Inventors: Yesook Kim, Kevin C. Johnson, Ravi M. Shanker
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Patent number: 6391882Abstract: A substituted 4-, 5-, 6-, and 7-indole derivative of Formula (I) wherein A is a group having formula (IIA), (IIB), (IIC) wherein X, U, Y, R3 to R12, Z, W, n and m are as defined above. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.Type: GrantFiled: February 2, 2001Date of Patent: May 21, 2002Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Ivan Mikkelsen, Christian Korg-Jensen
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Publication number: 20020058658Abstract: The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives.Type: ApplicationFiled: February 23, 2001Publication date: May 16, 2002Inventors: Gerhard Jaehne, Matthias Gossel, Martin Bickel
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Publication number: 20020058666Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: August 29, 2001Publication date: May 16, 2002Applicant: Neurogen CorporationInventor: Xiao Shu He
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Publication number: 20020058809Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: November 2, 2001Publication date: May 16, 2002Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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Patent number: 6387389Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.Type: GrantFiled: June 30, 1999Date of Patent: May 14, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa
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Patent number: 6384036Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: August 11, 2000Date of Patent: May 7, 2002Assignee: G.D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Publication number: 20020049215Abstract: Pyrazole-thiazole compounds that modulate and/or inhibit the activity of cyclin-dependent kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating cyclin-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: ApplicationFiled: August 8, 2001Publication date: April 25, 2002Inventors: Wesley Kwan Mung Chong, Rohit Kumar Duvadie
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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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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: 6369063Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 9, 2002Assignee: Cor Therapeutics, Inc.Inventors: Ting Su, Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6346622Abstract: where the substituents have the meanings indicated in the description, their preparation and use as serotonin antagonists.Type: GrantFiled: April 20, 2000Date of Patent: February 12, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Uta Dullweber, Dorothea Starck, Gerd Steiner, Alfred Bach, Franz Emling, Xavier Garcia-Ladona, Hans-Jürgen Teschendorf, Karsten Wicke
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Publication number: 20010051625Abstract: The present invention relates to substituted indane or dihydroindole compounds of 1Type: ApplicationFiled: July 26, 2001Publication date: December 13, 2001Applicant: H. Lundbeck A/SInventors: Jens Kristian Perregaard, Ivan Mikkelsen, Henrik Pedersen
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Publication number: 20010041796Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1).Type: ApplicationFiled: January 16, 2001Publication date: November 15, 2001Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyma
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Patent number: 6316617Abstract: This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.Type: GrantFiled: August 8, 2000Date of Patent: November 13, 2001Assignee: Neurogen CorporationInventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson
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Patent number: 6313116Abstract: Compounds that are inhibitors of phosphodiesterase and have therapeutic utility, are of formula (i) wherein R1 is C3-6 cycoalkyl, or C1-3 alkyl optionally substituted with one or more fluorine atoms; R2 is C1-6 alkyl, C3-6 cycloalkyl, CF3, CH2CF3, C2F5 or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, are each H, C1-3 alkyl, halogen, CF3 or CN, provided that both are not H; or a pharmaceutically-acceptable salt thereofType: GrantFiled: February 9, 2001Date of Patent: November 6, 2001Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Andrew Sharpe, Hannah Jayne Kendall, Richard John Davenport, Verity Margaret Sabin, George Martin Buckley, Marianna Dilani Richard, Alan Findlay Haughan
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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: 20010031752Abstract: The invention relates to substituted 8,8a-dihydro-3aH-indeno[1,2-d]thiazoles and to their physiologically acceptable salts and physiologically functional derivatives.Type: ApplicationFiled: February 23, 2001Publication date: October 18, 2001Inventors: Gerhard Jaehne, Hans-Jochen Lang, Matthias Gossel, Martin Bickel
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Patent number: 6291463Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: R1 and R2 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano or trifluoromethyl; Ar represents aryl or heteroaryl, each of which is optionally substituted with R3, R4 and/or R4; R3, R4, and R6 independently represent hydrogen, halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, perfluoro(C1-C6)alkyl, perfluoro(C1-C6)alkoxy, or SO2NH2; or R3 and R4 together with the atoms to which they are attached represent a ring having 5-7 atoms; and R5 represents hydrogen or C1-C6 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 30, 1999Date of Patent: September 18, 2001Assignee: Neurogen CorporationInventor: Xi Chen
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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: 6284759Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R1 and R2 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, alkylthio, hydroxy, (un)substitutedamino, cyano, nitro, sulfonamide, trifluoromethyl or trifluoromethoxy; R3, R4, R5, R6, and R8 are independently hydrogen or alkyl; and X is sulfur, oxygen or NR7 where R8 is defined herein; m is an integer chosen from 0, 1 or 2; and Ar is an aryl or heteroaryl group as further 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: September 30, 1999Date of Patent: September 4, 2001Assignee: Neurogen CorporationInventor: Xiao Shu He
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Patent number: 6277852Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof, wherein Z is oxygen, S(O)m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C1-C6)alkyl or phenyl; X is hydrogen, chloro, fluoro, bromo, iodo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, (C1-C6)alkyl S(O)a wherein a is 0, 1 or 2; or phenyl wherein the phenyl group is optionally substituted; Y is wherein M is oxygen or sulfur; X2 is hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkyl S(O)c wherein c is 0, 1 or 2; R1 is selected from wherein R6 is selected from the group consisting of hydrogen, optionally substituted (C1-C6)alkyl; and wherein R6 in G5 together with R7 form a 2 carbon chain; and R9 and R10 are independently hydrogen or (C1-C6)alkyl; R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally substituted; and R3 is —(CH2)tB, wherein t is 0-3 and B is hydrogType: GrantFiled: April 14, 1999Date of Patent: August 21, 2001Assignee: Pfizer INCInventor: Harry R. Howard
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Patent number: 6277853Abstract: The invention concerns novel indole piperazine derivatives of Formula (I): It also concerns a method for preparing said compounds and their use as therapeutically active substances, in particular for treating or preventing diseases related to the dysfunction of 5 -HT1-like receptors.Type: GrantFiled: February 23, 2000Date of Patent: August 21, 2001Assignee: Pierre Fabre MedicamentInventors: Michel Perez, Serge Halazy
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Patent number: 6262047Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: October 10, 1997Date of Patent: July 17, 2001Assignee: COR Therapeutics, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6255306Abstract: The present invention relates to compounds of the formulaType: GrantFiled: August 11, 1998Date of Patent: July 3, 2001Inventor: John E. Macor
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Patent number: 6251907Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 17, 1999Date of Patent: June 26, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 6245765Abstract: The invention is directed to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one, pharmaceutical compositions containing said ziprasidone mesylate dihydrates, and methods of adminsitering the ziprasidone mesylate dihydrates to treat psychotic diseases.Type: GrantFiled: August 30, 1999Date of Patent: June 12, 2001Assignee: Pfizer IncInventors: Frank R. Busch, Carol A. Rose, Russell J. Shine
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Patent number: 6245766Abstract: A method for treating a psychiatic condition or disorder selected from anxiety disorders such as panic disorder, posttraumatic stress disorder and phobias, psychotic episodes of anxiety, anxiety associated with psychosis, psychotic mood disorders such as severe major depressive disorder and mood disorders associated with psychotic disorders such as acute mania or depression associated with bipolar disorder, schizophrenia, behavioral manifestations of mental retardation, conduct disorder or autistic disorder, dementias such as dementias of the Alzheimer's type, and dyskinesias such as drug induced and neurodegeneration based dyskinesias in a mammal, including a human, comprising administering to said mammal a pharmaceutically effective amount of a compound of the formula or a pharmaceutically acceptable acid addition salt thereof, wherein n, X, Y and Ar are as defined above.Type: GrantFiled: December 18, 1998Date of Patent: June 12, 2001Assignee: Pfizer IncInventor: Eric J. Watsky
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Patent number: RE37478Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: December 9, 1998Date of Patent: December 18, 2001Assignee: Aventis Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau
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Patent number: RE37729Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: February 3, 1999Date of Patent: June 4, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler