The Additional Five-membered Hetero Ring Also Has Chalcogen As A Ring Member Patents (Class 514/254.02)
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Publication number: 20080125431Abstract: Compounds in accord with Formula I: wherein R1, L, A, B, D, E, m, n, x and y are as defined in the description, processes for the preparation of such compounds and to new intermediates employed in the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds in therapy and for the treatment of diseases mentioned in the specification.Type: ApplicationFiled: September 12, 2007Publication date: May 29, 2008Applicant: ASTRAZENECAInventors: Ian Egle, Babu Joseph, Abdelmalik Slassi, Methvin Isaac, Fupeng Ma, Joshua Clayton
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Publication number: 20080119462Abstract: The present invention provides a method for treating a vascular hyperpermeable disease (except macular edema), which method comprises administering to a patient in need thereof a vascular adhesion protein-1 (VAP-1) inhibitor in an amount sufficient to treat said patient for said disease.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Applicants: Sucampo AG, Astellas Pharma Inc.Inventors: Ryuji UENO, Akira Nagashima, Takayuki Inoue, Mitsuru Ohkubo, Kousei Yoshihara
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Publication number: 20080113996Abstract: Methods of prevention or treatment of renal diseases or conditions associated with abnormal ion flux, in particular autosomal dominant polycystic kidney disease, with a modulator of human peroxisome proliferator activated receptor gamma.Type: ApplicationFiled: March 1, 2006Publication date: May 15, 2008Applicant: SmithKline Beecham CorporationInventor: Kathleen Keating Brown
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Patent number: 7365077Abstract: Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same.Type: GrantFiled: November 6, 2002Date of Patent: April 29, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Christopher Norbert Johnson, David John Nash, Geoffrey Stemp
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Patent number: 7361654Abstract: The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Bristol-Myers Squibb Co.Inventors: James Sheppeck, T. G. Murali Dhar, Lidia Doweyko, John Gilmore, David Weinstein, Hai-Yun Xiao, Bingwei V. Yang, Arthur M. Doweyko
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Patent number: 7345043Abstract: Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.Type: GrantFiled: April 1, 2005Date of Patent: March 18, 2008Assignee: Miikana TherapeuticsInventors: Sampath K. Anandan, Xiao-Yi Xiao, Dinesh V. Patel, John Ward
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Patent number: 7335660Abstract: This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the treatment of central nervous system disorders, such as depression, bipolar disorder, and anxiety.Type: GrantFiled: December 6, 2002Date of Patent: February 26, 2008Assignee: Eli Lilly and CompanyInventors: Javier Agejas-Chicharro, Graham Henry Timms, Andrew Caerwyn Williams, Nicholas Paul Camp, Jeremy Gilmore, Ana Belen Bueno Melendo, Carlos Lamas-Peteira
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Publication number: 20080027053Abstract: This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.Type: ApplicationFiled: July 9, 2007Publication date: January 31, 2008Inventors: Mark J. Macielag, Manomi A. Tennakoon
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Publication number: 20080027040Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: December 20, 2004Publication date: January 31, 2008Applicant: Morphochem Aktiengesellschaft Fur KombinatorischeInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Muller, Michael W. Cappi
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Publication number: 20080027073Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula I show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: August 18, 2006Publication date: January 31, 2008Applicant: Laboratorios Del Dr. Esteve, S.A.Inventors: Maria De Las Ermitas Alcalde-Pais, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal
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Patent number: 7319097Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous systemType: GrantFiled: August 30, 2005Date of Patent: January 15, 2008Assignee: Biovitrum ABInventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Lori Sutin, Andrew Mott, Jan Tejbrant
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Publication number: 20070293505Abstract: A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.Type: ApplicationFiled: June 13, 2007Publication date: December 20, 2007Inventors: Andrew C. McCREARY, Gustaaf J.M. Van Scharrenburg, Martinus Th.M. Tulp
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Publication number: 20070280943Abstract: The present invention is directed to pharmaceutical methods for the treatment of CD30 positive diseases, such as Hodgkin's disease, by administration of a combination of at least one sheddase inhibitor and at least one anti-CD30 immunotherapeutic.Type: ApplicationFiled: June 4, 2007Publication date: December 6, 2007Inventors: Steven M. Friedman, Robert C. Newton, Peggy A. Scherle, Krishna Vaddi
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Publication number: 20070281945Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: May 31, 2007Publication date: December 6, 2007Applicant: WyethInventors: Kevin Liu, Albert Jean Robichaud, Hassan Mahmoud Elokdah
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Patent number: 7300934Abstract: Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.Type: GrantFiled: June 1, 2004Date of Patent: November 27, 2007Assignee: Roche Palo Alto LLCInventors: Tobias Gabriel, Nancy Elisabeth Krauss
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Patent number: 7300939Abstract: Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine compounds, pharmaceutical compositions containing such substituted 1-propiolylpiperazine compounds, and the use of such substituted 1-propiolylpiperazine compounds for modulating mGluR5 receptor activity or for treating or inhibiting pain and various other conditions, especially conditions at least partly mediated by the mGluR5 receptor.Type: GrantFiled: January 4, 2007Date of Patent: November 27, 2007Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Stefan Oberboersch, Michael Haurand, Ruth Jostock, Klaus Schiene
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Patent number: 7297699Abstract: 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.Type: GrantFiled: May 16, 2005Date of Patent: November 20, 2007Assignee: Solvay Pharmaceuticals, Inc.Inventors: Roelof W. Feenstra, Johannes A. M. van der Heijden, Cornelis G. Kruse, Stephen K. Long, Gustaaf J. M. van Scharrenburg
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Patent number: 7273881Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) its stereoisomers thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, where Z is S, O or NH; and R, R1, R2 Ra, Rb, Rc, Rd, Z, A and B are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: January 13, 2005Date of Patent: September 25, 2007Assignee: Bristol-Myers Squibb CompanyInventor: Bingwei Vera Yang
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Patent number: 7271169Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.Type: GrantFiled: September 7, 2005Date of Patent: September 18, 2007Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Dmitry Koltun
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Patent number: 7265134Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: August 13, 2002Date of Patent: September 4, 2007Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Thomas J. Tucker, John T. Sisko, Anthony M. Smith, William C. Lumma, Jr.
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Patent number: 7262198Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: June 13, 2006Date of Patent: August 28, 2007Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeff Zablocki
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Patent number: 7256187Abstract: The invention relates to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the rifamycin derivatives having an oxime group at the C-11 position.Type: GrantFiled: March 9, 2005Date of Patent: August 14, 2007Assignee: Cumbre Pharmaceuticals Inc.Inventors: Jing Li, Charles Z. Ding, Zhenkun Ma
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Patent number: 7253173Abstract: Compounds of general formula (I) wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.Type: GrantFiled: November 5, 2003Date of Patent: August 7, 2007Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Paul Jones, Daniel Pagé, Niklas Plobeck, Christopher Walpole
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Patent number: 7241761Abstract: The present invention relates to compounds of the general formula I wherein R1 is the group and R2, R?, R?, R3, R4, R5, R6, R7, X1, X1?, X2, and N are as defined in the specification. Compounds of the invention are useful for the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: December 1, 2005Date of Patent: July 10, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Patent number: 7238689Abstract: An isoxazoline derivative represented by the following general formula [I]: wherein R1 and R2 may be the same or different and are each an alkyl group; R3, R4, R5 and R6 are each a hydrogen atom; Y is an optionally substituted 5- to 6-membered aromatic heterocyclic group or fused aromatic heterocyclic group having a hetero atom selected from a nitrogen atom, a oxygen atom and a sulfur atom; and n is an integer: of 0 to 2. The isoxazoline derivative has an excellent herbicidal effect and an excellent selectivity between crop and weed.Type: GrantFiled: February 7, 2002Date of Patent: July 3, 2007Assignees: Ihara Chemical Industry Co., Ltd., Japan and Kumiai Chemical IndustryInventors: Masao Nakatani, Ryotaro Kugo, Masahiro Miyazaki, Koichiro Kaku, Makoto Fujinami, Ryohei Ueno, Satoru Takahashi
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Patent number: 7229994Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is independently selected from hydrogen and fluoro; R4 is independently selected from —OH, —NH2 and —NHSO2R5; and R5 is independently selected from hydrogen, —CF3 and C1–C6 alkyl, or salts thereof or separate enantiomers and salts thereof; where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo.Type: GrantFiled: May 16, 2002Date of Patent: June 12, 2007Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Patent number: 7220744Abstract: The present invention relates to compounds of formula I wherein R1, R2, X1, and X2 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. Such compounds are inhibitors of the glycine transporter 1 (GlyT-1) and can be used in the treatment of schizophrenia, cognitive impairment, and Alzheimer's disease.Type: GrantFiled: January 3, 2006Date of Patent: May 22, 2007Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Patent number: 7214694Abstract: Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.Type: GrantFiled: December 9, 2003Date of Patent: May 8, 2007Assignee: Pfizer IncInventors: Usa Datta, Paul Vincent Fish, Kim James, Gavin Alistair Whitlock
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Patent number: 7214679Abstract: Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.Type: GrantFiled: January 13, 2004Date of Patent: May 8, 2007Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sundeep Dugar, Gregory R. Luedtke, Xuefei Tan, Glen McEnroe
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Patent number: 7208496Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.Type: GrantFiled: June 7, 2004Date of Patent: April 24, 2007Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Tim Marquart
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Patent number: 7189712Abstract: Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.Type: GrantFiled: October 10, 2003Date of Patent: March 13, 2007Assignee: SmithKline Beecham CorporationInventors: Matthew Lee Brown, Mui Cheung, Scott Howard Dickerson, Cassandra Gauthier, Philip Anthony Harris, Robert Neil Hunter, Gregory Pacofsky, Michael Robert Peel, Jeffrey Alan Stafford
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Patent number: 7166608Abstract: This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR2; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C?O, SO2, or CH?CH—; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar2 represents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S; R1 represents optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S; R2 represents hydrogen, optionally substituted (C1-4)alkyl, optionally substituted (C1Type: GrantFiled: October 9, 2002Date of Patent: January 23, 2007Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Christopher Norbert Johnson, David John Nash, Geoffrey Stemp
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Patent number: 7163952Abstract: The present invention relates to an azole compound represented by the formula [I] wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.Type: GrantFiled: December 3, 2002Date of Patent: January 16, 2007Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Tomoyuki Ikemoto, Shohei Sakata, Hiroshi Maegawa, Atsunori Kashiwagi
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Patent number: 7160886Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 27, 2004Date of Patent: January 9, 2007Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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Patent number: 7157464Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: June 11, 2003Date of Patent: January 2, 2007Assignee: Chemocentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Patent number: 7151103Abstract: The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire.Type: GrantFiled: October 16, 2002Date of Patent: December 19, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Franco Borsini, Kenneth Robert Evans
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Patent number: 7135473Abstract: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH?CH, CH?N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.Type: GrantFiled: August 13, 2003Date of Patent: November 14, 2006Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
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Patent number: 7125876Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useflul in the treatment of diabetes.Type: GrantFiled: December 5, 2003Date of Patent: October 24, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Dmitry Koltun, Jeff Zablocki
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Patent number: 7125865Abstract: The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.Type: GrantFiled: July 21, 2003Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: A. Brian Jones, Alan D. Adams, Ahren I. Green, Shaei Y. Huang, Bruno Tse, Clare E. Gutteridge, Yuan Cheng
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Patent number: 7119086Abstract: The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopressin V1b receptors and/or for the ocytocin receptors and, furthermore, for certain compounds, affinity for the V1a receptors. The invention also relates to the process for preparing them, to the intermediate compounds of formula (IV) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.Type: GrantFiled: July 15, 2002Date of Patent: October 10, 2006Assignee: Sanofi-AventisInventors: Alain Di Malta, Georges Garcia, Richard Roux, Bruno Schoentjes, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
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Patent number: 7098212Abstract: The present invention relates to compounds of the formula I and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R1, R2, R3, R4 and R5 are as defined herein. Moreover, the present invention is also directed at pharmaceutical compositions comprising a compound of the formula I and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed at methods of using the herein described compounds and compositions for treating or preventing a disorder or condition that can be treated or prevented by antagonizing the CCR1 receptor in a mammal.Type: GrantFiled: October 18, 2002Date of Patent: August 29, 2006Inventors: Laura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Gregory D. Lundquist, Christopher S. Poss, Andrei Shavnya
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Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
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Patent number: 7094778Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: October 14, 2003Date of Patent: August 22, 2006Assignee: Syntex (U.S.A.) LLCInventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 7087610Abstract: The invention encompasses a series of benzothiazole compounds which inhibit HIV entry and are useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for using these compounds.Type: GrantFiled: May 9, 2005Date of Patent: August 8, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell
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Patent number: 7084144Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.Type: GrantFiled: May 19, 2004Date of Patent: August 1, 2006Assignee: The Jordanian Pharmaceutical MFG & Medical Equipment CO LTDInventor: Adnan Badwan
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Patent number: 7078406Abstract: The present invention is directed to a compound of Formula I: wherein A, R1, and R2 are defined herein. The present invention is also directed to compositions comprising compounds of Formula I, methods of using compounds of Formula I, and methods of making compounds of Formula I.Type: GrantFiled: July 14, 2004Date of Patent: July 18, 2006Assignee: Johnson & Johnson Pharmaceutical Research & Development, L.L.C.Inventors: Theodore E. Carver, Jr., James M. Rinker
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: RE39198Abstract: 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 amounts of one 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: November 15, 2000Date of Patent: July 18, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Yulin Chiang, Kenneth J. Bordeau, Edward J. Glamkowski