Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Additional Six-membered Nitrogen Hetero Ring Patents (Class 514/253.13)
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Patent number: 7494995Abstract: A compound selected from those of formula (I): wherein: R1 represents an NR3SO2R4 group wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents an alkyl group, aryl group or NR5R6 group, R2 represents an alkyl, cycloalkyl or cycloalkylalkyl group, and medicinal products containing the same which are useful in treating conditions treatable by antagonists of type H3 central histamine receptors.Type: GrantFiled: May 11, 2006Date of Patent: February 24, 2009Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage
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Patent number: 7494994Abstract: A compound selected from those of formula (I): wherein: X represents a C(O) or SO2 group, R1 represents an aryl group or a group NR3R4 wherein R3 and R4 are as defined in the description, R2 represents an alkyl, (C3-C8)cycloalkyl or (C3-C8)cycloalkyl-(C1-C6)alkyl group, its isomers, and addition salts thereof, and medicinal products containing the same which are useful in treating conditions treatable by antagonists of type H3 central histamine receptors.Type: GrantFiled: May 11, 2006Date of Patent: February 24, 2009Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage
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Patent number: 7494989Abstract: Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains and various diseases associated with the N-type calcium channels.Type: GrantFiled: September 17, 2007Date of Patent: February 24, 2009Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Kayo Otani, Seiji Niwa, Satoshi Iwayama, Akira Takahara, Hajime Koganei, Yukitsugu Ono, Shinichi Fujita, Tomoko Takeda, Masako Hagihara, Akiko Okajima
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Publication number: 20090048264Abstract: The invention is concerned with novel piperazine amide derivatives of formula (I) wherein R1 to R11, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: ApplicationFiled: August 6, 2008Publication date: February 19, 2009Inventors: Henrietta Dehmlow, Bernd Kuhn, Ulrike Obst Sander, Stephan Roever, Tanja Schulz-Gasch, Matthew Wright, Rene Wyler
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Publication number: 20090042855Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 3, 2008Publication date: February 12, 2009Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20090042852Abstract: The present invention relates to certain novel pyridin compounds of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, and processes for their preparation, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: January 4, 2006Publication date: February 12, 2009Applicant: ASTRAZENECA ABInventors: Peter Bach, Jonas Bostrom, Kay Brickmann, Leifeng Cheng, Fabrizio Giordanetto, Robert D. Groneberg, Darren Martin Harvey, Michael F. O'Sullivan, Fredrik Zetterberg, Krister Osterlund
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090036452Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090023711Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.Type: ApplicationFiled: January 5, 2007Publication date: January 22, 2009Applicant: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Jalaj Arora, Dean Brown
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Publication number: 20090005355Abstract: The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R1 is hydrogen atom or a substituent for amino group, R2 is hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, Z is oxygen atom or —N(R3)—, R3 is hydrogen atom or an optionally substituted alkyl group, R4a and R4b may be the same or different, and each is hydrogen atom or an optionally substituted alkyl group, or may be bonded to each other at the both ends to form an alkylene group, or a pharmaceutically acceptable salt thereof, which has an excellent tachykinin receptor antagonistic action.Type: ApplicationFiled: July 1, 2005Publication date: January 1, 2009Applicant: Tanabe Seiyaku Co., Ltd.Inventors: Tsutomu Miyake, Takeshi Yamanaka, Hidetoshi Asai, Yoshihiro Terakawa
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Publication number: 20090005393Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: January 16, 2007Publication date: January 1, 2009Inventors: Patrick Rene Angibaud, Laurence Francoise Marconnet-Decrane, Janine Arts
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Publication number: 20080312209Abstract: The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Z, X and B are as defined in the specification. The compounds are partial or full agonists at the GPR38 receptor. Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.Type: ApplicationFiled: July 12, 2005Publication date: December 18, 2008Inventors: Gregor James MacDonald, Steven James Stanway, Mervyn Thompson, Susan Marie Westaway
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Publication number: 20080306087Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 3, 2006Publication date: December 11, 2008Applicant: ASTRAZENECA ABInventors: James R. Empfield, Michael Laplante, Megan Murphy King, Thomas R. Simpson, Maxime C. Tremblay, James M. Woods, Jingbo Yan
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Publication number: 20080306066Abstract: Certain non-imidazole heterocyclic compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: August 6, 2008Publication date: December 11, 2008Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20080287453Abstract: A compound of formula (I) P—W—C(?X)-L-Q ??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.Type: ApplicationFiled: December 18, 2006Publication date: November 20, 2008Inventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
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Selected Cgrp-Antagonists, Processes for Preparing Them and Their Use as Pharmaceutical Compositions
Publication number: 20080280887Abstract: The invention relates to CGRP-antagonists of general formula (I), wherein R1, R2, R3, R4 and R5 are defined in claim 1, to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures salts and salt hydrates thereof, in particular to 10 salts thereof, which are physiologically compatible with acids or inorganic or organic bases and to compounds of general formula (I), wherein one or several hydrogen atoms are substituted by deuterium. Drugs containing said compounds, the use thereof and a method for the production thereof are also disclosed.Type: ApplicationFiled: September 27, 2006Publication date: November 13, 2008Inventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Gerhard Schaenzle, Dirk Stenkamp, Henri Doods, Kirsten Arndt -
Patent number: 7449457Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: December 2, 2002Date of Patent: November 11, 2008Assignee: Eli Lilly and CompanyInventors: David Kent Herron, Sajan Joseph, Angela Lynn Marquart, John Joseph Masters, David Mendel, Gerald Floyd Smith, Anne Louise Tebbe, Philip Parker Waid, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20080269215Abstract: The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein ring A, ring B, R1, R2, R3, R4, R5, m and n are as defined herein.Type: ApplicationFiled: November 14, 2006Publication date: October 30, 2008Applicant: GENENTECH INC.Inventors: Richard A. Goldsmith, Daniel P. Sutherlin, Kirk D. Robarge, Alan G. Olivero
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Patent number: 7435736Abstract: The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3-antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: GrantFiled: December 17, 2003Date of Patent: October 14, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Patent number: 7432268Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17?-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.Type: GrantFiled: November 14, 2005Date of Patent: October 7, 2008Assignee: Schering CorporationInventors: Timothy Guzi, Kamil Paruch, Alan Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena
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Patent number: 7423039Abstract: The invention relates to substituted (4-phenylpiperazin-1-yl)acylpiperidine derivatives of formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparation process and therapeutic application.Type: GrantFiled: May 26, 2006Date of Patent: September 9, 2008Assignee: Sanofi-aventisInventors: Victor Dos Santos, Jean Wagnon
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Publication number: 20080188485Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroarylalkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.Type: ApplicationFiled: March 26, 2008Publication date: August 7, 2008Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
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Publication number: 20080167321Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, W, V, R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: September 20, 2005Publication date: July 10, 2008Applicant: XENON PHARMACEUTICALS INC.Inventors: Rajender Kamboj, Vishnumurthy Kodumuru
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Publication number: 20080139556Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Raymond W. KOSLEY, Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Publication number: 20080119451Abstract: The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, integer m, integer n and W have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).Type: ApplicationFiled: January 17, 2006Publication date: May 22, 2008Applicant: ASTRAZENECA ABInventors: Keith Hopkinson Gibson, Elaine Sophie Elizabeth Stokes, Michael James Waring, David Michael Andrews, Zbigniew Stanley Matusiak
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Patent number: 7351702Abstract: This invention provides compounds of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; next to R3 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: May 23, 2002Date of Patent: April 1, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Publication number: 20080070924Abstract: This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK1-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression and tolerance in opioid-based treatments of pain.Type: ApplicationFiled: June 7, 2004Publication date: March 20, 2008Inventors: Frans Eduard Janssens, Francois Maria Sommen, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck, Theo Frans Meert
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Publication number: 20080004286Abstract: The present invention discloses a method of using compounds, which have HDM2 protein antagonist activity, to treat or prevent cancer, other diseases caused by abnormal cell proliferation, diseases associated with HDM2, or diseases caused by inadequate P53 activity.Type: ApplicationFiled: June 27, 2007Publication date: January 3, 2008Inventors: Yaolin Wang, Rumin Zhang, Yao Ma, Brian Robert Lahue, Gerald W. Shipps
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Patent number: 7314879Abstract: The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunctionType: GrantFiled: January 21, 2003Date of Patent: January 1, 2008Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Caño Ivan Collado, Oscar De Frutos-Garcia, Christopher William Doecke, Matthew Joseph Fisher, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Jeffrey Thomas Mullaney, Paul Leslie Ornstein, Chaoyu Xie
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Patent number: 7307081Abstract: The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.Type: GrantFiled: December 17, 2003Date of Patent: December 11, 2007Assignee: Schering CorporationInventors: Michael W. Miller, Jack D. Scott
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Publication number: 20070281923Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: May 25, 2007Publication date: December 6, 2007Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
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Patent number: 7294630Abstract: The present invention provides compounds of formula (I): wherein each R independently represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen or C1-4 alkyl group; R4 represents a trifluoromethyl group; R5 represents hydrogen, a C1-4 alkyl group or C(O)R6; R6 represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; or a pharmaceutically acceptable salt or solvate thereof; compositions containing the same, processes for their preparation and methods for their use in the treatment of conditions mediated by tachykinins.Type: GrantFiled: February 21, 2006Date of Patent: November 13, 2007Assignee: SmithKline Beecham CorporationInventor: Giuseppe Alvaro
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Patent number: 7276500Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine [sic], morpholine [sic], piperidine [sic], —NR5R6 and ?and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl [sic], pyridyl [sic], pyrimidyl [sic] and pyridazyl [sic], it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by by [sic] a maximum of two R8 radicalsType: GrantFiled: October 20, 2003Date of Patent: October 2, 2007Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Patent number: 7276509Abstract: The present invention relates to piperidine derivatives of formula (I): wherein R represents halogen or C1-4 alkyl; R1 represents hydrogen or C1-4 alkyl; R2 represents hydrogen, C1-4 alkyl; R3 represents hydrogen, C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen, C1-4 alkyl, C3-7 cycloalkyl, C(O)R6 or S(O)2R6; R6 represents C1-4 alkyl or C3-7 cycloalkyl; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p is an integer from 1 to 2; X and Y are independently C(O) or CH2; provided that i) X and Y are not both C(O) and ii) when X and Y are both CH2 and p is 1, R5 is not hydrogen, C1-4 alkyl or C(O)R6; and pharmaceutically acceptable salts and solvates thereof, the process for their preparation and their use in the treatment of conditions mediated by tachykinins.Type: GrantFiled: February 5, 2003Date of Patent: October 2, 2007Assignee: Glaxo Group LimitedInventors: Giuseppe Alvaro, Romano Di Fabio
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Patent number: 7214714Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.Type: GrantFiled: April 26, 2002Date of Patent: May 8, 2007Assignee: Taisho Pharmaceutical Co. Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Patent number: 7196080Abstract: The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein R1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like, R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like, R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, and n: 0 or 1).Type: GrantFiled: June 13, 2002Date of Patent: March 27, 2007Assignee: Astellas Pharma Inc.Inventors: Masahiro Iwata, Noriyuki Kawano, Hiroyuki Kaizawa, Tomofumi Takuwa, Issei Tsukamoto, Ryushi Seo, Kiyoshi Yahiro, Miki Kobayashi, Makoto Takeuchi
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Patent number: 7176205Abstract: The present invention relates to compounds of the formula wherein R1 and R1? are each independently hydrogen or methyl and X is —C(O)N(CH3)— or —N(CH3)C(O)—, and to pharmaceutically acceptable acid addition salts thereof for the treatment of numerous inflammatory conditions, migraine, rheumatoid arthritis, asthma, inflammatory bowel disease, mediation of the emetic reflex, Parkinson's disease, anxiety, depression, psychosis, motion sickness, induced vomiting, pain, headache, migraine, Alzheimer's disease, multiple sclerosis, attenuation of morphine withdrawal, cardiovascular changes, oedema, such as oedema caused by thermal injury, chronic inflammatory diseases such as rheumatoid arthritis, asthma/bronchial hyperreactivity and other respiratory diseases including allergic rhinitis, inflammatory diseases of the gut including ulcerative colitis and Crohn's disease, ocular injury and ocular inflammatory diseases, traumatic brain injury, motion sickness, emesis and psychoimmunologic and psychosomatic disorderType: GrantFiled: February 14, 2006Date of Patent: February 13, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Torsten Hoffmann, Patrick Schnider
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Patent number: 7157463Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: January 2, 2007Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Karin Briner, Christopher William Doecke, Matthew Joseph Fisher, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Jeffrey Thomas Mullaney, Chaoyu Xie
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Patent number: 7153824Abstract: The present invention is directed to methods of increasing oocyte production in a mammal. More specifically, the specification describes methods and compositions for inducing follicular maturation using a PDE inhibitor. The inhibitor may be used alone at high doses. Alternatively, the follicular maturation is achieved by combining a low dose of FSH with the PDE inhibitor treatment.Type: GrantFiled: April 1, 2004Date of Patent: December 26, 2006Assignee: Applied Research Systems ARS Holding N.V.Inventors: Stephen S. Palmer, Sean D. McKenna, Stephen J. Arkinstall, Aliza Eshkol, Michael C. MacNamee
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17 ?-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
Patent number: 7138396Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17?-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.Type: GrantFiled: January 28, 2005Date of Patent: November 21, 2006Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Alan K. Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena -
Patent number: 7119092Abstract: wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen, or a C1-4 alkyl group; R4 represents a trifluoromethyl group; R5 represents hydrogen, a C1-4 alkyl group or C(O)R6; R6 represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3 and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation and their use in the treatment of conditions mediated by tachykinins.Type: GrantFiled: October 12, 2001Date of Patent: October 10, 2006Assignee: SmithKline Beecham CorporationInventors: Giuseppe Alvaro, Paolo Maragni, Marsia Tampieri
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Patent number: 7115607Abstract: Selected substituted piperazine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: July 24, 2002Date of Patent: October 3, 2006Assignee: Amgen Inc.Inventors: Christopher H. Fotsch, Premilla Arasasingham, Yunxin Bo, Ning Chen, Martin H. Goldberg, Nianhe Han, Feng-Yin Hsieh, Michael G. Kelly, Qingyian Liu, Mark H. Norman, Duncan M. Smith, Markian Stec, Nuria Tamayo, Ning Xi, Shimin Xu
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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: 7098213Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graType: GrantFiled: October 14, 2005Date of Patent: August 29, 2006Assignee: Schering CorporationInventor: Michael W. Miller
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Patent number: 7060702Abstract: The present invention provides compounds of formula (I): wherein each R independently represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen or C1-4 alkyl group; R4 represents a trifluoromethyl group; R5 represents hydrogen, a C1-4 alkyl group or C(O)R6; R6 represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; or a pharmaceutically acceptable salt or solvate thereof; compositions containing the same, processes for their preparation and methods for their use in the treatment of conditions mediated by tachykinins.Type: GrantFiled: November 22, 2004Date of Patent: June 13, 2006Assignee: SmithKline Beecham CorporationInventors: Giuseppe Alvaro, Romano Di Fabio, Paolo Maragni, Marsia Tampieri, Maria Elvira Tranquillini
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Patent number: 7008946Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graType: GrantFiled: October 21, 2004Date of Patent: March 7, 2006Assignee: Schering CorporationInventor: Michael W. Miller
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Patent number: 6982256Abstract: The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof.Type: GrantFiled: September 9, 2002Date of Patent: January 3, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Christine Votteler, Bernd Kruss
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Patent number: 6953774Abstract: The present invention relates to methods of inducing ovulation in a female host comprising the administration of a non-polypeptide cyclic adenosine monophosphate (cAMP) level modulator to the female host. In another aspect, the invention provides for specific administration of the phosphodiesterase inhibitor prior to the luteal phase of the host's ovulatory cycle. Preferred non-polypeptide cAMP level modulator include phosphodiesterase inhibitors, particularly inhibitors of phosphodiesterase type 4.Type: GrantFiled: December 14, 2001Date of Patent: October 11, 2005Assignee: Applied Research Systems Ars Holding N.V.Inventors: Stephen Palmer, Sean McKenna, Mark Tepper, Aliza Eshkol, Michael C. MacNamee
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Patent number: 6936614Abstract: One aspect of the present invention relates to piperidine-piperazine compounds. A second aspect of the present invention relates to the use of the piperidine-piperazine compounds as ligands for various mammalian cellular receptors or transporters or both, including dopamine, serotonin or norepinephrine receptors or transporters, any combination of them, or all of them. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.Type: GrantFiled: March 24, 2004Date of Patent: August 30, 2005Assignee: Sepracor Inc.Inventors: Paul E. Persons, Heike Radeke