Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Additional Six-membered Hetero Ring (e.g., Nicotinic Acid, Etc.) Patents (Class 544/365)
  • Patent number: 7560553
    Abstract: The present invention provides a group of compounds found to increase the number of neurons derived from stem cells for use as a therapeutic agent in neurological conditions or diseases. In one embodiment of the present invention, the compounds are used to detect the mechanism by which the number of neurons is increased.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: July 14, 2009
    Assignee: Neuralstem, Inc.
    Inventors: Judith Kelleher-Andersson, Karl K. Johe
  • Publication number: 20090170850
    Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.
    Type: Application
    Filed: May 9, 2008
    Publication date: July 2, 2009
    Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
  • Publication number: 20090131417
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: November 17, 2008
    Publication date: May 21, 2009
    Inventors: Michael A. Letavic, Kiev S. Ly
  • Publication number: 20090124633
    Abstract: The present invention relates to heterocyclic substituted N-Oxides of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
    Type: Application
    Filed: March 26, 2007
    Publication date: May 14, 2009
    Inventors: Alfred Jonczyk, Wilfried Rautenberg
  • Publication number: 20090124602
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: August 7, 2008
    Publication date: May 14, 2009
    Inventors: FRANCOIS MALTAIS, GUY BEMIS, TIANSHENG WANG, JUAN-MIGUEL JIMENEZ, RONALD KNEGTEL, CHRIS DAVIS, DAMIEN FRAYSSE
  • Patent number: 7494989
    Abstract: 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: Grant
    Filed: September 17, 2007
    Date of Patent: February 24, 2009
    Assignee: 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
  • Publication number: 20090042852
    Abstract: 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: Application
    Filed: January 4, 2006
    Publication date: February 12, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Peter Bach, Jonas Bostrom, Kay Brickmann, Leifeng Cheng, Fabrizio Giordanetto, Robert D. Groneberg, Darren Martin Harvey, Michael F. O'Sullivan, Fredrik Zetterberg, Krister Osterlund
  • Publication number: 20090042855
    Abstract: 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: Application
    Filed: June 3, 2008
    Publication date: February 12, 2009
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
  • Publication number: 20090036452
    Abstract: 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: Application
    Filed: July 28, 2008
    Publication date: February 5, 2009
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20090036420
    Abstract: 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: Application
    Filed: July 28, 2008
    Publication date: February 5, 2009
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20090005393
    Abstract: 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: Application
    Filed: January 16, 2007
    Publication date: January 1, 2009
    Inventors: Patrick Rene Angibaud, Laurence Francoise Marconnet-Decrane, Janine Arts
  • Patent number: 7465733
    Abstract: A compound selected from those of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, alkyl, alkoxy, phenyl and cyano, X represents a bond, an oxygen atom or a group selected from —(CH2)m—, —OCH2— and —NR5—, wherein m represents 1 or 2, and R5 is as defined in the description, Y represents an oxygen atom or a group selected from NR7 and CHR8, wherein R7 and R8 are as defined in the description, Z represents a nitrogen atom or a CH group, n represents 1 or 2, Ak represents an alkylene chain, Ar represents an aryl or heteroaryl group, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: December 16, 2008
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Louis Peglion, Aimée Dessinges, Bertrand Goument, Mark Millan, Clotilde Mannoury La Cour
  • Publication number: 20080306087
    Abstract: 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: Application
    Filed: August 3, 2006
    Publication date: December 11, 2008
    Applicant: ASTRAZENECA AB
    Inventors: James R. Empfield, Michael Laplante, Megan Murphy King, Thomas R. Simpson, Maxime C. Tremblay, James M. Woods, Jingbo Yan
  • Publication number: 20080287453
    Abstract: 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: Application
    Filed: December 18, 2006
    Publication date: November 20, 2008
    Inventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
  • Patent number: 7449457
    Abstract: 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: Grant
    Filed: December 2, 2002
    Date of Patent: November 11, 2008
    Assignee: Eli Lilly and Company
    Inventors: 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
  • Publication number: 20080275027
    Abstract: The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.
    Type: Application
    Filed: July 17, 2006
    Publication date: November 6, 2008
    Inventors: Rachael Ann Ancliff, Mark James Bamford, Simon Teanby Hodgson, Christopher Allan Parr, Panayiotic Alexandrou Procopiou, David Matthew Wilson, Michael Woodrow
  • Publication number: 20080269215
    Abstract: 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: Application
    Filed: November 14, 2006
    Publication date: October 30, 2008
    Applicant: GENENTECH INC.
    Inventors: Richard A. Goldsmith, Daniel P. Sutherlin, Kirk D. Robarge, Alan G. Olivero
  • Patent number: 7432268
    Abstract: 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: Grant
    Filed: November 14, 2005
    Date of Patent: October 7, 2008
    Assignee: Schering Corporation
    Inventors: Timothy Guzi, Kamil Paruch, Alan Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena
  • Patent number: 7423049
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: May 8, 2006
    Date of Patent: September 9, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
  • Publication number: 20080167321
    Abstract: 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: Application
    Filed: September 20, 2005
    Publication date: July 10, 2008
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Rajender Kamboj, Vishnumurthy Kodumuru
  • Publication number: 20080139556
    Abstract: 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: Application
    Filed: December 6, 2006
    Publication date: June 12, 2008
    Applicant: 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
  • Patent number: 7342015
    Abstract: A heteroaryl derivative having the formula (I).
    Type: Grant
    Filed: June 27, 2002
    Date of Patent: March 11, 2008
    Assignee: H. Lundbeck A/S
    Inventors: Mario Rottländer, Ejner Knud Moltzen, Ivan Mikkelsen, Thomas Ruhland, Kim Andersen, Christian Krog-Jensen
  • Publication number: 20080045541
    Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.
    Type: Application
    Filed: February 5, 2005
    Publication date: February 21, 2008
    Applicant: Bayer-HealthCare AG
    Inventors: Heike Gielen-Haertwig, Barbara Albrecht, Marcus Bauser, Jorg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
  • Publication number: 20080027073
    Abstract: 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: Application
    Filed: August 18, 2006
    Publication date: January 31, 2008
    Applicant: 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
  • Patent number: 7294630
    Abstract: 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: Grant
    Filed: February 21, 2006
    Date of Patent: November 13, 2007
    Assignee: SmithKline Beecham Corporation
    Inventor: Giuseppe Alvaro
  • Patent number: 7285662
    Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.
    Type: Grant
    Filed: April 18, 2005
    Date of Patent: October 23, 2007
    Assignee: AstraZeneca AB
    Inventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
  • Patent number: 7276500
    Abstract: 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 radicals
    Type: Grant
    Filed: October 20, 2003
    Date of Patent: October 2, 2007
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Patent number: 7223757
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: May 29, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Neelakantan Balasubramanian, Upender Velaparthi, Kurt Zimmermann, Mark G. Saulnier, Peiying Liu, Xiaopeng Sang, David B. Frennesson, Karen M. Stoffan, James G. Tarrant, Anne Marinier, Stephan Roy
  • Patent number: 7220781
    Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.
    Type: Grant
    Filed: January 8, 2004
    Date of Patent: May 22, 2007
    Assignee: Tularik Limited
    Inventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
  • Patent number: 7196080
    Abstract: 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: Grant
    Filed: June 13, 2002
    Date of Patent: March 27, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Masahiro Iwata, Noriyuki Kawano, Hiroyuki Kaizawa, Tomofumi Takuwa, Issei Tsukamoto, Ryushi Seo, Kiyoshi Yahiro, Miki Kobayashi, Makoto Takeuchi
  • Patent number: 7186827
    Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: March 6, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Carl Alan Busacca, Nizar Haddad, Suresh R. Kapadia, Lana Smith Keenan, Jon Charles Lorenz, Chris Hugh Senanayake, Xudong Wei
  • Patent number: 7160877
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: June 22, 2004
    Date of Patent: January 9, 2007
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Patent number: 7160886
    Abstract: 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: Grant
    Filed: February 27, 2004
    Date of Patent: January 9, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
  • Patent number: 7122675
    Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.
    Type: Grant
    Filed: August 1, 2002
    Date of Patent: October 17, 2006
    Assignee: Schering Corporation
    Inventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
  • Patent number: 7119092
    Abstract: 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: Grant
    Filed: October 12, 2001
    Date of Patent: October 10, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: Giuseppe Alvaro, Paolo Maragni, Marsia Tampieri
  • Patent number: 7115607
    Abstract: 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: Grant
    Filed: July 24, 2002
    Date of Patent: October 3, 2006
    Assignee: 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
  • Patent number: 7098212
    Abstract: 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: Grant
    Filed: October 18, 2002
    Date of Patent: August 29, 2006
    Inventors: Laura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Gregory D. Lundquist, Christopher S. Poss, Andrei Shavnya
  • Patent number: 7067660
    Abstract: There is provided a process for the production a compound of general formula I: wherein A, R1, R2, R3 and R4 have meanings given in the description, which process comprises the dehydrogenation of a compound of general formula II,
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: June 27, 2006
    Assignee: Pfizer Inc.
    Inventors: Mark Edward Bunnage, Philip Charles Levett, Nicholas Murray Thomson
  • Patent number: 7060702
    Abstract: 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: Grant
    Filed: November 22, 2004
    Date of Patent: June 13, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: Giuseppe Alvaro, Romano Di Fabio, Paolo Maragni, Marsia Tampieri, Maria Elvira Tranquillini
  • Patent number: 7056922
    Abstract: A compound of the formula wherein D, E, F, G, L, T, W, X, Y, Z, U, A, R1, R2, R3, R4, R5, R6 R7 are as defined in the specification, pharmaceutical compositions thereof, and methods of use to treat diseases and as D3 receptor modulators.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: June 6, 2006
    Assignee: Pfizer Inc
    Inventors: Anton F. J. Fliri, Anthony R. Reinhold
  • Patent number: 7005520
    Abstract: There is provided a process for the production a compound of general formula I: wherein A, R1, R2, R3 and R4 have meanings given in the description, which process comprises the reaction of a compound of formula II, wherein Rx is a group substitutable by an aminopyrazole, with a compound of general formula III
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: February 28, 2006
    Assignee: Pfizer Inc.
    Inventors: Peter James Dunn, Catherine Dunne
  • Patent number: 6979691
    Abstract: Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is X is N or CH, W is —NR16R17, —NR16C(?O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: December 27, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guixue Yu, John Macor, Timothy Herpin, R. Michael Lawrence, George C. Morton, Rejean Ruel, Graham S. Poindexter, Edward H. Ruediger, Carl Thibault
  • Patent number: 6949539
    Abstract: 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: Grant
    Filed: June 1, 2001
    Date of Patent: September 27, 2005
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Mark Furber
  • Patent number: 6849622
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: February 1, 2005
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Patent number: 6846826
    Abstract: Certain 1,4-dihydropyridine compounds, useful as adrenergic blocking agents and as calcium channel blocking agents, the compounds having the formula wherein R1 is hydrogen, halogen, C1-6-alkyl, or C1-6-alkoxy, R3 is hydrogen, halogen, C1-6-alkyl, C1-6-alkoxy, or CF3(CH2)nO— wherein n is 1, 2, or 3, and R5 is —NHCH2CH2O— or —N(CH2CH2)2N—.
    Type: Grant
    Filed: March 26, 2002
    Date of Patent: January 25, 2005
    Inventor: Ing-Jun Chen
  • Patent number: 6777428
    Abstract: The present invention relates to a compound of formula I and a process for making: or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: August 17, 2004
    Assignee: Eli Lilly and Company
    Inventors: Joseph Herman Krushinski, Jr., Vincent Mancuso, Freddy Andre Napora, John Mehnert Schaus
  • Patent number: 6774230
    Abstract: The preparation of 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine dihydrate and other mirtazapine intermediates are described. These compounds are particularly useful in the preparation of mirtazapine.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: August 10, 2004
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Leonid Metzger, Shlomit Wizel
  • Patent number: 6770650
    Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: August 29, 2001
    Date of Patent: August 3, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Leyi Gong, Donald Roy Hirschfeld, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
  • Patent number: 6740682
    Abstract: The novel compound 3-amidinobenzoyl-D-phenylglycine-3-phenylanilide is useful as a serine protease inhibitor.
    Type: Grant
    Filed: November 19, 2001
    Date of Patent: May 25, 2004
    Assignee: Tularik Limited
    Inventor: John Walter Liebeschuetz
  • Patent number: 6723730
    Abstract: Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: April 20, 2004
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Alan Hutchinson, Robert W. DeSimone, Kevin J. Hodgetts, James E. Krause, Geoffrey G. White
  • Patent number: 5125102
    Abstract: A digitally trunked radio repeater system provides substantial improvements in timeliness of channel acquisition and channel drop, and in reliability of critical control signalling. The system uses a much higher digital signalling rate than is typically found in prior art systems, and uses a control channel to convey digital channel request and assignment messages between the central site and mobile transceivers. The mobile radio transceivers transmit channel requests on the control channel (if no response is received, the mobile retries during a retry time window which increases in duration in dependence on the number of retries). The mobile transceiver switches to a working channel in response to an assignement message received on the control channel. Subaudible digital signals transmitted on the control channel and on active working channels allow late entry, shifting to higher priority calls, and other advanced functions.
    Type: Grant
    Filed: January 3, 1990
    Date of Patent: June 23, 1992
    Assignee: Ericsson GE Mobile Communications Inc.
    Inventors: Jeffrey S. Childress, Marc A. Dissosway, Gerald M. Cooper, Houston H. Hughes, III