Ring Sulfur In The Polycyclo Ring System Patents (Class 546/202)
  • Patent number: 10131648
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R5, R6, W, and A are defined herein.
    Type: Grant
    Filed: September 7, 2017
    Date of Patent: November 20, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Hui Huang, Gee-Hong Kuo, Mark R. Player, Shyh-Ming Yang, Yue-Mei Zhang
  • Patent number: 9790199
    Abstract: A sulfoxide compound and method of producing benzothiophene derivatives using the same are provided. The sulfoxide compound is represented by formula (I), wherein R1 and R2 are individually and independently benzoyl group; alkyl, acyl or silyl group of C1-C6 straight chain or branched chain; or alkenyl group of C3-C6 straight chain or branched chain; and X is halogen atom. The sulfoxide compound reacts with alkynyl compound, and then the synthesis efficiency of benzothiophene derivatives can be effectively increased.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: October 17, 2017
    Assignee: NATIONAL SUN YAT-SEN UNIVERSITY
    Inventors: Ming-Jung Wu, Shih-Ming Wen
  • Patent number: 9751852
    Abstract: A sulfoxide compound and method of producing benzothiophene derivatives using the same are provided. The sulfoxide compound is represented by formula (I), wherein R1 and R2 are individually and independently benzoyl group; alkyl, acyl or silyl group of C1-C6 straight chain or branched chain; or alkenyl group of C3-C6 straight chain or branched chain; and X is halogen atom. The sulfoxide compound reacts with alkynyl compound, and then the synthesis efficiency of benzothiophene derivatives can be effectively increased.
    Type: Grant
    Filed: May 25, 2017
    Date of Patent: September 5, 2017
    Assignee: NATIONAL SUN YAT-SEN UNIVERSITY
    Inventors: Ming-Jung Wu, Shih-Ming Wen
  • Patent number: 8981119
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: March 17, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Tsukasa Ishihara, Kazuhiro Ikegai, Ikumi Kuriwaki, Hiroyuki Hisamichi, Nobuaki Takeshita, Ryuichi Takezawa
  • Publication number: 20150057278
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
    Type: Application
    Filed: September 10, 2012
    Publication date: February 26, 2015
    Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20150011557
    Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 8, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
  • Publication number: 20150011541
    Abstract: The present invention relates to compounds having a pipecolate sulfonamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate sulfonamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 8, 2015
    Inventors: Ranganath Gopalakrishnan, Felix Hausch
  • Publication number: 20150005275
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
  • Publication number: 20140371207
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: December 13, 2013
    Publication date: December 18, 2014
    Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Publication number: 20140364421
    Abstract: [Problem] A compound which is useful as an IK1 channel activator is provided. [Means for Solution] As a result of studies on the IK1 channel activator, the present inventors have found that a benzothiophene compound shows effectiveness on visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia, thereby completing the invention. A compound of the invention has an IK1 channel activation effect, and can also be used as an agent for preventing and/or treating visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia. In addition, the IK1 channel activator can be used as an agent for preventing and/or treating inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 11, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Tsukasa ISHIHARA, Kazuhiro IKEGAI, Ikumi KURIWAKI, Hiroyuki HISAMICHI, Nobuaki TAKESHITA, Ryuichi TAKEZAWA
  • Publication number: 20140329802
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: March 28, 2014
    Publication date: November 6, 2014
    Applicant: Astellas Pharma Inc.
    Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Patent number: 8729068
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: May 20, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Patent number: 8703957
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: April 22, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • Publication number: 20140066451
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Application
    Filed: November 4, 2013
    Publication date: March 6, 2014
    Applicant: BKG PHARMA APS
    Inventor: Birgit Kjaeldgaard GIWERCMAN
  • Patent number: 8614328
    Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: December 24, 2013
    Assignee: Celgene Corporation
    Inventors: Alexander L. Ruchelman, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
  • Publication number: 20130338106
    Abstract: Disclosed are compounds of Formula I: and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRa-, and Ra, and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.
    Type: Application
    Filed: February 23, 2012
    Publication date: December 19, 2013
    Inventors: John A. McCauley, Thomas J. Greshock, John Sanders, Heather H. Stevenson, Jonathan T. Kern, Ronald K. Chang
  • Patent number: 8604059
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: December 10, 2013
    Assignee: BKG Pharma APS
    Inventor: Birgit Kjældgaard Giwercman
  • Patent number: 8580965
    Abstract: Substituted sulfonamide compounds with bradykinin receptor (B1R) modulating activity; processes for the preparation thereof, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or inhibit pain and/or other disorders and/or disease states.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: November 12, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
  • Publication number: 20130261130
    Abstract: The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is —CON—R3R4, —NR5COR6, —NHR7, —OR8, —SR9, —CH2NR10R11, —(CH2)2-R12, —CH?CH—R12, —C?C—R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.
    Type: Application
    Filed: October 31, 2011
    Publication date: October 3, 2013
    Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Hans Allgeier
  • Publication number: 20130244998
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R are defined herein.
    Type: Application
    Filed: May 2, 2013
    Publication date: September 19, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Peter J. Connolly, Haiyan Bian, Xun Li, Li Liu, Mark J. Macielag, Mark E. McDonnell
  • Patent number: 8536342
    Abstract: Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: September 17, 2013
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kunihiko Higashiura, Taizo Ito, Takashi Ogino, Taisuke Hasegawa
  • Publication number: 20130237547
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Application
    Filed: March 28, 2013
    Publication date: September 12, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Jay M. Matthews
  • Patent number: 8492563
    Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: July 23, 2013
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Jordi Corbera-Arjona, Daniel Martinez-Olmo, David Vano-Domenech
  • Publication number: 20130165422
    Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Patent number: 8440667
    Abstract: Certain imidazopyrazines of Formula (I): and pharmaceutical compositions thereof are provided herein. Methods of treating patients responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity of Formula (I) effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: May 14, 2013
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Publication number: 20130102584
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R are defined herein.
    Type: Application
    Filed: October 20, 2011
    Publication date: April 25, 2013
    Inventors: Peter J. Connolly, Haiyan Bian, Xun Li, Li Liu, Mark J. Macielag, Mark E. McDonnell
  • Patent number: 8399683
    Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: March 19, 2013
    Assignee: TetraLogic Pharmaceuticals
    Inventors: Stephen M. Condon, Matthew G. Laporte
  • Publication number: 20130065882
    Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy
    Type: Application
    Filed: October 3, 2012
    Publication date: March 14, 2013
    Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
  • Publication number: 20130053369
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Patent number: 8377967
    Abstract: The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: February 19, 2013
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Taizo Ito, Hiroyuki Iwatsuki
  • Publication number: 20130029973
    Abstract: A compound has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating hyperphosphatemia, preventing hyperphosphatemia, or both. The compound is a tetrahydrobenzothiophene compound. A pharmaceutical composition for treating hyperphosphatemia includes the compound or salt thereof. A method of treating hyperphosphatemia includes administering to a subject an effective amount of the compound or salt thereof.
    Type: Application
    Filed: April 27, 2011
    Publication date: January 31, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Patent number: 8350041
    Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: January 8, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
  • Patent number: 8344149
    Abstract: Crystalline raloxifene hydrochloride in hydrated form, particularly the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and uses thereof.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: January 1, 2013
    Assignee: Cipla Limited
    Inventors: Srinivas Laxminarayan Pathi, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
  • Publication number: 20120302562
    Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
    Type: Application
    Filed: May 23, 2012
    Publication date: November 29, 2012
    Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
  • Publication number: 20120302539
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 29, 2012
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
  • Patent number: 8304434
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: September 30, 2008
    Date of Patent: November 6, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengcheng Patrick Shao, Sriram Tyagarajan, Feng Ye
  • Patent number: 8247564
    Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: August 21, 2012
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Sarah Dunham
  • Publication number: 20120178781
    Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Application
    Filed: February 29, 2012
    Publication date: July 12, 2012
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank Ivy CARROLL, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
  • Patent number: 8217032
    Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: July 10, 2012
    Assignee: Eli Lilly and Company
    Inventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
  • Patent number: 8198304
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: June 12, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Publication number: 20120129100
    Abstract: An actinic ray-sensitive or radiation-sensitive resin composition including: (PA) a compound having a proton acceptor functional group and undergoing decomposition upon irradiation with an actinic ray or radiation to generate a compound reduced in or deprived of proton acceptor property or changed to be acidic from being proton acceptor-functioning, wherein a molar extinction coefficient ? of the compound (PA) at a wavelength of 193 nm as measured in acetonitrile solvent is 55,000 or less, and a pattern forming method using the composition are provided.
    Type: Application
    Filed: August 17, 2010
    Publication date: May 24, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Akinori Shibuya, Shuhei Yamaguchi, Shohei Kataoka, Michihiro Shirakawa, Takayuki Kato, Naohiro Tango
  • Publication number: 20120129828
    Abstract: The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
    Type: Application
    Filed: June 18, 2009
    Publication date: May 24, 2012
    Inventors: Victor J. Cee, Jian Lin, Xiang Y. Yu, Zhaoda Zhang
  • Publication number: 20120122880
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Application
    Filed: April 20, 2010
    Publication date: May 17, 2012
    Applicant: BKG PHARMA APS
    Inventor: Birgit Kjaeldgaard Giwercman
  • Publication number: 20120123127
    Abstract: Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.
    Type: Application
    Filed: July 26, 2010
    Publication date: May 17, 2012
    Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventors: Kunihiko Higashiura, Taizo Ito, Takashi Ogino, Taisuke Hasegawa
  • Publication number: 20120095010
    Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
    Type: Application
    Filed: December 22, 2011
    Publication date: April 19, 2012
    Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
  • Patent number: 8153659
    Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: April 10, 2012
    Assignee: Celgene Corporation
    Inventors: Alexander L. Ruchelman, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
  • Patent number: 8153658
    Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: April 10, 2012
    Assignee: Astellas Pharma, Inc.
    Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
  • Patent number: 8153682
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: April 10, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Patent number: 8148422
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally