Spiro Ring System Patents (Class 514/278)
  • PREVENTIVES/REMEDIES FOR STRESS URINARY INCONTINENCE AND METHOD OF SCREENING THE SAME
    Publication number: 20140155369
    Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.
    Type: Application
    Filed: January 16, 2014
    Publication date: June 5, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Izumi KAMO, Tadatoshi HASHIMOTO
  • Anti-Inflammation Compounds
    Publication number: 20140155387
    Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 5, 2014
    Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREA
    Inventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
  • Spiroxazolidinone compounds
    Patent number: 8742110
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: June 3, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu
  • 1,3,8-trisubstituted-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as ligands of the ORL-1 receptor
    Patent number: 8741916
    Abstract: The present invention is directed to novel 1,3,8-trisubstituted-1,3,8-triaza-spiro[4.5]decan-4-one derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor.
    Type: Grant
    Filed: February 14, 2008
    Date of Patent: June 3, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles C. Bignan, Dennis J. Hlasta, Richard R. Ryan
  • NOVEL COMPOSITIONS AND METHODS OF PREVENTING OR AMELIORATING ABNORMAL THROMBUS FORMATION AND CARDIOVASCULAR DISEASE
    Publication number: 20140147448
    Abstract: The invention includes compositions and methods useful for treating preventing abnormal thrombus formation and subsequent cardiovascular disease in diabetic patients and patients with increased cardiovascular risk.
    Type: Application
    Filed: June 5, 2012
    Publication date: May 29, 2014
    Applicant: Yale University
    Inventors: John Hwa, WaiHo Tang
  • Novel Imidazolines as dual inhibitors of MDM2 and MDMX
    Publication number: 20140148443
    Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 29, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
  • Substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides, preparation and therapeutic use thereof
    Patent number: 8735385
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • Fused Substituted Aminopyrrolidine Derivative
    Publication number: 20140142096
    Abstract: A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.
    Type: Application
    Filed: November 19, 2013
    Publication date: May 22, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Hisashi Takahashi, Satoshi Komoriya, Takahiro Kitamura, Takashi Odagiri, Hiroaki Inagaki, Toshifumi Tsuda, Kiyoshi Nakayama, Makoto Takemura, Kenichi Yoshida, Rie Miyauchi, Masatoshi Nagamochi
  • Neural tourniquet
    Patent number: 8729129
    Abstract: Disclosed is a method of reducing bleed time in a subject by activation of the cholinergic anti-inflammatory pathway in said subject. The cholinergic anti-inflammatory pathway can be activated by direct or indirect stimulation of the vagus nerve. The cholinergic anti-inflammatory pathway can also be activated by administering an effective amount of cholinergic agonist or acetylcholinesterase inhibitor to the subject.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: May 20, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Kevin J. Tracey, Carol Ann Amella, Christopher Czura
  • Anti-viral compounds, compositions, and methods of use
    Patent number: 8729077
    Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: May 20, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Don Roberts, Wieslaw Kazmierski, Richard Grimes
  • Compositions and methods for treating alcohol use disorders, pain and other diseases
    Patent number: 8729081
    Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.
    Type: Grant
    Filed: October 12, 2009
    Date of Patent: May 20, 2014
    Assignee: VM Discovery Inc.
    Inventor: Jay Jie-Qiang Wu
  • METHODS FOR TREATING SPINAL MUSCULAR ATROPHY
    Publication number: 20140135305
    Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.
    Type: Application
    Filed: December 12, 2013
    Publication date: May 15, 2014
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Sergey V. Paushkin, Charles Romfo, Ellen Welch, Nikolai Naryshkin
  • Spiroheterocyclic pyrrolidinedione herbicidal compositions
    Patent number: 8722578
    Abstract: Herbicidal compositions containing as active ingredients spiroheterocyclic pyrrolidine dione compounds.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: May 13, 2014
    Assignee: Syngenta Participations AG
    Inventors: Werner Zambach, Ottmar Franz Hueter, Jean Wenger, Marcela Goeghova, Thomas Pitterna, Peter Maienfisch, Stephane André´Marie Jeanmart, Michel Muehlebach
  • COMPOUNDS AND METHODS FOR MODULATING MITOCHONDRIAL METABOLISM AND REACTIVE OXYGEN SPECIES PRODUCTION
    Publication number: 20140128352
    Abstract: Compounds that modulate mitochondrial reactive oxygen species (ROS) production are provided. The compounds may modulate ROS production at defined sites without also altering energy production. Methods of using and identifying such compounds are also provided.
    Type: Application
    Filed: September 20, 2013
    Publication date: May 8, 2014
    Applicant: Buck Institute for Research on Aging
    Inventors: Martin D. Brand, Adam Orr
  • PYRANOPYRIDONE INHIBITORS OF TANKYRASE
    Publication number: 20140121231
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof wherein X, M, Y, R1 and R2 are as defined herein. The compounds have activity as anticancer agents.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 1, 2014
    Inventors: David Robert Bolin, Javier de Vicente Fidalgo, Johannes Hermann, Parcharee Tivitmahaisoon, Lin Yi, Mark Zak
  • DISPIROPYRROLIDINE DERIVATIVES
    Publication number: 20140121196
    Abstract: A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
    Type: Application
    Filed: November 14, 2013
    Publication date: May 1, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
  • TRPV4 ANTAGONISTS
    Publication number: 20140121206
    Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: GlaxoSmithKliine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • Method of treating cancer using a survivin inhibitor
    Patent number: 8710068
    Abstract: Disclosed herein are methods of treating cancer by administering to a patient a small molecule inhibitor of Survivin. Also disclosed herein are methods of inhibiting Survivin dimerization in a patient by administering a compound of formula (I), (II), (III), or (IV). Methods of inducing cell cycle arrest in cancer cells, comprising G2/M stage arrest, in a patient by administering a compound of formula (I), (II), (III), or (IV) are also disclosed. Further disclosed herein are methods of inducing apoptosis in cancer cells in a patient by administering a compound of formula (I), (II), (III), or (IV).
    Type: Grant
    Filed: January 19, 2010
    Date of Patent: April 29, 2014
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Alan Berezov, Qiang Wang, Ramachandran Murali, Mark I. Greene
  • TRPV4 ANTAGONISTS
    Publication number: 20140113916
    Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 24, 2014
    Applicant: GlaxoSmithKLine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • FILAMIN A BINDING ANTI-INFLAMMATORY AND ANALGESIC
    Publication number: 20140113895
    Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 24, 2014
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • NEW 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION
    Publication number: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • Aryl ether-base kinase inhibitors
    Patent number: 8703953
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: April 22, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, John E. Macor, Joanne J. Bronson, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
  • Spiro fused 1-amino-piperdine pyrrolidine dione derivatives with pesticidal activity
    Patent number: 8703165
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: April 22, 2014
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Tandem process for preparing N-alkyl morphinans
    Patent number: 8703949
    Abstract: The present invention provides processes for the preparation of N-alkyl morphinans without the isolation of nor-morphinan intermediates. In particular, the invention provides tandem hydrolysis/alkylation reactions for the synthesis of N-alkyl morphinans.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: April 22, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Subo Liao, Peter X. Wang, David W. Berberich, Douglas C. Miller
  • HYDANTOIN DERIVATIVES AS KV3 INHIBITORS
    Publication number: 20140107139
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: June 7, 2012
    Publication date: April 17, 2014
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Anne Decor, Dieter Hamprecht, Agostino Marasco
  • METHODS OF USE OF CYCLOPAMINE ANALOGS
    Publication number: 20140107142
    Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Michael J. Grogan, Karen J. McGovern, Martin R. Tremblay, William Matsui
  • KINASE INHIBITORS AND METHODS OF USE THEREOF
    Publication number: 20140107141
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.
    Type: Application
    Filed: October 11, 2013
    Publication date: April 17, 2014
    Applicants: The General Hospital Corporation d/b/a Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michel Weiwer, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop
  • Inhibitors of histone deacetylase
    Patent number: 8697717
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: April 15, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Patrick Rene Angibaud, Lieven Meerpoel, Alexey Borisovich Dyatkin
  • METHODS AND COMPOSITIONS FOR TREATMENT OF DISORDERS AMELIORATED BY MUSCARINIC RECEPTOR ACTIVATION
    Publication number: 20140099356
    Abstract: Methods for the treatment of CNS disorders using combinations of muscarinic activators and inhibitors, and medicaments comprising muscarinic activators and inhibitors.
    Type: Application
    Filed: April 9, 2013
    Publication date: April 10, 2014
    Applicant: Pure Tech Ventures, LLC
    Inventor: Pure Tech Ventures, LLC
  • Dantagonists, methods of synthesis and methods of use
    Patent number: 8691836
    Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: April 8, 2014
    Assignee: Altos Therapeutics, LLC
    Inventors: Gary W. Luehr, Arathi Sundaram, Priyadarshini Jaishankar, Philip W. Payne, Pascal Druzgala
  • ANTI-ANDROGENS FOR THE TREATMENT OF NON-METASTATIC CASTRATE-RESISTANT PROSTATE CANCER
    Publication number: 20140088129
    Abstract: Described herein are methods of treating non-metastatic castrate-resistant prostate cancer with anti-androgens.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 27, 2014
    Applicant: Aragon Pharmaceuticals, Inc.
    Inventor: Isan Chen
  • IMIDAZOPYRIDINE COMPOUNDS
    Publication number: 20140088080
    Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
  • PHARMACEUTICAL FORMULATIONS: SALTS OF 8-[1-3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXYMETHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE AND TREATMENT METHODS USING THE SAME
    Publication number: 20140088128
    Abstract: Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
    Type: Application
    Filed: March 19, 2013
    Publication date: March 27, 2014
    Applicant: OPKO Health, Inc.
    Inventor: OPKO Health, Inc.
  • Fused pyridine derivatives
    Patent number: 8680089
    Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 25, 2014
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
  • NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS
    Publication number: 20140080788
    Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Application
    Filed: April 27, 2012
    Publication date: March 20, 2014
    Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
  • NOVEL TRPV3 MODULATORS
    Publication number: 20140080803
    Abstract: Disclosed herein are modulators of TRPV3 of Formula (I) wherein p is 1, 2, 3, or 4, and G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Application
    Filed: October 23, 2012
    Publication date: March 20, 2014
    Applicant: AbbVie Inc.
    Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Eric A. Voight
  • SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    Publication number: 20140080823
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 20, 2014
    Applicant: DAC S.R.L.
    Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
  • PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
    Publication number: 20140080801
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 20, 2014
    Applicant: Genentech, Inc.
    Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
  • Bicyclic heterocyclic spiro compounds
    Patent number: 8673931
    Abstract: There are disclosed bicyclic heterocyclic spiro compounds; pharmaceutical compositions comprising these compounds; and methods for the treatment in a mammal of diseases and conditions which are susceptible to modulation of the M1 muscarinic receptor, including Alzheimer's disease, insulin resistance syndrome and type 2 diabetes. Other embodiments are also disclosed.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: March 18, 2014
    Inventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
  • Compounds
    Patent number: 8674113
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
  • CHEMOKINE RECEPTOR ANTAGONISTS AND USE THEREOF
    Publication number: 20140072576
    Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 13, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Masaya KOKUBO, Motoyuki TANAKA, Hiroshi OCHIAI, Yoshikazu TAKAOKA, Shiro SHIBAYAMA
  • COMBINATION THERAPY WITH NANOPARTICLE COMPOSITIONS OF TAXANE AND HEDGEHOG INHIBITORS
    Publication number: 20140072630
    Abstract: The present invention provides combination therapy methods of treating a proliferative disease (such as cancer) comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a hedgehog inhibitor that inhibits a hedgehog signaling pathway.
    Type: Application
    Filed: February 28, 2013
    Publication date: March 13, 2014
    Applicant: ABRAXIS BIOSCIENCE, LLC
    Inventor: Abraxis BioScience, LLC
  • Spirocyclic nitriles as protease inhibitors
    Publication number: 20140073662
    Abstract: The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 13, 2014
    Applicant: Sanofi
    Inventors: Manfred SCHUDOK, Michael WAGNER, Armin BAUER, Anna KOHLMANN
  • ALKOXY PYRAZOLES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
    Publication number: 20140073629
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Jehrod Burnett BRENNEMAN, John GINN, Michael D. LOWE, Christopher Ronald SARKO, Edward S. TASBER, Zhonghua ZHANG
  • Spiperone derivatives and methods of treating disorders
    Patent number: 8664237
    Abstract: Described herein are spiperone derivative compounds which have been found to be useful in methods of stimulating CaCC and treating disorders (or symptoms thereof) associated with CaCC including cystic fibrosis, wherein a compound of the invention is administered to a subject.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: March 4, 2014
    Assignee: The Johns Hopkins University
    Inventors: William B. Guggino, Erik M. Schwiebert, Lihua Liang
  • METHOD OF CONTROLLING NEONICOTINOID RESISTANT HEMIPTERA
    Publication number: 20140057930
    Abstract: The invention relates to a method of controlling insects from the order hemiptera that resistant to neo-nicotinoid insecticides using spiroheterocyclic pyrrolidine dione derivatives.
    Type: Application
    Filed: May 26, 2011
    Publication date: February 27, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Russell Slater, Alfred Rindlisbacher, Peter Maienfisch, Phillippe Camblin, Alain Gaume
  • INHIBITORS OF BETA-SECRETASE
    Publication number: 20140057927
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Application
    Filed: August 27, 2013
    Publication date: February 27, 2014
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Cornelia Dorner-Ciossek, Ulrike Gross, Niklas Heine, Achim Sauer
  • Cyclopamine tartrate salt and uses thereof
    Patent number: 8658664
    Abstract: The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides highly water-soluble analogs of cyclopamine that are potent, hedgehog signaling inhibitors less toxic than cyclopamine. The compounds of the present invention are particularly useful in treating cancers associated with hedgehog signalling.
    Type: Grant
    Filed: August 9, 2010
    Date of Patent: February 25, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Jingwu Xie, Massoud Garrossian
  • CYCLOPENTYLPYRAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS
    Publication number: 20140051660
    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 R1, R2, R3, Q, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Michael WINTERS, Zhihua Sui, Christopher Flores
  • Use of Aminoindane Compounds in Treating Overactive Bladder and Interstitial Cystitis
    Publication number: 20140051702
    Abstract: The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 20, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Sandeep Gupta, Tony Priestley, Nicholas James Laping