Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/112)
  • Patent number: 10253153
    Abstract: The present invention provides a linker for solid phase synthesis of nucleic acid, which consists of a compound represented by the formula (I) or the formula (II), a support for solid phase synthesis of nucleic acid, which has a structure represented by the formula (III), and a production method of a nucleic acid, which uses the support: wherein each symbol is as defined in the SPECIFICATION.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: April 9, 2019
    Assignee: Nitto Denko Corporation
    Inventors: Eri Maeta, Kenjiro Mori, Shohei Horie, Takahiko Ito, Shoichiro Saito, Ryuhei Nagao
  • Patent number: 10053468
    Abstract: The present invention relates to compound (I) or a salt thereof which has a ROR?t inhibitory action. wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: August 21, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Hiroyuki Watanabe, Shoji Fukumoto, Tsuneo Oda, Hidekazu Tokuhara, Yoshihide Tomata, Naoki Ishii, Michiko Tawada, Mitsunori Kono, Atsuko Ochida, Takashi Imada, Yoshiyuki Fukase, Tomoya Yukawa
  • Patent number: 10035791
    Abstract: The present disclosure relates to a bicyclic compound, a pharmaceutical composition thereof, and its novel use. More particularly, the present disclosure relates to the bicyclic compound according to Formula I or Formula II, the pharmaceutical composition for treating a stroke, and the use of the bicyclic compound treating the stroke.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: July 31, 2018
    Assignee: China Medical University
    Inventors: Kuo-Hsiung Lee, Yu Zhao, Sheng-Chu Kuo, Chung-Y. Hsu, Woei-Cherng Shyu, Yu-Chian Chen, Chen-Huan Lin, Wei Lee, Chun-Wei Chiang, Chang-Hai Tsai
  • Patent number: 10028942
    Abstract: The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: July 24, 2018
    Assignee: Genentech, Inc.
    Inventors: Anthony Estrada, Wen Liu, Snahel Patel, Michael Siu
  • Patent number: 9949963
    Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: April 24, 2018
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Sean Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
  • Patent number: 9630924
    Abstract: The present invention provides a heterocyclic compound having a ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification. or a salt thereof.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: April 25, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Tsuneo Oda, Mitsunori Kono, Atsuko Ochida, Takashi Imada, Hidekazu Tokuhara, Yoshihide Tomata, Naoki Ishii, Michiko Tawada, Yoshiyuki Fukase, Tomoya Yukawa, Shoji Fukumoto
  • Patent number: 9617261
    Abstract: The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: April 11, 2017
    Assignee: CMG PHARMACEUTICAL CO., LTD.
    Inventors: Gilnam Lee, Hye Sun Jeon, Ki Joon Jeon, Chul Yun Rhim, Jin Sung Kim, Jeongbeob Seo, Suk Young Cho, Choung Soo Kim, Jung Shin Lee, Eun Kyung Choi, Jung Jin Hwang, Bongcheol Kim
  • Patent number: 9555022
    Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: January 31, 2017
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Marcus Koppitz, Detlef Stöckigt, Olaf Prien
  • Patent number: 9394289
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: July 19, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
  • Patent number: 9290491
    Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: March 22, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sean M. Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
  • Patent number: 9283183
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: March 15, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
  • Patent number: 9243098
    Abstract: Conventional cross-linked cyclic olefin polymers do not have a sufficiently low linear expansion coefficient. A compound having a structure represented by the following formula (a).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: January 26, 2016
    Assignee: Canon Kabushiki Kaisha
    Inventors: Seiji Okada, Ryo Ogawa
  • Patent number: 9233961
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: January 12, 2016
    Assignees: Novartis AG, University of Washington through its Center for Commercialization
    Inventors: Arnab Kumar Chatterjee, Fang Liang, Casey Jacob Nelson Mathison, Pranab Kumar Mishra, Valentina Molteni, Advait Suresh Nagle, Frantisek Supek, Liying Jocelyn Tan, Agnes Vidal, Michael Herman Gelb, Frederick Simmons Buckner, Hari Babu Tatipaka, Neil Richard Norcross, John Robert Gillespie
  • Patent number: 9133213
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Grant
    Filed: July 2, 2013
    Date of Patent: September 15, 2015
    Assignee: Morphochem Aktiengesellschaft Für Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
  • Publication number: 20150148541
    Abstract: Provided herein are novel and selective high affinity ?3?4 nicotinic acetycholine receptor ligands and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, drug addiction or pain using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of selectively antagonizing receptors such as, for example, the ?3?4 nicotinic acetycholine receptor using the compounds and compositions disclosed herein.
    Type: Application
    Filed: January 20, 2015
    Publication date: May 28, 2015
    Inventors: Nurulain Zaveri, Faming Jiang, Lawrence Toll
  • Patent number: 9040565
    Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: May 26, 2015
    Assignee: Orexo AB
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Dirk Stenkamp
  • Patent number: 9040532
    Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: May 26, 2015
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
  • Patent number: 9040533
    Abstract: The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R20, R21, Q, Y1, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: May 26, 2015
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Jeffrey Michael Marra, Naoki Tsuno, Tatsuhiko Ueno, Xiaoming Zhou
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150119362
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 30, 2015
    Inventors: Mark E. Gurney, Timothy J. Hagen, Joel R. Walker, Xuesheng Mo, A. Samuel Vellekoop, Robert Campbell, Lei Zhu, Donna L. Romero
  • Patent number: 8999966
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr.
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20150087650
    Abstract: The present invention relates to 1-aza-bicy-cloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R?); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Application
    Filed: December 3, 2014
    Publication date: March 26, 2015
    Applicant: NOVARTIS AG
    Inventors: Dominik FEUERBACH, Werner Müller, Bernard Lucien ROY, Thomas TROXLER, Konstanze HURTH, Mathias FREDERIKSEN
  • Publication number: 20150065523
    Abstract: The present invention provides compounds of formula (I) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein X is NH, or O; Q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; A is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; B may assume different meanings from A and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
    Type: Application
    Filed: March 18, 2013
    Publication date: March 5, 2015
    Inventors: Luigi Piero Stasi, Lucio Claudio Rovati
  • Publication number: 20150057443
    Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
    Type: Application
    Filed: August 21, 2014
    Publication date: February 26, 2015
    Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
  • Publication number: 20150056699
    Abstract: This invention provides a compound having the structure wherein A is a ring structure, with or without substitution; Z is present or absent and when present is wherein n is 0, 1, 2, 3, or 4; Y is —(CR11R12)—, —NH(CR11R12)—, or —O(CR11R12)—, wherein R11 and R12 are each hydrogen or combine to form a carbonyl; R1, R2, R3, R4, R5 and R6 are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester or amide; ? represents a bond, which is present or absent and when ? is present, then R7 and R8 are absent; R7 and R8 are present when ? is absent and are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester, amide or R5 and R7 combine to form a carbonyl or R6 and R8 combine to form a carbonyl; R9 and R10 are each hydrogen o
    Type: Application
    Filed: August 24, 2012
    Publication date: February 26, 2015
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Dalibor Sames, Xiaoguang Li, Shu Li, Andrew Kruegel, Richard Karpowicz, Ignacio Carrera, Souvik Rakshit
  • Patent number: 8957102
    Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: February 17, 2015
    Assignee: Neopharm Co., Ltd.
    Inventors: Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
  • Patent number: 8952180
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: September 25, 2012
    Date of Patent: February 10, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 8952034
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: February 10, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Publication number: 20150025105
    Abstract: Disclosed herein are indolizine compounds of general formula I, wherein R1-R7, X and Y are as disclosed in the application, useful as inhibitors of lipoprotein associated phospholipase A2 (Lp-PLA2) and/or 15-lipoxygenase (15-LOX), as well as methods of preparation and use thereof, and compositions thereof Advantageously, certain compounds disclosed herein are capable of inhibiting both Lp-PLA2 and 15-LOX. Accordingly, provided herein are methods of inhibiting one or both of Lp-PLA2 and 15-LOX, and methods of treating diseases or conditions associated with Lp-PLA2 and/or 15-LOX.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 22, 2015
    Inventors: Praveen Rao PERAMPALLI NEKKAR, Saad NAMBIL KABIR
  • Patent number: 8937184
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: January 20, 2015
    Assignee: Abbvie B.V.
    Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
  • Publication number: 20150018332
    Abstract: The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: January 15, 2015
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
  • Publication number: 20140377223
    Abstract: The present invention relates to novel Substituted Biphenylene Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein Y1, Y2, R1, R2, R4, Ra and Rb are as defined herein. The present invention also relates to compositions comprising at least one Substituted Biphenylene Compound, and methods of using the Substituted Biphenylene Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 21, 2011
    Publication date: December 25, 2014
    Inventors: Joseph A. Kozlowski, Bandarpalle B. Shankar
  • Patent number: 8916708
    Abstract: Compounds of formula (I) are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory wherein R1 is a radical of formula (IA) or (IB) or (IC): 10 Y is —O— or —S(O)p—wherein p is 0, 1 or 2; A is an optionally substituted cycloalkylene radical having 5, 6 or 7 ring atoms fused to a phenyl ring; and R2, R3b and R4b are as defined in the claims.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: December 23, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Chi-kit Woo, Monique Bodil Van Niel
  • Patent number: 8916583
    Abstract: The invention provides sprayable aqueous compositions containing zolpidem or single stereoisomer, mixtures of stereoisomers, pharmaceutically acceptable salts or prodrugs thereof, a solubilizing agent, a water soluble polymer with bioadhesive property. When administered intranasally using a spray device, zolpidem is rapidly absorbed with prolonged intranasal residence time and improved bioavailability. The compositions can be applied for the treatment of insomnia-related disorders such as difficulties with sleep initiation or middle of the night awakenings.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Renascence Therapeutics Limited
    Inventors: Yanfeng Wang, Benjamin T. K. Lee, Tony C. Y. Ho, Melvin K. M. Toh
  • Patent number: 8912210
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: December 16, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
  • Patent number: 8912330
    Abstract: This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: December 16, 2014
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Jiwei Qi, Yihan Wang, Feng Li, William C. Shakespeare, Anna Kohlmann, David C. Dalgarno, Xiaotian Zhu
  • Publication number: 20140357662
    Abstract: The present invention provides compounds of formula (I): wherein A, R1, R2, R3 IX, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.
    Type: Application
    Filed: November 15, 2012
    Publication date: December 4, 2014
    Inventors: Derek Edward John, Basil Hartzoulakis, Simon D. Edwards
  • Publication number: 20140343042
    Abstract: The invention relates to the design and synthesis of novel anabaseine-based compounds, which are useful in treating or preventing a wide variety of conditions, including nervous system diseases or disorders, such as, schizophrenia, Alzheimer's disease, Parkinson's disease, drug dependence, and substance addiction, and compositions, kits, and methods thereof. The invention also provides novel anabaseine-based compounds, compositions, kits, and methods thereof for treating or preventing non-nerve system diseases or disorders (such as, inflammation and cancer) in a subject identified in need thereof. Certain enantiomeric compounds of the invention exhibited enhanced selectivity toward ?7 nAChRs relative to alpha4beta2 nAChRs. Other enantiomeric compounds of the invention exhibited enhanced selectivity for alpha4beta2 nAChRs relative to ?7 nAChRs.
    Type: Application
    Filed: December 11, 2012
    Publication date: November 20, 2014
    Inventors: William R. Kem, Ferenc Soti, Hong Xing
  • Patent number: 8889708
    Abstract: This invention relates to bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Ralf Anderskewitz, Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters
  • Publication number: 20140323458
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Patent number: 8871783
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: October 28, 2014
    Assignee: Boehringer Ingelheim International GmBh
    Inventors: Ralf Anderskewitz, Marc Grundl, Gerd Morschhaeuser, Thorsten Oost, Alexander Pautsch
  • Publication number: 20140315912
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).
    Type: Application
    Filed: July 18, 2011
    Publication date: October 23, 2014
    Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
  • Publication number: 20140315794
    Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Application
    Filed: November 21, 2013
    Publication date: October 23, 2014
    Applicant: MERIAL LIMITED
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
  • Patent number: 8865742
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Publication number: 20140275155
    Abstract: This invention relates to bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias GRAUERT, Ralf ANDERSKEWITZ, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
  • Publication number: 20140275159
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Matthias GRAUERT, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
  • Patent number: 8835454
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group of: are useful as HIV attachment inhibitors.
    Type: Grant
    Filed: August 28, 2012
    Date of Patent: September 16, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, John F. Kadow, Nicholas A. Meanwell
  • Patent number: RE46314
    Abstract: A method of preparing genipin-rich materials from the fruit of Genipa americana fruit for their use as a cross-linking agent and as a raw material to produce colors is disclosed. The genipin-rich materials can be used in a broad range of applications including personal care, cosmetics, dietary supplements, packaging, textiles, beverages, foodstuffs, drugs, and animal feeds.
    Type: Grant
    Filed: April 4, 2016
    Date of Patent: February 21, 2017
    Assignee: WILD Flavors, Inc.
    Inventors: Shaowen Wu, Gregory Horn
  • Patent number: RE47153
    Abstract: A method of preparing genipin-rich materials from the fruit of Genipa americana fruit for their use as a cross-linking agent and as a raw material to produce colors is disclosed. The genipin-rich materials can be used in a broad range of applications including personal care, cosmetics, dietary supplements, packaging, textiles, beverages, foodstuffs, drugs, and animal feeds.
    Type: Grant
    Filed: February 21, 2017
    Date of Patent: December 11, 2018
    Assignee: WILD Flavors, Inc.
    Inventors: Shaowen Wu, Gregory Horn