The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
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Patent number: 9585882Abstract: In one aspect, the invention relates to compounds having the formula I: where R1, R2a, R2b, and R3-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: GrantFiled: January 29, 2015Date of Patent: March 7, 2017Assignee: Theravance Biopharma R&D IP, LLCInventors: Melissa Fleury, Anne-Marie Beausoliel, Adam D. Hughes, Daniel D. Long, Donna A. A. Wilton
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Patent number: 9579304Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: February 22, 2016Date of Patent: February 28, 2017Assignee: Aptinyx, Inc.Inventors: John A. Lowe, III, M. Amin Khan
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Patent number: 9546139Abstract: Provided are a novel pyridine carboxylic acid based compound used as a P2X1 and P2X3 receptor antagonist, a production method for the same and a composition comprising the same. The compound according to the present invention is a powerful antagonist of P2X1 and P2X3 receptors, and hence can be used as a drug for treating or preventing diseases involving neurological pain or chronic inflammatory diseases which are diseases caused by P2X1 and P2X3 receptor activity.Type: GrantFiled: December 20, 2010Date of Patent: January 17, 2017Assignee: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Yong-Chul Kim, Kwan-Young Jung, Joong Heui Cho
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Patent number: 9512141Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 receptor agonist for use in the treatment of several disorders, such as pain, atherosclerosis and glaucoma.Type: GrantFiled: December 4, 2013Date of Patent: December 6, 2016Assignee: HOFFMANN-LA ROCHE INC.Inventors: Baledi Dhurwasulu, Uwe Grether, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch
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Patent number: 9512134Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: January 29, 2014Date of Patent: December 6, 2016Assignee: Aptinyx, Inc.Inventors: John A. Lowe, III, M. Amin Khan
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Patent number: 9511058Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.Type: GrantFiled: July 7, 2014Date of Patent: December 6, 2016Assignee: Rigel Pharmaceuticals Inc.Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
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Patent number: 9504670Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: November 4, 2015Date of Patent: November 29, 2016Assignee: Aptinyx, Inc.Inventors: John A. Lowe, III, M. Amin Khan
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Patent number: 9499539Abstract: The invention relates generally to the creation and use of cyclic sulfonamide containing derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds for the treatment of hyperproliferative diseases and angiogenesis mediated diseases.Type: GrantFiled: November 4, 2013Date of Patent: November 22, 2016Assignee: NantBioScience, Inc.Inventors: Chunlin Tao, Chengzhi Yu, Forrest Arp, Paul Weingarten, Patrick Soon-Shiong
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Patent number: 9487489Abstract: The invention relates inter alia to halogen-substituted compounds of the general formula (I) in which the radicals A1-A4, T, n, W, Q, R1 and Z1-Z3 have the meanings given in the description. Also described are processes for preparing the compounds of the formula (I) and possible intermediates for the preparation of these compounds. The compounds according to the invention are particularly suitable for controlling insects, arachnids and nematodes in agriculture and ectoparasites in veterinary medicine.Type: GrantFiled: February 3, 2014Date of Patent: November 8, 2016Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Michael Maue, Kerstin Ilg, Anne Decor, Thomas Bretschneider, Julia Johanna Hahn, Werner Hallenbach, Reiner Fischer, Hans-Georg Schwarz, Ulrich Goergens, Klaus Raming, Johannes Koebberling, Walter Huebsch, Andreas Turberg, Niels Lindner
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Patent number: 9487491Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.Type: GrantFiled: August 29, 2014Date of Patent: November 8, 2016Assignees: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
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Patent number: 9421268Abstract: Oral liquid pharmaceutical compositions containing as active ingredient Nepadutant, PGS as solubilizer and optionally a chelating agent. Such compositions are found to be very stable and suitable for paediatric use in the treatment of gastro-intestinal diseases.Type: GrantFiled: July 12, 2013Date of Patent: August 23, 2016Assignee: LABORATORI GUIDOTTI S.P.A.Inventors: Claudia Lewerenz, Reinhard Schmitz, Maria Altamura
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Patent number: 9416126Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. 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 LRRK-2 kinase is involved.Type: GrantFiled: February 27, 2014Date of Patent: August 16, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Wei Li, Joel Harris, Andrew Stamford, Marc Poirier, Paul Tempest
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Patent number: 9376429Abstract: The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and the use thereof. A compound represented by formula 1 according to the invention, or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof may be effectively used for the prevention or treatment of pain, for example, acute pain, chronic pain, neuropathic pain, post-surgery pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, or paroxysmal extreme pain disorder (PEPD).Type: GrantFiled: October 15, 2013Date of Patent: June 28, 2016Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Ha Young Kim, In Woo Kim, Sun Ah Jun, Yun Soo Na, Hyung Geun Lee, Min Jae Cho, Jun Hee Lee, Hyo Shin Kim, Yun Soo Yoon, Kyung Ha Chung, Ji Duck Kim
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Patent number: 9333193Abstract: The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein.Type: GrantFiled: September 20, 2011Date of Patent: May 10, 2016Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Timothy L. MacDonald, Eric R. Houpt, Thomas E. Ballard, Jr.
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Patent number: 9290507Abstract: The present invention encompasses compounds of general formula (1) where in the groups R0 to R3 and L are defined as in claim 1, which are suitable for the 5 treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: GrantFiled: March 25, 2011Date of Patent: March 22, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 9266859Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.Type: GrantFiled: January 13, 2015Date of Patent: February 23, 2016Assignee: Eli Lilly and CompanyInventor: Gary G Deng
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Patent number: 9249119Abstract: The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof.Type: GrantFiled: February 1, 2013Date of Patent: February 2, 2016Assignee: SANOFIInventors: Csaba Huszár, Adrienn Hegedus, Zsolt Dombrády
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Patent number: 9216182Abstract: The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to the inhibition of H3 receptor.Type: GrantFiled: October 8, 2012Date of Patent: December 22, 2015Assignee: Novartis AGInventors: Tie-Lin Wang, Xuechun Zhang
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Patent number: 9212146Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: GrantFiled: June 18, 2013Date of Patent: December 15, 2015Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
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Patent number: 9193695Abstract: The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.Type: GrantFiled: September 30, 2011Date of Patent: November 24, 2015Assignee: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Takeshi Kuwada, Mitsukane Yoshinaga, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki, Naoki Miyakoshi
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Patent number: 9187468Abstract: The topical ophthalmic use of certain 2,4-diamino-substituted 1,3-triazines for preventing or alleviating ocular pain in patients is disclosed. Topical ocular pharmaceutical composition are also disclosed.Type: GrantFiled: February 13, 2014Date of Patent: November 17, 2015Assignee: NOVARTIS AGInventors: Martha E. Gadd, Peter G. Klimko, Karen C. David, Kenneth C. Appell, Mark R. Hellberg
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Patent number: 9157077Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: GrantFiled: September 20, 2013Date of Patent: October 13, 2015Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Patent number: 9115120Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: GrantFiled: August 23, 2013Date of Patent: August 25, 2015Assignee: Board of Regents, The University of Texas SystemsInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu
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Patent number: 9096543Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.Type: GrantFiled: May 9, 2013Date of Patent: August 4, 2015Assignee: Karyopharm Therapeutics Inc.Inventors: Vincent Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
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Patent number: 9096580Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 26, 2013Date of Patent: August 4, 2015Assignee: Bristol-Myers Squibb CompanyInventor: Kap-Sun Yeung
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Patent number: 9079865Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for 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: GrantFiled: July 29, 2012Date of Patent: July 14, 2015Assignee: Karyopharm Therapeutics Inc.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
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Patent number: 9061030Abstract: Compounds of Formula IA and Formula IB are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: GrantFiled: November 2, 2011Date of Patent: June 23, 2015Assignee: IRONWOOD PHARMACEUTICALS, INC.Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde
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Patent number: 9051269Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: GrantFiled: November 19, 2012Date of Patent: June 9, 2015Assignee: Constellation Pharmaceuticals, Inc.Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Nasveschuk
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Publication number: 20150148327Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: June 17, 2013Publication date: May 28, 2015Applicant: Merck Canada Inc.Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
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Publication number: 20150148330Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 16, 2015Publication date: May 28, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Publication number: 20150141396Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.Type: ApplicationFiled: July 3, 2013Publication date: May 21, 2015Applicant: Ares Trading S.A.Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
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Publication number: 20150141395Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: March 26, 2013Publication date: May 21, 2015Inventor: Kap-Sun Yeung
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Publication number: 20150141398Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: January 23, 2015Publication date: May 21, 2015Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
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Patent number: 9034864Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.Type: GrantFiled: March 7, 2014Date of Patent: May 19, 2015Assignee: Eli Lilly and CompanyInventors: Danwen Huang, Joshua O Odingo
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Publication number: 20150133423Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.Type: ApplicationFiled: January 13, 2015Publication date: May 14, 2015Inventor: Gary G. Deng
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Patent number: 9029531Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: GrantFiled: November 21, 2013Date of Patent: May 12, 2015Assignee: Agios Pharmaceuticals, Inc.Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
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Publication number: 20150126485Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 9, 2013Publication date: May 7, 2015Applicant: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Publication number: 20150126484Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: September 12, 2012Publication date: May 7, 2015Applicant: MERCK PATENT GMBHInventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Yufang Xiao, Hui Qiu, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
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Publication number: 20150126364Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d, R14 and R14a are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: May 13, 2013Publication date: May 7, 2015Applicant: E I Du Pont de Nemours and CompanyInventors: Thomas Francis Pahutski, JR., Matthew James Campbell, Dominic Ming-Tak Chan, Jeffrey Keith Long, Thomas Martin Stevenson
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Publication number: 20150119375Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: ApplicationFiled: May 6, 2013Publication date: April 30, 2015Applicant: Bayer Cropscience AGInventors: Pierre-Yves Coqueron, Mazen Es-Sayed, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Stephane Brunet, Helene Lachaise, Jean-Pierre Vors
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Patent number: 9018388Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: GrantFiled: March 24, 2014Date of Patent: April 28, 2015Assignee: Dow AgroSciences LLCInventors: Erich W. Baum, Gary D. Crouse, William H. Dent, III, Thomas C. Sparks, Lawrence C. Creemer
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Publication number: 20150111867Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
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Publication number: 20150111866Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.Type: ApplicationFiled: April 26, 2013Publication date: April 23, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
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Publication number: 20150111857Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
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Publication number: 20150111875Abstract: The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
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Publication number: 20150111865Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.Type: ApplicationFiled: April 25, 2013Publication date: April 23, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Jun Takeuchi, Masahiro Ikura, Masato Higashino, Maki Iwahashi, Kazuya Hashimura
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Patent number: 9012443Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: December 6, 2012Date of Patent: April 21, 2015Assignee: Amgen Inc.Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
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Publication number: 20150099729Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
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Publication number: 20150099728Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
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Publication number: 20150099719Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: October 6, 2014Publication date: April 9, 2015Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda