Spiro Ring System Patents (Class 514/278)
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Patent number: 9108944Abstract: Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.Type: GrantFiled: February 16, 2011Date of Patent: August 18, 2015Assignee: ARAGON PHARMACEUTICALS, INC.Inventors: Nicholas D. Smith, Celine Bonnefous, Jackaline D. Julien
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Patent number: 9096599Abstract: This invention relates to novel spiroindoline compounds of formula (I) that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: GrantFiled: August 3, 2012Date of Patent: August 4, 2015Assignee: Intervet Inc.Inventors: Christophe Pierre Alain Chassaing, Sandra Koch, Jürgen Lutz
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Patent number: 9044469Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.Type: GrantFiled: August 12, 2013Date of Patent: June 2, 2015Assignee: Trevena, Inc.Inventors: Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C. K. Yuan
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Publication number: 20150148363Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) for the treatment of diabetes, metabolic syndrome and obesity.Type: ApplicationFiled: January 30, 2015Publication date: May 28, 2015Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Publication number: 20150148349Abstract: The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 27, 2013Publication date: May 28, 2015Applicant: NOVARTIS AGInventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
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Publication number: 20150148334Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: June 27, 2014Publication date: May 28, 2015Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Publication number: 20150148318Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.Type: ApplicationFiled: September 26, 2014Publication date: May 28, 2015Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
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Patent number: 9040693Abstract: The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like ; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O—(alkylene)—Y, —O—Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.Type: GrantFiled: October 17, 2006Date of Patent: May 26, 2015Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kohsuke Ohno, Takashi Miyagi, Tomonaga Ozawa, Nobuhiko Fushimi
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Publication number: 20150141403Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: December 1, 2014Publication date: May 21, 2015Inventors: Jose Maria CID-NUNEZ, Daniel OEHLRICH, Andres Avelino TRABANCO-SUAREZ, Gary John TRESADERN, Juan Antonio VEGA RAMIRO, Gregor James MACDONALD
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Publication number: 20150141406Abstract: The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: May 31, 2013Publication date: May 21, 2015Inventors: Hiroshi Nara, Masaki Daini, Akira Kaieda, Taku Kamei, Toshihiro Imaeda, Fumiaki Kikuchi
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Patent number: 9034891Abstract: There are provided certain bicyclic heterocyclic compounds that act as M1 muscarinic receptor modulators. Compositions containing these compounds and their use are also disclosed.Type: GrantFiled: March 14, 2013Date of Patent: May 19, 2015Assignee: ISRAEL INSTITUTE FOR BIOLOGICAL RESEARCHInventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
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Patent number: 9034890Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.Type: GrantFiled: February 27, 2013Date of Patent: May 19, 2015Inventor: Steven A. Rich
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Publication number: 20150133400Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.Type: ApplicationFiled: September 15, 2014Publication date: May 14, 2015Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
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Publication number: 20150133481Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.Type: ApplicationFiled: June 4, 2013Publication date: May 14, 2015Applicant: Aragon Pharmaceuticals, Inc.and Sloan -Kettering Institute for Cancer ResearchInventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nichola D. Smith
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Patent number: 9029544Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.Type: GrantFiled: February 17, 2011Date of Patent: May 12, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Daniela Berta, Klaus Fuchs, Riccardo Giovannini, Dieter Wolfgang Hamprecht, Ingo Konetzki, Ruediger Streicher, Thomas Trieselmann
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Publication number: 20150126496Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.Type: ApplicationFiled: October 10, 2014Publication date: May 7, 2015Applicant: Massachusetts Institute of TechnologyInventors: Damon Theron Page, Mriganka Sur
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Patent number: 9023760Abstract: A compound of the formula (1) wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: GrantFiled: May 19, 2011Date of Patent: May 5, 2015Assignee: Syngenta Participations AGInventors: Michel Muehlebach, Jürgen Harry Schaetzer
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Publication number: 20150118258Abstract: The present invention relates to fluorinated bridged spiro[2.4]heptane derivatives of formula (I), wherein n and R1 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: May 15, 2013Publication date: April 30, 2015Inventors: Olivier Corminboeuf, Davide Pozzi
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Publication number: 20150111910Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.Type: ApplicationFiled: May 22, 2013Publication date: April 23, 2015Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
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Publication number: 20150111914Abstract: The present invention is directed to spirolactam analogues which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which 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: ApplicationFiled: May 3, 2013Publication date: April 23, 2015Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
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Publication number: 20150111882Abstract: The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases.Type: ApplicationFiled: May 10, 2013Publication date: April 23, 2015Applicant: Ares Trading S.A.Inventors: Anna Quattropani, Dominique Swinnen
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Publication number: 20150111915Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.Type: ApplicationFiled: December 30, 2014Publication date: April 23, 2015Applicant: LEO PHARMA A/SInventor: Simon Feldbaek NIELSEN
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Publication number: 20150105415Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kazuyuki OHMOTO, Masashi KATO, Yoshifumi KAGAMIISHI, Junichiro MANAKO
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Publication number: 20150105354Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLCInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Patent number: 9005578Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: GrantFiled: May 28, 2013Date of Patent: April 14, 2015Assignees: Fluoropharma, Inc., The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Patent number: 9006260Abstract: The present invention relates to certain spirocyclic compounds that are inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 (11?HSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.Type: GrantFiled: September 14, 2012Date of Patent: April 14, 2015Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Colin Zhang
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Publication number: 20150099738Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: ApplicationFiled: June 30, 2014Publication date: April 9, 2015Inventors: Mark L. BEHNKE, Alfredo C. CASTRO, Lawrence K. CHAN, Catherine A. EVANS, Louis GRENIER, Michael J. GROGAN, Yves LEBLANC, Tao LIU, Stephane PELUSO, Daniel A. SNYDER, Thomas T. TIBBITTS
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Publication number: 20150099771Abstract: The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which 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: ApplicationFiled: May 3, 2013Publication date: April 9, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
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Publication number: 20150099730Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.Type: ApplicationFiled: September 6, 2013Publication date: April 9, 2015Applicant: Janssen Pharmaceutica, NVInventor: Peter J. Connolly
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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: 20150099734Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
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Publication number: 20150099732Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.Type: ApplicationFiled: March 7, 2013Publication date: April 9, 2015Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
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Patent number: 9000183Abstract: Cyclohexane-1,2?-indene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 13, 2013Date of Patent: April 7, 2015Assignee: Astrazeneca ABInventors: Sofia Karlstrom, Peter Soderman, Laszlo Rakos, Liselotte Ohberg, Karin Kolmodin, Lars Sandberg
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Patent number: 8999968Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: GrantFiled: July 3, 2013Date of Patent: April 7, 2015Assignee: University Health NetworkInventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
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Patent number: 8999971Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: GrantFiled: August 21, 2014Date of Patent: April 7, 2015Assignee: Aerpio Therapeutics Inc.Inventors: Robert Shalwitz, Joseph H. Gardner
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Patent number: 9000182Abstract: 2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. methods of therapy, and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 13, 2013Date of Patent: April 7, 2015Assignee: AstraZeneca ABInventors: Sofia Karlstrom, Gabor Csjernyik, Britt-Marie Swahn, Lars Sandberg, Karin Kolmodin, Peter Soderman, Liselotte Ohberg
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Patent number: 9000184Abstract: Cyclohexane-1,2?-naphthalene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 13, 2013Date of Patent: April 7, 2015Assignee: AstraZeneca ABInventors: Sofia Karlstrom, Lars Sandberg, Peter Soderman, Karin Kolmodin, Liselotte Ohberg
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Patent number: 8993567Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: March 27, 2014Date of Patent: March 31, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
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Patent number: 8993586Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: September 26, 2014Date of Patent: March 31, 2015Assignee: Pfizer Inc.Inventors: David A. Griffith, Robert L. Dow, Scott W. Bagley, Aaron Smith
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Publication number: 20150087626Abstract: 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: ApplicationFiled: July 4, 2011Publication date: March 26, 2015Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
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Publication number: 20150086491Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 5, 2014Publication date: March 26, 2015Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
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Publication number: 20150087618Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 2, 2014Publication date: March 26, 2015Applicant: AbbVie Inc.Inventors: Mary E. Bellizzi, David A. Betebenner, Jean C. Califano, William A. Carroll, Daniel D. Caspi, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Yi Gao, Charles W. Hutchins, Douglas K. Hutchinson, Tammie K. Jinkerson, Warren M. Kati, Ryan G. Keddy, Allan C. Krueger, Wenke Li, Dachun Liu, Clarence J. Maring, Mark A. Matulenko, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, John K. Pratt, John T. Randolph, Todd W. Rockway, Kathy Sarris, Michael D. Tufano, Seble H. Wagaw, Rolf Wagner, Kevin R. Woller
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Patent number: 8987287Abstract: The application is directed to compounds of Formula I?-A and especially to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R5a, Y, Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I?-A, and especially compounds of Formula I-A, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.Type: GrantFiled: December 13, 2013Date of Patent: March 24, 2015Assignee: Purdue Pharma L.P.Inventors: R. Richard Goehring, Laykea Tafesse, Mark A. Youngman
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Publication number: 20150080367Abstract: 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, m, n and the C-linked Ring 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: ApplicationFiled: November 21, 2014Publication date: March 19, 2015Applicant: Genentech, Inc.Inventors: Frederick Cohen, Malcolm Huestis, Cuong Ly, Snahel Patel, Michael Siu, Xianrui Zhao
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Publication number: 20150080393Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.Type: ApplicationFiled: September 5, 2014Publication date: March 19, 2015Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
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Patent number: 8980905Abstract: Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.Type: GrantFiled: June 24, 2011Date of Patent: March 17, 2015Assignee: Leo Pharma A/SInventor: Simon Feldbæk Nielsen
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Publication number: 20150072978Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: November 17, 2014Publication date: March 12, 2015Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew J. Souers
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Publication number: 20150065487Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20150064234Abstract: It has been discovered that pharmacological inhibition of K+ channels (using the FDA-approved broad-spectrum K+ channel antagonist 4-AP) positively benefitted smn mutant phenotypes, a result that is consistent with the defective excitability of motor circuits by their interneuron or sensory neuron inputs being a critical consequence of SMN depletion. Based on these observations, certain embodiments of the invention are directed to methods of treatment of SMA by administering therapeutically effective amounts of one or more potassium channel antagonists, including 4-aminopyridine, 4-(dimethylamino)pyridine, 4-(methylamino)pyridine, and 4-(aminomethyl)pyridine. Other embodiments are directed to new pharmaceutical formulations comprising two or more potassium channel antagonists.Type: ApplicationFiled: March 26, 2013Publication date: March 5, 2015Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventor: Brian D. Mccabe
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Publication number: 20150065477Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.Type: ApplicationFiled: March 14, 2013Publication date: March 5, 2015Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen