Additional Hetero Ring Which Is Unsaturated Patents (Class 544/405)
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Publication number: 20150045349Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. 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: February 19, 2013Publication date: February 12, 2015Inventors: Hiroyuki Nagamiya, Masato Yoshida, Masaki Seto, Shogo Marui, Tsuneo Oda, Yuji Ishichi, Hideo Suzuki, Tomokazu Kusumoto, Takatoshi Yogo, Chul Yun Rhim, Cheolhwan Yoon, Gil Nam Lee, Hyun Bin Kang, Kwang Ok Kim, Hye Sun Jeon
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Publication number: 20150045312Abstract: Methods of treating autism, autistic spectrum disorders or Fragile X syndrome comprised of administering molecules that engage the cystine-glutamate exchange (System xc?) and/or elevate the extracellular levels of glutathione in the CNS. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.Type: ApplicationFiled: August 11, 2014Publication date: February 12, 2015Inventors: Michael Neary, Chad Beyer
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Publication number: 20150045374Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.Type: ApplicationFiled: January 3, 2013Publication date: February 12, 2015Inventors: Kerim Babaoglu, Kyla L. Bjornson, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu
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Publication number: 20150038502Abstract: The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 19, 2012Publication date: February 5, 2015Inventors: Dansu Li, Anthony J. Roecker
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Patent number: 8946231Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: GrantFiled: March 15, 2010Date of Patent: February 3, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Craig M. Potteiger
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Patent number: 8946230Abstract: Aryl- and heteroaryl-nitrogen heterocyclic compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, p, q, R1, R2, R3, X1, X2, X3, Y1 and Y2 are defined herein; and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: May 9, 2011Date of Patent: February 3, 2015Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Kristin L. Andrews, Michael J. Frohn, Paul E. Harrington, Alexander J. Pickrell, Robert M. Rzasa
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Patent number: 8946233Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: January 16, 2014Date of Patent: February 3, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20150031661Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: March 24, 2014Publication date: January 29, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
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Publication number: 20150031682Abstract: The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.Type: ApplicationFiled: February 15, 2013Publication date: January 29, 2015Inventors: Yassir Younis, Kelly Chibale, Michael John Witty, David Waterson
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Publication number: 20150031708Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating CFTR mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 9, 2008Publication date: January 29, 2015Inventors: Sara Hadida-Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
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Publication number: 20150031686Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.Type: ApplicationFiled: March 6, 2013Publication date: January 29, 2015Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
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Patent number: 8940742Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: GrantFiled: March 15, 2013Date of Patent: January 27, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. Castro, Katrina Chan, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Liansheng Li, Tao Liu, Yi Liu, Pingda Ren, Daniel A. Snyder, Martin R. Tremblay
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Publication number: 20150025065Abstract: The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: July 15, 2014Publication date: January 22, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Elke LANGKOPF, Holger WAGNER
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Publication number: 20150025046Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.Type: ApplicationFiled: February 27, 2013Publication date: January 22, 2015Inventors: Mihir Mandal, Timothy A. Blizzard, Helen Chen, Harry Chobanian, Yan Guo, Barbara Pio, Zhicai Wu, Tesfaye Biftu, William J. Greenlee, Johnny Zhaoning Zhu
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Publication number: 20150025087Abstract: The invention provides compounds of formula (I) and methods of treating a Mycobacterium infection or tuberculosis, or inhibiting DprE1 with the same.Type: ApplicationFiled: July 10, 2014Publication date: January 22, 2015Inventors: Maruti N. Naik, Shahul Hameed PEER MOHAMED, Radha K. Shandil, Vikas Narayan Shinde, Pravin S. Shirude, Monalisa Chatterji
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Publication number: 20150018314Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
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Publication number: 20150018373Abstract: Provided is a compound having a melanin-concentrating hormone receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of obesity and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: July 8, 2014Publication date: January 15, 2015Inventors: Hideyuki IGAWA, Masashi TAKAHASHI, Keiko KAKEGAWA, Minoru IKOMA, Jumpei AIDA
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Publication number: 20150018313Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT, Armin HECKEL
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Publication number: 20150018332Abstract: 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: ApplicationFiled: July 26, 2012Publication date: January 15, 2015Applicant: KARYOPHARM THERAPEUTICS INC.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
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Publication number: 20150018315Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
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Patent number: 8933085Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: November 18, 2011Date of Patent: January 13, 2015Assignee: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Patent number: 8927721Abstract: The present invention provides, for example, the following compound: wherein ring Z is pyridine or a carbocycle, each of which is substituted or unsubstituted, ring A is a carbocycle or a heterocycle, each of which is substituted or unsubstituted, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R4a and R4b are each independently hydrogen or substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.Type: GrantFiled: October 27, 2011Date of Patent: January 6, 2015Assignee: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Yuuji Kooriyama
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Publication number: 20150005294Abstract: The invention provides novel substituted azaheterocyclic compounds compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.Type: ApplicationFiled: January 10, 2013Publication date: January 1, 2015Applicants: CANCER RESEARCH TECHNOLOGY LIMITED, MERCK PATENT GMBHInventors: Kai Schiemann, Frank Stieber, Christina Esdar
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Publication number: 20150005275Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: May 6, 2014Publication date: January 1, 2015Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
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Patent number: 8921373Abstract: The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: June 22, 2011Date of Patent: December 30, 2014Assignee: Shionogi & Co., Ltd.Inventor: Noriyuki Kurose
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Patent number: 8920941Abstract: It is an object to provide a novel material having a bipolar property, a light emitting element provided with the novel material, and a display device that includes the light emitting element. It is an object to provide a pyrazine derivative represented by the following general formula (g-1).Type: GrantFiled: December 22, 2006Date of Patent: December 30, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroko Murata, Masakazu Egawa, Harue Nakashima, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Patent number: 8921370Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: December 22, 2011Date of Patent: December 30, 2014Assignee: H. Lundbeck A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Publication number: 20140378448Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: ApplicationFiled: September 4, 2014Publication date: December 25, 2014Inventors: Akihiro OKANO, Muneyoshi MAKABE
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Publication number: 20140378474Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: January 25, 2013Publication date: December 25, 2014Applicant: NOVARTIS AGInventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
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Publication number: 20140378447Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: ApplicationFiled: September 4, 2014Publication date: December 25, 2014Inventors: Akihiro OKANO, Muneyoshi MAKABE, Kouki OGAWA
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Publication number: 20140371201Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Inventors: Matthew WEISS, Alessandro BOEZIO, Christiane BOEZIO, John R. BUTLER, Margaret Yuhua CHU-MOYER, Erin F. DIMAURO, Thomas DINEEN, Russell GRACEFFA, Angel GUZMAN-PEREZ, Hongbing HUANG, Charles KREIMAN, Daniel LA, Isaac E. MARX, Benjamin Charles MILGRIM, Hanh Nho NGUYEN, Emily PETERSON, Karina ROMERO, Brian SPARLING
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Publication number: 20140371238Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: ApplicationFiled: March 13, 2014Publication date: December 18, 2014Applicant: FLATLEY DISCOVERY LABInventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
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Publication number: 20140371073Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: ApplicationFiled: September 11, 2012Publication date: December 18, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Pierre Joseph Marcel Jung, Joerg Leipner, Mathilde Denise Lachia, Alain De Mesmaeker
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Publication number: 20140371230Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: June 25, 2014Publication date: December 18, 2014Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 8912181Abstract: A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.Type: GrantFiled: January 6, 2012Date of Patent: December 16, 2014Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
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Publication number: 20140364408Abstract: 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: ApplicationFiled: July 29, 2012Publication date: December 11, 2014Applicant: KARYOPHARM THERAPEUTICS INC.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
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Publication number: 20140364433Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
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Publication number: 20140349991Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.Type: ApplicationFiled: July 17, 2014Publication date: November 27, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
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Publication number: 20140350030Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.Type: ApplicationFiled: September 17, 2012Publication date: November 27, 2014Inventors: Dario Doller, Guiying Li
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Publication number: 20140349973Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: December 10, 2012Publication date: November 27, 2014Applicant: Viamet Pharmaceuticals, IncInventors: William J. Hoekstra, Christopher M. Yates
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Publication number: 20140350026Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.Type: ApplicationFiled: November 9, 2012Publication date: November 27, 2014Inventors: Xianjin Luo, Weidong Ye
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Patent number: 8895589Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: August 23, 2012Date of Patent: November 25, 2014Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20140343078Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.Type: ApplicationFiled: July 29, 2014Publication date: November 20, 2014Inventors: Michael EISSENSTAT, Dehui DUAN, Ji-Hye KANG
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Publication number: 20140343077Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.Type: ApplicationFiled: August 22, 2012Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant
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Publication number: 20140343030Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: May 16, 2014Publication date: November 20, 2014Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, Ding-Quan Qian, Song Mei, Ganfeng Cao, Yongchun Pan, Qun Li, Zhongjiang Jia
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Publication number: 20140336195Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: May 21, 2012Publication date: November 13, 2014Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
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Publication number: 20140336167Abstract: 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: May 10, 2013Publication date: November 13, 2014Applicant: ABBVIE INC.Inventors: Ramzi F. Sweis, Michael L. Curtin, Marina A. Pliushchev, Todd M. Hansen, Kenton Longenecker
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Publication number: 20140336186Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: July 9, 2014Publication date: November 13, 2014Inventors: Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER
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Publication number: 20140329825Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.Type: ApplicationFiled: November 26, 2012Publication date: November 6, 2014Applicant: NOVARTIS AGInventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
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Publication number: 20140329836Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: December 5, 2013Publication date: November 6, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu