A Ring Nitrogen Is Shared By The Two Cyclos Of The Bicyclo Ring System (e.g., Pyrrolo [1,2-a]pyrimidine, Imidazo[1,2-a]pyrimidine, Etc.) Patents (Class 514/259.1)
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Patent number: 8853125Abstract: The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, etc.Type: GrantFiled: September 23, 2009Date of Patent: October 7, 2014Assignee: BASF SEInventors: Steffen Groβ, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Prashant Deshmukh, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Faraneh Oloumi
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Publication number: 20140294805Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: October 2, 2014Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
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Publication number: 20140275119Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicants: NOVARTIS AG, IRM LLCInventors: Fang LIANG, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh NAGLE, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL
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Publication number: 20140256736Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Applicant: XENON PHARMACEUTICALS INC.Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
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Publication number: 20140235647Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: September 27, 2012Publication date: August 21, 2014Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
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Patent number: 8809344Abstract: Various tetrahydropyrazolo[1,5-a]pyrimidine compounds, compositions, methods of making, and methods for the prevention and treatment of HCV infections and associated diseases are disclosed. The invention further relates to biomarkers for identification of HCV strains which are resistant to the tetrahydropyrazolo[1,5-a]pyrimidine compounds.Type: GrantFiled: October 29, 2009Date of Patent: August 19, 2014Assignee: Apath, LLCInventors: Urszula Slomczynska, Paul Olivo, Jodi Beattie, Gale Starkey, Amine Noueiry, Robert Roth
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Publication number: 20140228349Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.Type: ApplicationFiled: October 9, 2012Publication date: August 14, 2014Inventors: Mark Laurence Boys, Laurence E. Burgess, C. Todd Eary, Robert Groneberg, Bruno P. Hache, Darren Harvey, Erik James Hicken, Christopher F. Kraser, Ellen Laird, David A. Moreno, Mark C. Munson, Li Ren, John E. Robinson, Stephen T. Schlachter
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Patent number: 8785452Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: GrantFiled: June 17, 2009Date of Patent: July 22, 2014Assignees: Institut National de la Sante et de la Recherche Medicale, Institut Pasteur KoreaInventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
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Publication number: 20140194418Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.Type: ApplicationFiled: January 20, 2012Publication date: July 10, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
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Publication number: 20140179695Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
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Publication number: 20140179714Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.Type: ApplicationFiled: February 11, 2014Publication date: June 26, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
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Publication number: 20140171452Abstract: Disclosed is an antidepressant, neuroprotectant, amyloid ? deposition inhibitor, or age retardant composition containing a heterocyclic compound having the general formula (I):Type: ApplicationFiled: February 12, 2014Publication date: June 19, 2014Applicant: ZENYAKU KOGYO KABUSHIKI KAISHAInventors: Yoshimasa YAMAGUCHI, Ryogo YUI, Toshiyuki MATSUNO, Kenichi SAITOH, Hitoshi MIYASHITA, Takeshi NAGATA
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Publication number: 20140171414Abstract: Compounds of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and conditions in which HNE is implicated.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Lilian ALCARAZ, Robert Andrew Heald, Jonathan Mark Sutton, Elisabetta Armani, Carmelida Capaldi
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Publication number: 20140142121Abstract: Described are mitochondria-targeted anti-tumor agents, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation.Type: ApplicationFiled: May 29, 2013Publication date: May 22, 2014Inventors: Dario C. Altieri, Byoung Heon Kang
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Patent number: 8729074Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: GrantFiled: March 19, 2010Date of Patent: May 20, 2014Assignee: Amgen Inc.Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
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Patent number: 8722708Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.Type: GrantFiled: June 12, 2006Date of Patent: May 13, 2014Assignees: Merck Sharp & Dohme Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X. H. Le, Gang Qian, Yuefei Shao
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Patent number: 8691826Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.Type: GrantFiled: September 13, 2012Date of Patent: April 8, 2014Assignee: Chiesi Farmaceutici S.p.A.Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
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Patent number: 8691825Abstract: The instant invention provides for substituted fused pyrimidine compounds of Formula A that inhibit Akt activity: In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: March 29, 2010Date of Patent: April 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
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Publication number: 20140094474Abstract: Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14?, R15, R15?, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.Type: ApplicationFiled: April 20, 2012Publication date: April 3, 2014Applicant: ORION CORPORATIONInventors: Olli Törmakängas, Gerd Wohlfahrt, Harri Salo, Rathna Durga Ramasurbamanian, Pranab Kumar Patra, Arputharaj Ebenezer Martin, Terhi Heikkinen, Anniina Vesalainen, Anu Moilanen, Arja Karjalainen
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Publication number: 20140088110Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Swen HÖLDER, Armin ZÜLCH, Thomas BÄR, Thomas MAIER, Astrid ZIMMERMANN, Thomas BECKERS, Volker GEKELER, Hemant JOSHI, Yogesh MUNOT, Umesh BHISE, Sunil CHAVAN, Sachin SHIVATARE, Sarvesh PATEL, Vikas GORE
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Patent number: 8680113Abstract: Compounds having Formula I: wherein the variables Ar1, Ar2, R1, R2 and R3 are defined herein, pharmaceutical compositions, and methods of using such compounds or compositions for inhibiting Bmi-1 expression.Type: GrantFiled: July 1, 2009Date of Patent: March 25, 2014Assignee: PTC Therapeutics, Inc.Inventors: Young-Choon Moon, Nadiya Sydorenko, Thomas Davis, Liangxian Cao, Daniel J. Medina, Marites A. Rafanan
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Publication number: 20140066434Abstract: The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: April 6, 2012Publication date: March 6, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: William C. Shakespeare
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Patent number: 8653260Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: June 20, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20140038954Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.Type: ApplicationFiled: February 13, 2012Publication date: February 6, 2014Applicant: AMGEN INC.Inventors: Oleg Epstein, Ryan White, Vinod F. Patel, Jason Human
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Publication number: 20140038941Abstract: A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R1 represents optionally substituted lower alkyl, and the like; R2 represents an optionally substituted cycloalkyl, and the like; Q represents a hydrogen atom, and the like; R3 represents —C(?O)NR8R9 (wherein R8 and R9 may be the same or different, and each represents a hydrogen atom, and the like), and the like; L1 represents —CR11AR11B— (wherein R11A and R11B may be the same or different, and each represents a hydrogen atom, and the like), and the like; and W1 and W2 may be the same or different, and each represents C—R12 (wherein R12 represents a hydrogen atom, and the like), and the like.Type: ApplicationFiled: February 1, 2012Publication date: February 6, 2014Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Takashi Sawada, Tomohiro Danjo, Keiichi Motosawa, Takayuki Furuta, Maki Ichioka, Masamori Sugawara, Noriaki Uesaka
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Patent number: 8633198Abstract: Antiviral compositions and methods are contemplated that are especially effective in the treatment and prevention of influenza A viruses. Also presented are cellular assays to identify small molecule compounds having antiviral properties, particularly as it relates to detection of influenza A RNA-dependent RNA polymerase activity in a mammalian cell independent of other influenza A components. Preferred assays allow for identification of viral replication inhibitors that do not disrupt normal cellular activity.Type: GrantFiled: September 19, 2012Date of Patent: January 21, 2014Assignee: Nant Holdings IP, LLCInventors: Kayvan Niazi, Shahrooz Rabizadeh, Anne-Laure Le Ny, Oleksandr Buzko, Justin Golovato, Patrick Soon-Shiong
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Publication number: 20140011805Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.Type: ApplicationFiled: July 12, 2013Publication date: January 9, 2014Inventors: Paul B. Yu, Gregory D. Cuny, Kenneth D. Bloch, Randall T. Peterson, Charles C. Hong
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Patent number: 8618113Abstract: The invention relates to a method of treatment or prophylaxis of demyelinating disease, in particular the neurodegenerative phase of demyelinating disease, which comprises administration of an acid sensing ion channel (ASIC) antagonist. The invention also relates to a pharmaceutical composition comprising an ASIC antagonist in combination with an additional therapeutic agent, in particular an anti-inflammatory or immunmodulatory agent.Type: GrantFiled: July 16, 2007Date of Patent: December 31, 2013Assignee: Medical Research CouncilInventors: Lars Fugger, Manuel Friese
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Patent number: 8614218Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: GrantFiled: March 25, 2010Date of Patent: December 24, 2013Assignee: Bayer Intellectual Property GmbHInventors: Swen Hölder, Matthias Vennemann, Gerrit Beneke, Armin Zülch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
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Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Publication number: 20130317002Abstract: Compounds of formula (I) or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: February 2, 2010Publication date: November 28, 2013Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventor: Barbara Beckers
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Publication number: 20130310391Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: January 9, 2012Publication date: November 21, 2013Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Christian Sirrenberg, Thomas J.J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
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Publication number: 20130310362Abstract: The present invention relates to compounds of formula (I), a N-oxide or tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6, R7, R10, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: February 5, 2010Publication date: November 21, 2013Applicant: BAYER PHARMA AKTIEGESELLSCHAFTInventor: Barbara Beckers
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Publication number: 20130296342Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.Type: ApplicationFiled: June 28, 2013Publication date: November 7, 2013Applicant: OTSUKA PHARMACEUTICAL FACTORY, INC.Inventors: Irina NEAGU, Michael OHLMEYER, Vidyadhar M. PARADKAR, Kurt W. SAIONZ, Koushi IWATA, Takashi OKAMURA, Tadao SHIBUTANI
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Publication number: 20130296319Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 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: ApplicationFiled: July 11, 2013Publication date: November 7, 2013Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Patent number: 8563560Abstract: Disclosed herein are bicyclic guanidine salts, useful as cure catalysts for electrodeposited coatings. The bicyclic guanidine salts are formed as the reaction product of reactants comprising (a) a compound having the general formula CXn, wherein X is N, O, or S and wherein n is 2 to 4; (b) an acid; (c) dipropylene triamine; and (d) water, and an associated method for forming a bicyclic guanidine salt from the same reaction ingredients.Type: GrantFiled: February 25, 2011Date of Patent: October 22, 2013Assignee: PPG Industries Ohio, Inc.Inventors: Charles R. Hickenboth, Christopher A. Dacko, Steven R. Zawacky, Gregory J. McCollum
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Patent number: 8563561Abstract: The 3-(3-pyrimidin-2ylbenzyl)-1,2,4-triazolo[4,3-b]pyrimidine compounds of formula in which R1, R2, R3, R3, R4 have the meanings indicated herein, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: November 18, 2009Date of Patent: October 22, 2013Assignee: Merck Patent GmbHInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20130231354Abstract: Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: November 9, 2011Publication date: September 5, 2013Applicant: Bristol-Meyers Squibb CompanyInventors: Joel F. Austin, David B. Frennesson, Mark G. Saulnier
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Publication number: 20130225591Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.Type: ApplicationFiled: September 14, 2010Publication date: August 29, 2013Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
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Patent number: 8519135Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: GrantFiled: January 13, 2009Date of Patent: August 27, 2013Assignee: Chemocentryx, Inc.Inventors: Wei Chen, Antoni Krasinski
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Publication number: 20130210839Abstract: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2?X3 is CR5—CR6?CR7, N—CR6?CR7, CR5—N?CR7 or CR5—CR6?N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, 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: ApplicationFiled: October 27, 2011Publication date: August 15, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Genta Tadano
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Publication number: 20130196979Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
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Publication number: 20130190172Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 5, 2011Publication date: July 25, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Thomas Francis Pahutski, JR.
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Publication number: 20130190332Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: July 7, 2011Publication date: July 25, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Stuart Ince, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer, William Scott
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Patent number: 8492374Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: GrantFiled: April 28, 2010Date of Patent: July 23, 2013Assignee: Industrial Technology Research InstituteInventors: On Lee, Chih-Hung Chen, Chi-Y Hung, Yow-Lone Chang, Ting-Shou Chen
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Publication number: 20130184273Abstract: Compounds of formula (I), which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: July 11, 2011Publication date: July 18, 2013Applicant: Bayer Intellectual Property GmbHInventors: Stuart Ince, Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
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Publication number: 20130150380Abstract: Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C—R1 or N; —X1-X2— is CR15?N— or —NR19—CO—; and R1-R6, R15, R15 and R19 are as defined in the claims.Type: ApplicationFiled: March 10, 2011Publication date: June 13, 2013Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Christine Edwards, Janusz Kulagowski, Harry Finch
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Publication number: 20130131039Abstract: Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.Type: ApplicationFiled: April 11, 2011Publication date: May 23, 2013Applicant: Array BioPharma Inc.Inventors: Laurence E. Burgess, Mark Laurence Boys, Robert D. Groneberg, Darren M. Harvey, Timothy Kercher, Christopher F. Kraser, Ellen Laird, Eugene Tarlton, Qian Zhao, Lily Huang
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Patent number: 8410264Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: GrantFiled: August 19, 2010Date of Patent: April 2, 2013Assignee: Novartis AGInventors: Miao Dai, Xingnian Fu, Feng He, Lei Jiang, Yue Li, Fang Liang, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Xiaoxia Yan, Zhengtian Yu, Ji Yue Zhang
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Patent number: 8410117Abstract: The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R1, R2 and R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.Type: GrantFiled: March 17, 2011Date of Patent: April 2, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Ruben Alvarez Sanchez, Konrad Bleicher, Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinzen, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph