Spiro Patents (Class 546/15)
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Patent number: 8791133Abstract: The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.Type: GrantFiled: October 16, 2012Date of Patent: July 29, 2014Assignee: SanofiInventors: Karl Schoenafinager, Henning Steinhagen, Bodo Scheiper, Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Jacques Mauger, Pavel Safar
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Publication number: 20140200223Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.Type: ApplicationFiled: December 18, 2013Publication date: July 17, 2014Inventors: Salvacion Cacatian, David A. Claremon, Lawrence Wayne Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian Mckeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
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Patent number: 8778236Abstract: A novel photochromic compound which develops a color of a neutral tint and has high color optical density, high fading speed and excellent durability. The present invention is a chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as the basic skeleton in which a hetero ring having two hetero atoms including at least one sulfur atom is directly bonded to the 6-position and the 7-position of the indeno(2,1-f)naphtho(1,2-b)pyran structure via the hetero atom like the compound represented by the following formula (18).Type: GrantFiled: March 7, 2012Date of Patent: July 15, 2014Assignee: Tokuyama CorporationInventors: Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Toshiaki Takahashi, Mitsuyoshi Sando, Shinobu Izumi
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Patent number: 8778938Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 3, 2011Date of Patent: July 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Patent number: 8772288Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 3, 2009Date of Patent: July 8, 2014Assignee: Almirall, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
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Publication number: 20140179724Abstract: The application is directed to compounds of Formula I?-A especially to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R5a, Y, Z 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: ApplicationFiled: December 13, 2013Publication date: June 26, 2014Applicant: Purdue Pharma L.P.Inventors: R. Richard GOEHRING, Laykea TAFESSE, Mark A. YOUNGMAN
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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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Patent number: 8759367Abstract: The present invention relates to compounds for modulating sonic hedgehog signaling and preventing or treating cancer.Type: GrantFiled: October 4, 2011Date of Patent: June 24, 2014Assignees: The Wistar Institute, The Trustees of the University of PennsylvaniaInventors: Nadia Dahmane, Jeffrey D. Winkler, Andre Isaacs
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Publication number: 20140171461Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R3a, R4, Y, and Z are defined as set forth in the specification. The invention is also directed to use of 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: ApplicationFiled: December 13, 2013Publication date: June 19, 2014Applicant: Purdue Pharma L.P.Inventors: Jae Hyun PARK, Laykea Tafesse
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Patent number: 8754095Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: June 17, 2014Assignee: SanofiInventor: Zhongli Gao
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Patent number: 8754096Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: November 10, 2011Date of Patent: June 17, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Heather E. Stevenson, Cheng Wang, C. Blair Zartman
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Patent number: 8742109Abstract: This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: GrantFiled: September 14, 2012Date of Patent: June 3, 2014Assignee: Xenon Pharmaceuticals Inc.Inventors: Jean-Jacques Cadieux, Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Qi Jia, Stefanie Abel, Emad El-Sayed, Elke Huthmann, Thomas Isarno
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Publication number: 20140147412Abstract: Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.Type: ApplicationFiled: July 9, 2012Publication date: May 29, 2014Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Jiancun Zhang, Yingjun Zhang, Hongming Xie, Qingyun Ren, Huichao Luo, Tianzhu Yu, Yumei Tan
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Publication number: 20140142302Abstract: A 1,5-naphthyridine derivative represented by Formula [1] (in which R1, R2, R3, R4 and R5 represent a hydrogen atom, -L-Z (in which Z represents a non-aromatic heterocyclic group or the like; and L represents a single bond or the like), or the like, R6 represents -L-Z or the like, R7 and R8 represent a hydrogen atom or the like, and Q represents an oxygen atom or the like), or a salt thereof has an excellent inhibitory activity with respect to the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway, and is useful for treatments such as prophylactic treatments and therapeutic treatments of diseases in which the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway are involved.Type: ApplicationFiled: January 28, 2014Publication date: May 22, 2014Applicant: FUJIFILM CorporationInventors: Hidetomo FURUYAMA, Hideki KURIHARA, Kentarou FURUYA, Takahiro TERAO, Shinichirou SEKINE, Daisuke NAKAGAWA
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Publication number: 20140142300Abstract: An organic electroluminescence (EL) material and an organic EL device, the organic EL material being represented by Formula 1, below:Type: ApplicationFiled: November 19, 2013Publication date: May 22, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventor: Hiroaki ITOI
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Publication number: 20140134193Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.Type: ApplicationFiled: October 31, 2013Publication date: May 15, 2014Applicant: PFIZER INC.Inventors: Chakrapani SUBRAMANYAM, Frank Erich KOEHN, Kenneth John DIRICO, Alessandra S. EUSTAQUIO, Michael Eric GREEN, Haiyin HE, Min HE, Christopher John O'DONNELL, Sujiet PUTHENVEETIL, Anokha RATNAYAKE, Jesse Alexander TESKE, Hui Yu YANG
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Publication number: 20140121206Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.Type: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: GlaxoSmithKliine, LLCInventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
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Publication number: 20140121231Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof wherein X, M, Y, R1 and R2 are as defined herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: June 19, 2013Publication date: May 1, 2014Inventors: David Robert Bolin, Javier de Vicente Fidalgo, Johannes Hermann, Parcharee Tivitmahaisoon, Lin Yi, Mark Zak
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Publication number: 20140121196Abstract: A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.Type: ApplicationFiled: November 14, 2013Publication date: May 1, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
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Publication number: 20140117329Abstract: An amine-based compound and an organic light-emitting device including the amine-based compound are provided.Type: ApplicationFiled: August 5, 2013Publication date: May 1, 2014Inventors: Ji-Youn LEE, Yoon-Hyun KWAK, Bum-Woo PARK, Sun-Young LEE, Jong-Won CHOI, WHA-IL CHOI, So-Yeon KIM
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Patent number: 8709308Abstract: The chromene compound is represented by the following formula (I), wherein R3 at the 11-position is a sulfur-containing substituent selected from the group consisting of thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group, heteroarylthio group, sulfonyl group and sulfinyl group, R1 and R2 at the 6-position and the 7-position are a combination of an aryl group or a heteroaryl group and an electron donating group having a Hammett constant ?p of ?0.1 or less, or R1 and/or R2 is sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group.Type: GrantFiled: January 26, 2012Date of Patent: April 29, 2014Assignee: Tokuyama CorporationInventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Mitsuyoshi Sando, Shinobu Izumi
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Publication number: 20140113916Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: ApplicationFiled: June 15, 2012Publication date: April 24, 2014Applicant: GlaxoSmithKLine, LLCInventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
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Patent number: 8703949Abstract: The present invention provides processes for the preparation of N-alkyl morphinans without the isolation of nor-morphinan intermediates. In particular, the invention provides tandem hydrolysis/alkylation reactions for the synthesis of N-alkyl morphinans.Type: GrantFiled: August 3, 2011Date of Patent: April 22, 2014Assignee: Mallinckrodt LLCInventors: Subo Liao, Peter X. Wang, David W. Berberich, Douglas C. Miller
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Patent number: 8703448Abstract: The invention relates to the preparation of amino-cyclopamines by the enzymatic transamination of a corresponding keto-cyclopamines in the presence of a cofactor and an amino donor.Type: GrantFiled: July 1, 2011Date of Patent: April 22, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian C. Austad, Adilah Bahadoor, Jitendra D. Belani, Somarajannair Janardanannair, Charles W. Johannes, Gregg F. Keaney, Priscilla L. White, Sheldon L. Wallerstein
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Patent number: 8703165Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.Type: GrantFiled: November 30, 2010Date of Patent: April 22, 2014Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20140107139Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.Type: ApplicationFiled: June 7, 2012Publication date: April 17, 2014Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe Alvaro, Anne Decor, Dieter Hamprecht, Agostino Marasco
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Publication number: 20140107141Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.Type: ApplicationFiled: October 11, 2013Publication date: April 17, 2014Applicants: The General Hospital Corporation d/b/a Massachusetts General Hospital, The Broad Institute, Inc.Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michel Weiwer, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop
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Patent number: 8691120Abstract: A photochromic chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as its basic skeleton, an aryl group or a heteroaryl group at the 6-position carbon atom of the structure and an electron donor group having a Hammett constant ?p of not more than ?0.1 at the 7-position carbon atom.Type: GrantFiled: September 15, 2010Date of Patent: April 8, 2014Assignee: Tokuyama CorporationInventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Mitsuyoshi Sando, Kazuhiro Teranishi
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Publication number: 20140088080Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
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Patent number: 8680089Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: GrantFiled: January 17, 2011Date of Patent: March 25, 2014Assignee: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Publication number: 20140080803Abstract: Disclosed herein are modulators of TRPV3 of Formula (I) wherein p is 1, 2, 3, or 4, and G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: October 23, 2012Publication date: March 20, 2014Applicant: AbbVie Inc.Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Eric A. Voight
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Publication number: 20140081027Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
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Publication number: 20140073629Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: September 3, 2013Publication date: March 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Jehrod Burnett BRENNEMAN, John GINN, Michael D. LOWE, Christopher Ronald SARKO, Edward S. TASBER, Zhonghua ZHANG
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Patent number: 8669365Abstract: The invention provides novel derivatives of cyclopamine having the following formula:Type: GrantFiled: August 27, 2008Date of Patent: March 11, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, André B. Charette, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
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Publication number: 20140057927Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.Type: ApplicationFiled: August 27, 2013Publication date: February 27, 2014Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Cornelia Dorner-Ciossek, Ulrike Gross, Niklas Heine, Achim Sauer
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Publication number: 20140051577Abstract: The invention relates to substituted 5-(bicyclo[4.1.0]hept-3-en-2-yl)penta-2,4-dienes and 5-(bicyclo[4.1.0]hept-3-en-2-yl)pent-2-ene-4-ines of the formula (I) and salts thereof, where the radicals R1, R2, R3, R4, R5, [X—Y] and Q are each as defined in the description, to processes for preparation thereof and to the use thereof for enhancing stress tolerance in plants with respect to abiotic stress, and/or for increasing plant yield.Type: ApplicationFiled: March 28, 2012Publication date: February 20, 2014Inventors: Jens Frackenpohl, Thomas Müller, Ines Heinemann, Pascal Von Koskull-Döring, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Martin Jeffrey Hills
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Publication number: 20140051660Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui, Christopher Flores
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Publication number: 20140045813Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
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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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Publication number: 20140038936Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: May 7, 2013Publication date: February 6, 2014Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
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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: 20140031341Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.Type: ApplicationFiled: December 19, 2011Publication date: January 30, 2014Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENTInventors: Jerome Aubert, Martin Steinhoff
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Publication number: 20140031379Abstract: A camsylate salt of (1r,1?R,4R)-4-methoxy-5?-methyl-6?-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3?H-dispiro[cyclohexane-1,2?-inden-1?2?-imidazole]-4?-amine, pharmaceutical compositions containing the salt and therapeutic uses of the salt for treating A?-related pathologies such as Alzheimer's Disease, Down's syndrome, ?-amyloid angiopathy and conditions such as 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.Type: ApplicationFiled: June 13, 2013Publication date: January 30, 2014Applicant: ASTRAZENECA ABInventors: Martin Hans Bohlin, Craig Robert Stewart
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Patent number: 8637497Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: GrantFiled: July 18, 2011Date of Patent: January 28, 2014Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Patent number: 8633190Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.Type: GrantFiled: October 26, 2010Date of Patent: January 21, 2014Assignee: H. Lundbeck A/SInventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
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Patent number: 8633315Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.Type: GrantFiled: March 22, 2012Date of Patent: January 21, 2014Assignee: Amgen Inc.Inventors: Wenge Zhong, Stephen Hitchcock, Patel F. Vinod, Michael Croghan, Bryant Yang
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Publication number: 20140011827Abstract: The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: March 14, 2012Publication date: January 9, 2014Inventors: Ian M. Bell, Justin Belardi
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Publication number: 20140011808Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 17, 2013Publication date: January 9, 2014Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
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Publication number: 20140011777Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: September 9, 2013Publication date: January 9, 2014Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk
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Publication number: 20140005168Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: June 26, 2013Publication date: January 2, 2014Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Vickie H. Tsui, Xiaojing Wang