The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/143)
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Patent number: 11787804Abstract: The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.Type: GrantFiled: June 23, 2022Date of Patent: October 17, 2023Assignee: The Regents of the University of CaliforniaInventors: William E. Lowry, Michael E. Jung, Heather R. Christofk, Xiaoguang Liu, Aimee Flores
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Patent number: 10364221Abstract: A monomer, an organic layer composition, an organic layer, and a method of forming a pattern, the monomer being represented by the following Chemical Formula 1:Type: GrantFiled: June 8, 2016Date of Patent: July 30, 2019Assignee: SAMSUNG SDI CO., LTD.Inventors: Hyo Young Kwon, Sunhae Kang, Ran Namgung, Younhee Nam, Yumi Heo, Young Min Kim, Soohyoun Mun
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Patent number: 9572794Abstract: Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.Type: GrantFiled: August 6, 2015Date of Patent: February 21, 2017Assignee: Vanderbilt UniversityInventors: Heidi E. Hamm, Shaun R. Stauffer, Craig W. Lindsley, Wandong Wen, Summer E. Young, Matthew T. Duvernay, Kayla J. Temple
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Patent number: 9556166Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.Type: GrantFiled: May 10, 2012Date of Patent: January 31, 2017Assignee: Proteostasis Therapeutics, Inc.Inventors: Megan Foley, Bradley Tait, Matthew Cullen
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Patent number: 9079895Abstract: The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds.Type: GrantFiled: November 20, 2013Date of Patent: July 14, 2015Assignee: University of DundeeInventors: Jeremy Besnard, Andrew Lee Hopkins, Ian Gilbert, Gian Filippo Ruda, Keren Abecassis
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Publication number: 20150111886Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
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Publication number: 20150105384Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 9, 2014Publication date: April 16, 2015Applicant: Acetylon Pharmaceuticals, Inc.Inventors: Simon Stewart Jones, Min Yang, David Lee Tamang
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Publication number: 20150094304Abstract: 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 ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: December 11, 2014Publication date: April 2, 2015Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
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Publication number: 20150011550Abstract: Use of a synthetic compound selected from the group consisting of JKF-006, JKF-011 and JKF-027 in the preparation of a medicament for treating Alzheimer's disease.Type: ApplicationFiled: January 25, 2013Publication date: January 8, 2015Applicant: BEIJING JOEKAI BIOTECHNOLOGY LLCInventor: Weiwei Ma
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Patent number: 8916071Abstract: A chromene compound which has a sulfur-containing substituent represented by the following formula (2) at the 6-position and/or 7-position carbon atom of an indeno(2,1-f)naphtho(1,2-b)pyran structure and is excellent in photochromic properties and stability at a high temperature. In the formula (2), ring X is an aromatic hydrocarbon ring or aromatic heterocyclic ring, R3 and R4 are each independently an alkyl group, haloalkyl group, cycloalkyl group, alkoxy group, amino group, heterocyclic group containing a ring member nitrogen atom and bonded to the ring X bonded thereto via the nitrogen atom, halogen atom, aryloxy group or aryl group, and “a” is an integer of 0 to 4.Type: GrantFiled: September 21, 2012Date of Patent: December 23, 2014Assignee: Tokuyama CorporationInventors: Yasutomo Shimizu, Shinobu Izumi, Junji Takenaka, Junji Momoda
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Patent number: 8906911Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: March 29, 2013Date of Patent: December 9, 2014Assignee: AbbVie Inc.Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
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Patent number: 8906913Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.Type: GrantFiled: June 22, 2010Date of Patent: December 9, 2014Assignee: Panacea Biotec LimitedInventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Publication number: 20140357634Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Applicant: GRÜNENTHAL GMBHInventors: BERT NOLTE, WOLFGANG SCHRÖDER, KLAUS LINZ, WERNER ENGLBERGER, HANS SCHICK, HEINZ GRAUBAUM, BIRGIT ROLOFF, SIGRID OZEGOWSKI, JÓZSEF BÁLINT, HELMUT SONNENSCHEIN
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Publication number: 20140343050Abstract: Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.Type: ApplicationFiled: March 30, 2012Publication date: November 20, 2014Applicant: APTOEX TECHNOLOGIES, INC.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Tao Xin, Wanren Li, Jolanta Maria Wodzinska, Vrajlal S. Rabadia, Christopher John Feeney
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Patent number: 8853209Abstract: Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mdl-1 protein, such as leukemia and lymphoma, are disclosed.Type: GrantFiled: April 15, 2011Date of Patent: October 7, 2014Assignee: AbbVie Inc.Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
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Publication number: 20140256725Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.Type: ApplicationFiled: September 14, 2012Publication date: September 11, 2014Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Matthijs Poulie, Cornelis Marius Timmers, Saskia Vertaik
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Publication number: 20140235629Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: September 26, 2012Publication date: August 21, 2014Inventors: Michael D. Bartberger, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Duquette, John Eksterowicz, Brian M. Fox, Jiasheng Fu, Ana Gonzalez Buenrostro, Felix Gonzalez Lopez De Turiso, Darin J. Gustin, Julie A. Heath, Michael G. Johnson, Frank Kayser, David John Kopecky, Yihong Li, Zhihong Li, Zhihua Ma, Joel Micintosh, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yosup Rew, Philip M. Roveto, Michael J. Schmitt, Daqing Sun, Xiaodong Wang, Malgorzata Wanska, Christine Weathers, Xuelei Yan
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Publication number: 20140228359Abstract: The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.Type: ApplicationFiled: July 20, 2012Publication date: August 14, 2014Applicant: UNIVERSITE JOSEPH FOURIERInventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Louis Max Maurin, Nikolaevna Olga Burchak
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Patent number: 8796268Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 11, 2011Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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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: 8742100Abstract: The present invention generally relates to inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt), in particularly to compounds that inhibit Icmt activity and pharmaceutical compositions thereof. The invention also relates to methods of disease treatment using the same.Type: GrantFiled: July 30, 2010Date of Patent: June 3, 2014Assignee: National University of SingaporeInventors: Jo Lene Leow, Mei-Wang Casey, Patrick J. Casey, Mei Lin Go, Kumar Gorla Suresh
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Publication number: 20140148452Abstract: The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: University of DundeeInventors: Jeremy Besnard, Andrew Lee Hopkins, Ian Gilbert, Gian Filippo Ruda, Keren Abecassis
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Publication number: 20140128391Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.Type: ApplicationFiled: November 1, 2013Publication date: May 8, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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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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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: 20140073584Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.Type: ApplicationFiled: September 30, 2013Publication date: March 13, 2014Applicant: SIGNALRX PHARMACEUTICALS, INC.Inventors: Guillermo A. Morales, Kevin Weber, Jessica Newblom, Joseph R. Garlich
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Publication number: 20140057906Abstract: 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 ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: October 21, 2013Publication date: February 27, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Peter D.J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Publication number: 20140057909Abstract: The present invention relates to an indole derivative, The indole derivative according to the present invention effectively inhibits the activity of diacylglycerol acyltransferase (DGAT) which induces metabolic diseases, such as obesity, diabetes, hyperlipidemia, or fatty liver and the like in lipid metabolism, thereby effectively regulating lipid metabolism and energy metabolism, and thus can be useful in pharmaceutical compositions for preventing or treating metabolic disease.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Hyun Sun LEE, Mun-Ock KIM, Yongseok CHOI, Kyeong Lee, Jeong-Jun PARK, Jee-Hee SEO, Hwayoung JUNG, Sungchan CHO
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Publication number: 20140051683Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.Type: ApplicationFiled: April 23, 2013Publication date: February 20, 2014Applicant: AbbVie Inc.Inventors: Xilu WANG, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
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Publication number: 20140051751Abstract: Environmentally-friendly alternatives to organometallic antifoulants that are efficacious at preventing biofouling by organisms such as the zebra mussel. Preferred antifoulant compositions utilize compounds having a Lipophilic-Amide-Spacer-ElectroNegative (“LASEN”) structural motif, such as capsaicin, and compounds having a TetraHydroCannibinoid (“THC”) structural motif. The antifoulant compositions are non-toxic, and effective.Type: ApplicationFiled: October 25, 2013Publication date: February 20, 2014Applicants: The Board of Regents of the University of Texas System, University of North Texas Health Science Center at Fort WorthInventors: John A. Schetz, Robert F. McMahon
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Publication number: 20140011807Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.Type: ApplicationFiled: March 15, 2012Publication date: January 9, 2014Applicants: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD., MITSUBISHI TANABE PHARMA CORPORATIONInventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie
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Publication number: 20140005386Abstract: Novel p53-Mdm2 antogonists that conform to Formula I or to Formula II: where the prescribed substituent groups are defined, are useful in treating or preventing cancer. In particular, the compounds and their pharmaceutical compositions are useful for treating relapsed/refractory acute myeloid and lymphoid leukemia and refractory chronic lymphocytic leukemia/small cell lymphocytic lymphomas.Type: ApplicationFiled: September 8, 2011Publication date: January 2, 2014Inventor: Alexander Doemling
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Publication number: 20140004174Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: May 20, 2013Publication date: January 2, 2014Applicant: Pharmacyclics, Inc.Inventors: Erik VERNER, Sriram BALASUBRAMANIAN, Joseph J. BUGGY
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Publication number: 20130336919Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: January 4, 2013Publication date: December 19, 2013Applicant: ARDELYX, INC.Inventor: Ardelyx, Inc.
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Publication number: 20130303538Abstract: The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.Type: ApplicationFiled: January 20, 2012Publication date: November 14, 2013Inventors: Joachim Nozulak, Dieter Oser
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Publication number: 20130303539Abstract: Compounds, compositions and methods useful for treating ocular diseases are provided. In particular, antagonists of TRPV4, their synthesis, pharmaceutical compositions thereof and methods of treating ocular diseases such as glaucoma, are disclosed.Type: ApplicationFiled: March 15, 2013Publication date: November 14, 2013Inventors: David Krizaj, Glenn D. Prestwich, Peter Barabas, Yong Xu, Daniel Ryskamp
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Patent number: 8575230Abstract: Environmentally-friendly alternatives to organometallic antifoulants that are efficacious at preventing biofouling by organisms such as the zebra mussel. Preferred antifoulant compositions utilize compounds having a Lipophilic-Amide-Spacer-ElectroNegative (“LASEN”) structural motif, such as capsaicin, and compounds having a TetraHydroCannibinoid (“THC”) structural motif. The antifoulant compositions are non-toxic, and effective.Type: GrantFiled: April 16, 2008Date of Patent: November 5, 2013Assignees: University of North Texas Health Science Center at Fort Worth, The Board of Regents of the University of Texas SystemInventors: John A. Schetz, Robert F. McMahon
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Publication number: 20130289270Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid.Type: ApplicationFiled: January 6, 2012Publication date: October 31, 2013Applicant: The Regents of the University of CaliforniaInventors: Neil K. Garg, Stephen D. Ramgren, Amanda L. Silberstein, Kyle W. Quasdorf
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Publication number: 20130274260Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.Type: ApplicationFiled: December 13, 2011Publication date: October 17, 2013Inventors: Gerard Griffioen, Tom Van Dooren, Verónica Rojas De La Parra, Sara Allasia, Arnaud Marchand, Amuri Kilonda, Patrick Chaltin
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Patent number: 8557807Abstract: The invention, relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as P1-3 kinase.Type: GrantFiled: January 23, 2009Date of Patent: October 15, 2013Assignee: Signal Rx Pharmaceuticals, Inc.Inventors: Guillermo A. Morales, Kevin T. Weber, Jessica M. Newblom, Xiaodong Peng, Jingdong Su, Joseph R. Garlich
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Publication number: 20130252955Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: ApplicationFiled: May 16, 2013Publication date: September 26, 2013Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Publication number: 20130196960Abstract: The present disclosure relates to compounds useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders either alone or in combination therapy.Type: ApplicationFiled: February 9, 2011Publication date: August 1, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
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Publication number: 20130178471Abstract: 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 ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: February 28, 2013Publication date: July 11, 2013Applicant: Vextex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130178453Abstract: The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).Type: ApplicationFiled: February 9, 2011Publication date: July 11, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara Mermerían, Wayne C. Schairer, Galen John Carey
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Publication number: 20130158021Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.Type: ApplicationFiled: October 26, 2012Publication date: June 20, 2013Applicant: Massachusetts Institute of TechnologyInventor: Massachusetts Institute of Technology
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Publication number: 20130131060Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.Type: ApplicationFiled: December 10, 2010Publication date: May 23, 2013Applicant: Johannes Gutenberg-Universität MainzInventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
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Publication number: 20130102776Abstract: An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6 alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6 alkyl group and the like; R4 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6 alkyl group and the like; R8 represents hydrogen atom, a C1-6 alkyl group and the like; A represents —O—, —S—, or —CH2—; D represents —C? or —N?; X represents methylene group, —O—, or —CO—; Q represents —N? or —C(R8)?; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.Type: ApplicationFiled: April 28, 2011Publication date: April 25, 2013Applicants: RIKEN, THE UNIVERSITY OF TOKYOInventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Nae Saito, Hirofumi Nakano, Masanao Abe, Akiko Tanaka, Teruki Honma, Shigeyuki Yokoyama, Keiko Tsuganezawa, Hitomi Yuki
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Patent number: 8415349Abstract: The invention provides derivatives of azabicyclo alkane having formula (ID), and the method for making them, wherein each substitute in formula (ID) is same as defined in the description.Type: GrantFiled: September 14, 2012Date of Patent: April 9, 2013Assignee: Jiangsu Hansoh Pharmaceuticals Co., Ltd.Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
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Publication number: 20130081213Abstract: The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline.Type: ApplicationFiled: March 2, 2011Publication date: April 4, 2013Inventor: Aziz Fadli
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Publication number: 20130072677Abstract: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria.Type: ApplicationFiled: April 20, 2011Publication date: March 21, 2013Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTDInventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi