Ring Nitrogen In The Bicyclo Ring System Patents (Class 514/235.2)
-
Publication number: 20140045847Abstract: The present invention relates to a crystalline form of a pharmaceutically acceptable salt of a morpholino sulphonyl indole derivative, that is capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The present invention also relates to a process for the preparation of the crystalline form of said compound.Type: ApplicationFiled: April 19, 2012Publication date: February 13, 2014Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Suneel Manohar Babu Chennamsetty, Kishor Joshi, Yogesh Chinchwade, Yogesh Hulawale, Selvam Paramasivan, Meenakshi Sivakumar, Sivaramakrishnan Hariharan
-
Publication number: 20140045843Abstract: Provided herein are methods of treating, preventing and/or managing cancers, which comprise administering to a patient 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: Celgene CorporationInventors: Peter H. Schafer, Anita Gandhi
-
Publication number: 20140045825Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: Exelixis, Inc.Inventor: James William Leahy
-
Publication number: 20140045844Abstract: Provided herein are methods of using compounds and compositions for modulating leukocytic activity, including activity of B cells and/or T cells monocytes, macrophages, and other lymphoid or myeloid-derived cell types, in immune-related diseases or inflammatory diseases. Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: Celgene CorporationInventors: Peter H. Schafer, Rajesh Chopra, Anita Gandhi
-
Publication number: 20140038961Abstract: The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-oxType: ApplicationFiled: March 28, 2012Publication date: February 6, 2014Applicant: Actelion Pharmaceuticals Ltd.Inventors: Markus Gude, Christian Hubschwerlen, Philippe Panchaud
-
Publication number: 20140038962Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.Type: ApplicationFiled: September 20, 2013Publication date: February 6, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
-
Patent number: 8642595Abstract: This invention relates to novel annellated 4-(indazolyl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: GrantFiled: May 29, 2009Date of Patent: February 4, 2014Assignee: Bayer Intellectual Property GmbHInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
-
Publication number: 20140031336Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: April 19, 2012Publication date: January 30, 2014Applicant: Glaxosmithkline LLCInventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
-
Patent number: 8637681Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).Type: GrantFiled: March 31, 2011Date of Patent: January 28, 2014Assignee: Qilu Pharmaceutical Co., Ltd.Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Boyan Xu, Shousheng Yan, Zongru Guo, Minghui Zhang, Dong Lin, Zhantao Zhang, Haojie Zhou
-
Publication number: 20140024618Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: ApplicationFiled: September 23, 2013Publication date: January 23, 2014Applicant: LG LIFE SCIENCES LTD.Inventors: Soon Ha KIM, Hyoung Jin KIM, Sun Young KOO, Sung Bae LEE, Heui Sul PARK, Seung Hyun YOON, Seung Yup PAEK, Hyo Shin KWAK, Dong Ook SEO, Eok PARK
-
Patent number: 8633187Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: GrantFiled: March 5, 2012Date of Patent: January 21, 2014Assignee: GlaxoSmithKline LLCInventors: Steven David Knight, Stanley J. Schmidt
-
Publication number: 20140018364Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: September 18, 2013Publication date: January 16, 2014Applicant: Astrazeneca ABInventors: Kevin FOOTE, Johannes Wilhelmus, Maria NISSINK, Paul TURNER
-
Publication number: 20140018365Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 26, 2011Publication date: January 16, 2014Applicants: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCCHAFTEN E.V., LEAD DISCOVERY CENTER GMBHInventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
-
Publication number: 20140018354Abstract: The present invention provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR. The invention also provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR and modulators of the unfolded protein response.Type: ApplicationFiled: July 23, 2010Publication date: January 16, 2014Inventors: Nathaniel Moorman, Thomas Shenk
-
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
-
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
-
Patent number: 8623862Abstract: The present invention relates to compounds corresponding to formula (I): X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: GrantFiled: September 13, 2011Date of Patent: January 7, 2014Assignee: SanofiInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
-
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
-
Publication number: 20140005143Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.Type: ApplicationFiled: July 8, 2011Publication date: January 2, 2014Applicants: Daiichi Sankyo Company, Limited, Ube Industries, Ltd.Inventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
-
Patent number: 8618096Abstract: Methods and compositions for treating disease caused by increased iron levels are disclosed Fluoregenic compounds and methods of using the same are also described.Type: GrantFiled: July 21, 2009Date of Patent: December 31, 2013Assignee: The Regents of the University of CaliforniaInventors: Adam Renslo, Sumit Mahajan
-
Publication number: 20130345212Abstract: The present invention relates to compounds of the formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds as activators of AMPK.Type: ApplicationFiled: March 5, 2012Publication date: December 26, 2013Applicant: GLAXOSMITHKLINE LLCInventors: Alain Claude-Marie Daugan, Olivier Mirguet, Yann Lamotte
-
Publication number: 20130345200Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: August 7, 2013Publication date: December 26, 2013Applicant: GlaxoSmithKline LLCInventors: James Brackley, III, Joelle Lorraine Burgess, Seth Grant, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
-
Publication number: 20130338158Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification.Type: ApplicationFiled: July 19, 2013Publication date: December 19, 2013Applicant: Allergan, Inc.Inventors: Richard L. Beard, John E. Donello, Tien T. Duong, Xiaoxia Liu, Haiging Yuan
-
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.
-
Publication number: 20130331380Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: ApplicationFiled: February 21, 2013Publication date: December 12, 2013Applicant: LES LABORATOIRES SERVIERInventors: Vincent Lacoste, Pauline Lacoste, LES LABORATOIRES SERVIER
-
Publication number: 20130330377Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.Type: ApplicationFiled: July 18, 2011Publication date: December 12, 2013Applicant: Exelixis Inc.Inventor: Jo Ann Wilson
-
Patent number: 8604030Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.Type: GrantFiled: March 25, 2010Date of Patent: December 10, 2013Assignee: Kowa Company, Ltd.Inventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata
-
Patent number: 8604055Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.Type: GrantFiled: June 28, 2006Date of Patent: December 10, 2013Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dagar, Shanavas Alikunju
-
Patent number: 8604190Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.Type: GrantFiled: October 6, 2009Date of Patent: December 10, 2013Assignee: Janssen Pharmaceutica NVInventors: Micheal D. Gaul, Bao-Ping Zhao, Daniel A. Hutta
-
Publication number: 20130324518Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: July 26, 2013Publication date: December 5, 2013Applicant: Celgene CorporationInventors: Hon-Wah MAN, Roger Shen-Chu CHEN, Weihong ZHANG
-
Patent number: 8592416Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.Type: GrantFiled: May 19, 2010Date of Patent: November 26, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
-
Patent number: 8586620Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: May 6, 2011Date of Patent: November 19, 2013Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
-
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
-
Publication number: 20130303522Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: ApplicationFiled: July 22, 2013Publication date: November 14, 2013Applicant: LABORATORIOS SALVAT, S.A.Inventors: Juan Lorenzo CATENA RUIZ, Carme SERRA COMAS, Oscar REY PUIGGROS, Albert ANTOLIN HERNANDEZ, Esther MONLLEO MAS
-
Publication number: 20130303528Abstract: Compositions for the treatment of neurodegenerative diseases are disclosed. Methods of treating and monitoring progression of a neurodegenerative disease are disclosed. According to the present invention, a selective CB2 receptor modulator may be administered to a mammal for the treatment of a neurodegenerative disease.Type: ApplicationFiled: March 29, 2013Publication date: November 14, 2013Inventors: Paul L. Prather, John P. Crow
-
Patent number: 8580784Abstract: A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-dihydroquinoline compound.Type: GrantFiled: July 14, 2011Date of Patent: November 12, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
-
Publication number: 20130296295Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: March 15, 2013Publication date: November 7, 2013Inventor: ABBVIE INC.
-
Publication number: 20130296303Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: July 17, 2013Publication date: November 7, 2013Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
-
Publication number: 20130296320Abstract: Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, particularly, cancer. The present invention provides a compound represented by the following general formula (I) or a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are the same or different and each represent C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are the same or different and each represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.; R4 represents a hydrogen atom, —CO—R6, —N(R7)(R8) etc.Type: ApplicationFiled: January 6, 2012Publication date: November 7, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
-
Publication number: 20130289033Abstract: 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, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.Type: ApplicationFiled: December 13, 2011Publication date: October 31, 2013Inventors: Gerard Griffioen, Tom Van Dooren, Verónica Rojas De La Parra, Arnaud Marchand, Sara Alassia, Amuri Kilonda, Patrick Chaltin
-
Publication number: 20130289027Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).Type: ApplicationFiled: January 23, 2012Publication date: October 31, 2013Applicant: ViiV Healthcare UK LimitedInventors: Martha Alicia De La Rosa, Simon Haydar, Brian Alvin Johns, Emile Johann Velthuisen
-
Publication number: 20130281451Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.Type: ApplicationFiled: April 3, 2013Publication date: October 24, 2013Applicant: ANNJI PHARMACEUTICAL CO., LTD.Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
-
Publication number: 20130281450Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.Type: ApplicationFiled: March 12, 2013Publication date: October 24, 2013Inventors: John K. Pratt, Dachun Liu, Chang H. Park, George S. Sheppard, Lisa A. Hasvold, Le Wang
-
Publication number: 20130281432Abstract: Pyridone and pyrazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 31, 2011Publication date: October 24, 2013Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
-
Publication number: 20130281397Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter Ronald Young
-
Patent number: 8563551Abstract: A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 30, 2011Date of Patent: October 22, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
-
Publication number: 20130273005Abstract: This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.Type: ApplicationFiled: December 8, 2011Publication date: October 17, 2013Applicant: GILEAD SCIENCES, INC.Inventors: William E. Delaney, John O. Link, Hongmei Mo, David W. Oldach, Adrian S. Ray, William J. Watkins, Cheng Yong Yang, Weidong Zhong
-
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
-
Publication number: 20130274253Abstract: The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.Type: ApplicationFiled: December 22, 2011Publication date: October 17, 2013Applicant: SANOFIInventors: Maurice Brollo, Jean-Christophe Carry, Victor Certal, Eric Didier, Gilles Doerflinger, Youssef EL Ahmad, Bruno Filoche-Romme, Frank Halley, Karl Andreas Karlsson, Laurent Schio, Fabienne Thompson
-
Patent number: 8557812Abstract: The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.Type: GrantFiled: August 22, 2005Date of Patent: October 15, 2013Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Guoping Wang, Guozhi Tang, Renxiao Wang, Zaneta Nikolovska-Coleska, Dajun Yang, Liang Xu