Acyclic Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/116)
-
Publication number: 20130225569Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupusType: ApplicationFiled: July 29, 2011Publication date: August 29, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
-
Publication number: 20130210768Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. 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 metabotropic glutamate receptors are involved, such as schizophrenia.Type: ApplicationFiled: June 6, 2011Publication date: August 15, 2013Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
-
Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
-
Patent number: 8466163Abstract: The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.Type: GrantFiled: December 11, 2007Date of Patent: June 18, 2013Assignee: Bionomics LimitedInventors: Bernard Luke Flynn, Jason Hugh Chaplin, Dharam Paul, Damian Wojciech Grobelny, Brian Kelly
-
Publication number: 20130131055Abstract: This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-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: ApplicationFiled: November 15, 2010Publication date: May 23, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Martin Michels, Hans Briem, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch
-
Publication number: 20130109649Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 25, 2012Publication date: May 2, 2013Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
-
Patent number: 8431595Abstract: Furanopyridine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: GrantFiled: August 20, 2010Date of Patent: April 30, 2013Assignee: The University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
-
Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
-
Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
-
Publication number: 20130023415Abstract: Substituted pyridines of the formula (I) in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula (I) and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.Type: ApplicationFiled: March 21, 2011Publication date: January 24, 2013Applicant: BASF SEInventors: Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Hans Wolfgang Hoeffken, Thomas Mietzner
-
Publication number: 20130023557Abstract: The invention therefore relates to compounds of the formula I in which X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.Type: ApplicationFiled: June 25, 2012Publication date: January 24, 2013Applicant: SANOFIInventors: Dieter KADEREIT, Matthias SCHAEFER, Stephanie HACHTEL, Thomas HUEBSCHLE, Katrin HISS
-
Publication number: 20130023558Abstract: Carboxylic acid derivatives having an oxazolo[4,5-c]pyridine ring The invention therefore relates to compounds of the formula I in which X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.Type: ApplicationFiled: June 25, 2012Publication date: January 24, 2013Applicant: SANOFIInventors: Dieter KADEREIT, Matthias SCHAEFER, Stephanie HACHTEL, Thomas HUEBSCHLE, Katrin HISS
-
Publication number: 20120316195Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 16, 2010Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
-
Publication number: 20120309964Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.Type: ApplicationFiled: February 24, 2011Publication date: December 6, 2012Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
-
Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
-
Publication number: 20120302576Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
-
Publication number: 20120289497Abstract: 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: ApplicationFiled: January 17, 2011Publication date: November 15, 2012Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
-
Publication number: 20120289702Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.Type: ApplicationFiled: December 28, 2010Publication date: November 15, 2012Applicant: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
-
Publication number: 20120283260Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: July 24, 2012Publication date: November 8, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
-
Publication number: 20120258973Abstract: The invention relates to compound of the formula (I?) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: December 20, 2010Publication date: October 11, 2012Applicant: NOVARTIS AGInventors: Sangamesh Babiger, Dirk Behnke, Claudia Betschart, Vinod Chaudhari, Murali Chebrolu, Simona Cotesta, Samuel Hintermann, Arndt Meyer, Chetan Pandit
-
Publication number: 20120238599Abstract: The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.Type: ApplicationFiled: March 19, 2012Publication date: September 20, 2012Applicant: CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.Inventors: Gilnam Lee, Han Won Cho, Eun Jin Song, Hye Sun Jeon, Min Jeong Kim, Jeongbeob Seo, Albert Charles Gyorkos, Suk Young Cho
-
Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
-
Patent number: 8269008Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.Type: GrantFiled: December 2, 2008Date of Patent: September 18, 2012Assignee: FibroGen, Inc.Inventors: Michael P. Arend, Heng Cheng, Lee A. Flippin, Danny Ng, Eric D. Turtle, Min Wu
-
Publication number: 20120220571Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X is O or N(R3); and R1, R2, R3 and Y are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: August 16, 2010Publication date: August 30, 2012Inventors: John S. Wai, Dai-shi Su, Catherine M. Wiscount
-
Patent number: 8252793Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: GrantFiled: August 17, 2011Date of Patent: August 28, 2012Assignees: Alcon Research, Ltd., Astellas Pharma Inc.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
-
Publication number: 20120214824Abstract: The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: December 8, 2011Publication date: August 23, 2012Inventors: Bradley Tait, Christopher Borella, Robert Chambers, Matthew Cullen
-
Publication number: 20120214805Abstract: The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.Type: ApplicationFiled: October 28, 2010Publication date: August 23, 2012Inventors: Joel M. Harris, Andrew Stamford, William J. Greenlee, Santhosh Francis Neelamkavil
-
Publication number: 20120208838Abstract: A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: ApplicationFiled: October 22, 2010Publication date: August 16, 2012Inventors: Amjad Ali, Christopher Franklin, Ravi Nargund, Michael Man-Chu Lo, Lin Yan, Pei Huo
-
Publication number: 20120202845Abstract: A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: ApplicationFiled: September 20, 2010Publication date: August 9, 2012Inventors: Amjad Ali, Michael Man-Chu Lo, Lin Yan
-
Patent number: 8236958Abstract: Two new crystalline monohydrates and two new crystalline anhydrates of gaboxadol are disclosed together with methods for preparing them.Type: GrantFiled: July 12, 2007Date of Patent: August 7, 2012Assignee: H. Lundbeck A/SInventor: Vincent Brett Cooper
-
Patent number: 8193216Abstract: The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.Type: GrantFiled: August 16, 2011Date of Patent: June 5, 2012Assignee: H. Lundbeck A/SInventors: Daniel J. Kumke, Jerry A. Murry, Bryon L. Simmons, Feng Xu
-
Publication number: 20120136153Abstract: A compound having the formula in racemic form, enantiomerically enriched form or enantiomerically pure form, and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: July 5, 2011Publication date: May 31, 2012Inventors: DENNIS P. CURRAN, BOM DAVID, THOMAS G. BURKE
-
Publication number: 20120094983Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.Type: ApplicationFiled: March 15, 2011Publication date: April 19, 2012Inventors: James A. Johnson, Yoon Jeon, John Lloyd, Heather Finlay
-
Publication number: 20120058893Abstract: Ketosultams and diketopyridines of the formula (I) and use thereof as herbicides are described. In this formula (I), G, X, Y and Z are each radicals such as hydrogen and organic radicals such as alkyl. W represents organic radicals such as alkyl. A represents a heterocycle.Type: ApplicationFiled: August 31, 2011Publication date: March 8, 2012Applicant: BAYER CROPSCIENCE AGInventors: Stefan LEHR, Christian WALDRAFF, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER
-
Publication number: 20120046285Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: August 17, 2011Publication date: February 23, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
-
Patent number: 8119635Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: August 19, 2009Date of Patent: February 21, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
-
Publication number: 20120035409Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 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: ApplicationFiled: February 5, 2010Publication date: February 9, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Mario Lobell, Nicole Teusch, Shendong Yuan
-
Patent number: 8088923Abstract: The present invention provides a concise synthetic method for generating lactam-fused beta-lactones that feature, in some embodiments, a tertiary fused carbinol, quaternary carbons, and a reactive beta-lactone moiety available for further reactions. The present invention further provides compounds synthesized by this method as well as methods of using these compounds as inhibitors of the proteasome and fatty acid synthase.Type: GrantFiled: July 9, 2007Date of Patent: January 3, 2012Assignee: The Texas A&M University SystemInventors: Daniel Romo, Huda Henry-Riyad, Changsuk Lee, Henry Nguyen, Vikram C. Purohit, Seongho Oh
-
Publication number: 20110319394Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.Type: ApplicationFiled: June 22, 2011Publication date: December 29, 2011Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
-
Publication number: 20110311482Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: December 13, 2010Publication date: December 22, 2011Inventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
-
Publication number: 20110301190Abstract: The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.Type: ApplicationFiled: August 16, 2011Publication date: December 8, 2011Applicant: H. LUNDBECK A/SInventors: Daniel J. Kumke, Jerry A. Murry, Bryon L. Simmons, Feng Xu
-
Patent number: 8071593Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: May 8, 2008Date of Patent: December 6, 2011Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
-
Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
-
Publication number: 20110251396Abstract: Preferred embodiments of the present invention are related to novel therapeutic drugs and drug combinations, and associated methods, for treating and/or preventing complications in patients with diabetes, metabolic syndrome, and/or hypertension. More particularly, aspects of the present invention are related to the use of cicletanine as a monotherapy or in combination with other agents for treatment of disease. Cicletanine, as either a monotherapy or in combination with other drugs, may have the form of a non-racemic mixture of the negative (?) and positive (+) enantiomers of cicletanine, or as either the (?) or (+) enantiomer alone.Type: ApplicationFiled: January 17, 2011Publication date: October 13, 2011Inventors: Glenn Cornett, Jim Page
-
Publication number: 20110245505Abstract: A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro and R1, R2 are independently C1-C10-alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R3—O—N?O (III) wherein R3 is C1-C8-alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from ?45 to 40° C., to obtain an oxime compound (IV) where Z, Z1, R1 and R2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C1-C10-aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.Type: ApplicationFiled: December 7, 2009Publication date: October 6, 2011Applicant: BASF SEInventors: Michael Rack, Joachim Gebhardt, Frederik Menges, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
-
Publication number: 20110230497Abstract: The present invention is directed to biologically active amides which are ligands at the NPY Y5 receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from certain disorders which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, this invention also provides uses of a compound of the invention for the manufacture of a medicament for treating a subject suffering from certain disorders.Type: ApplicationFiled: November 2, 2009Publication date: September 22, 2011Applicant: H. Lundbeck A/SInventors: John Matthew Peterson, Chien-An Chen, Bin Chen, Lingyun Wu, Michael Lloyd Sabio
-
Patent number: 8022206Abstract: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.Type: GrantFiled: February 6, 2009Date of Patent: September 20, 2011Assignee: OSI Pharmaceuticals, LLCInventors: An-Hu Li, Arno G. Steinig, Andrew Kleinberg, Qinghua Weng, Mark J. Mulvihill, Jing Wang, Xin Chen, Ti Wang, Hanqing Dong, Meizhong Jin
-
Patent number: 8022057Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: November 7, 2008Date of Patent: September 20, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Toufike Kanouni, Michael B. Wallace
-
Patent number: 8022084Abstract: The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.Type: GrantFiled: January 26, 2006Date of Patent: September 20, 2011Assignee: H. Lundbeck A/SInventors: Daniel J. Kumke, Jerry A. Murry, Bryon L. Simmons, Feng Xu
-
Publication number: 20110224439Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.Type: ApplicationFiled: November 13, 2008Publication date: September 15, 2011Inventors: Frederik Menges, Joachim Gebhardt, Michael Rach, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schroeder