Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 544/250)
-
Patent number: 7982035Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: July 10, 2008Date of Patent: July 19, 2011Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
-
Publication number: 20110165118Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
-
Publication number: 20110152298Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below where the substituents have the meanings defined in claim (I) and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: June 23, 2011Applicant: SHIRE LLCInventors: Bernard T. Golding, Richard Franklin, Angus Macleod, Peter Cicala
-
Publication number: 20110152259Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).Type: ApplicationFiled: February 24, 2011Publication date: June 23, 2011Inventors: Anandan Palani, Jing Su, Dong Xiao, Xianhai Huang, Ashwin U. Rao, Xiao Chen, Haiqun Tang, Jun Qin, Ying R. Huang, Robert G. Aslanian, Brain A. McKittrick, Syliva J. Degrado
-
Patent number: 7964608Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis.Type: GrantFiled: January 23, 2009Date of Patent: June 21, 2011Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew Kostura, Mustafa Guzel
-
Publication number: 20110142796Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: ApplicationFiled: December 18, 2008Publication date: June 16, 2011Applicant: Amgen IncInventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. Mcgee, Rajiv Sharma, Xiaodong Wang, Dustin L. Mcminn, Jeffrey T. Mihalic, Jeffrey Deignan
-
Publication number: 20110144138Abstract: Pyrimido isoquinoline derivatives represented by formula (I): wherein: R1, R2, R3, R4, R7, R8, R9, R10, and are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
-
Patent number: 7960400Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: GrantFiled: August 27, 2007Date of Patent: June 14, 2011Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
-
Publication number: 20110136813Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: ApplicationFiled: May 27, 2009Publication date: June 9, 2011Inventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
-
Publication number: 20110130414Abstract: The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.Type: ApplicationFiled: September 8, 2010Publication date: June 2, 2011Applicant: TORRENT PHARMACEUTICALS LIMITEDInventors: Sanjay Srivastava, Laxmikant Chhipa, Ramesh Chandra Gupta, Shailesh Deshpande, Anita Chaudhari, Anookh Mohanan, Chaitanya Dutt, Vijay Chauthaiwale, Murali Badanthadka, Prashant G. Jamadarkhana
-
Publication number: 20110118245Abstract: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.Type: ApplicationFiled: March 17, 2009Publication date: May 19, 2011Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
-
Patent number: 7943615Abstract: The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-4 enzyme is involved.Type: GrantFiled: December 8, 2006Date of Patent: May 17, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Scott D. Edmondson, Anthony Mastracchio
-
Patent number: 7932259Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.Type: GrantFiled: April 21, 2008Date of Patent: April 26, 2011Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Dai Nozawa, Mikako Yamaguchi, Tomoko Tamita, Ludo E. J. Kennis, Marcel F. L. De Bruyn, Jean-Pierre A. M. Bongartz, Frans M. A. Van Den Keybus, Yves E. M. Van Roosbroeck, Marcel G. M. Luyckx, Robert J. M. Hendrickx
-
Publication number: 20110086851Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: April 14, 2011Inventors: Bernard Golding, Richard Franklin
-
Publication number: 20110083984Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 5, 2007Publication date: April 14, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Martin Hentemann, Jill Wood, William Scott, Martin Michels, Ann-Marie Campbell, Ann-Marie Bullion, Bruce R. Rowley, Aniko Redman
-
PHARMACEUTICAL FORMULATIONS COMPRISING SALTS OF A PROTEIN KINASE INHIBITOR AND METHODS OF USING SAME
Publication number: 20110086112Abstract: The present invention relates to pharmaceutical formulations comprising the protein kinase inhibitor, MP470, and methods of using same in treating conditions involving undesirable cell proliferation, such as cancer.Type: ApplicationFiled: October 18, 2010Publication date: April 14, 2011Applicant: SUPERGEN, INC.Inventors: David J. Bearss, Rajashree Joshi-Hangal, Xiao-Hui Liu, Pasit Phiasivongsa, Sanjeev G. Redkar, Hariprasad Vankayalapati -
Publication number: 20110077257Abstract: The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I): wherein p, n, A, B, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.Type: ApplicationFiled: September 3, 2010Publication date: March 31, 2011Applicant: SANOFI-AVENTISInventors: Raymond Walter KOSLEY, JR., Rosy SHER
-
Publication number: 20110071170Abstract: A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1).Type: ApplicationFiled: October 29, 2010Publication date: March 24, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hitoshi Ohki, Tooru Okayama, Masahiro Ikeda, Masahiro Ota, Yoshihiro Shibata, Toshiyuki Nakanishi, Yasusi Ueda, Nobuyuki Suzuki, Shinji Matuura
-
Publication number: 20110071172Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim (I): and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin
-
2H- PYRIMIDO [2, 1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS
Publication number: 20110071171Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin -
Publication number: 20110071136Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.Type: ApplicationFiled: September 16, 2010Publication date: March 24, 2011Applicant: CYLENE PHARMACEUTICALS, INCInventors: Mustapha HADDACH, Fabrice PIERRE
-
Publication number: 20110071174Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Inventors: Bernard Golding, Richard Franklin
-
Publication number: 20110071173Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Inventors: Bernard Golding, Richard Franklin, Angus Macleod
-
Patent number: 7910597Abstract: This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: GrantFiled: November 28, 2007Date of Patent: March 22, 2011Assignee: Shire LLCInventors: Richard Franklin, Bernard T. Golding
-
Publication number: 20110065690Abstract: The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Applicants: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Jolanta Grembecka, Tomasz Cierpicki, Jay Hess
-
Publication number: 20110065712Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.Type: ApplicationFiled: September 16, 2010Publication date: March 17, 2011Applicant: CYLENE PHARMACEUTICALS , INC.Inventors: Mustapha HADDACH, Fabrice Pierre
-
Publication number: 20110059997Abstract: The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors. In general formulas 1 and 2 R1 represents hydrogen or C1-C3 alkyl; R2 represents C1-C3 alkyl; R3 represents hydrogen, one or more optionally identical halogens, C1-C3 alkyl or hydroxyl optionally substituted with C1-C3 alkyl; n represents the whole numbers 1, 2 or 3.Type: ApplicationFiled: January 23, 2009Publication date: March 10, 2011Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Nikolay Filippovich Savchuk
-
Publication number: 20110054170Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: ApplicationFiled: August 30, 2010Publication date: March 3, 2011Applicant: FLORIDA STATE UNIVERSITY RESEARCH FOUNDATIONInventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
-
Publication number: 20110046374Abstract: The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such quinazolines.Type: ApplicationFiled: August 25, 2010Publication date: February 24, 2011Applicant: NOVALED AGInventors: Josef Salbeck, Manfred Kussler, Andrea Lux
-
Publication number: 20110021511Abstract: The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.Type: ApplicationFiled: December 21, 2007Publication date: January 27, 2011Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBHInventors: Claudia Reichelt, Alexander Schulze, Mohammed Daghish, Friedrich-Alexander Ludwig, Jochen Heinicke, Konrad Herrmann, Maj Schuster, Sven Letschert, Kenneth Mugridge, Joseph DeAngelo
-
Publication number: 20110021493Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.Type: ApplicationFiled: September 2, 2008Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Hartmut Schirok, Ying Li-Sommer, Michael Brands, Mario Lobell, Adrian Tersteegen, Herbert Himmel, Karl-Heinz Schlemmer, Dieter Lang, Kirsten Petersen, Matthias Renz, Dominik Mumberg, Jens Hoffman, Gerhard Siemeister, Ulf Bömer
-
Publication number: 20110015214Abstract: The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutically active agent and as pharmaceutical compositions for prophylaxis and/or treatment of proliferative diseases such as cancer.Type: ApplicationFiled: February 19, 2008Publication date: January 20, 2011Inventors: Pèter Bánhegyi, Kéri György, Lászlõ Örfi, Zsolt Szekélyhidi, Frigyes Wáczek
-
Publication number: 20110015201Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.Type: ApplicationFiled: February 12, 2009Publication date: January 20, 2011Inventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
-
Publication number: 20110009394Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: January 7, 2009Publication date: January 13, 2011Applicant: Glaxo Group LimitedInventors: Pamela Brown, Steven Dabbs, Alan Joseph Hennessy
-
Publication number: 20110003786Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: ApplicationFiled: July 2, 2010Publication date: January 6, 2011Inventors: Robin Alec FAIRHURST, Marc GERSPACHER, Robert MAH
-
Publication number: 20100324029Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: ApplicationFiled: February 5, 2008Publication date: December 23, 2010Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
-
Patent number: 7855206Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 9, 2007Date of Patent: December 21, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Hong Dong
-
Patent number: 7855214Abstract: The present invention relates to compounds useful as inhibitors of Tec family protein kinases. These compounds have the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, G, Cy1, and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: January 26, 2005Date of Patent: December 21, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Sanjay Patel, David Kay, Ronald Knegtel, Oliver Philps
-
Publication number: 20100311966Abstract: An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.Type: ApplicationFiled: December 26, 2008Publication date: December 9, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
-
Publication number: 20100305318Abstract: The present invention relates to a process for preparation of Anagrelide Hydrochloride Monohydrate.Type: ApplicationFiled: December 18, 2008Publication date: December 2, 2010Applicant: WATSON PHARMA PRIVATE LIMITEDInventors: Manjunath Narayan Bhanu, Samir Naik, Sadanand Maurya, Kishor Mahajan
-
Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
-
Publication number: 20100298297Abstract: This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.Type: ApplicationFiled: March 20, 2007Publication date: November 25, 2010Applicant: BAYER HEALTHCARE AGInventors: Chengzhi Zhang, Kanwar Sidhu, Mario Lobell, Gaeten Ladouceur, Qian Zhao, Zheng Liu, Kristen Allegue, Chetan Darne, Jason Newcom
-
Publication number: 20100292256Abstract: The invention relates to substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions comprising the said compounds as active ingredients, and to novel medicaments and method for treatment and prophylaxis of various CNS diseases. 2-Alkylamino-3-arylsulfonylcycloalkyl[e]pyrazolo[1,5-a]pyrimidines of general formula 1 and 2-alkylamino-3-arylsulfonylcycloalkyl[d]pyrazolo[1,5-a]pyrimidines of general formula 2, wherein: R1 is hydrogen or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is hydrogen, one or more optionally identical halogen atoms, C1-C3 alkyl or hydroxyl group optionally substituted with C1-C3 alkyl; n is the whole numbers 1, 2 or 3.Type: ApplicationFiled: January 23, 2009Publication date: November 18, 2010Inventor: Andrey Alexandrovich IVASHCHENKO
-
Publication number: 20100280026Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: February 26, 2010Publication date: November 4, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
-
Publication number: 20100267749Abstract: The invention relates to the novel 4,5,6-trisubstituted furo[2,3-d]pyrimidine derivatives of formula (I), to methods for their production, their use in the treatment and/or prophylaxis of diseases and their use in the production of drugs for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: November 3, 2008Publication date: October 21, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
-
Publication number: 20100261714Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: April 8, 2010Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Claudio STURINO, Patrick DEROY, Martin DUPLESSIS, Paul J. EDWARDS, Anne-Marie FAUCHER, Teddy HALMOS, Clint JAMES, Jean-Eric LACOSTE, Eric MALENFANT, Joannie MINVILLE, Louis MORENCY, Sebastien MORIN, Martin TREMBLAY, Christiane YOAKIM
-
Patent number: 7807687Abstract: The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such quinazolines.Type: GrantFiled: March 12, 2008Date of Patent: October 5, 2010Assignee: Novaled AGInventors: Josef Salbeck, Manfred Kussler, Andrea Lux
-
Publication number: 20100249102Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: April 6, 2010Publication date: September 30, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur Taveras
-
Publication number: 20100239496Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: March 23, 2010Publication date: September 23, 2010Applicant: Siemens Medical Solutions USA, Inc.Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharia, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
-
Patent number: 7799775Abstract: This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.Type: GrantFiled: February 25, 2005Date of Patent: September 21, 2010Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Michitaka Sato, Teruaki Matsui, Akira Asagarasu, Hiroyuki Hayashi, Sei-ichi Araki, Satoru Tamaoki, Nobuyuki Takahashi, Yukinao Yamauchi, Yoshiko Yamamoto, Norio Yamamoto, Chisato Ogawa