Polycyclo Ring System Having The Asymmetrical Triazine Ring As One Of The Cyclos Patents (Class 544/183)
-
Publication number: 20110183983Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.Type: ApplicationFiled: August 28, 2009Publication date: July 28, 2011Applicant: NEOPHARM CO., LTD.Inventors: Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
-
Publication number: 20110183972Abstract: The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer.Type: ApplicationFiled: February 10, 2009Publication date: July 28, 2011Applicant: SHENYANG PHARMACEUTICAL UNIVERSITYInventors: Linxiang Zhao, Jinling Lv, Rui Wang, Dan Liu, Yongkui Jing
-
Patent number: 7982033Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.Type: GrantFiled: November 2, 2007Date of Patent: July 19, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Ping Chen
-
Publication number: 20110165183Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).Type: ApplicationFiled: July 31, 2009Publication date: July 7, 2011Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar
-
Publication number: 20110160207Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
-
Publication number: 20110152243Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 21, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Neil Wishart, Theresa Dunstan, Jeremy J. Edmunds, Anna M. Ericsson, Catherine R. Ferenz, Adrian D. Hobson, David C. Ihle, Kent D. Stewart, Lei Wang, Lu Wang
-
Publication number: 20110124623Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.Type: ApplicationFiled: January 28, 2011Publication date: May 26, 2011Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
-
Publication number: 20110112083Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.Type: ApplicationFiled: June 5, 2009Publication date: May 12, 2011Applicant: LEGOCHEM BIOSCIENCE LTD.Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
-
Publication number: 20110098467Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: ApplicationFiled: December 31, 2010Publication date: April 28, 2011Inventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
-
Patent number: 7932383Abstract: Crystalline form, Form N-1, of [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising the Form N-1 of Compound I as well as a method of using the Form N-1 of Compound I in the treatment of cancer and other proliferative diseases.Type: GrantFiled: June 8, 2009Date of Patent: April 26, 2011Assignee: Bristol-Myers Squibb CompanyInventor: John E. Thornton
-
Patent number: 7919528Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: May 30, 2003Date of Patent: April 5, 2011Assignee: GlaxoSmithKline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Siegfried B. Christensen, IV, Joseph M. Karpinski, Jinhwa Lee, Domingos J. Silva
-
Publication number: 20110071288Abstract: The invention relates to 2,4-dibromoropyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing the intermediate.Type: ApplicationFiled: January 2, 2008Publication date: March 24, 2011Applicant: Bristol-Myers Squibb CompanyInventor: Upender Velaparthi
-
Publication number: 20110065918Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: Ajinomoto Co., Inc.Inventors: Shingo MAKINO, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
-
Publication number: 20110065709Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D?, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: March 19, 2009Publication date: March 17, 2011Applicant: Amgen Inc.Inventors: Ryan White, Jason Human
-
Publication number: 20110039838Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: ApplicationFiled: October 25, 2010Publication date: February 17, 2011Inventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
-
Publication number: 20110028479Abstract: The present application relates to new, substituted pyrrolo[2,1-f][1,2,4]triazine derivatives of the formula (I) as prostacyclin (PGI2) IP receptor activators for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: October 16, 2008Publication date: February 3, 2011Inventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
-
Patent number: 7879855Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.Type: GrantFiled: March 26, 2009Date of Patent: February 1, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
-
Publication number: 20110021518Abstract: 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: December 1, 2006Publication date: January 27, 2011Applicant: BAYER HEALTHCARE LLC.Inventors: Steven Magnuson, Julie Dixon, Barton Phillips, Uday Khire, Lei Wang, Zhonghua Zhang, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Philip Wickens, Alan Olague
-
Patent number: 7875612Abstract: A cell population expressing folate receptors is selectively targeted with a non-peptide folic acid analogue. The non-peptide folic acid analogue is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.Type: GrantFiled: April 24, 2002Date of Patent: January 25, 2011Assignees: Purdue Research Foundation, Endocyte, Inc.Inventors: Mark A. Green, Chun-Yen Ke, Christopher P. Leamon
-
Publication number: 20110009413Abstract: Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ?NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflType: ApplicationFiled: January 16, 2009Publication date: January 13, 2011Applicant: UNIVERSITY OF GREENWICHInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
-
Patent number: 7868000Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R1, R2, R3, R4, R6, R7 and R7a are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 12, 2006Date of Patent: January 11, 2011Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, William J. Greenlee, Xiaoxiang Liu, Mihirbaran Mandal, Johannes H. Voigt, Corey O. Strickland
-
Patent number: 7868017Abstract: The present invention relates to a 9-azabicyclo[3.3.1]nonane derivative of formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 9-azabicyclo[3.3.1]nonane derivatives and to their use in therapy.Type: GrantFiled: September 29, 2006Date of Patent: January 11, 2011Assignee: N.V. OrganonInventors: Susan Elizabeth Napier, Matilda Jane Bingham, Margaret Jean Huggett, Mark Huggett, Yasuko Kiyoi, Olaf Nimz
-
Publication number: 20100330069Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: ApplicationFiled: January 8, 2010Publication date: December 30, 2010Applicant: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
-
Patent number: 7855288Abstract: A compound of formula (I): wherein the substituents are as defined in the specification as inhibitor of C-Jun N terminal Kinases (JNK) and P-38 Kinases.Type: GrantFiled: October 25, 2005Date of Patent: December 21, 2010Assignee: Novartis AGInventor: Qing Dong
-
Patent number: 7846925Abstract: The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.Type: GrantFiled: July 10, 2003Date of Patent: December 7, 2010Assignee: Merck Serono SAInventors: Thomas Rueckle, Xuliang Jiang, Pascale Gaillard, Dennis Church, Tania Grippi Vallotton
-
Patent number: 7846931Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: September 24, 2008Date of Patent: December 7, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
-
Patent number: 7838672Abstract: The use of fused ring-1,2,4-benzotriazine derivatives as herbicides or plant growth regulators for the control of undesired plants or vegetation, compounds and compositions thereof, and processes for their preparation. The invention relates to the use of a compound of the formula (I) or a salt thereof: wherein A-W, X, Y, Z, R1, R2, R3 and R4 are defined in the description, as herbicides or plant growth regulators for the control of undesired plants or vegetation, to compounds and compositions thereof, and to processes for their preparation.Type: GrantFiled: July 17, 2004Date of Patent: November 23, 2010Assignee: Bayer CropScience GmbHInventors: Arnim Kohn, Wolfgang Giencke, Hendrick Helmke, Kenneth Garcia Marques, Thomas Auler, Martin Hills, Gyorgy Hajos, Zsuzsanna Riedl, Dieter Feucht
-
Patent number: 7834178Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein.Type: GrantFiled: February 28, 2007Date of Patent: November 16, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Jun Li, Jeffrey A. Robl, Lawrence J. Kennedy
-
Publication number: 20100273800Abstract: 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 22, 2008Publication date: October 28, 2010Inventors: Steven Magnuson, Philip Wickens, Zhonghua Zhang, Ning Qi, Xin Ma
-
Patent number: 7820814Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: March 6, 2009Date of Patent: October 26, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa, Louis Lombardo, Jeffrey Robl
-
Publication number: 20100267671Abstract: The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: ApplicationFiled: February 9, 2010Publication date: October 21, 2010Inventors: Jay Jie-Qiang Wu, Ling Wang
-
Patent number: 7816521Abstract: The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation.Type: GrantFiled: March 1, 2005Date of Patent: October 19, 2010Assignee: Auckland Uniservices LimitedInventors: William Alexander Denny, Michael Patrick Hay, Kevin Owen Hicks, Frederik Pruijn, William Robert Wilson, Karin Pchalek
-
Publication number: 20100240646Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: ApplicationFiled: June 3, 2010Publication date: September 23, 2010Inventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
-
Publication number: 20100216765Abstract: Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: April 6, 2010Publication date: August 26, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, David J. Hosfield, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
-
Patent number: 7759343Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: GrantFiled: October 28, 2008Date of Patent: July 20, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
-
Publication number: 20100179125Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: September 2, 2009Publication date: July 15, 2010Applicant: Bayer HealthCare LLCInventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
-
Publication number: 20100137318Abstract: A compound of a formula (I): wherein R1 represents a C3-10 branched alkyl group which may be substituted; R2 represents a hydrogen atom or a C1-4 alkyl group which may be substituted; R3 represents a C1-4 alkyl group which may be substituted or a halogen atom; R4 represents a C1-4 alkyl group which may be substituted; and ring 1 represents a cyclic group which has planarity and may have a substituent group, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a medicinal component having CRF antagonistic activity for the prevention and/or treatment of a neuropsychiatric disease, a peripheral organ disease and the like.Type: ApplicationFiled: April 25, 2008Publication date: June 3, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Tetsuji Saito, Tetsuo Obitsu, Yoshifumi Kagamiishi
-
Publication number: 20100137319Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: ApplicationFiled: February 5, 2010Publication date: June 3, 2010Inventors: Harold Mastalerz, Dolatral M. Vyas, George L. Trainor, Ashvinikumar V. Gavai
-
Publication number: 20100130498Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.Type: ApplicationFiled: March 31, 2008Publication date: May 27, 2010Applicant: Deutshes Institut Fur Ernahrungsforschung Potsdam- RehbruckeInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
-
Patent number: 7713972Abstract: The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotriazinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl group, R2 is methyl group; R3 is a hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; substituted or unsubstituted C1-C6 alkyl group; substituted or unsubstituted C2-C6 alkenyl group; saturated or unsaturated heterocycloalkyl group which is substituted or unsubstituted; a group: —NR5R6, —C(O)R7, —SO2R7, —OR8, —NR8COR7, —NR8S02R7; A is CR4; and B is CH.Type: GrantFiled: June 11, 2004Date of Patent: May 11, 2010Assignee: Asubio Pharma Co., Ltd.Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
-
Patent number: 7713973Abstract: Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: GrantFiled: October 14, 2005Date of Patent: May 11, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, David J. Hosfield, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
-
Patent number: 7713966Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: GrantFiled: November 20, 2007Date of Patent: May 11, 2010Assignee: Alantos Pharmaceuticals Holding, Inc.Inventors: Christian Gege, Matthias Schneider, Carine Chevrier, Hongbo Deng, Irving Sucholeiki, Brian M. Gallagher, Jr., Michael Bosies, Christoph Steeneck, Xinyuan Wu, Matthias Hochgürtel, Bert Nolte, Arthur Taveras
-
Publication number: 20100081662Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.Type: ApplicationFiled: November 2, 2007Publication date: April 1, 2010Inventors: Brian E. Fink, Ping Chen
-
Publication number: 20100081610Abstract: The present invention relates to ?-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.Type: ApplicationFiled: August 21, 2007Publication date: April 1, 2010Inventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranaheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Srivastava
-
Publication number: 20100075958Abstract: This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.Type: ApplicationFiled: July 20, 2009Publication date: March 25, 2010Applicant: Bayer Pharmaceuticals CorporationInventors: Julie A. Dixon, Catherine Brennan, Karl Miranda, Brent Chandler, Barton Phillips, Jianmei Fan, Michael Brands, Andrea McClure, Benjamin Jones, Wenlang Fu, Donald Bierer, Steven Magnuson, Harold C.E. Kluender
-
Publication number: 20100063038Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 1, 2006Publication date: March 11, 2010Inventors: Julie Dixon, Barton Phillips, Furahi Achebe, Harold Kluender, Jason Newcom, Kyle Parcella, Stephen J. O'Connor, Steven Magnuson, Zhenqui Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler
-
Publication number: 20100056781Abstract: The invention relates to 2,4-dibromoropyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing the intermediate.Type: ApplicationFiled: January 7, 2008Publication date: March 4, 2010Inventor: Brian E. Fink
-
Patent number: 7671199Abstract: The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound I has been shown to be useful for the treatment of certain types of cancer.Type: GrantFiled: April 20, 2007Date of Patent: March 2, 2010Assignee: Britsol-Myers Squibb CompanyInventors: Gerard A. Crispino, Mourad Hamedi, Thomas L. LaPorte, John E. Thornton, Jaan A. Pesti, Zhongmin Xu, Paul C. Lobben, David K. Leahy, Jale Muslehiddinoglu, Chiajen Lai, Lori Ann Spangler, Robert P. Discordia, Francis S. Gibson
-
Patent number: 7662842Abstract: Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.Type: GrantFiled: July 19, 2006Date of Patent: February 16, 2010Assignees: Ohio State Univesity Research Foundation, The University of Tennessee Research FoundationInventors: Duane D. Miller, James T. Dalton, Veeresa Gududuru, Eunju Hurh
-
Publication number: 20100022503Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: January 4, 2008Publication date: January 28, 2010Inventors: Marco Dodier, Claude A. Quesnelle, Anne Marinier