Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
-
Patent number: 7629459Abstract: A compound represented by formula (I): Formula (I) wherein Z1 is atoms necessary for forming an aromatic ring; Z2 is atoms necessary for forming an aromatic hetero ring; V1 and V2 each are a substituent, and at least one of V1 and V2 is a hydroxyl, primary- or secondary- or tertiary-amino, acylamino, or sulfonamido group; r is 1 to 4; s is 1 to 4; the ring formed by Z1 or Z2 may have a substituent other than V1 or V2; M1 is a counter ion; m1 is the number necessary for neutralizing charge; and X1 and X2 each are a carbon or hetero atom, and at least one of X1 and X2 is a hetero atom.Type: GrantFiled: November 17, 2005Date of Patent: December 8, 2009Assignee: Fujifilm CorporationInventors: Katsumi Kobayashi, Yasuhiro Ishiwata, Nobuo Seto, Kiyoshi Takeuchi
-
Publication number: 20090291955Abstract: Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: November 10, 2006Publication date: November 26, 2009Inventors: Sheldon N. Crane, Joel Stéphane Robichaud, Serge Léger, Yeeman K. Ramtohul
-
Publication number: 20090291956Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.Type: ApplicationFiled: May 20, 2009Publication date: November 26, 2009Inventors: Lingkai Weng, Lei Qiao, Jiacheng Zhou, Pingli Liu, Yongchun Pan
-
Publication number: 20090286768Abstract: Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.Type: ApplicationFiled: May 19, 2009Publication date: November 19, 2009Applicant: OSI Pharmaceuticals, Inc.Inventors: Andrew P. Crew, Meizhong Jin, Mridula Kadalbajoo, Andrew Kleinberg, Mark J. Mulvihill, Jing Wang
-
Publication number: 20090281079Abstract: This invention relates to novel 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: November 30, 2006Publication date: November 12, 2009Applicant: BAYER HEALTHCARE LLVInventors: Julie Dixon, Steven Magnuson, Barton Phillips, Yamin Wang, Tandy Li, Kyle Parcella, Jason Newcom, Harold Kluender, Zhenqiu Hong, Brent Chandler, Zhonghua Zhang, Kristen Allegue, Zheng Liu
-
Publication number: 20090275569Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: September 9, 2008Publication date: November 5, 2009Inventors: Xianchang Gong, Kathy Barrett, Jianguo Cao, Colleen Gritzen, Glenn Noronha, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Ningning Zhao, Elena Dneprovskaia, Binqi Zeng, Glenn Noronha
-
Publication number: 20090270374Abstract: Bicyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: July 18, 2007Publication date: October 29, 2009Inventors: Llius Ballell, David Barros, Gerald Brooks, Julia Castro Pichel, Steven Dabbs, Robert A. Daines, David Thomas Davies, Jose Maria Fiandor Roman, Israil Pendrak, Modesto J. Remuinan Blanco, Jason Anthony Rossi, Ilaria Giordano, Alan Joseph Hennessy, James B. Hoffman, Graham Elgin Jones, Timothy James Miles, Neil David Pearson, Lihua(lily) Zhang
-
Patent number: 7605160Abstract: The present 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 and TrkC thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: August 8, 2007Date of Patent: October 20, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Ping Chen
-
Publication number: 20090258855Abstract: The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.Type: ApplicationFiled: October 18, 2007Publication date: October 15, 2009Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth Anne Jefferson
-
Publication number: 20090258877Abstract: The invention relates to substituted triazolotriazines and triazolopyrazines and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular haematologic disorders, preferably of leukopenias and neutropenias.Type: ApplicationFiled: December 12, 2008Publication date: October 15, 2009Applicant: BAYER HEALTHCARE AGInventors: Stephan Siegel, Andreas Wilmen, Niels Svenstrup, Mark Jean Gnoth, Stefan Heitmeier, Ulrich Rester, Adrian Tersteegen, Michael Gerisch
-
Publication number: 20090253704Abstract: The present invention discloses pyrrolotriazinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.Type: ApplicationFiled: April 3, 2009Publication date: October 8, 2009Inventors: Dmitry Koltun, Eric Parkhill, Jeff Zablocki
-
Publication number: 20090247531Abstract: 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: ApplicationFiled: June 8, 2009Publication date: October 1, 2009Inventor: John E. Thornton
-
Publication number: 20090239838Abstract: 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: March 26, 2009Publication date: September 24, 2009Inventors: 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: 20090232780Abstract: This invention generally provides compounds, pharmaceutical compositions, and methods for their use, which include methods that result in increased expression in an Atoh1 gene (e.g., Hath1) in a biological cell. More specifically, the invention relates to the treatment of diseases and/or disorders that would benefit from increased Atoh1 expression, e.g., a hearing impairment or imbalance disorder associated with a loss of auditory hair cells, or a disorder associated with abnormal cellular proliferation.Type: ApplicationFiled: February 9, 2009Publication date: September 17, 2009Applicant: Massachusetts Eye & Ear InfirmaryInventors: Albert Edge, Sang-Jun Jeon, Kathleen Seyb, Marcie Glicksman, Lixin Qiao, Gregory D. Cuny
-
Publication number: 20090227562Abstract: The present invention relates to a combination of a selective noradrenaline reuptake inhibitor (NRI) and a phospho-diesterase type 5 (PDEV) inhibitor. Such a combination is particularly useful in the treatment of pain.Type: ApplicationFiled: July 8, 2005Publication date: September 10, 2009Applicant: Pfizer Inc.Inventor: Bernadette Hughes
-
Publication number: 20090227567Abstract: Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, or NH2, preferably methyl, and X, R1 through R6, and Z are as described in the specification. Advantageously the groups -ZR4R5 taken together comprise an —NH-substituted aryl.Type: ApplicationFiled: May 21, 2009Publication date: September 10, 2009Inventors: Katerina Leftheris, John Hynes, Stephen T. Wrobleski, Joel Barrish
-
Publication number: 20090221587Abstract: Compounds of formula (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: ApplicationFiled: August 14, 2006Publication date: September 3, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andre Jeanguenat, Roger Graham Hall, Olivier Loiseleur, Stephan Trah, Patricia Durieux, Andrew Edmunds, Andrew Edmunds, Andre Stoller
-
Publication number: 20090221570Abstract: The present invention relates to the use of PDE 5 inhibitors generally and in particular of known 2-phenyl-substituted imidazotriazinone derivatives for manufacturing medicaments for the treatment of pathological states which can be treated by raising cGMP levels in certain tissues, such as, for example, of, for example: primary pulmonary hypertension, secondary pulmonary hypertension, pulmonary arterial hypertension, portopulmonary hypertension, hepatopulmonary syndrome, pulmonary hypertension caused by medicaments (amphetamines), interstitial lung disease, pulmonary hypertension occurring with HIV, thromboembolic pulmonary hypertension, pulmonary hypertension in children and neonates, pulmonary hypertension induced by atmospheric hypoxia (altitude sickness), COPD, emphysema, chronic bronchial asthma, mucoviscidosis-related pulmonary hypertension, right heart failure, left heart failure and global failure, and which can be treated by raising cGMP levels in certain tissues, such as, for example, isolated systType: ApplicationFiled: March 27, 2006Publication date: September 3, 2009Applicant: Bayer Helthcare AGInventors: Helmut Haning, Peter Serno, Erwin Bischoff, Ernst Ulbrich
-
Publication number: 20090220554Abstract: Transglutaminase inhibitors and methods of use thereof are provided.Type: ApplicationFiled: October 25, 2006Publication date: September 3, 2009Inventors: John Griffin, Guido Lanza, Paul Boardman, Andrew Spencer
-
Publication number: 20090215782Abstract: The invention relates generally to neovascularization and endothelial repair of tissues impaired by trauma or disease. Particularly, the invention relates to the function of endothelial progenitor cells in neovascularization and endothelial repair. More particularly, the invention relates to methods and pharmaceutical compositions for the treatment of tissues impaired by trauma or disease. In particular, the present invention relates to the use of a type V phosphodiesterase inhibitor in the preparation of a medicament for the treatment of a condition which is susceptible to the treatment with circulating EPCs wherein the treatment is effected by the proliferation of endothelial progenitor cells.Type: ApplicationFiled: April 18, 2005Publication date: August 27, 2009Inventor: Carlo Foresta
-
Publication number: 20090214529Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat a kinesin Eg5 protein-mediated disorder.Type: ApplicationFiled: May 22, 2008Publication date: August 27, 2009Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Ching-Cheng Wang, Hung-Chuan Chen, Shu-Huei Wang, Mei-Chun Lin, Tien-Lan Shieh, Ying-Huey Huang, Shih-Chieh Chuang, Chi-Hsin Richard King
-
Publication number: 20090215783Abstract: The present invention relates to composition and methods for inducing or inhibiting differentiation of stem cells. The invention also relates to applications in the treatment of medical conditions, e.g., osteoporosis, bone fracture, bone injuries, myocardiac infarction, cardiomyopathy, degenerative muscle diseases, myopathy, and urinary incontinence.Type: ApplicationFiled: May 30, 2007Publication date: August 27, 2009Applicant: CHOONGWAE PHARMA CORPORATIONInventor: Se Woong Oh
-
Publication number: 20090215781Abstract: The invention provides ?-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, R1 and R2 as set out in the description and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.Type: ApplicationFiled: March 15, 2006Publication date: August 27, 2009Applicant: INSTITUTE FOR CHEMICAL GENOMICSInventors: Michael Kahn, Masakatsu Eguchi
-
Patent number: 7576084Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: April 16, 2004Date of Patent: August 18, 2009Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
-
Patent number: 7572795Abstract: Compounds having the Formula (I), including pharmaceutically acceptable salts thereof, wherein at least one of X1, X2 or X3 is and any remaining X1, X2 or X3 is hydrogen, which are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, A1, A2 and m are as described herein.Type: GrantFiled: March 6, 2007Date of Patent: August 11, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, Katerina Leftheris, Vivekananda M. Vrudhula, James Lin
-
Patent number: 7566711Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: April 15, 2005Date of Patent: July 28, 2009Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
-
Publication number: 20090186886Abstract: The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.Type: ApplicationFiled: March 31, 2006Publication date: July 23, 2009Applicant: Auckland Uniservices LimitedInventors: Michael Patrick Hay, Adrian Blaser, William Alexander Denny, Kevin Owen Hicks, Ho Huat Lee, Karin Pchalek, Frederik Bastiaan Pruijn, Bronwyn Gae Siim, William Robert Wilson, Shangjin Yang
-
Patent number: 7563791Abstract: This invention relates to novel 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: GrantFiled: June 3, 2005Date of Patent: July 21, 2009Assignee: 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: 20090181972Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.Type: ApplicationFiled: December 5, 2006Publication date: July 16, 2009Inventors: Philippe Guedat, Guillaune Boissy, Catherine Borg-Capra, Frederic Colland, Laurent Daviet, Etienne Formstecher, Xavier Jacq, Jean-Christophe Rain, Remi Delansorne, Ilaria Peretto, Stefano Vignando
-
Publication number: 20090181971Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: August 13, 2007Publication date: July 16, 2009Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
-
Publication number: 20090176742Abstract: The invention provides ?-mimetic structure of formula (I), wherein A is —(C?O)—(CHR3)— or —(C?O)—; B is —(NR5)— or —(CHR6)—; D is —(C?O)—(CHR7)— or —(C?O)—; E is -(ZR8)— or —(C?O)—, where Z is nitrogen or CH; —(XR9)n—, —(CHR10)—(NR6)—, —(C?O)—(XR12)—, —(C?N—W—R1)—, —(C?O)—, —(X—(C?O)—R13)—, —(X—(C?O)—NR13R14)—, —(X—(SO2)—R13)—, or —(X—(C?O)—OR13)—, where X is nitrogen or CH, and n=0 or 1; W is —Y(C?O)—, —(C?O)—(NH)—, —(SO2)—, —(CHR14)—, —(C?O)—(NR15)—, substituted or unsubstituted oxadiazole, substituted or unsubstituted triazole, substituted or unsubstituted thiadiazole, substituted or unsubstituted 4,5-dihydrooxazole, substituted or unsubstituted 4,5-dihydrothiazole, substituted or unsubstituted 4,5-dihydroimidizole, or nothing, where Y is oxygen or sulfur; and R1, R2, R3, R4, R5, R6, R7, R8, R9 R10, R11, R12, R13, R14, and R15 are the same or different and independently selected from an amino acid side chain moiety or derivative thereof, the remainder of the molecule, a linker and a solid support, and sterType: ApplicationFiled: September 25, 2007Publication date: July 9, 2009Applicants: UNIVERSITY OF WASHINGTON, INSTITUTE FOR CHEMICAL GENOMICSInventors: William R. HENDERSON, Michael KAHN
-
Publication number: 20090170853Abstract: 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: ApplicationFiled: March 6, 2009Publication date: July 2, 2009Inventors: Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa, Louis Lombardo, Jeffrey Robl
-
Publication number: 20090163504Abstract: A method for healing a wound comprising the step of topically administering a wound healing composition to a wounded area, wherein the wound healing composition comprises a first medicament characterized as a phosphodiesterase type five inhibitor and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 24, 2009Publication date: June 25, 2009Inventors: Matthew H. Kopacki, Michael J. Torsiello
-
Publication number: 20090163468Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: ApplicationFiled: December 2, 2008Publication date: June 25, 2009Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joesph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
-
Publication number: 20090156594Abstract: The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.Type: ApplicationFiled: May 21, 2008Publication date: June 18, 2009Applicant: SGX Pharmaceuticals, Inc.Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth A. Jefferson, Jorg Hendle, Patrick S. Lee, Angelina Marie Thayer, Gavin Charles Hirst
-
Publication number: 20090156602Abstract: The invention provides a pharmaceutical combination comprising: a) at least one agent selected from Bcr-Abl, Flt-3, FAK and RAF kinase inhibitors; and b) at least one JAK kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: November 22, 2005Publication date: June 18, 2009Inventors: Nigel Graham Cooke, Paul W. Manley
-
Publication number: 20090156604Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: ApplicationFiled: August 14, 2008Publication date: June 18, 2009Inventors: Swen HOLDER, Armin Zulch, Thomas Bar, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
-
Publication number: 20090156555Abstract: Compounds having the Formula (I), including pharmaceutically acceptable salts thereof wherein at least one of X1, X2 or X3 is and any remaining X1, X2 or X3 is hydrogen, which are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, A1, A2 and m are as described herein.Type: ApplicationFiled: February 12, 2009Publication date: June 18, 2009Inventors: Chunjian Liu, Katerina Leftheris, Vivekananda M. Vrudhula, James Lin
-
Publication number: 20090143356Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.Type: ApplicationFiled: October 26, 2006Publication date: June 4, 2009Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
-
Publication number: 20090136521Abstract: An improved method for selectively depleting hypoxic cells within the bone marrow is disclosed. The method can be used to enhance engraftment of hematopoietic stem cells (HSCs) in the bone marrow of a host subject. Also disclosed is a method for treating a cancer within the bone marrow of a host subject.Type: ApplicationFiled: September 29, 2006Publication date: May 28, 2009Applicants: Genetix Pharmaceuticals , Inc., Dana-Farber Cancer Institute , Inc.Inventors: Kalindi Parmar, Peter Mauch, Julian Down
-
Publication number: 20090131442Abstract: A method of treating bone pain caused by osteoarthritis by administering to a patient an effective amount of a composition containing a bone edema medication, such as a vasoactive medication or phosphodiesterase inhibitor, including a PDE-5 inhibitor.Type: ApplicationFiled: November 16, 2007Publication date: May 21, 2009Inventor: Joseph Bernstein
-
Publication number: 20090131425Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: ApplicationFiled: May 9, 2008Publication date: May 21, 2009Applicant: Abbott LaboratoriesInventors: Michael R. Michaelides, Zhiqin Ji
-
Patent number: 7534792Abstract: 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: July 5, 2007Date of Patent: May 19, 2009Assignee: 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: 20090124609Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 15, 2008Publication date: May 14, 2009Applicant: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie Springer, Markian Stec, Ning Xi, Kevin Yang
-
Patent number: 7531539Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of such as TrkA, TrkB, TrkC, Jak2, Jak3 and CK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: August 8, 2007Date of Patent: May 12, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Ping Chen, Ashok Vinayak Purandare, Honghe Wan
-
Publication number: 20090111692Abstract: The invention relates to 3-(pyridin-2-yl)-[1,2,4]-triazines of formula (I) and their use in the control of parasitic fungi and to herbicides that contain said compounds as an effective ingredient thereof.Type: ApplicationFiled: April 11, 2007Publication date: April 30, 2009Inventors: Wassilios Grammenos, Thomas Grote, Jochen Dietz, Jan Klaas Lohmann, Jens Renner, Bernd Muller, Sarah Ulmschneider
-
Publication number: 20090105243Abstract: 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: October 28, 2008Publication date: April 23, 2009Inventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
-
Patent number: 7521450Abstract: 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: August 2, 2007Date of Patent: April 21, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa, Louis Lombardo, Jeffrey Robl
-
Patent number: 7517988Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: November 14, 2007Date of Patent: April 14, 2009Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Hon C. Hui
-
Patent number: 7517882Abstract: Pyrimidine- and triazine-based chemical compounds that are useful, for example, as protein kinase inhibitors for treating cancer, neurological disorders, autoimmune disorders, and other diseases, and methods of using such compounds.Type: GrantFiled: September 17, 2007Date of Patent: April 14, 2009Assignee: Polaris GroupInventors: Shaosong Chu, Zhe Nie, Carin L. Perretta, Philip Eugene Erickson