Nitrogen Bonded Directly To Ring Carbon Of The 1,3-diazine Ring Of The Quinazoline Ring System Patents (Class 514/266.4)
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Publication number: 20100215772Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: October 30, 2009Publication date: August 26, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Julian M.C. Golec, Daniel David Robinson, John Studley
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Publication number: 20100216767Abstract: The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: ApplicationFiled: December 20, 2007Publication date: August 26, 2010Inventors: Mina Aikawa, Payman Amiri, Steven Bashman, Jeffrey Dove, Rama Jain, Xiaodong Lin, Jeremy Murray, Savithri Ramurthy, Alice Rico, Wei Shu, Sharadha Subramanian, Xiaojing Michael Wang, Robert L. Warne, Yasheen Zhou
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Patent number: 7781441Abstract: The present invention relates to compounds of formula I wherein R, R1, R2, R3, R4, aryl, n, and m are as defined in the specification and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. Such compounds have good activity on the 5-HT5A receptor. Therefore, the invention provides methods for the treatment of certain CNS disorders with such compounds.Type: GrantFiled: April 27, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Publication number: 20100210709Abstract: Methods of preventing the development and reversing or partially reversing opioid tolerance in a subject are provided herein. Such methods include the step of administering to a subject in need thereof a therapeutically effective amount of a PDGFR modulator or EGFR modulator alone or together with an opiate analgesic. The methods can also be used for the treatment of refractory neuropathic pain, physical dependence or addiction.Type: ApplicationFiled: October 8, 2008Publication date: August 19, 2010Inventor: Gutstein B. Howard
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Publication number: 20100203043Abstract: The present invention relates to a method for the treatment, prevention and/or diagnosis of metastatic prostate cancer. More specifically inhibitors of Epidermal Growth Factor Receptor (EGFR) are used in the preparation of a pharmaceutical composition for treating or preventing metastatic prostate cancer. The EGFR inhibitors can for instance be EGFR inhibitors, EGFR signaling inhibitors and/or inhibitors of kinases downstream of EGFR kinases. The EGFR inhibitors can also be used in detection, screening, prediction and treatment monitoring methods for metastatic prostate cancer.Type: ApplicationFiled: April 11, 2008Publication date: August 12, 2010Inventors: Anne H. Ree, Ase Bratland, Pieter Jacob Boender, Robby Ruijtenbeek
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Patent number: 7772232Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: GrantFiled: April 13, 2005Date of Patent: August 10, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd
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Publication number: 20100196366Abstract: Disclosed is the identification, provision and use of a panel of biomarkers that predict sensitivity or resistance to EGFR inhibitors, and products and processes related thereto. In one embodiment, a method is described for selecting a cancer patient who is predicted to benefit from therapeutic administration of an EGFR inhibitor, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitor. Also described is a method to identify molecules that interact with the EGFR pathway to allow or enhance responsiveness to EGFR inhibitors, as well as a plurality of polynucleotides or antibodies for detection of the expression of genes that are indicative of sensitivity or resistance to EGFR inhibitors, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitors. A method to identify a compound with the potential to enhance the efficacy of EGFR inhibitors is also described.Type: ApplicationFiled: July 23, 2008Publication date: August 5, 2010Inventors: Paul A. Bunn, Christopher D. Coldren, Wilbur A. Franklin, Mark W. Geraci, Barbara A. Helfrich, Fred R. Hirsch, Razvan Lapadat, Michio Sugita, Samir E. Witta
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Publication number: 20100197688Abstract: The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.Type: ApplicationFiled: May 28, 2009Publication date: August 5, 2010Inventors: Philippe G. Nantermet, Hamaka A. Rajapakse, Takeshi Sagara, John M. Sanders, Hong Zhu
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Publication number: 20100196365Abstract: The present invention relates to the use of compounds of formula (I) in the treatment of Epidermal Growth Factor Receptor (EGFR) family members dependent diseases or diseases that have acquired resistance to agents that target EGFR family members, use of said compounds for the manufacture of pharmaceutical compositions for the treatment of said diseases, combinations of said compounds with EGFR modulators for said use, methods of treating said diseases with said compounds and pharmaceutical preparations for the treatment of said diseases comprising said compounds alone or in combination, especially with an EGFR modulator.Type: ApplicationFiled: July 23, 2008Publication date: August 5, 2010Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Sauveur-Michel Maira
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Publication number: 20100189775Abstract: The present invention provides pharmaceutical compositions for the treatment of hepatocellular carcinoma (HCC) comprising Notch3 inhibitors and a chemotherapeutic agent, methods for the preparation of said compositions and a medical treatment comprising the administration of said pharmaceutical compositions in patients in need thereof.Type: ApplicationFiled: July 25, 2007Publication date: July 29, 2010Inventors: Luigi Bolondi, Catia Giovannini, Pasquale Chieco, Kenneth Marcu
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Publication number: 20100190807Abstract: The invention relates to the inhibition of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to methods for inhibiting increases in MAPT expression induced by the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.Type: ApplicationFiled: August 26, 2009Publication date: July 29, 2010Inventors: Donald Porter, Igor Roninson
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Publication number: 20100189683Abstract: This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Ascenta Therapeutics, Inc.Inventors: Jon T. Holmlund, Mel Sorensen, Lance Leopold, Dajun Yang
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Publication number: 20100183606Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Inventors: ROBERT M BORZILLERI, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Publication number: 20100183728Abstract: The present invention features methods for treating, stabilizing, preventing, and/or delaying cancer by administering nanoparticles that comprise rapamycin or a derivative thereof. The invention also provides compositions (e.g., unit dosage forms) comprising nanoparticles that comprise a carrier protein and rapamycin or a derivative thereof. The invention further provides combination therapy methods of treating cancer comprising administering to an individual an effective amount of nanoparticles that comprise rapamycin or a derivative thereof and a second therapy.Type: ApplicationFiled: March 7, 2008Publication date: July 22, 2010Inventors: Neil P. Desai, Patrick Soon-Shiong, Vuong Trieu
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Patent number: 7754729Abstract: A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).Type: GrantFiled: December 23, 2008Date of Patent: July 13, 2010Inventor: Hesheng Zhang
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Publication number: 20100168142Abstract: The present invention relates to salt forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide, methods for preparation thereof, pharmaceutical compositions comprising the same and their use thereof. The salt forms of the present invention, which possess excellent tumor inhibitory activity, good bioavailability and low toxicity in an animal body, are suitable for the use of preparation of anti-tumor medicaments.Type: ApplicationFiled: February 4, 2008Publication date: July 1, 2010Inventors: Jianhui Guo, Yong Jiang
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Publication number: 20100166699Abstract: The invention provides a combination comprising an ancillary compound (e.g.Type: ApplicationFiled: June 21, 2006Publication date: July 1, 2010Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Neil Thomas Thompson, Robert George Boyle, Ian Collins, Michelle Dawn Garrett, John Francis Lyons, Kyla Merriom Thompson
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Publication number: 20100160338Abstract: The present invention relates to new benzenesulfonamide modulators of alpha-1A adrenergic receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 18, 2009Publication date: June 24, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100160316Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: March 1, 2010Publication date: June 24, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jesus E. Gonzalez, III, Dean M. Wilson, Andreas P. Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin J. Petzoldt, Lev Tyler Dewey Fanning, Timothy D. Neubert, Roger D. Tung, Esther Martinborough, Nicole Zimmerman
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Publication number: 20100158914Abstract: The invention concerns uses of anti-KL? agents, and detection of KL? and/or FGF19 and/or FGFR4.Type: ApplicationFiled: April 1, 2008Publication date: June 24, 2010Inventor: Luc Desnoyers
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Publication number: 20100150844Abstract: 8-quinolinol (8Q) and derivatives thereof for use in the treatment of proliferative diseases such as cancer, in particular slow metabolizing quiescent cancer stem cells.Type: ApplicationFiled: July 30, 2007Publication date: June 17, 2010Applicant: The Johns Hopkins UniversityInventors: Ying Zhang, Jiangbing Zhou, Hao Zhang
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Publication number: 20100150896Abstract: The present invention relates to new diaminoquinazoline inhibitors of dihydrofolate reductase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 11, 2009Publication date: June 17, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100144639Abstract: The present invention relates to the use of specific EGF-receptor antagonists for preparing a pharmaceutical composition for the prevention and/or treatment of benign prostatic hyperplasia and/or prostatic hypertrophy, a method for the treatment or prevention of benign prostatic hyperplasia/prostatic hypertrophy comprising administering an EGF-receptor antagonist of groups (A), (B) or (C), described herein optionally in combination with known compounds for the treatment of benign prostatic hyperplasia/prostatic hypertrophy, as well as associated pharmaceutical compositions.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Thomas SINGER, Stefan PLATZ, Florian COLBATZKY
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Publication number: 20100144731Abstract: Novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided.Type: ApplicationFiled: September 3, 2009Publication date: June 10, 2010Applicant: Dr. Reddy's Laboratories Ltd.Inventors: Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti
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Publication number: 20100143296Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100143299Abstract: This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR?R? and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-?/-oxide, a solvate or a pro-drug thereof.Type: ApplicationFiled: July 20, 2007Publication date: June 10, 2010Applicant: Gilead Sciences, Inc.Inventors: Ling-Jie Gao, Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
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Publication number: 20100136116Abstract: The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph A substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 ?m to 15 ?m and 90 volume-% of the particles (D90) ranging from about 14 ?m to 30 ?m, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles.Type: ApplicationFiled: August 17, 2007Publication date: June 3, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
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Publication number: 20100129470Abstract: Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a cytotoxic agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating brain cancer.Type: ApplicationFiled: October 8, 2009Publication date: May 27, 2010Applicant: Myriad Pharmaceuticals, IncorporatedInventor: MARK LAUGHLIN
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Patent number: 7718663Abstract: An object of the present invention is to provide an antipruritic agent having a novel action mechanism. The present invention provides an antipruritic agent comprising a compound represented by the following general formula (1): wherein R1 represents a hydrogen atom or alkyl; the ring Q represents a cyclohexylene group or a phenylene group; A1 and A2 represent a single bond or an alkylene group; E represents —NHCO—; A3 represents a single bond or a divalent saturated or unsaturated aliphatic hydrocarbon group; R3 represents a non-cyclic aliphatic hydrocarbon group; and R4 and R5 are the same or different and each represents a hydrogen atom or alkyl, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: April 28, 2003Date of Patent: May 18, 2010Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiko Okano, Tatsuya Oyama
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Publication number: 20100120803Abstract: The present invention relates to 3,4-dihydroquinazoline derivatives, a process of preparing them and a pharmaceutical composition including them. The 3,4-dihydroquinazoline derivatives of the present invention have excellent T-type calcium channel blocking effect and anti-cancer activity.Type: ApplicationFiled: May 6, 2008Publication date: May 13, 2010Applicant: DONGWOO SYNTECH CO., LTD.Inventors: Jae Yeol Lee, Dong Joon Choo, Young Deuk Kim, Chun Rim Oh
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Publication number: 20100113474Abstract: A combination of a 4-anilino-3-cyanoquinoline compound (e.g. HKI-272, SKI-606, EKB-569) and a capecitabine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described.Type: ApplicationFiled: August 4, 2009Publication date: May 6, 2010Applicant: WyethInventors: Charles Michael Zacharhuk, Susan Elizabeth Quinn, Kenneth Kuan-Yuen Wang, Florence Marie Helene Binlich
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Patent number: 7709479Abstract: The use of a compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O) or S(O)2, NH or NR12 where R12 is hydrogen or C1-6 alkyl; R5 is selected from a group NHC(O)OR9, NHC(O)R9, NHS(O)2R9, C(O)R9, C(O)OR9, S(O)R9, S(O)OR9, S(O)2OR9, C(O)NR10 R11, S(O)NR10R11 S(O)ONR10R11, where R9, R10 or R11 are various specified organic groups; R6 is hydrogen, optionally substituted hydrocarbyl or optionally substituted heterocyclyl; R7 and R8 are various specified organic groups, and R1, R2, R3, R4 are independently selected from halogeno, cyano, nitro, C1-3alkylsulphanyl, —N(OH)R13— (wherein R7 is hydrogen, or C1-3alkyl), or R15X1— (wherein X1 represents a direct bond, —O—, —CH2—, —OCO—, carbonyl, —S—, —SO—, —SO2—, —NR16CO—, —CONR16—, —SO2NR16—, —NR17SO2— or —NR18— (wherein R16, R17 and R18 each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl), and R9 is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxyType: GrantFiled: September 18, 2000Date of Patent: May 4, 2010Assignee: AstraZenecaInventors: Andrew Austen Mortlock, Nicholas John Keen, Frederic Henri Jung, Andrew George Brewster
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Publication number: 20100104558Abstract: The present invention relates to uses, methods and compositions for treating immune-mediated glomerulonephritis, such as crescentic glomerulonephritis. More specifically, the invention relates to the use of an EFGR antagonist or of an inhibitor of EGFR or HB-EGF expression for the treatment of said diseases.Type: ApplicationFiled: October 31, 2006Publication date: April 29, 2010Applicant: INSERM (Inetitut National de la Sante et la Recherche Medicale )Inventors: Pierre Louis Tharaux, Martin Flamant
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Publication number: 20100104567Abstract: The present invention provides a pharmaceutical composition comprising a combination of an Flt-3 inhibitor and at least one compound, the said pharmaceutical composition wherein an Flt-3 inhibitor is an indazole derivative represented by Formula (I) (wherein R1 represents substituted or unsubstituted aryl, or the like) or a pharmaceutically acceptable salt thereof, the said pharmaceutical composition wherein an Flt-3 inhibitor is a pyrimidine derivative represented by Formula (II) [wherein —X—Y—Z— represents —O—CR17?N— (wherein R17 represents a hydrogen atom, lower alkyl, or the like), R15 represents —NR22aR22b (wherein R22a and R22b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), and R16 represents —NR24aR24b (wherein R24a and R24b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like] or a pharmaceutically acceptable salt thereof, or the like.Type: ApplicationFiled: March 5, 2008Publication date: April 29, 2010Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Yukimasa Shiotsu, Kenichi Ishii, Hiroyuki Ishida, Makiko Shimizu
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Publication number: 20100104565Abstract: The present invention relates to combinations of the xanthenone acetic acids class such as 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and EGFR signalling pathway inhibitors. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations.Type: ApplicationFiled: August 25, 2006Publication date: April 29, 2010Inventors: Colin Green, Lloyd Kelland, Sally Kelland, Gail Rowlinson-Brusza
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Publication number: 20100098691Abstract: The present invention relates to a pharmaceutical composition for the treatment of cancer as well as methods of treatment of cancer that are based on the finding that certain benzimidazole based anti-cancer agents can be used in combination with a second anti-cancer agent to achieve desirable therapeutic outcomes. More specifically the present invention relates to a pharmaceutical composition including a benzimidazole based anti-cancer agent and a second anti-cancer agent. The invention also relates to methods of treatment of cancer including administration of a benzimidazole based anti-cancer agent and a second anti-cancer agent to a patient in need thereof.Type: ApplicationFiled: March 7, 2008Publication date: April 22, 2010Applicant: S'BIO PTE LTDInventors: Kay Lin Goh, Hwee Hoon Khng, Vasantha Malar Sabanayagam, Kanda Sangthongpitag, Walter Stunkel, Yong Cheng Tan, Jeanette Marjorie Wood
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Patent number: 7700608Abstract: A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof.Type: GrantFiled: August 3, 2005Date of Patent: April 20, 2010Assignee: Shire Holdings AGInventor: Richard Franklin
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Publication number: 20100093773Abstract: Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a vascular disrupting agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating cancer.Type: ApplicationFiled: October 6, 2009Publication date: April 15, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventors: MARK LAUGHLIN, Mark B. Anderson, Adam Willardsen, Chris Pleiman
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Publication number: 20100093772Abstract: A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof.Type: ApplicationFiled: October 16, 2009Publication date: April 15, 2010Applicant: Shire Holdings AGInventor: Richard Franklin
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Publication number: 20100087457Abstract: In general, the invention relates to a pharmaceutical dose having (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride as the active ingredient that upon administration to a subject provides a Cmax of about 1 ng/mL to about 250 ng/mL. The dose may be used in methods of treating cancer through the administration of (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride. The composition of the invention is formulated with one or more pharmaceutically acceptable excipients, salts or carriers.Type: ApplicationFiled: October 7, 2009Publication date: April 8, 2010Applicant: Myriad Pharmaceuticals, IncInventor: MARK LAUGHLIN
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Publication number: 20100087458Abstract: Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a cytotoxic agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating melanoma.Type: ApplicationFiled: October 7, 2009Publication date: April 8, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventor: Mark Laughlin
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Patent number: 7691866Abstract: New substituted quinazoline, quinoxaline, quinoline and isoquinoline compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: GrantFiled: October 15, 2004Date of Patent: April 6, 2010Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian
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Publication number: 20100081675Abstract: Fused multicyclic compounds of formula (I): wherein R?, R?, X, Y, Z, A, B, C, D, and n are defined herein. Also disclosed are a method for inhibiting protein kinase (e.g., Aurora kinase) activity and a method for treating a protein kinase mediated disorder (e.g., cancer) with these compounds.Type: ApplicationFiled: September 22, 2009Publication date: April 1, 2010Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Yu-Sheng Chao
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Publication number: 20100075916Abstract: The present invention relates to new substituted quinazoline inhibitors of vascular endothelial growth factor receptor tyrosine kinase, epidermal growth factor receptor tyrosine kinase, and/or REarranged during Transfection tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 4, 2009Publication date: March 25, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar, Manouchehr M. Shahbaz
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Publication number: 20100069414Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.Type: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Thomas METZ, Flavio SOLCA, Birgit JUNG, Anke BAUM
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Publication number: 20100069383Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: July 10, 2009Publication date: March 18, 2010Applicant: Myriad Pharmaceuticals, IncorporatedInventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Ashantai Yungai, Robert J. Halter, Yevgeniya Klimova, Kazuyuki Suzuki, Matthew Reeder
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Publication number: 20100068197Abstract: Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: July 9, 2009Publication date: March 18, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Kazuyuki Suzuki, Robert J. Halter, In Chul Kim, Matthew Reeder, Ashantai Yungai
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Publication number: 20100069369Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.Type: ApplicationFiled: September 1, 2009Publication date: March 18, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
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Publication number: 20100055100Abstract: Methods using mass spectral data analysis and a classification algorithm provide an ability to determine whether a non-small-cell lung cancer patient, head and neck squamous cell carcinoma or colorectal cancer patient has likely developed a non-responsiveness to treatment with a drug targeting an epidermal growth factor receptor pathway. As the methods of this disclosure require only simple blood samples, the methods enable a fast and non-intrusive way of measuring when drugs targeting the EGFR pathway cease to be effective in certain patients. This discovery represents the first known example of true personalized selection of these types of cancer patients for treatment using these classes of drugs not only initially, but during the course of treatment.Type: ApplicationFiled: September 8, 2009Publication date: March 4, 2010Inventors: Heinrich Röder, Maxim Tsypin, Julia Grigorieva
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Publication number: 20100056506Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: April 19, 2007Publication date: March 4, 2010Applicant: PFIZER PRODUCTS INC.Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken