Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
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Publication number: 20100317607Abstract: Compounds of a compound of compound of general formula (I) wherein X1, X2, A, R1R2, R3 and R4 are as defined herein; are useful as anti-mycobacterial agents, especially agents for the treatment of tuberculosis.Type: ApplicationFiled: June 24, 2008Publication date: December 16, 2010Applicant: INFECTIOUS DISEASE RESEARCH INSTITUTEInventors: Graham Michael Wynne, Olivier De Moor, Peter David Johnson, Richard John Vickers
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Patent number: 7851630Abstract: The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.Type: GrantFiled: September 29, 2004Date of Patent: December 14, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Jacobus A. J. Den Hartog, Samuel David, Daniel Jasserand, Gustaaf J. M. Van Scharrenburg, Herman H. Van Stuivenberg, Tinka Tuinstra
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Patent number: 7846938Abstract: The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below. These compounds are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and may further act as HDAC inhibitors. The invention further relates to the use of these tartrate salts in the treatment of EGFR-TK related diseases and disorders such as cancer.Type: GrantFiled: September 10, 2008Date of Patent: December 7, 2010Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Patent number: 7838530Abstract: The invention concerns quinazoline derivatives of Formula (I), wherein each of R1a, R1b, R2, R3 and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.Type: GrantFiled: September 22, 2004Date of Patent: November 23, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Laurent Francois Andre Hennequin, Christopher Thomas Halsall
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Patent number: 7829566Abstract: Quinazolines of the formula I in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein IbIX antagonists.Type: GrantFiled: December 14, 2005Date of Patent: November 9, 2010Inventors: Werner Mederski, Ralf Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, James Vickers, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark R. Player, Edward Jaeger, Richard Soll
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Patent number: 7825245Abstract: The present invention relates to quinazoline derivatives of formula I: wherein X, Y, Z, R1, R2, R3, and R4 are as defined herein. The invention also relates to a method of preparing these compounds, and use of these compounds for inhibiting tumor growth.Type: GrantFiled: November 13, 2007Date of Patent: November 2, 2010Inventors: Wenlin Huang, Xiaohong Zhou
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Publication number: 20100273808Abstract: This invention provides a compound of formula (I): or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; processes for the synthesis or manufacture of the compound of formula (I), or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; and the use of said compound, or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof, for the treatment of patients suffering from or subject to diseases, disorders or conditions involving cell survival, proliferation, and migration, including cardiovascular disease (e.g., arteriosclerosis and vascular reobstruction), cancer, (e.g., AML and malignant glioma)glomerulosclerosis, fibrotic disease and inflammation.Type: ApplicationFiled: November 20, 2009Publication date: October 28, 2010Applicant: Millennium Pharmaceticals, Inc.Inventors: Ian Armitage, Michael E. Bourland, Craig J.S. Boyle, Martin Ian Cooper, Abu J. Ferdous, Marianne Langston
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Patent number: 7820683Abstract: A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: GrantFiled: September 14, 2006Date of Patent: October 26, 2010Assignee: AstraZeneca ABInventors: Robert Hugh Bradbury, Bernard Christophe Barlaam, Richard Ducray
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Publication number: 20100267718Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, Rd, X and n are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibiting effect on the signal transduction mediated by tyrosine kinases, their use in treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract and the preparation thereof.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Inventors: Frank HIMMELSBACH, Rainer Soyka, Birgit Jung
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Publication number: 20100260674Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.Type: ApplicationFiled: January 26, 2010Publication date: October 14, 2010Applicant: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Publication number: 20100261738Abstract: The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2-methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I). The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans.Type: ApplicationFiled: September 11, 2007Publication date: October 14, 2010Applicant: NATCO PHARMA LIMITEDInventors: Ramanadham Jyothi Prasad, Bhujanga rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
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Publication number: 20100249100Abstract: 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 29, 2010Publication date: September 30, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
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Publication number: 20100240649Abstract: 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: ApplicationFiled: May 26, 2010Publication date: September 23, 2010Inventor: Hesheng ZHANG
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Publication number: 20100234371Abstract: The invention relates to bicyclic heterocycles of general formula (I), in which Ra, Rb, Rc, Rd, Re and X are as defined in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, in particular, the physiologically-acceptable salts thereof with inorganic and organic acids with useful pharmacological properties, in particular, an inhibitory effect on signal transduction brought about by tyrosine kinases, the use thereof for the treatment of diseases, in particular of tumour diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and airways and production thereof.Type: ApplicationFiled: August 3, 2006Publication date: September 16, 2010Inventors: Frank Himmelsbach, Birgit Jung
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Patent number: 7790884Abstract: To provide a compound which has an excellent activity to modulate the functions of CCR4 or TARC and/or MDC and can be used for the prevention and/or treatment of various inflammatory diseases, allergic diseases, autoimmune diseases and the like. An acylaminopiperidine compound represented by the formula (I) or a pharmaceutically acceptable salt thereof. [Symbols in the formula represent the following meanings; A: a single bond or C1-C6 alkylene, R1: phenyl which may be substituted, etc., R2: —H or C1-C6 alkyl, R3: —H, C1-C6 alkyl or C3-C8 cycloalkyl, R4: pyrrolidin-2-yl which may be substituted, etc., and D: benzene ring or pyrazole ring].Type: GrantFiled: March 23, 2007Date of Patent: September 7, 2010Assignee: Astellas Pharma Inc.Inventors: Toru Kontani, Noriyuki Kawano, Naoyuki Masuda, Koji Kato, Hiroshi Nagata, Hiroshi Inami, Tadashi Terasaka, Kazuhiro Yokoyama, Takahiro Miyazaki
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Publication number: 20100222344Abstract: A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: ApplicationFiled: November 29, 2006Publication date: September 2, 2010Inventor: Bernard Christophe Barlaam
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Patent number: 7786131Abstract: The present invention relates to pyrimido [5,4-d] pyrimidine compounds of Formula II or a pharmaceutically acceptable salt thereof, wherein Q is and X, E1, E2, E3, R6 and p are as defined herein. The compounds of this invention are irreversible inhibitors of tyrosine kinases and are useful in the treatment of cancer, atherosclerosis, restenosis, endometriosis and psoriasis.Type: GrantFiled: May 20, 2003Date of Patent: August 31, 2010Assignee: Warner-Lambert CompanyInventors: Alexander James Bridges, William Alexander Denny, Ellen Myra Dobrusin, Annette Marian Doherty, David William Fry, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Jeffrey B. Smaill, Hairong Zhou
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Publication number: 20100204470Abstract: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.Type: ApplicationFiled: June 25, 2007Publication date: August 12, 2010Inventors: Josef Wieser, Hannes Lengauer, Elfriede Klingler, Arthur Pichler, Hubert Sturm
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Patent number: 7772243Abstract: This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n—-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.Type: GrantFiled: May 5, 2005Date of Patent: August 10, 2010Assignee: Warner-Lambert Company LLCInventors: Stephen Alan Fakhoury, Helen Tsenwhei Lee, Jessica Elizabeth Reed, Kevin Matthew Schlosser, Karen Elaine Sexton, Haile Tecle, Roy Thomas Winters
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Publication number: 20100197915Abstract: The invention provides lapatinib intermediates and improved processes for preparing lapatinib intermediates. The invention also provides processes for preparing lapatinib base and lapatinib ditosylate.Type: ApplicationFiled: August 6, 2009Publication date: August 5, 2010Inventors: Leonid METSGER, Slavik YURKOVSKI, Sofia GOROHOVSKY-ROSENBERG, Noa KIPNIS, Dikla LAVY
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Publication number: 20100190977Abstract: This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.Type: ApplicationFiled: April 5, 2010Publication date: July 29, 2010Inventors: Stephen Alan Fakhoury, Helen Tsenwhei Lee, Jessica Elizabeth Reed, Kevin Matthew Schlosser, Karen Elaine Sexton, Haile Tecle, Roy Thomas Winters
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Patent number: 7763627Abstract: A compound according to Formula IV: or a pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof, wherein R1, R2, R3, R4, R5 and X are as defined in the specification.Type: GrantFiled: April 8, 2004Date of Patent: July 27, 2010Assignee: Exelixis, Inc.Inventors: Mohamed Abdulkader Ibrahim, James William Leahy, Joan C. Sangalang, Kevin Luke Schnepp, Xian Shi, John M. Nuss
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Publication number: 20100179120Abstract: The present invention provides a novel amide derivative and a pharmaceutically acceptable salt thereof which selectively and effectively inhibits the growth of cancer cells induced by the overexpression of an epidermal growth factor receptor and also prevents the development of drug resistance caused by the mutation of EGFR tyrosine kinase, and a pharmaceutical composition comprising same as an active ingredient.Type: ApplicationFiled: June 5, 2008Publication date: July 15, 2010Applicant: HANMI PHARM. CO., LTD.Inventors: Kwang-Ok Lee, Mi Young Cha, Mi Ra Kim, Young Hee Jung, Chang Gon Lee, Se Young Kim, Keukchan Bang, Bum Woo Park, Bo Im Choi, Yun Jung Chae, Mi Young Ko, Han Kyong Kim, Young-Gil Ahn, Maeng Sup Kim, Gwan Sun Lee
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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: 20100174074Abstract: Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same.Type: ApplicationFiled: March 26, 2008Publication date: July 8, 2010Inventors: Ahmed Kamal, Bandari Rajendra Prasad
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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: 20100168123Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: September 25, 2009Publication date: July 1, 2010Inventors: Ian S. Mitchell, Keith L. Spencer, Peter Stengel, Yongxin Han, Nicholas C. Kallan, Mark Munson, Guy P.A. Vigers, James Blake, Anthony Piscopio, John Josey, Scott Miller, Dengming Xiao, Rui Xu, Chang Rao, Bing Wang, April L. Bernacki
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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: 20100152442Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, R1 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.Type: ApplicationFiled: February 16, 2010Publication date: June 17, 2010Inventors: Robert Hugh Bradbury, Laurent Francois Andre Hennequin, Jason Grant Kettle
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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: 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: 20100130741Abstract: The present invention provides an improved and commercially viable process for preparation of erlotinib substantially free of N-methoxyethyl impurity, namely N-[(3-ethynylphenyl)-(2-methoxyethyl)]-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, and its pharmaceutically acceptable acid addition salts thereof in High purity and in high yield. According to the present invention, erlotinib or a pharmaceutically acceptable acid addition salt of erlotinib substantially free of N-methoxyethyl impurity is prepared by isolating erlotinib or a pharmaceutically acceptable salt of erlotinib from a solvent medium comprising dimethyl sulfoxide and an alcoholic solvent.Type: ApplicationFiled: July 11, 2007Publication date: May 27, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
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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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Patent number: 7718658Abstract: 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: GrantFiled: August 31, 2005Date of Patent: May 18, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
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Publication number: 20100120804Abstract: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L? are suitable leaving groups, with a compound of formula (III) UNH2 ??(III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L?.Type: ApplicationFiled: January 22, 2010Publication date: May 13, 2010Inventors: Malcom Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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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: 20100105668Abstract: The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N?CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-Type: ApplicationFiled: November 24, 2009Publication date: April 29, 2010Inventors: Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Gaston Stanislas Marcella Diels, Werner Constant Johan Embrechts, Peter ten Holte, Frederik Jan Rita Rombouts, Carsten Schultz-Fademrecht
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Publication number: 20100094004Abstract: A process for the preparation of a salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4˜halo-6,7-bis(2-methoxyethoxy) quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine.Type: ApplicationFiled: April 3, 2008Publication date: April 15, 2010Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
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Publication number: 20100087459Abstract: The present invention provides novel crystalline and amorphous lapatinib compounds and processes for preparing themType: ApplicationFiled: August 26, 2009Publication date: April 8, 2010Inventors: Leonid METSGER, Ariel MITTELMAN, Slavik YURKOVSKI
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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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Patent number: 7687508Abstract: This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.Type: GrantFiled: July 25, 2007Date of Patent: March 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Robert J. Cherney, John Hynes, Soo S. Ko, Anurag S. Srivastava, Zili Xiao, Michael G. Yang
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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: 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: 20100069413Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: November 19, 2009Publication date: March 18, 2010Inventors: Andreas D. Christ, Rainer E. Martin
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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: 20100056517Abstract: The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.Type: ApplicationFiled: November 15, 2007Publication date: March 4, 2010Applicants: GENENTECH, INC., WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCInventors: Jonathan Bayldon Baell, Guillaume Laurent Lessene, Brad Edmund Sleebs, Wayne J. Fairbrother, John A. Flygare, Michael F.T. Koeler
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Patent number: 7659279Abstract: The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use as therapeutic agents in the treatment of erbB tyrosine kinase mediated diseases such as cancer.Type: GrantFiled: April 27, 2004Date of Patent: February 9, 2010Assignee: AstraZeneca ABInventors: Laurent Francois Andre Hennequin, Alleyn Plowright
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Publication number: 20100022505Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb and Rc are defined as in claim 1, their tautomers, their stereoisomers, their mixtures and their salts, in particular their physiologically acceptable salts with inorganic or organic acids and bases, which have valuable pharmacological properties, in particular an inhibitory action on the signal transduction mediated by tyrosine kinases, their use for the treatment of illnesses, in particular of tumoral diseases and of benign prostatic hyperplasia (BPH), of diseases of the lung and of the airways, and the preparation thereof.Type: ApplicationFiled: January 30, 2008Publication date: January 28, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Birgil Jung, Ralf Lotz, Markus Ostermeier
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Publication number: 20100022566Abstract: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).Type: ApplicationFiled: October 3, 2006Publication date: January 28, 2010Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Masahiko Okano, Tatsuya Oyama