Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
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Patent number: 8563719Abstract: The present invention provides a process for making lapatinib and its pharmaceutically acceptable salt by use of new intermediates. A new process for obtaining a pharmaceutical form of lapatinib ditosylate monohydrate is also provided.Type: GrantFiled: March 23, 2011Date of Patent: October 22, 2013Assignee: Scinopharm Taiwan, Ltd.Inventors: Yung-Fa Chen, Julian Paul Henschke, Yuanlian Liu, Guodong Chu, Xiaoheng Zhang
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Publication number: 20130274252Abstract: The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.Type: ApplicationFiled: November 2, 2012Publication date: October 17, 2013Inventors: Anjali Pandey, Robert M. Scarborough, Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shinichi Ide, Eiji Tsukuda, Junko Sasaki, Shoji Oda
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Publication number: 20130266563Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.Type: ApplicationFiled: May 17, 2013Publication date: October 10, 2013Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
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Patent number: 8552018Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: GrantFiled: March 18, 2011Date of Patent: October 8, 2013Assignees: Arizona Board of Regents on behalf of the University of Arizona, Astex Pharmaceutials, Inc.Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Steven L. Warner, James Welsh
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Publication number: 20130252942Abstract: The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: November 11, 2011Publication date: September 26, 2013Inventors: Bayard R. Huck, Reinaldo Jones, Yufang Xiao, Constantin Neagu, Donald Bankston, Andreas Goutopoulos
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Publication number: 20130252978Abstract: 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: May 23, 2013Publication date: September 26, 2013Applicant: HETERO RESEARCH FOUNDATIONInventors: BANDI PARTHASARADHI REDDY, KURA RATHNAKAR REDDY, RAPOLU RAJI REDDY, DASARI MURALIDHARA REDDY, THUNGATHURTHY SRINIVAS RAO
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Publication number: 20130245256Abstract: This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: September 7, 2012Publication date: September 19, 2013Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
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Publication number: 20130244994Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: ApplicationFiled: February 15, 2013Publication date: September 19, 2013Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
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Publication number: 20130236473Abstract: A major object of the present invention is to provide a novel therapeutic or prophylactic agent for at least one disease or symptom selected from the group consisting of autoimmune diseases, inflammatory diseases, allergic diseases, and symptoms accompanying organ transplants; the therapeutic or prophylactic agent artificially controls the activity of IL-6 amplifier, thus controlling immune reactions in living organisms. Another object of the present invention is to provide an immunosuppressant, an inflammatory cytokine production inhibitor, and an IL-6 amplifier inhibitor. The compound that inhibits expression of the function of a protein belonging to ErbB1 pathway provided as means for achieving the object is capable of suppressing the activity of IL-6 amplifier, thereby reducing production of inflammatory cytokine such as IL-6.Type: ApplicationFiled: September 14, 2011Publication date: September 12, 2013Applicant: OSAKA UNIVERSITYInventors: Toshio Hirano, Masaaki Murakami
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Patent number: 8530486Abstract: A compound of the formula (I) wherein X is CR1 or N; Y is CR3 or N; R1, R3, R4, R5 and R6 are independently H, F, Cl, Br, I, or a hydrocarbon group which optionally contains one or more heteroatoms; R7 is a heterocyclic group including one or more N atoms; R? is Rx or NRyRz wherein Rx, Ry and Rz are each H or the same or different groups, including cyclic groups formed by Ry and Rz with the N atom, of up to 20 C atoms and optionally including up to 3 further heteroatoms selected from N, O and S; or a pharmaceutically acceptable salt, ester or solvate thereof.Type: GrantFiled: January 2, 2009Date of Patent: September 10, 2013Assignee: Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en PatientenzorgInventors: Rogier Adriaan Smits, Regorius Leurs, Iwan Jozef Philomena De Esch
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Patent number: 8530654Abstract: Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.Type: GrantFiled: February 15, 2008Date of Patent: September 10, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Eiichi Yamamoto, Osamu Asano, Jun Niijima, Kazumasa Nara
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Publication number: 20130225613Abstract: 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: April 2, 2013Publication date: August 29, 2013Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Masahiko OKANO, Tatsuya OYAMA
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Publication number: 20130217709Abstract: The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: July 28, 2011Publication date: August 22, 2013Applicant: MERCK PATENT GMBHInventors: Bayard R. Huck, Xiaoling Chen, Constantin Neagu, Reinaldo Jones, Yufang Xiao, Igor Mochalkin
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Publication number: 20130217661Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.Type: ApplicationFiled: March 18, 2013Publication date: August 22, 2013Applicant: HUTCHISON MEDIPHARMA ENTERPRISES LIMITEDInventor: Hutchison Medipharma Enterprises Limited
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Patent number: 8513262Abstract: 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: GrantFiled: January 22, 2010Date of Patent: August 20, 2013Assignee: GlaxoSmithKline LLCInventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
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Publication number: 20130210844Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: February 7, 2013Publication date: August 15, 2013Applicant: Glenmark Pharmaceuticals S.A.Inventor: Glenmark Pharmaceuticals S.A.
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Publication number: 20130210842Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.Type: ApplicationFiled: July 22, 2011Publication date: August 15, 2013Applicant: GENERICS [UK] LIMITEDInventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
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Patent number: 8507502Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: November 9, 2009Date of Patent: August 13, 2013Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
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Publication number: 20130184297Abstract: The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.Type: ApplicationFiled: August 30, 2011Publication date: July 18, 2013Applicant: XUANZHU PHARMA CO., LTD.Inventors: Zhenhua Huang, Yanyan Dong
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Publication number: 20130178624Abstract: 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 C1-4Type: ApplicationFiled: January 18, 2013Publication date: July 11, 2013Applicant: Janssen Pharmaceutica N.V.Inventor: Janssen Pharmaceutica N.V.
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Publication number: 20130172373Abstract: Provided are certain quinazoline compounds, compositions thereof and methods of use thereof. These quinazoline compounds can effectively inhibit the overexpression and/or overactivity of epidermal growth factor receptor (EGFR).Type: ApplicationFiled: May 25, 2011Publication date: July 4, 2013Applicant: Hutchison Medipharma LimitedInventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
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Publication number: 20130164847Abstract: The present invention pertains to methods of using protein tyrosine kinase (PTK) inhibitors for inducing cell differentiation of mesenchymal stem cells into cardiac cells, and a pharmaceutical composition comprising the differentiated cardiac cells thereof to treat heart diseases. The transplantation of mesenchymal stem cells to the heart provides immunological and functional improvements, but does not provide electrical stability. However, the mesenchymal stem cells treated with PTK inhibitors are induced to be differentiated into cardiogenic cells to provide electrical stability as the electromechanical integration with host heart tissue is improved, and it is thus possible to effectively treat cardiac diseases such as cardiac infarction, cardiac insufficiency, arrhythmia and the like.Type: ApplicationFiled: August 17, 2011Publication date: June 27, 2013Applicant: PHARMICELL. CO., LTD.Inventors: Ki-Chul Hwang, Yang-Soo Jang
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Publication number: 20130165458Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRa Rb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.Type: ApplicationFiled: December 27, 2011Publication date: June 27, 2013Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Jiann-Jyh Huang, Chu-Bin Liao, Pao-Nien Chen
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Patent number: 8471012Abstract: 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: GrantFiled: August 31, 2011Date of Patent: June 25, 2013Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivas Rao
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Patent number: 8466165Abstract: 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: April 5, 2010Date of Patent: June 18, 2013Assignee: 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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Patent number: 8455506Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (I) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.Type: GrantFiled: April 14, 2009Date of Patent: June 4, 2013Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Stephen Gould
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Publication number: 20130137867Abstract: A novel crystal of antitumor drug erlotinib base and its preparation method are provided in the present invention. A preparation method of erlotinib hydrochloride with high-purity is also provided in the present invention.Type: ApplicationFiled: August 12, 2011Publication date: May 30, 2013Applicant: Zhejiang Huahai Pharmaceutical Co., Ltd.Inventors: Ke Xiang, Min Xu
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Publication number: 20130137708Abstract: The present invention sets forth a new chemical genetic approach for engineering kinase enzymes with a cysteine gatekeeper residue as well as for developing electrophilic inhibitors thereto. The present invention also provides a Src proto-oncogenic tyrosine kinase with a cysteine gatekeeper that recapitulates wild type activity and can be irreversibly inhibited both in vitro and in cells. The present invention also provides methods and compositions for modulating kinases and for treating kinase-associated diseases.Type: ApplicationFiled: November 30, 2012Publication date: May 30, 2013Applicant: The Regents of The University of CaliforniaInventor: The Regents of The University of California
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Publication number: 20130137711Abstract: The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof.Type: ApplicationFiled: November 19, 2012Publication date: May 30, 2013Inventors: Shanghai Allist Pharmaceuticals, Inc., Jun Cheng
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Publication number: 20130137677Abstract: The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: July 1, 2011Publication date: May 30, 2013Applicant: MERCK PATENT GMBHInventors: Bayard R. Huck, Constantin Neagu, Reinaldo Jones, Lizbeth Celeste DeSelm, Yufang Xiao, Srinivasa R. Karra, Ruoxi Lan, Igor Mochalkin, Amanda E. Sutton, Thomas E. Richardson
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Patent number: 8450482Abstract: Processes for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline, salts thereof, and the intermediates used in the process are described.Type: GrantFiled: April 22, 2010Date of Patent: May 28, 2013Assignee: Astrazeneca ABInventors: Kay Alison Boardman, Oliver Robert Cunningham, William Robert Fraser Goundry, David Dermot Patrick Laffan
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Publication number: 20130131341Abstract: 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: November 19, 2012Publication date: May 23, 2013Applicant: NATCO PHARMA LIMITEDInventor: Natco Pharma Limited
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Publication number: 20130123270Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.Type: ApplicationFiled: March 26, 2012Publication date: May 16, 2013Applicant: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Prakash Raman, Francois Soucy, Qing Ye, Shomir Ghosh
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Publication number: 20130123497Abstract: There is provided a crystalline form of Lapatinib, termed APO-I, and methods for making APO-I. There is also provided a crystalline solvate form of Lapatinib, termed APO-II, and methods for making APO-II.Type: ApplicationFiled: April 21, 2011Publication date: May 16, 2013Applicant: APOTEX PHARMACHEM INC.Inventors: Carlos Zetina-Rocha, Eduardo Gustavo Cammisa, Gamini Weeratunga
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Publication number: 20130109706Abstract: Quinazoline derivatives are provided that specifically inhibit proliferation of T cells without affecting the level of IL-2 secreted from said T cells. These compounds as well as pharmaceutical composition comprising them are useful for the treatment of indications mediated by T cell proliferation.Type: ApplicationFiled: January 27, 2011Publication date: May 2, 2013Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERSALEM LTD.Inventors: Alexander Levitzki, Idit Sagiv
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Patent number: 8431586Abstract: 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: GrantFiled: October 3, 2006Date of Patent: April 30, 2013Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiko Okano, Tatsuya Oyama
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Patent number: 8426430Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.Type: GrantFiled: June 30, 2008Date of Patent: April 23, 2013Assignee: Hutchison Medipharma Enterprises LimitedInventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
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Patent number: 8404698Abstract: Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also disclosed.Type: GrantFiled: June 16, 2008Date of Patent: March 26, 2013Assignee: Rexahn Pharmaceuticals, Inc.Inventors: Young Bok Lee, Chang Ho Ahn
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Patent number: 8404839Abstract: 4-(3-chloro-2-fluoroanilino)-7 methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.Type: GrantFiled: October 14, 2011Date of Patent: March 26, 2013Assignee: Astrazeneca ABInventor: Andrew Hornby Dobson
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Patent number: 8399461Abstract: The present invention relates to bicyclic heterocycles of general formula the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: November 3, 2007Date of Patent: March 19, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung
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Patent number: 8399667Abstract: 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: GrantFiled: February 16, 2010Date of Patent: March 19, 2013Assignee: Astrazeneca ABInventors: Robert Hugh Bradbury, Laurent Francois Andre Hennequin, Jason Grant Kettle
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Publication number: 20130065902Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.Type: ApplicationFiled: March 21, 2011Publication date: March 14, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Heinz Fretz, Julien Hazemann, Sylvia Richard-Bildstein, Romain Siegrist
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Patent number: 8394954Abstract: Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same.Type: GrantFiled: March 26, 2008Date of Patent: March 12, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Bandari Rajendra Prasad
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Patent number: 8389531Abstract: 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: GrantFiled: July 11, 2007Date of Patent: March 5, 2013Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
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Patent number: 8372856Abstract: Erlotinib hydrochloride hydrate is formed from an aqueous solution and is useful as a pharmaceutical and as a purification intermediate.Type: GrantFiled: October 25, 2007Date of Patent: February 12, 2013Assignee: Synthon BVInventor: Raymond J. H. Westheim
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Publication number: 20130035350Abstract: This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HER1 tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: December 21, 2010Publication date: February 7, 2013Inventors: Qiang Zhang, Hongwen Zhu
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Publication number: 20130029942Abstract: 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: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.
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Publication number: 20130018033Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: August 27, 2010Publication date: January 17, 2013Applicant: ARRAY BIOPHARMA INC.Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Wendy Lee, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Guiling Zhao, Alexandre J. Buckmelter, Jonas Grina, Joshua D. Hansen, Ellen Laird, David Moreno, Li Ren, Steven Mark Wenglowsky
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Publication number: 20130012528Abstract: This invention relates to novel compounds and hydrochloric acid salts thereof. More specifically, this invention relates to novel compounds and hydrochloric acid salts thereof derived from erlotinib. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an epidermal growth factor receptor tyrosine kinase (EGFR) inhibitor, such as erlotinib.Type: ApplicationFiled: July 5, 2011Publication date: January 10, 2013Inventor: Xueheng Cheng
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Patent number: 8349855Abstract: 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: GrantFiled: September 11, 2007Date of Patent: January 8, 2013Assignee: Natco Pharma LimitedInventors: Ramanadham Jyothi Prasad, Bhujanga rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary