Acyclic Nitrogen Containing Patents (Class 544/119)
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Publication number: 20110201592Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: October 23, 2008Publication date: August 18, 2011Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Jamieson Caldwell, Antony William Oliver, Tony Michael Raynham, Emma Jane Welsh, Cornelius Albertus Johannes Matijssen
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Publication number: 20110190293Abstract: Quinazolinone compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.Type: ApplicationFiled: April 12, 2011Publication date: August 4, 2011Inventors: Weibo Wang, Liana M. Lagniton, Ryan N. Constantine, Manoj C. Desai
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Publication number: 20110190272Abstract: The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-IR kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.Type: ApplicationFiled: May 6, 2009Publication date: August 4, 2011Applicant: ASTRAZENECA ABInventors: Kevin Daly, Del Valle David, David Scott, Qing Ye
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Patent number: 7977333Abstract: Substituted and pyridines and pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1 and R2 may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using these materials are also disclosed.Type: GrantFiled: November 24, 2003Date of Patent: July 12, 2011Assignee: Bayer Healthcare LLCInventors: Jacques P. Dumas, Stephen J. Boyer, Julie A. Dixon, Teddy K. Joe, Harold C. E. Kluender, Wendy Lee, Dhanapalan Nagarathnam, Robert N. Sibley, Ning Su
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Publication number: 20110136806Abstract: 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: February 15, 2011Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Birgit JUNG
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Publication number: 20110135599Abstract: The present application includes novel inhibitors of HCV, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Applicant: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Mingzhe Ji, Choung U. Kim, Hyung-jung Pyun, Xiaoning C. Sheng, Qiaoyin Wu
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Publication number: 20110136805Abstract: 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: ApplicationFiled: November 3, 2007Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Birgit Jung
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Publication number: 20110130399Abstract: The invention relates to new phthalazine derivatives of formula I, and to processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment especially of a disease that responds to the inhibition of especially the vascular endothelial growth factor receptor kinase, preferably the treatment of a proliferative disease, or the treatment of inflammatory rheumatic or rheumatoid arthritis and/or pain; and the use of such a compound alone or in combination with one or more other pharmaceutically active compounds for the manufacture of a pharmaceutical preparation for the treatment of said diseases in an animal.Type: ApplicationFiled: November 24, 2010Publication date: June 2, 2011Applicant: NOVARTIS AGInventors: Guido BOLD, Paul William MANLEY
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Publication number: 20110124642Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring Z1, R1, p, R3, and R4 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: November 18, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Brian S. Brown, Tongmei Li, Arturo Perez-Medrano, Sridhar Peddi
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Publication number: 20110118258Abstract: Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.Type: ApplicationFiled: May 15, 2008Publication date: May 19, 2011Inventors: Stephen Martin Courtney, Mark Whittaker, Owen Clifford Mather, Christopher John Yarnold, Oliver Robin Barker, Christian Aldo Georges Napoleon Montalbetti, Thomas Hesterkamp, Mihaly Daniel Gardiner
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Publication number: 20110118245Abstract: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.Type: ApplicationFiled: March 17, 2009Publication date: May 19, 2011Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
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Publication number: 20110105479Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.Type: ApplicationFiled: January 10, 2011Publication date: May 5, 2011Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
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Publication number: 20110098283Abstract: The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.Type: ApplicationFiled: May 17, 2010Publication date: April 28, 2011Inventors: Leslie Dakin, Claude Afona Ogoe, David Scott, XiaoLan Zheng
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Publication number: 20110092497Abstract: Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.Type: ApplicationFiled: December 16, 2010Publication date: April 21, 2011Inventors: Martin James Inglis Andrews, Paul Edwards, Reginald Christophe Xavier Brys, Philip Huxley, Wolfgang Schmidt, Veronique Birault, Mark Stuart Chambers, Clifford John Harris, Angus Macleod, Kim Louise Hirst, Juha Andrew Clase, Gregory Bar
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Patent number: 7928133Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: July 24, 2007Date of Patent: April 19, 2011Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
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Publication number: 20110077245Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R3, L, X, Y and Z have defined meanings.Type: ApplicationFiled: December 3, 2010Publication date: March 31, 2011Inventors: Marcel Jozef Maria Van der Aa, Albertus Henricus Maria Theresia Van Heertum, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20110077233Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: October 25, 2010Publication date: March 31, 2011Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Publication number: 20110071149Abstract: The present invention relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I: or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present invention further provides novel compounds and compositions as well as their methods of preparation and use of the same as JAK3 inhibitors in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.Type: ApplicationFiled: February 11, 2010Publication date: March 24, 2011Applicants: REACTION BIOLOGY CORP., SYNERGA LIMITEDInventors: Haiching MA, Sorin Vasile FILIP
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Publication number: 20110071144Abstract: The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group seleType: ApplicationFiled: April 23, 2010Publication date: March 24, 2011Inventors: Andrew Peter THOMAS, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Patent number: 7910731Abstract: The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.Type: GrantFiled: February 26, 2008Date of Patent: March 22, 2011Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
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Publication number: 20110053933Abstract: The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: wherein, each of R1 and R2 independently represents a group such as a hydrogen atom or a halogen atom; R3 represents a group such as a hydrogen atom; each of R4 and R5 independently represents a group such as a hydrogen atom, a halogen atom or a C1-4 alkyl group; each of R6 and R7 independently represents a hydrogen atom or a C1-4 alkyl group; X represents a group such as a C3-10 cycloalkyl group, C6-10 aryl group or a 5- to 10-membered heterocyclic group, which may be substituted with substituent(s) selected from substituent group ?; Y represents a group such as —CO—, —O— or —NRa—, and Ra represents a group such as a hydrogen atom or a C1-4 alkyl group.Type: ApplicationFiled: March 24, 2009Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kayoko Motoki, Kiichi Kawagoe, Shigeyuki Nishinaka, Sachie Masuda, Atsunobu Sakamoto, Satoru Kaneko, Tsuyoshi Arita, Aki Yokomizo
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Publication number: 20110053932Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFR?, PDGFR?, PKC?, p38, Src, SIK, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: June 18, 2008Publication date: March 3, 2011Inventors: Taebo Sim, Truc Ngoc Nguyen, Baogen Wu, Yun He, Yongping Xie, Xing Wang, Guobao Zhang, Nathanael Schiander Gray
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Publication number: 20110039844Abstract: In view of the great potential the quinazoline class of compounds offer, we started the synthesis and screening of a large number of new chemical entities with novel structural features. It has been surprisingly and unexpectedly found that quinazolines having 3-Ethynyl anilino group at the 4th position and specifically substituted alkoxy groups in the 6 and 7 positions, impart much enhanced and special anti-proliferative properties when compared to other prominent members of the quinazoline class of drugs. Also, surprisingly the compounds of this invention are much less toxic and the safety profile is exceedingly beneficial for therapeutic applications. The novel chemical entities described in this invention are designated by the general structure (I) and have not been synthesized earlier nor investigated for their therapeutic benefits and safety profile. Compound (I) is NRC-2694, when structure (A).Type: ApplicationFiled: January 18, 2008Publication date: February 17, 2011Applicant: Natco Pharma LimitedInventors: Ramanadham Jyothi Prasad, Bhujanga Rao Adibhatla Satya, Bollepalli Nageshwar Rao, Nannapaneni Venkaiah Chowdary
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Publication number: 20110039845Abstract: A 2-aminoquinazoline derivative represented by formula (I) {wherein R1 represents a hydrogen atom, or the like, R2 represents a hydrogen atom, R3 represents formula (II) [wherein A1 represents formula (III), or the like, R8 represents lower alkyl, or the like, and R9 represents optionally substituted aryl, or the like], R4 represents hydroxy, or the like, and R5 represents optionally substituted aryl, or the like}, or a pharmaceutically acceptable salt thereof is provided.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hajime Kashima, Tomoyuki Nishikawa, Yusuke Yamada, Toshihiro Seike, Yoshisuke Nakasato, Hiroshi Umehara
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Publication number: 20110034459Abstract: Compounds of formula (I) in which: R1 is: R2 is —CH3 or —CH2CH3; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the compound of formula (I) and a pharmaceutically acceptable carrier. Processes for preparing the compound of formula (I). Methods of inhibiting a receptor tyrosine kinase in a subject in need thereof. Methods of inhibiting the growth of a tumor cell in a subject in need thereof. Methods of treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods of treating HER2 positive breast cancer in a subject in need of treatment for HER2 positive breast cancer. Methods of treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 9, 2010Publication date: February 10, 2011Applicant: Natco Pharma Ltd.Inventors: Bhujanga rao ADIBHATLA KALI SATYA, Ramanadham Jyothi Prasad, Bollepalli Nageshwara Rao, Nannapaneni Venkaiah Chowdary
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Publication number: 20110021495Abstract: 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: January 15, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jesus Gonzalez, III, Dean Wilson, Andreas Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin Petzoldt, Lev T.D. Fanning, Timothy Neubert, Roger Tung, Esther Martinborough, Nicole Hilgraf
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Publication number: 20110009391Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: July 26, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Alain Jean BRAUN, Olivier CRESPIN, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Cecile PASCAL, Christophe PHILIPPO, Olivier VENIER
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Patent number: 7855204Abstract: This invention relates to novel quinazoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by inhibiting cell surface tyrosine receptor kinases.Type: GrantFiled: January 22, 2009Date of Patent: December 21, 2010Assignee: Concert Pharmaceuticals Inc.Inventor: Roger Tung
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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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Publication number: 20100317659Abstract: Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: February 26, 2010Publication date: December 16, 2010Inventors: Sunny Abraham, Qi Chao, Michael J. Hadd, Mark W. Holladay, Gang Liu, Eduardo Setti
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Publication number: 20100311965Abstract: An object of the present invention is to provide compounds which are useful as protein kinase inhibitors.Type: ApplicationFiled: December 26, 2008Publication date: December 9, 2010Applicants: CARNA BIOSCIENCES INC., CRYSTAL GENOMICS, INC.Inventors: Masaaki Sawa, Koichi Yokota, Hideki Moriyama, Myoungyoup Shin, Seonggu Ro, Joong Myung Cho
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Publication number: 20100305119Abstract: A method of treating an anthrax infection wherein a compound of formula I wherein R1 and R2 represent, independently of one another unsubstituted or specifically substituted C1-4alkoxy; and R3 represents hydrogen; cyano; unsubstituted or specifically substituted C1-6alkyl; C3-6cycloalkyl; C2-6alkenyl; C7-18bicyclyl; aryl, aryl-C1-4alkyl, aryl-Q-C1-4alkyl heteroaryl, heterocyclyl or heterocyclyl-C1-6alkyl, wherein aryl denotes a mono- or poly-nucleous group with 6 to 14 ring carbon atoms; heterocyclyl denotes a 4- to 6-membered non-aromatic heterocyclic group comprising 1 to 3, nitrogen, oxygen and/or sulfur atoms; heteroaryl denotes a mono- or polynuclear heteroaromatic group consisting 5- and/or 6-membered rings and comprising 5 to 13 carbon atoms and 1 to 4, nitrogen, oxygen and/or sulfur atoms; and Q means —SO— or —SO2—; or a pharmaceutically acceptable salt, solvate or hydrate or a prodrug thereof; is administered to said subject in a quantity effective to inhibit, suppress, or expel an anthrax infType: ApplicationFiled: September 25, 2006Publication date: December 2, 2010Inventors: Jurg Dreier, William Barrow, Esther Barrow
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Publication number: 20100298322Abstract: 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: ApplicationFiled: January 2, 2009Publication date: November 25, 2010Inventors: Rogier Adriaan Smits, Regorius Leurs, Iwan Jozef Philomena De Esch
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Publication number: 20100298324Abstract: The invention described herein relates to certain 4-oxo-2-thioxo-1,2,3,4-tetrahydro-7-quinazolinecarboxamide derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: December 19, 2008Publication date: November 25, 2010Applicant: SMITH KLINE BEECHAM CORPORATIONInventors: Dimitar B. Gotchev, Jian Jin, Yonghui Wang
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Publication number: 20100280008Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: June 30, 2010Publication date: November 4, 2010Applicant: Amgen Inc.Inventors: Holly Deak, Stephanie Geuns-Meyer, Brian L. Hodous, Zihao Hua, Matthew Martin, Hanh Nho Nguyen, Philip Olivieri, Kathleen Panter, Karina Romero, Laurie Schenkel, Ryan White
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Publication number: 20100267949Abstract: A method of synthesizing 6,7-substituted 4-anilino quinazoline employs 3,4-substituted benzoic acid as an initial reactant, and the 6,7-substituted 4-anilino quinazoline is obtained by an esterifying step, a nitrating step, a reducing step, a cyclizing step, and an one-pot reaction. In the above method, the initial reactant has low cost and yield. of the 6,7-substituted 4-anilino quinazoline is high, therefore, production cost can be reduced effectively, and competitive power of the product of the 6,7-substituted 4-anilino quinazoline can be improved.Type: ApplicationFiled: May 13, 2009Publication date: October 21, 2010Inventors: Kae-Shyang Shih, Yu-Jung Hsieh, Ching-Wei Liu
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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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Patent number: 7816351Abstract: Disclosed herein are 5,?-dimethylthieno[2,3-d]pyrimidine derivatives useful as antiviral agents. More particularly, disclosed are 5,?-dimethylthieno[2,3-djpyrimidine derivatives represented by Formula 1, having an excellent inhibitory effect on the proliferation of hepatitis C virus (HCV), pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the prevention and treatment of hepatitis C virus (HCV), containing, as active ingredients, these compounds. The 5,6-dimethylthieno[2,3-d]pyrimidine derivatives represented by Formula 1 have an excellent effect of inhibiting the proliferation of hepatitis C virus and also have low toxicity. Thus, these compounds are available as agents for the prevention and treatment of hepatitis C.Type: GrantFiled: September 23, 2005Date of Patent: October 19, 2010Assignee: Equispharm Co., LtdInventors: Cheol Kyu Han, Jeonghyeok Yoon, Nam-Doo Kim, Jin-ah Kim
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Publication number: 20100256120Abstract: The invention concerns a compound of the Formula I wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen and R4 is, (1-6C)alkyl or (1-6C)alkoxy; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: August 7, 2006Publication date: October 7, 2010Inventors: Dearg Sutherland Brown, Ian Alun Nash, Steve Swallow
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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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Publication number: 20100234324Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R3 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: June 16, 2008Publication date: September 16, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
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Publication number: 20100222331Abstract: The present invention encompasses compounds of general Formula (1) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Bodo Betzemeier, Guido Boehmelt, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Daniel Kuhn, Jens Juergen Quant, Ulrich Reiser, Otmar Schaaf, Flavio Solca, Heinz Stadtmueller, Ulrike Tontsch-Grunt, Matthias Treu, Stephan Karl Zahn
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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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Publication number: 20100221259Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Publication number: 20100216791Abstract: The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.Type: ApplicationFiled: August 15, 2007Publication date: August 26, 2010Applicant: ASTRAZENECAInventors: Brian Aquila, Donald J. Cook, Craig Johnstone, Stephen Lee, Paul Lyne, David Alan Rudge, Melissa Vasbinder, Haixia Wang
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Publication number: 20100204224Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels.Type: ApplicationFiled: July 7, 2006Publication date: August 12, 2010Applicant: VERNALIS R & D LIMITEDInventors: Richard Hamlyn, Glyn Addison, Christopher Geoffrey Earnshaw, Harry Finch, Mike Huckstep, Rosemary Lynch, Sarah Mellor
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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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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: 20100190766Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson