Piperidinyl Or Tetrahydropyridyl Patents (Class 514/266.22)
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Publication number: 20110312936Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.Type: ApplicationFiled: June 16, 2011Publication date: December 22, 2011Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
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Publication number: 20110311519Abstract: Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazoline analogue such as halofuginone.Type: ApplicationFiled: June 17, 2011Publication date: December 22, 2011Applicant: Washington UniversityInventors: Steven L. Teitelbaum, Carl J. DeSelm
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Patent number: 8080557Abstract: 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, L1, L2, X, Y and Z have defined meanings.Type: GrantFiled: June 28, 2005Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica, NVInventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacbous Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20110294807Abstract: Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: January 8, 2010Publication date: December 1, 2011Inventor: Henrik C. Hansen
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Publication number: 20110293691Abstract: Provided herein are multimodal barrier materials useful for preventing adhesions in a subject, which may include a collagen, a collagen deposition inhibitor and/or a chitosan.Type: ApplicationFiled: April 28, 2011Publication date: December 1, 2011Inventors: Kurt R. Weber, Steve J. Hodges, Scott A. Washburn
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Patent number: 8067436Abstract: 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: GrantFiled: May 24, 2007Date of Patent: November 29, 2011Assignee: 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, Morrisson B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
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Publication number: 20110288022Abstract: The invention provides for the use of carbonic anhydrase activators; protein kinase C activators and FGF-18 to treat depressive disorders. The invention also relates to improved animal models and methods for screening and identifying compounds the treatment of depressive disorders.Type: ApplicationFiled: June 3, 2011Publication date: November 24, 2011Inventors: Miao-Kun Sun, Daniel L. Alkon
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Publication number: 20110281867Abstract: Compositions and methods are provided for using tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using Abl-family tyrosine kinase inhibitors to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses.Type: ApplicationFiled: December 16, 2010Publication date: November 17, 2011Inventors: Daniel KALMAN, William Gerard Bornmann, Patrick Michael Reeves, Alyson Irene Swimm
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Publication number: 20110281860Abstract: The present invention relates to the use of quinazoline derivatives, which show EGFR inhibitory activity, for the prevention and/or treatment of virus-induced diseases, preferably virus induced respiratory diseases and exacerbation in chronic airway diseases such as COPD or asthma.Type: ApplicationFiled: August 13, 2009Publication date: November 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Birgit Jung
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Publication number: 20110263532Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.Type: ApplicationFiled: August 11, 2009Publication date: October 27, 2011Applicant: President and Fellows of Harvard CollegeInventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee
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Publication number: 20110262566Abstract: Provided is a therapeutic agent for lower urinary tract symptom consisting of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof or a combination of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof and a compound selected from the group consisting of ?1-adrenergic receptor blockers, 5-? reductase inhibitors, antiandrogen drugs, ?3-adrenergic receptor agonists, phosphodiesterase V inhibitors, plant preparations, amino acid preparations, herbal medicines and the like. Also provided is a method of using in combination the above-described therapeutic agent and a surgical treatment such as bladder distention or surgery.Type: ApplicationFiled: November 2, 2009Publication date: October 27, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Natsuko Goto, Setsuko Yamamoto
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Publication number: 20110245225Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R5 and X 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: November 12, 2009Publication date: October 6, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTINGInventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
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Publication number: 20110237610Abstract: 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: ApplicationFiled: October 12, 2010Publication date: September 29, 2011Applicant: AstraZeneca ABInventors: Bernard Christophe Barlaam, Laurent Francois Andre Hennequin, Christopher Thomas Halsall
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Publication number: 20110212100Abstract: This invention provides methods and compositions for modulating the development and/or expansion of Th17 cells for use, for example, in the treatment of autoimmune diseases, persistent inflammatory diseases, infectious diseases and other Th17 related and/or IL-17 related diseases.Type: ApplicationFiled: August 15, 2008Publication date: September 1, 2011Inventors: Tracy Keller, Malcolm Whitman, Mark S. Sundrud, Anjana Rao
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Publication number: 20110212165Abstract: The present invention relates to pharmaceutical compositions comprising as an active ingredient an isolated, chirally pure D-enantiomer of the quinazolinone derivative halofuginone having increased therapeutic activity and decreased side effects compared to the corresponding racemic mixtures, the composition being substantially free of the L-enantiomer and useful in the treatment of diseases and disorders associated with fibrotic conditions or cell proliferation.Type: ApplicationFiled: May 6, 2011Publication date: September 1, 2011Inventors: Mordechai Erez, Karin Halevi
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Publication number: 20110212939Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity.Type: ApplicationFiled: July 10, 2009Publication date: September 1, 2011Applicant: Prosidion LimitedInventors: Lisa Sarah Bertram, Philip Graham Clarke, Graham John Dawson, Peter Timothy Fry, Matthew Colin Thor Fyfe, William Gattrell, Revathy Perpetua Jeevaratnam, John Keily, Thomas Martin Krulle, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Simon Andrew Swain
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Publication number: 20110207741Abstract: Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.Type: ApplicationFiled: February 22, 2011Publication date: August 25, 2011Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Samuel Dudley
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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: 20110201632Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 15, 2009Publication date: August 18, 2011Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
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Publication number: 20110195956Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: August 31, 2009Publication date: August 11, 2011Inventors: Matthew Burger, Jiong Lan
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Patent number: 7994182Abstract: The subject of the present invention are quinazoline derivatives and their pharmaceutically acceptable salts of general formula (I), that inhibit a DNA-repairing enzyme, poly(ADP-ribose) polymerase (PARP), enabling them to be used for the preparation of pharmaceutical compositions for preventing or treating illnesses where PARP-inhibition yields a beneficial effect. In general formula (I) R1 stands for either hydrogen or a group of general formula (a); R2 stands for a) hydrogen or C1-6 alkyl group, if R1 is other than hydrogen, and b) if R1 is hydrogen, then R2 may be a group of general formula (b), (c) or (d). The subject of the present invention also embraces the preparation processes of the compounds described above.Type: GrantFiled: April 30, 2004Date of Patent: August 9, 2011Assignee: Pecsi TudomanyegyetemInventors: Balázs Sümegi, Kálmán Hideg, Tamás Kálai
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Publication number: 20110190322Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for wound healing preferably in diabetic patients.Type: ApplicationFiled: August 13, 2009Publication date: August 4, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas Klein, Michael Mark
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Publication number: 20110178066Abstract: Chemical agents, such as derivatives of hydroxypiperidine moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: July 21, 2010Publication date: July 21, 2011Inventors: Norman E. Ohler, Jeffrey W. Watthey, Qin Zong, Paul E. Young, Kathryn J. Strand, Stanislaw Pikul
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Publication number: 20110152297Abstract: The invention concerns quinazoline derivatives of the Formula I, or pharmaceutically acceptable salts thereof: wherein each of R1, R2, R3, R4 and m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, and, for example, EGFR tyrosine kinase.Type: ApplicationFiled: February 24, 2006Publication date: June 23, 2011Inventors: Christopher Thomas Halsall, Laurent Francois Andre Hennequin, Alleyn Thomas Plowright, Richard Storey, Kieran Lennon
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Publication number: 20110152243Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 21, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Neil Wishart, Theresa Dunstan, Jeremy J. Edmunds, Anna M. Ericsson, Catherine R. Ferenz, Adrian D. Hobson, David C. Ihle, Kent D. Stewart, Lei Wang, Lu Wang
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Publication number: 20110136839Abstract: The present invention is a novel analgesic combination and its use. It is classified to he an invention in the field of medicine and technology. The purpose of this invention is to solve the problem that existing analgesics does not effectively attenuate pain or produces serious side-effects in clinic. The ingredients of the analgesic combination include ketanserin and propranolol. This combination is used to make a drug to treat pain. Because the ingredients of the analgesic combination target peripheral receptors, the unwanted effects could be only minimal. The big advantage of this combination is that each of the ingredients acts on the different receptors producing the synergizing analgesic. Therefore, the analgesia that the combination produces is remarkable and the effective doses are low.Type: ApplicationFiled: August 30, 2010Publication date: June 9, 2011Inventor: Yanguo HONG
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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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Patent number: 7951955Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: GrantFiled: May 1, 2008Date of Patent: May 31, 2011Assignee: Biota Scientific Management Pty LtdInventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Patent number: 7947690Abstract: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.Type: GrantFiled: October 17, 2005Date of Patent: May 24, 2011Assignee: Astellas Pharma Inc.Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
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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: 20110117084Abstract: This invention relates to novel quinazoline derivatives and their acceptable acid addition 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 inhibitory activity against the VEGF receptor tyrosine kinase.Type: ApplicationFiled: January 22, 2009Publication date: May 19, 2011Applicant: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Publication number: 20110105505Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 28, 2009Publication date: May 5, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNGInventors: Frank Stieber, Timo Heinrich, Dirk Wienke
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Publication number: 20110097321Abstract: The invention relates to agents which possess anti-angiogenic activity and are accordingly useful in methods of treatment of disease states associated with angiogenesis in the animal or human body. More specifically the invention concerns a combination of an antagonist of the biological activity of Angiopoietin-2 and an antagonist of the biological activity of VEGF-A, and/or KDR, and/or Flt1, and uses of such antagonists.Type: ApplicationFiled: September 24, 2010Publication date: April 28, 2011Applicant: ASTRAZENECA ABInventors: David Charles BLAKEY, Jeffrey Lester BROWN, Stephen Charles EMERY
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Publication number: 20110092480Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.Type: ApplicationFiled: December 20, 2010Publication date: April 21, 2011Inventors: Steven Joseph Brickner, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
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Patent number: 7928107Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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: March 3, 2006Date of Patent: April 19, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Andreas Termin, Jesus Gonzalez, Lev Fanning, Timothy Neubert, Paul Krenitsky, Pramod Joshi, Dennis Hurley, Urvi Sheth
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Publication number: 20110086870Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human, which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises one of: the administration of ZD6474 in combination with 5-FU; the administration of ZD6474 in combination with CPT-11; and the administration of ZD6474 in combination with 5-FU and CPT-11; to a pharmaceutical composition comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11; to a combination product comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11, for use in a method of treatment of a human or animal body by therapy; to a kit comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11; to the use of one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11, iType: ApplicationFiled: December 20, 2010Publication date: April 14, 2011Applicant: AstraZeneca ABInventors: Stephen Robert Wedge, Anderson Joseph Ryan
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Publication number: 20110077246Abstract: 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: ApplicationFiled: December 6, 2010Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO.Inventors: Frank HIMMELSBACH, Birgit JUNG, Flavio SOLCA
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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: 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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Publication number: 20110065736Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.Type: ApplicationFiled: April 15, 2010Publication date: March 17, 2011Applicant: AstraZeneca ABInventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Publication number: 20110039840Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: April 14, 2009Publication date: February 17, 2011Applicant: DAC S.R.L.Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
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Publication number: 20110039823Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: ApplicationFiled: April 11, 2008Publication date: February 17, 2011Applicant: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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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: 20110028473Abstract: Methods employing and uses of a compound of formula (I) in inhibiting the growth of a tumor cell in a subject in need thereof. Methods employing and uses of a compound of formula (I) in treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods employing and uses of a compound of formula (I) in treating HER-2 positive breast cancer in a subject in need of treatment for HER-2 positive breast cancer. Methods employing and uses of a compound of formula (I) in 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 3, 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: 20110027362Abstract: The present invention provides a tablet having improved dissolution property, which comprises (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof as an active component, and a production method thereof. A film-coated tablet obtained by mixing granulated particles obtained by granulating a mixture containing (a) the aforementioned active component, (b) one or more kinds of fillers selected from lactose, D-mannitol, erythritol and crystalline cellulose, (c) a cellulose-based disintegrant and (d) a water-soluble binder with a later powder containing (e) one or more kinds of fillers selected from lactose, D-mannitol and crystalline cellulose and/or (f) a cellulose-based disintegrant, forming the mixture, and applying film coating.Type: ApplicationFiled: February 10, 2009Publication date: February 3, 2011Inventors: Makiko Yanagida, Hiroyuki Nishii, Masayuki Nakazono
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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: 20110020338Abstract: The invention relates to the use of compounds of formula (I) or (II) in the treatment of mammalian target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.Type: ApplicationFiled: March 24, 2009Publication date: January 27, 2011Inventor: Carlos Garcia-Echeverria
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Patent number: 7875621Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions containing compounds of formula (I) wherein R1, R3, L, X, Y and Z have defined meanings.Type: GrantFiled: June 28, 2005Date of Patent: January 25, 2011Assignee: Janssen Pharmaceutica NVInventors: Marcel Jozef Maria Van Der Aa, Albertus Henricus Maria Theresia Van Heertum, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijin Leopold Wouters
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Patent number: 7863281Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, A, B, C, D, E and X are defined as in claim 1, 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: December 19, 2007Date of Patent: January 4, 2011Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Birgit Jung, Flavio Solca