Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
Type:
Application
Filed:
October 30, 2009
Publication date:
June 24, 2010
Inventors:
Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Xiaogao Liu, Bin Ma, Daniel M. Scott, Zhan Shi, Jermaine Thomas, Arthur G. Taveras, Guo Zhu Zheng
Abstract: The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.
Type:
Application
Filed:
December 18, 2009
Publication date:
June 10, 2010
Inventors:
Hartmut REHWINKEL, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
Abstract: Disclosed are methods for the preparation of compounds of formula (I): wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description.
Type:
Grant
Filed:
August 13, 2009
Date of Patent:
June 8, 2010
Assignee:
Glaxo Group Limited
Inventors:
Markus Bergauer, Barbara Bertani, Matteo Biagetti, Steven Mark Bromidge, Alessandro Falchi, Colin Philip Leslie, Giancarlo Merlo, Domenica Antonia Pizzi, Marilisa Rinaldi, Luigi Piero Stasi, Jessica Tibasco, Antonio Kuok Keong Vong, Simon Edward Ward
Abstract: 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:
Grant
Filed:
September 2, 2004
Date of Patent:
May 11, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jesus E. Gonzalez, III, Dean M. Wilson, Andreas P. Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin J. Petzoldt, Lev Tyler Dewey Fanning, Timothy D. Neubert, Roger D. Tung, Esther Martinborough, Nicole Zimmerman
Abstract: The invention relates to substituted quinazolines and to methods for the production thereof, in addition to the use thereof in the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, especially against cytomegaloviruses.
Abstract: Compositions of midazolam, a benzodiazapine, in concentrations of 35-100 mg/ml are disclosed for the treatment of anxiety, epilepsy and epileptic seizures, invasive surgical procedures and diagnostic procedures and sedation. These compositions are particularly characterized by a solubilizer such an propylene glycol. Preferably, the compositions are aqueous solutions for intranasal administration.
Type:
Grant
Filed:
January 13, 2005
Date of Patent:
April 20, 2010
Inventor:
Franciscus Wilhelmus Henricus Maria Merkus
Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 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 anti-invasive agent in the containment and/or treatment of solid tumor disease.
Type:
Grant
Filed:
November 21, 2005
Date of Patent:
April 13, 2010
Assignee:
AstraZeneca AB
Inventors:
Laurent François André Hennequin, Patrick Ple
Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 protease that comprise a compound comprising the formula: wherein Q is selected from the group of CO, SO, SO2, or C?NR9; and R1, R2, R3 and R4 are as defined herein.
Type:
Grant
Filed:
March 24, 2004
Date of Patent:
March 30, 2010
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
Abstract: The present invention relates to a compound of formula (I) or isomers thereof, or pharmaceutically acceptable salts or hydrates thereof. The present invention further relates to processes for the preparation of the compounds of formula (I) and optical isomers, and to the use of the compounds of formula (I), or isomers thereof, or pharmaceutically acceptable salts or hydrates thereof as medicaments, in particular as medicaments for the treatment and prevention of Hepatitis B.
Type:
Application
Filed:
January 3, 2008
Publication date:
March 25, 2010
Applicant:
BEIJING MOLECULE SCIENCE AND TECHNOLOGY CO., LTD
Abstract: The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly ?-type, ?-type, ?-type, ?-type, and ?-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.
Abstract: The present invention relates generally to therapeutic agents, formulations comprising them and their use in the treatment, amelioration and/or prophylaxis of glioma brain tumours and related conditions. The therapeutic agent comprises two fused 6-membered rings with at least a nitrogen at position 1 and a hydroxyl at position 8.
Type:
Application
Filed:
June 22, 2007
Publication date:
March 18, 2010
Applicant:
PRANA BIOTECHNOLOGY LIMITED
Inventors:
Ashley Bush, Penelope Jane Huggins, Jack Gordon Parsons, Gaik Beng Kok, Vijaya Kenche
Abstract: 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:
Grant
Filed:
March 3, 2004
Date of Patent:
March 16, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jesus E. Gonzalez, III, Dean Mitchell Wilson, Andreas Peter Termin, Peter Diederik Jan Grootenhuis, Yulian Zhang, Benjamin John Petzoldt, Lev Tyler Dewey Fanning, Timothy Donald Neubert, Roger Tung, Esther Martinborough, Nicole Zimmerman
Abstract: The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein.
Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
Type:
Grant
Filed:
April 10, 2006
Date of Patent:
February 2, 2010
Assignee:
Novartis AG
Inventors:
Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
Abstract: The present invention provides novel anthranilic acid derivative useful as potential anticancer agent. More particularly, the present invention relates novel anthranilic acid derivative of general formula (8), R?=alkyl-2-methoxyphenyl piperazine (or) benzyl, R=2 methoxy phenyl, piperazine, 2-pyridyl piperazine, 2-pyrimidyl piperazine, 4-quinazolinyl piperazine, 9H-9-fluorenylamine, 4-{(2{amino-5-(methoxy)-4-[(phenylmethyl)oxy]phenyl}carbonyl)hexahydro-1-pyrazinyl], and [(4[2 amino-4-(benzyloxy)-5-methoxybenzoyl]aminophenyl)sulfonyl]-4-benzamine; X?H (or) pyrazine-2-carbonyl. The present invention also provides a process for the preparation of novel anthranilic acid derivative of general formula (8), which is useful as potential anticancer agent.
Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
Type:
Application
Filed:
September 18, 2009
Publication date:
January 21, 2010
Applicant:
Idenix Pharmaceuticals, Inc.
Inventors:
Christophe Claude Parsy, Francois-Rene Alexandre, Dominique Surleraux, Michel Derock, Frederic Leroy
Abstract: The invention provides Compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, wherein R3, R4, G, Y, W and R5 are as defined in the specification. The invention also provides the use of such Compounds in the treatment or Prophylaxis of a condition associated with a disease or disorder associated with thyroid receptor activity.
Type:
Application
Filed:
July 4, 2006
Publication date:
January 7, 2010
Applicant:
KARO BIO AB
Inventors:
Ana Maria Garcia Collazo, Eva Kristina Koch, Anton Joakim Lofstedt, Aiping Cheng, Thomas Fredrik Hansson, Edouard Zamaratski
Abstract: Novel imidazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)- signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
Abstract: 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:
Application
Filed:
March 3, 2006
Publication date:
December 17, 2009
Inventors:
Dean Wilson, Andreas Termin, Jesus Gonzalez, Lev Fanning, Timothy Neubert, Paul Krenitsky, Pramod Joshi, Dennis Hurley, Urvi Sheth
Abstract: A quinazoline derivative of the formula I: wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula I, are useful in the treatment of hyperproliferative disorders such as a cancer.
Type:
Grant
Filed:
January 31, 2005
Date of Patent:
December 15, 2009
Assignee:
AstraZeneca AB
Inventors:
Benedicte Delouvrie, Craig Steven Harris, Laurent Francois Andre Hennequin, Christopher Thomas Halsall, Janet Elizabeth Pease, Peter Mark Smith
Abstract: The present invention provides a process for producing a 4(3H)-quinazolinone derivative, which is useful as a medicinal substance, with better efficiency in an industrial scale. The process comprises the steps of reacting 4-hydroxy-N-tert-butoxycarbonylpiperidine with 4-fluoro-1-nitrobenzene in the presence of sodium hydride, reacting the resulting product with cyclobutanone, reducing the resulting product to give 4-(1-cyclobutyl-4-piperidinyl)oxyaniline, and reacting this compound with 2-methyl-5-trifluoromethyl-4H-3,1-benzoxazin-4-one to give 3-{4-[(1-cyclobutyl-4-piperidinyl)oxy]phenyl}-2-methyl-5-trifluoromethyl-4(3H)-quinazolinone.
Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8,R9, R10, and are as described herein.
Type:
Grant
Filed:
July 25, 2007
Date of Patent:
December 8, 2009
Assignee:
Bristol-Myers Squibb Company
Inventors:
Percy H. Carter, John V. Duncia, Boguslaw M. Mudryk, Michael E. Randazzo, Zili Xiao, Michael G. Yang, Rulin Zhao
Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
Type:
Application
Filed:
October 30, 2006
Publication date:
October 22, 2009
Inventors:
Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
Abstract: The invention relates to compounds of the formula I, which are appropriate for the treatment of kinase, e.g. PI3K-related, diseases, such as proliferative diseases, inflammatory diseases, obstructive airways disorders and transplantation related diseases.
Abstract: This invention relates to novel processes for the preparation of compounds of the formula [1], wherein R1, R2, R3 and R4 are as defined in the claims and description as well as pharmaceutically acceptable salts thereof. The compounds of the formula [1] are hexacyclic compounds having potent anti-tumor activity.
Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Type:
Grant
Filed:
September 12, 2002
Date of Patent:
September 29, 2009
Assignee:
MethylGene, Inc.
Inventors:
Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
Abstract: Compounds of formula (Ia): where x, y, G, L, M, W, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, are disclosed, as well as pharmaceutical compositions comprising the compounds. These compounds and pharmaceutical compositions are useful in treating SCD-mediated diseases or conditions.
Abstract: The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
Abstract: The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along with the corresponding pharmaceutical compositions, for the treatment of pain and inflammatory disorders. Compounds of this invention are extremely potent analgesics, suitable for the treatment of both inflammatory and neuropathic pain. Particularly for the treatment of neuropathic pain the compounds of the invention have been proved largely superior to the standards currently in the clinical use. These compounds are not acting through inhibition of COX or NOS enzymes but are effective in inhibiting inflammatory cytokine production induced by inflammatory stimuli.
Type:
Application
Filed:
July 31, 2006
Publication date:
September 10, 2009
Applicant:
Rottapharm S.p.A.
Inventors:
Antonio Giordani, Stefano Mandelli, Simona Zanzola, Francesca Tarchino, Gianfranco Caselli, Teresa Simonetta Fiorentino, Silvio Mazzari, Francesco Makovec, Lucio Claudio Rovati
Abstract: The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative and antiangiogenic activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, or associated with unregulated angiogenesis including growth and metastasis of solid tumors, ocular diseases and especially retinopathies, or arthritis, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers (such as leukemia), ocular diseases and arthritis.
Abstract: The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.
Type:
Application
Filed:
June 16, 2008
Publication date:
August 20, 2009
Applicant:
KALYPSYS, INC.
Inventors:
Timothy Gahman, David Thomas, Hengyuan Lang, Mark Eben Massari
Abstract: A compound of formula (I) wherein Ra, Rb, Rc, A, B, C, D, and X are as defined herein, or a tautomer, stereoisomer, or salt thereof, particularly a physiologically acceptable salt thereof. In addition, pharmaceutical compositions comprising an effective amount of a compound of formula (I), methods for the treatment or prophylaxis of benign or malignant tumors, diseases of the airways and lungs, polyps, diseases of the gastrointestinal tract, bile duct, gall bladder, kidneys, and skin, and methods for making compounds of formula (I) are disclosed.
Type:
Application
Filed:
April 14, 2009
Publication date:
August 13, 2009
Applicant:
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
Inventors:
Frank HIMMELSBACH, Elke LANGKOPF, Stefan BLECH, Birgit JUNG, Thomas METZ, Flavio SOLCA
Abstract: The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as “combi-molecules”, that combine two major mechanisms of anti-tumor action. A combi-molecule is capable of degrading to a ligand involved in cell signaling pathways and to an agent capable of damaging DNA. More specifically, the present invention relates to molecules capable of blocking epidermal growth factor receptor (EGFR) mediated signal transduction and capable of damaging DNA. The present invention also relates to a general method of synthesis of these combi-molecules.
Type:
Grant
Filed:
February 26, 2002
Date of Patent:
August 11, 2009
Assignee:
McGill University
Inventors:
Bertrand J. Jean-Claude, Fabienne Dudouit, Stephanie Matheson
Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
Abstract: Compounds, pharmaceuticals, kits, and methods are provided for use with DPP-IV and other S9 protease that comprise a compound comprising the formula: wherein Q is selected from the group of CO, SO, SO2, or C?NR9; and R1, R2, R3 and R4 are as defined herein.
Type:
Grant
Filed:
March 24, 2004
Date of Patent:
June 23, 2009
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
Abstract: 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.
Abstract: A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided. A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.
Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.
Type:
Grant
Filed:
December 12, 2005
Date of Patent:
May 26, 2009
Assignee:
ACADIA Pharmaceuticals, Inc.
Inventors:
Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).
Type:
Application
Filed:
March 22, 2007
Publication date:
April 23, 2009
Applicant:
ACTELION PHARMACEUTICALS LTD.
Inventors:
Christian Hubschwerlen, Jean-Philippe Surivet, Georg Rueedi, Cornelia Zumbrunn-Acklin
Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
Abstract: The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative and antiangiogenic activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, or associated with unregulated angiogenesis including growth and metastasis of solid tumors, ocular diseases and especially retinopathies, or arthritis, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers (such as leukemia), ocular diseases and arthritis.
Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.
Type:
Grant
Filed:
July 4, 2003
Date of Patent:
March 17, 2009
Assignee:
AstraZeneca AB
Inventors:
Laurent Francois Andre Hennequin, Keith Hopkinson Gibson, Kevin Michael Foote
Abstract: 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.
Abstract: An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously administered, can suppress the growth of cancer cells. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; Q represents NR10, CR11R2, carbonyl, O, S(?O)m, wherein m is 0 to 2, or urea; R1 to R3 each independently represent H, OH, halogen, nitro, amino, alkyl, alkoxy or the like in which the alkyl and alkoxy groups are optionally substituted; R4 represents H; R5 to R8 each independently represent H, halogen, alkyl, or alkoxy; and R9 represents an optionally substituted carbocyclic or heterocyclic group.
Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.
Type:
Grant
Filed:
June 18, 2007
Date of Patent:
February 3, 2009
Assignee:
Pfizer, Inc.
Inventors:
David W. Piotrowski, Yu Hui, John W. Benbow
Abstract: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.
Type:
Grant
Filed:
November 19, 2004
Date of Patent:
January 27, 2009
Assignee:
Aventis Pharma S.A.
Inventors:
Patrick Mailliet, Abdelazize Laoui, Jean-Francois Riou, Gilles Doerflinger, Jean-Louis Mergny, Francois Hamy, Thomas Caulfield
Abstract: The invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, n and m are as defined herein. The compounds of formula I are useful in the treatment of hyperproliferative diseases, such as cancer. The invention further relates to processes of making the compounds of formula I and to methods of using such compounds in the treatment of hyperproliferative diseases.
Type:
Grant
Filed:
February 27, 2008
Date of Patent:
December 29, 2009
Assignees:
Pfizer, Inc., OSI Pharmaceuticals, Inc.
Inventors:
Rodney Caughren Schnur, Lee Daniel Arnold