The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/266.24)
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Publication number: 20090028868Abstract: Method of treating persons having carcinoma, sarcoma or hematopoietic cancer by administering (i) a compound of the formula (I) and (ii) an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and pharmaceutical compositions for use in said method. A method for treating gastric cancer, colon cancer, lung cancer, breast cancer, pancreas cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma and leukemia by administering a compound of the formula (I).Type: ApplicationFiled: July 30, 2008Publication date: January 29, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kosaku Fujiwara, Naomi Shimazaki
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Publication number: 20090012069Abstract: Disclosed are novel compounds of general formula (I) where the symbols are as defined in the specification, their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The compounds are useful in the treatment of diabetes and related diseases.Type: ApplicationFiled: June 24, 2005Publication date: January 8, 2009Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Harikishore Pingali
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Publication number: 20080306097Abstract: Disclosed herein is a method of treating breast cancer that has metastasized to the brain in a mammal by administration of 4-quinazolinamines and pharmaceutical compositions containing the same. In particular, the method relates to methods of treating breast cancer brain metastases which overexpress erbB2 by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof.Type: ApplicationFiled: December 16, 2005Publication date: December 11, 2008Applicant: SMITHKLINE BEECHAM (CORK) LIMITEDInventor: Stephen Rubin
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Publication number: 20080306057Abstract: This invention relates to a method of treating and/or preventing endometriosis comprising administering a PI3K inhibitor. The PI3K inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis-related infertility.Type: ApplicationFiled: August 28, 2006Publication date: December 11, 2008Applicant: LABORATORIES SERONO SAInventors: Stephen Palmer, Selvaraj Nataraja
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Publication number: 20080306096Abstract: 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: December 19, 2006Publication date: December 11, 2008Applicant: ASTRAZENECA ABInventors: Brian Aquila, Jayachandran Ezhuthachan, Paul Lyne, Timothy Pontz, Xiaolan Zheng
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Patent number: 7456189Abstract: Compounds of the formula having an inhibitory action on the signal transduction mediated by tyrosine kinases, and being useful for the treatment of oncoses and of benign prostate hyperplasia (BPH), of diseases of the lung and of the airways. Exemplary compounds are: (R)-4-(1-Phenylethylamino)-6-[1-(tert-butyloxycarbonyl)piperidin-4-yloxy]-7-methoxy-quinazoline and (R)-4-(1-Phenylethylamino)-6-(piperidin-4-yloxy)-7-methoxyquinazoline dihydrochloride.Type: GrantFiled: September 23, 2004Date of Patent: November 25, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung
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Publication number: 20080279845Abstract: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.Type: ApplicationFiled: May 2, 2008Publication date: November 13, 2008Inventors: Pamela B. Conley, Patrick Andre, Uma Sinha
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Publication number: 20080261974Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.Type: ApplicationFiled: September 22, 2006Publication date: October 23, 2008Inventors: Kevin J Duffy, Duke M. Fitch, Rosanna Tedesco, Michael N. Zimmerman
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Publication number: 20080254040Abstract: The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.Type: ApplicationFiled: June 17, 2008Publication date: October 16, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Martin Friedrich STEFANIC, Frank HILBERG, Gerd MUNZERT, Flavio SOLCA, Anke BAUM, Jacobus C.A. van MEEL
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Publication number: 20080214584Abstract: The present invention provides a method for treating cancer, which includes selecting a patient coexpressing HER2 and HER3, and administering an effective amount of a HER2 inhibitor to the patient.Type: ApplicationFiled: December 27, 2007Publication date: September 4, 2008Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yoshikazu Ohta, Shinji Takagi
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Publication number: 20080206338Abstract: The present invention relates to controlled release formulations comprising an alpha-adrenergic receptor antagonist. More particularly, the present invention relates to controlled release matrix formulation comprising alfuzosin hydrochloride and a combination of hydrophilic and hydrophobic polymers prepared by direct compression.Type: ApplicationFiled: February 20, 2008Publication date: August 28, 2008Inventors: Nagaprasad Vishnubhotla, Vinodkumar Gurunath Indure, Sindhuja Balakrishnan, Sivakumaran Meenakshisunderam
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Publication number: 20080206330Abstract: Oral pharmaceutical formulations containing ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.Type: ApplicationFiled: April 18, 2006Publication date: August 28, 2008Inventors: Barry Howard Carter, Dwayne A. Campbell
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Publication number: 20080194597Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 20, 2007Publication date: August 14, 2008Applicant: Portola Pharmaceuticals, Inc.Inventors: ROBERT M. SCARBOROUGH, Wolin Huang, Charles K. Marlowe, Kim A. Kane-Maguire
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Publication number: 20080194578Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2007Publication date: August 14, 2008Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
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Publication number: 20080182865Abstract: Disclosed is the use of a combination of histone deacetylase inhibitors and kinase inhibitors with anti-EGFR activity.Type: ApplicationFiled: September 25, 2007Publication date: July 31, 2008Inventors: Samir E. Witta, Paul A. Bunn, Harry A. Drabkin, Robert M. Gemmill, Daniel Chuen-Fong Chan
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Publication number: 20080160081Abstract: Alfuzosin compositions comprising alfuzosin and a release-retarding matrix comprising about 40 to about 80% (by weight) hydroxypropyl methyl cellulose with a maximum apparent viscosity of about 5600 cP, wherein the compositions are bioequivalent to the reference dosage form of NDA #021287 are disclosed. Alfuzosin compositions comprising alfuzosin and a release-retarding matrix comprising about 40 to about 80% (by weight) hydroxypropyl methyl cellulose (HPMC) with a maximum apparent viscosity of about 5600 cP, wherein the dissolution profile of the compositions are substantially identical to the dissolution profile of the reference dosage form of NDA #021287 are also disclosed. Methods of making and using the alfuzosin compositions are also disclosed.Type: ApplicationFiled: December 10, 2007Publication date: July 3, 2008Applicant: MUTUAL PHARMACEUTICAL COMPANY, INC.Inventors: Gandha V. Naringrekar, Kristin Arnold, Jie Du
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Publication number: 20080153830Abstract: The present disclosure provides for improved methods for treating pain, including pain associated with chronic inflammatory diseases, neuropathic pain and cancer by using ?-adrenergic antagonists and ?-adrenergic agonists (particularly ?2-adrenergic agonists) alone or in combination.Type: ApplicationFiled: October 15, 2007Publication date: June 26, 2008Inventors: CHERI LUBAHN, Dianne Lorton
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Publication number: 20080146562Abstract: The present invention includes novel compounds of the formula wherein: X is absent, or trans or cis CHCH; R1 is (C1-C10)alkyl unsubstituted or substituted by one to three hydroxy, (C2-C10)alkenyl unsubstituted or substituted by one to three hydroxy, (C2-C10)alkynyl unsubstituted or substituted by one to three hydroxy, or aryl unsubstituted or substituted by one to three hydroxy; R2 is hydrogen, alkyl or aryl, wherein R1 and R2 when taken together form a (C2-C10)cycloalkyl unsubstituted or substituted by one to three hydroxy; and R3 and R4 are, independently of each other, H, halogen, or wherein: P and R are each independently selected from CH2, CH2CH2 and CH2CHT, wherein T is alkyl; Q is O, S, NH or NCH3; and Y is absent or —CH2CH2)nO—, and n=1 or 2; with the proviso that at least one of R3 and R4 is halogen, and that when R4 is halogen, R3 is hydrogen and Y is absent, neither R1 nor R2 are alkyl; or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 12, 2007Publication date: June 19, 2008Inventors: Suzanne Chamberland, Francois Malouin, Roger Leger, Ving J. Lee
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Publication number: 20080138412Abstract: A sustained release alfuzosin hydrochloride formulation contains alfuzosin hydrochloride as about 1% to about 5% by weight of the formulation, hydrophilic polymers as about 35% to about 75% by weight of the formulation, hydrophobic polymers as about 10% to about 30% by weight of the formulation, disintegrating agents as 10% to 30% by weight of the formulation and a binder as about 2% to about 12% by weight of the formulation. The hydrophilic and hydrophobic polymers are used as the release-modulating agent to control the dissolution profile of the alfuzosin hydrochloride formulation so that the formulation releases alfuzosin hydrochloride slowly and continuously as the formulation passed through the gastrointestinal tract. The present invention also relates to a method for preparing the above formulation.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Inventors: Fu-Yung Lin, Fang-Hsiung Hsiao, Ya-Ching Chang Chien
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Publication number: 20080132499Abstract: Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: ApplicationFiled: September 17, 2007Publication date: June 5, 2008Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Carroll Anna Crew Scarborough, Shawn M. Bauer, Anjali Pandey
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Publication number: 20080125428Abstract: The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and at least one additional EGFR and/or erbB-2 inhibitor. In particular, the method relates to methods of treating cancers by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof in combination with at least one additional EGFR and/or erbB-2 inhibitor.Type: ApplicationFiled: August 25, 2005Publication date: May 29, 2008Inventor: David Rusnak
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Publication number: 20080095844Abstract: The present invention relates to sustained release pharmaceutical compositions comprising alfuzosin, a rate-controlling polymer and optionally one or more pharmaceutically acceptable excipients; process for preparing such compositions and method of using the compositions.Type: ApplicationFiled: August 20, 2007Publication date: April 24, 2008Inventors: Rajhans Sujay Kamalakar, Bhutada Pravin Meghraj, Patel Hasmukh Mathurbhai
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Patent number: 7348332Abstract: The present invention relates to compounds of formula wherein R1, R2, and n are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I for 5-HT5A receptor related diseases, such as anxiety, depression, sleep disorders and schizophrenia.Type: GrantFiled: April 5, 2006Date of Patent: March 25, 2008Assignee: Hoffmann-La Rochse Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Publication number: 20080051422Abstract: This invention relates to novel 4-aminoquinazolines, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates 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 administering inhibitors of the EGFR and HER-2.Type: ApplicationFiled: August 22, 2007Publication date: February 28, 2008Applicant: Concert Pharmaceuticals Inc.Inventor: Roger Tung
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Publication number: 20080039473Abstract: The present disclosure is directed to modulators of alpha-adrenergic receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of hypertension, cardiac failure, prostatitis, and benign prostatic hyperplasia, and any other condition in which it is beneficial to modulate an alpha-adrenergic receptor.Type: ApplicationFiled: August 8, 2007Publication date: February 14, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. GANT, Sepehr SARSHAR
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Patent number: 7326712Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: GrantFiled: October 14, 2004Date of Patent: February 5, 2008Assignees: Arizona Board of Regents on behalf of The University of Arizona, Supergen, Inc.Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Steven L. Warner
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Patent number: 7304059Abstract: Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: February 1, 2006Date of Patent: December 4, 2007Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Charles A. Blum, Harry Brielmann, Timothy M. Caldwell, Stéphane De Lombaert, Kevin J. Hodgetts, Xiaozhang Zheng, Taeyoung Yoon
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Patent number: 7223756Abstract: The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R1, Z, n and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animalType: GrantFiled: November 20, 2002Date of Patent: May 29, 2007Assignee: AstraZeneca ABInventors: Nelly Corine Moore, Keith Oldham
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Patent number: 7189734Abstract: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.Type: GrantFiled: April 7, 2006Date of Patent: March 13, 2007Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Karen Elizabeth Lackey
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Patent number: 7157466Abstract: Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.Type: GrantFiled: June 28, 2001Date of Patent: January 2, 2007Assignee: SmithKline Beecham (Cork) LimitedInventors: Michael Scott McClure, Martin Howard Osterhout, Frank Roschangar, Mark Joseph Sacchetti
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Patent number: 7157467Abstract: The invention concerns the use of the quinazoline derivatives of Formula (I) Wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions such as autoimmune diseases like transplant rejection or rheumatoid arthritis in a warm-blooded animal.Type: GrantFiled: November 20, 2002Date of Patent: January 2, 2007Assignee: AstraZeneca ABInventors: Nelly Corine Moore, Keith Oldham
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Patent number: 7141577Abstract: The invention concerns quinazoline derivatives of Formula I (A Chemical Formula should be inserted here—please see paper copy enclosed) wherein each of Z, m, R1, n and R3 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 agent in the containment and/or treatment of solid tumor disease.Type: GrantFiled: April 15, 2002Date of Patent: November 28, 2006Assignee: AstraZeneca ABInventor: Patrick Ple
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Patent number: 7141576Abstract: A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as pharmaceutical combinations and compositions containing the same.Type: GrantFiled: January 14, 2002Date of Patent: November 28, 2006Assignee: SmithKline Beecham (Cork) LimitedInventors: Karen Elizabeth Lackey, Neil Spector, Edgar Raymond Wood, III., Wenle Xia
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Patent number: 7115615Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R1, n, R2 and R3 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 tumour disease.Type: GrantFiled: August 15, 2001Date of Patent: October 3, 2006Assignee: AstraZenecaInventors: Laurent Francois Andre Hennequin, Patrick Ple, Christine Marie Paul Lambert
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Patent number: 7109333Abstract: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) ?wherein L and L? are suitable leaving groups, with a compound of formula (III) UNH2??(III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L?.Type: GrantFiled: February 3, 2005Date of Patent: September 19, 2006Assignee: SmithKline Beecham CorporationInventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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Patent number: 7109332Abstract: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided.Type: GrantFiled: September 29, 2004Date of Patent: September 19, 2006Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Anjali Pandey, Shawn M. Bauer, Xiaoming Zhang, Zhaozhong J. Jia
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Patent number: 7105669Abstract: A compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2 or NR10 where R10 is hydrogen or C1-6 alkyl, and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are various specified organic groups. These compounds are inhibitors of aurora 2 kinase, and are useful in the treatment of cancer.Type: GrantFiled: September 18, 2000Date of Patent: September 12, 2006Assignee: AstraZeneca ABInventors: Andrew Austen Mortlock, Nicholas John Keen
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Patent number: 7084147Abstract: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.Type: GrantFiled: February 18, 2005Date of Patent: August 1, 2006Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Karen Elizabeth Lackey
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Patent number: 7022849Abstract: Quinazoline and pyrido[2,3-d]pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, L, Y1, Y2, Y3 and Z are as described herein, are provided which are useful in treating T-cell mediated diseases.Type: GrantFiled: June 17, 2002Date of Patent: April 4, 2006Assignee: Bristol-Myers Squibb Co.Inventors: William J. Pitts, Joseph Barbosa
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Patent number: 7019012Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction medType: GrantFiled: December 17, 2001Date of Patent: March 28, 2006Assignee: Boehringer Ingelheim International Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca
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Patent number: 7001904Abstract: The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2, R3 and R5 is hydrogen or (1-6C)alkyl, provides that one of the parts of groups R2 and R4 together, R3 and R4 together and R5 and R4 together forms a bond; R6 is an optionally substituted group selected from (2-6C) alkenyl, (2-6C) alkynyl, (3-7C)cycloalkyl and (3-7C) cycloalkenyl, or R6 is a substituted (1-6C) alkyl group; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-bloodedType: GrantFiled: June 19, 2001Date of Patent: February 21, 2006Assignee: AstraZeneca ABInventor: Jeffrey Philip Poyser
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Patent number: 6982264Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: GrantFiled: June 27, 2002Date of Patent: January 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Roy Hom, John Tucker
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Patent number: 6962922Abstract: A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N?X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Warner-Lambert Company LLCInventors: Bernard Gaudilliere, Henri Jacobelli, Joseph Armand Picard, Michael William Wilson
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Patent number: 6919338Abstract: The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6alkyl; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2, R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed.Type: GrantFiled: June 21, 2001Date of Patent: July 19, 2005Assignee: AstraZeneca ABInventors: Andrew Mortlock, Frederic Jung
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Patent number: 6911446Abstract: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to quinazoline compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: January 26, 2001Date of Patent: June 28, 2005Assignee: Sugen, Inc.Inventors: Peng C. Tang, Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
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Patent number: 6897214Abstract: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.Type: GrantFiled: May 2, 2002Date of Patent: May 24, 2005Assignee: Zeneca LimitedInventors: Andrew John Barker, Craig Johnstone
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6849625Abstract: The invention concerns quinazoline derivatives of Formula I wherein each of m, R1, n, R2 and R3 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 tumour disease.Type: GrantFiled: October 9, 2001Date of Patent: February 1, 2005Assignee: AstraZeneca ABInventors: Christine Marie Paul Lambert, Patrick Ple
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Publication number: 20040204417Abstract: The invention concerns compounds of general formula (1), wherein, in particular; W represents H, SO2R5. CO(CH2)nR5, (CH2)nR6, CS(CH2)nR5; X represents S or NH; Y represents (CH2)p, CO, (CH2)pCO, CH═CH—CO; Z represents a hetcrocycle, imidazole, benzimidazole, isoxazole, tetrazole, oxadiazole, thiadazole, pyridine, quinazoline, quinoxaline, quinoline, thiophene; R1 represents COOR6, CONR6R7, CO—NH—CH(R6)—COOR7, CH2NR6R7, CH2OR6, (CH2)pR6, CH═CHR6; R2 represents in particular hydrogen, C1-C10 alkyl, a substituted or unsubstituted phenyl; R5 and R6 represents hydrogen, C1—C6 alkyl; R5 represents a substituted or unsubstituted phenyl or naphthyl; R6 and R7, identical or different, represent hydrogen, C1—C15 alkyl, a hetcrocycle. an aryl; n represents 0 to 10; p represents 1 to 6.Type: ApplicationFiled: May 20, 2004Publication date: October 14, 2004Inventors: Michel Perez, Marie Lamothe, Bridget Hill, Chantal Etievant
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Publication number: 20040152708Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.Type: ApplicationFiled: November 7, 2003Publication date: August 5, 2004Inventors: Yong Li, Kurt Sundermann, Li Tang, David Myles