Piperidinyl Or Tetrahydropyridyl Patents (Class 514/266.22)
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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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Patent number: 7452912Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: December 11, 2002Date of Patent: November 18, 2008Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
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Publication number: 20080280879Abstract: 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: May 8, 2008Publication date: November 13, 2008Inventors: Steven Jospeh BRICKNER, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Micheal A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
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Publication number: 20080275045Abstract: This invention relates to novel potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions.Type: ApplicationFiled: March 13, 2006Publication date: November 6, 2008Applicant: NeuroSearch A/SInventors: Birgitte L. Eriksen, Lene Teuber, Charlotte Hougaard, Ulrik Svane Sorensen
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Publication number: 20080275069Abstract: This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (I) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.Type: ApplicationFiled: May 30, 2005Publication date: November 6, 2008Inventors: Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
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Publication number: 20080275029Abstract: The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B; wherein the ring Q is a benzene ring; J2-J1 is N?CR7 or R1aN—CO; G is OH or NR5R6; E is CONR7, NR7CO, C(R8)?C(R8) or (X)m(CR8R8a)n where X is O, S or NR7; provided that when J2-J1 is R1aN—CO, E is other than NR7CO; m and n are each 0 or 1, where m+n=1 or 2; A is a bond and R4 and R4a are absent or A is a saturated optionally substituted C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R1, R1a, R2, and R3 are each H; halogen; C1-6 hydrocarbyl optionally substituted by halogen, OH or C1-2 alkoxy; CN; CONHR8; NH2; NHCOR10 or NHCONHR10; R4 is H or C1-4 alkyl; R4a is H, C1-4 alkyl or a group R9; R5 and R6 are each selected from H, R9 and C1-4 hydrocarbyl optionallyType: ApplicationFiled: November 9, 2005Publication date: November 6, 2008Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSInventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Hannah Fiona Sore, David Winter Walker, John Caldwell, Ian Collins
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Publication number: 20080255165Abstract: 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: February 22, 2006Publication date: October 16, 2008Inventors: Mordechai Erez, Karin Halevi
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Patent number: 7429597Abstract: The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula wherein B, X1 to X3 and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I as well as the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, and their stereoisomers have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.Type: GrantFiled: December 18, 2003Date of Patent: September 30, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Henning Priepke, Roland Pfau, Kai Gerlach, Uwe Ries, Wolfgang Wienen, Eckhart Bauer, Herbert Nar
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Publication number: 20080221094Abstract: The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a squaramide moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.Type: ApplicationFiled: March 7, 2008Publication date: September 11, 2008Inventors: Harald Bluhm, Christian Gege, Matthias Hochgurtel, Arthur Taveras
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Publication number: 20080200433Abstract: According to the present invention, a molecular chaperone function regulator containing a quinazoline derivative represented by the following formula (I) wherein each symbol is as defined in Claims, or a pharmaceutically acceptable salt thereof, a hydrate or solvate thereof, an optically active form or racemate thereof or a diastereomer mixture thereof as an active ingredient can be provided.Type: ApplicationFiled: September 1, 2005Publication date: August 21, 2008Inventors: Tsuyoshi Suzuki, Akihiro Fujii, Hideo Nakamura, Tsutomu Yoshikawa
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Publication number: 20080200436Abstract: 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 the administration of ZD6474 in combination with androgen ablation; to a pharmaceutical composition comprising ZD6474 and an antiandrogen; to a combination product comprising ZD6474 and an antiandrogen for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and an antiandrogen; to the use of ZD6474 and an antiandrogen in the manufacture of a medicament for use in 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.Type: ApplicationFiled: November 1, 2005Publication date: August 21, 2008Inventor: Stephen Robert Wedge
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Publication number: 20080194532Abstract: Compositions containing quaternary ammonium compounds in which the nitrogen atom is substituted by at least one alkyl group having at least 12 carbon atoms, where composition includes at least 20% in weight by weight of the total composition, of ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 14 carbon atoms and more than 5%, preferably more than 7% in weight by weight of the total composition, of ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 16 carbon atoms. Ophthalmic oil-in-water emulsions containing such compositions, and the ophthalmic emulsions being are useful for eye care or for the treatment of eye conditions.Type: ApplicationFiled: January 30, 2008Publication date: August 14, 2008Applicant: NOVAGALI PHARMA SAInventors: Laura Rabinovich-Guilatt, Gregory Lambert, Frederic Lallemand, Betty Philips
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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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Patent number: 7407963Abstract: A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing the compound, their use, and processes for preparing them.Type: GrantFiled: June 27, 2005Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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Publication number: 20080176876Abstract: 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: June 28, 2005Publication date: July 24, 2008Inventors: Marcel Josef Maria Van Der AA, Albertus Henricus Maria Van Heertum, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20080161328Abstract: Provided are 5-substituted quinazolinone compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: September 26, 2007Publication date: July 3, 2008Inventors: George W. Muller, Hon-Wah Man
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Publication number: 20080161329Abstract: The invention relates to the pharmaceutical use of specific substance P antagonists, in particular 1-acylpiperidine substance P antagonists, especially N-benzoyl-2-benzyl-4-(azanaphthoyl-amino)-piperidines, e.g. of formula wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and pharmaceutically acceptable salts thereof for treatment of chronic fatigue syndrome (CFS) in the absence of serotonin agonist/selective serotonin reuptake inhibitory therapy, or for the treatment of fibromyalgia or associated functional symptoms.Type: ApplicationFiled: January 14, 2008Publication date: July 3, 2008Inventors: Lothar Farber, Wolfgang Mueller, Thomas Stratz
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Publication number: 20080161297Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.Type: ApplicationFiled: September 18, 2007Publication date: July 3, 2008Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young
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Publication number: 20080139591Abstract: The invention relates to a method for preventing and treating visceral pain and gastrointestinal disorders such as functional bowel disorders and inflammatory bowel diseases through the use of effective amounts of a compound acting as CGRP antagonist.Type: ApplicationFiled: June 8, 2007Publication date: June 12, 2008Inventors: Henri DOODS, Kirsten ARNDT, Thierry BOUYSSOU, Stephan Georg MUELLER, Klaus RUDOLF, Gerhard SCHAENZLE
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Patent number: 7384940Abstract: Described herein are methods for treating cancer and other disease conditions in individuals who have either developed a resistance to conventional tyrosine kinase inhibitor (TKI) therapy or who are non-responsive ab initio to conventional TKI therapy. In various embodiments, the methods include administering to a patient a resistance-surmounting quantity of a TKI on a weekly or semi-weekly basis. Alternate embodiments of the present invention include a diagnostic method for assessing an individual's probability of being resistant to TKI therapy, based upon an expression level of epithelial membrane protein-1 (EMP-1); one of the genes believed to be responsible for TKI resistance. The methods of the present invention may be particularly useful in the treatment of lung, breast, prostate, ovarian, brain and colon cancers. The methods of the present invention may be effective in blocking the HER-2 kinase domain either in addition to or in lieu of blocking the EGFR kinase domain.Type: GrantFiled: June 4, 2003Date of Patent: June 10, 2008Assignee: Cedars-Sinai Medical CenterInventor: David B. Agus
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Publication number: 20080125435Abstract: The present invention relates to aryl-3-[(het)aryl-piperidin-4-yl]-thioureas, processes for the production thereof and the use thereof for the production of pharmaceutical agents for the treatment of diseases and indications which are connected with the EP2 receptor.Type: ApplicationFiled: September 6, 2007Publication date: May 29, 2008Inventors: Nico Brauer, Bernd Buchmann, Christoph Huwe, Marcus Koppitz, Antonius Ter Laak, Gernot Langer, Bernhard Lindenthal, Olaf Peters, Tim Wintermantel
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Publication number: 20080096881Abstract: The invention concerns quinazoline derivatives of Formula (I): wherein each of R1, X1, R2, R3, R5, n and m 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 EGF and erbB receptor tyrosine kinases.Type: ApplicationFiled: September 15, 2004Publication date: April 24, 2008Applicant: ASTRAZENECA ABInventors: Laurent Francois Andre Hennequin, Bernard Christophe Barlaam, Robert Hugh Bradbury
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Publication number: 20080090853Abstract: A compound of formula (I) wherein: R1 is an aryl group, unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, aryl C1-C6 alkoxy, hydroxy, halo, CN, COR6, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, halo C1-C4 alkyl, and halo C1-C4 alkoxy; W is CH and X is N, or W is N and X is CH, or W and X are CH; Y is C2-C4alkyl, R2 is hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, aryl C1-C6 alkoxy, hydroxy, halo, CN, COR6, carboxy, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C1-C6 alkyl, or mono to perfluoro-C1-C6 alkoxy; n is 0-5; R3 is C1-C4 alkyl; R4 is C1-C4 alkyl; R5 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, halo C1-C4 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl C1-C4 alkyl, C5-C8cycloalkenyl, C5-C8cycloalkenyl C1-C4 alkyl, 3-8-membered heterocycloalkyl, 3-8-membered heterocycloalkyl C1-C4 alkyl, C6-C14 aryl, C6-C14 arType: ApplicationFiled: January 25, 2007Publication date: April 17, 2008Inventor: Colin Andrew LEACH
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Patent number: 7358256Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: March 27, 2006Date of Patent: April 15, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Ping Chen, Yufen Zhao
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Publication number: 20080070915Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compnounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.Type: ApplicationFiled: June 28, 2005Publication date: March 20, 2008Inventors: Jerome Emile Georges Guillemont, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Patent number: 7345049Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: December 22, 2004Date of Patent: March 18, 2008Assignee: Ajinomoto Co., Inc.Inventors: Kazuyuki Sagi, Tatsuya Okuzumi, Tatsuhiro Yamada, Shunsuke Kageyama, Yoichiro Shima, Tadakiyo Nakagawa, Munetaka Tokumasu, Masayuki Sugiki, Hajime Ito, Itsuya Tanabe, Tamotsu Suzuki, Akira Nakayama, Kazuyuki Ubukata, Kenji Shinkai, Yasuhiro Tanaka, Misato Noguchi, Ayatoshi Andou, Yoriko Yamamoto, Noriyasu Kataoka, Koichi Fujita
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Publication number: 20080058342Abstract: The present invention relates to compounds of the Formula (I): wherein: ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which moiety may be saturated or unsaturated, which may be aromatic or non-aromatic, and which optionally may contain 1-3 heteroatoms selected independently from O, N and S; is —O— —NH— or —S—; is 0, 1, 2, 3, 4 or 5; is 0, 1, 2 or 3; and R2 and R1 are as defined herein; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm blooded animals; processes for the preparation of such compounds; pharmaceutical compositions containing a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 5, 2004Publication date: March 6, 2008Inventor: Laurent Francois Andre Hennequin
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Publication number: 20080045550Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: June 21, 2007Publication date: February 21, 2008Inventors: Andreas D. Christ, Rainer E. Martin
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Patent number: 7329665Abstract: An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents —CH? or nitrogen atom; and R represents a C1-C4 alkyl group and so on], or pharmaceutically acceptable salts thereof, has a selective antagonism for the M3 muscarinic receptor and depressant action on the frequency of rhythmic bladder contractions, and it is useful for the treatment of pollakiuria and urinary incontinence.Type: GrantFiled: August 2, 2002Date of Patent: February 12, 2008Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Masami Muraoka, Kazuki Matsui, Takaaki Yamamoto, Koji Morishita, Masatoshi Yuri, Seiji Katayama, Naohito Ohashi
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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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Publication number: 20070254885Abstract: The use of type V phosphodiesterase inhibitors as a novel independent therapeutic modality in the treatment of exercise induced pulmonary hemorrhage in equine is described. The type V phosphodiesterase inhibitor is injected into the horse intravenously as a stand-alone agent from about one-half hour to about seven (7) days prior to the onset of strenuous exercise.Type: ApplicationFiled: May 1, 2007Publication date: November 1, 2007Inventor: Bryan J. Perry
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Patent number: 7285557Abstract: A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are providedType: GrantFiled: October 15, 2002Date of Patent: October 23, 2007Assignee: SmithKline Beecham P.L.C.Inventors: Andrew J Carpenter, Joel P Cooper, Anthony L Handlon, Donald L Hertzog, Clifton E Hyman, Yu C Guo, Jason D Speake, David Richard Witty
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Publication number: 20070225271Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: March 15, 2007Publication date: September 27, 2007Inventors: Alfred Binggeli, Andreas Christ, Hans-Peter Maerki, Rainer Eugen Martin
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Patent number: 7271260Abstract: The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihydroquinazoline derivatives of the present invention can be effectively used for preventing and treating angina pectoris, high blood pressure, myocardial disease, pain and epilepsy by blocking the T-type calcium channel.Type: GrantFiled: December 20, 2004Date of Patent: September 18, 2007Assignee: Korea Institute of Science and TechnologyInventors: Yong Sup Lee, Jae Yeol Lee, Hyewhon Rhim
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Patent number: 7265125Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.Type: GrantFiled: April 7, 2005Date of Patent: September 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Philippe Guerry, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7230000Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed.Type: GrantFiled: November 28, 2000Date of Patent: June 12, 2007Assignee: Cytokinetics, IncorporatedInventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
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Patent number: 7230001Abstract: The present invention relates to compounds of general formula R—Z1—Z2—Z3—R1, ??(I) wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: October 24, 2000Date of Patent: June 12, 2007Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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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: 7214674Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; R 1 is halogen, cyano, or C1-6 alkoxy; a is 0,1, 2 or 3 ; b is 0 or 1 ; R 2 is hydrogen, C1-6 alkyl, C1-6 alkanoyl, fluoroC1-6 alkanoyl, C1-6 alkylsulfonyl, fluoroC1-6 alkylsulfonyl, carbamoyl, C1-6 alkylcarbamoyl or arylC1-6 alkyl; and R 3 , together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.Type: GrantFiled: February 17, 2003Date of Patent: May 8, 2007Assignee: Glaxo Group LimitedInventor: Simon E Ward
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Patent number: 7211580Abstract: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.Type: GrantFiled: July 23, 2003Date of Patent: May 1, 2007Assignee: Cytokinetics, IncorporatedInventors: Gustave Bergnes, Whitney W. Smith, Bing Yao, David J. Morgans, Jr., Andrew MacDonald
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Patent number: 7183274Abstract: Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods of treatment.Type: GrantFiled: June 21, 2004Date of Patent: February 27, 2007Assignee: Gruenenthal GmbHInventors: Helmut Heinrich Buschmann, Stefanie Frosch, Tieno Germann, Oswald Karl Zimmer, Fritz Theil
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Patent number: 7173038Abstract: 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 piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, 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 a 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 number of disease states including cancer and rheumatoid arthritis.Type: GrantFiled: November 1, 2000Date of Patent: February 6, 2007Assignee: AstraZeneca ABInventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
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Patent number: 7148230Abstract: The invention concerns quinazoline derivatives of Formula I wherein R1 and R2 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, particularly EGF, receptor tyrosine kinases.Type: GrantFiled: June 1, 2004Date of Patent: December 12, 2006Assignee: AstraZeneca ABInventors: Robert Hugh Bradbury, Jason Grant Kettle, James McCabe, Andrew Turner, Laurent Francois Andre Hennequin
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Patent number: 7112590Abstract: The invention relates to compounds that are heterocyclic derivatives of dipeptides and dipeptides mimetics and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 4, 2001Date of Patent: September 26, 2006Assignees: LEK Pharmaceuticals d.d., University of Ljubljana, Faculty of PharmacyInventors: Danijel Kikelj, Lucija Peterlin, Petra Marinko, Matej Breznik, Mojca Stregnar, Bakija Alenka Trampuz, Marjana Fortuna
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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: 7094780Abstract: Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, cycloalkyl, aryl, hetero-cyclic, and heteroaryl; R5, R6, and R8 include H, alkyl, alkoxy, halo, NO2, CN, NH2, alkyl and dialkylamino; R7 includes hydrogen, alkyl, cycloalkyl, hetero-cyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 12, 2000Date of Patent: August 22, 2006Assignee: Warner Lambert Company LLCInventors: Paul Bird, Edmund Lee Ellsworth, Dai Quoc Nguyen, Joseph Peter Sanchez, Howard Daniel Hollis Showalter, Rajeshwar Singh, Michael Andrew Stier, Tuan Phong Tran, Brian Morgan Watson, Judy Yip
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Patent number: 7060705Abstract: The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: November 1, 2002Date of Patent: June 13, 2006Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, William F. Hoffman
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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