The Additional Hetero Ring Is A Diazole Ring (including Hydrogenated) Patents (Class 548/312.4)
- Additional diverse hetero ring attached directly or indirectly to a diazole ring by nonionic bonding (Class 548/313.1)
- The diazole rings are bonded directly to each other (Class 548/313.4)
- Ring nitrogens of two diazole rings attached directly to the same atom or chain, which chain may include a ring, by nonionic bonding (Class 548/313.7)
- Two diazole rings are bonded directly to the same carbon atom or carbon chain, which chain may include a ring (Class 548/314.4)
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Publication number: 20110021538Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.Type: ApplicationFiled: April 1, 2009Publication date: January 27, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
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Patent number: 7825142Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: GrantFiled: August 24, 2009Date of Patent: November 2, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D. P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Publication number: 20100249117Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: May 11, 2010Publication date: September 30, 2010Inventors: Yonghong SONG, Zhaozhong J. JIA, Anjali PANDEY, Robert M. SCARBOROUGH, Carroll SCARBOROUGH
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Publication number: 20100249085Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.Type: ApplicationFiled: May 8, 2008Publication date: September 30, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephen Boyer, Michael Härter, Philip L. Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
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Publication number: 20100234374Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.Type: ApplicationFiled: December 21, 2006Publication date: September 16, 2010Inventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Raffaele Ingenito, Carsten Schultz-Fademrecht
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Publication number: 20100210617Abstract: The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two caType: ApplicationFiled: June 21, 2006Publication date: August 19, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Steven John Woodhead, Robert Downham, Christopher Hamlett, Steven Howard, Hannah Fiona Sore, Marinus Leendert Verdonk, David Winter Walker, Richard William Arthur Luke
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Publication number: 20100190780Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: February 9, 2010Publication date: July 29, 2010Inventors: Christian Laggner, Maria Rosa Cuberes-Altisent, Joerg Holenz, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-LLobet
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Publication number: 20100184772Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: October 10, 2007Publication date: July 22, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Helmut H. Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
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Patent number: 7745440Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: GrantFiled: October 6, 2005Date of Patent: June 29, 2010Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally
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Publication number: 20100160324Abstract: The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or —Y—(B)n—; B is C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C1-8 hydrocarbyl group; with the proviso that R1 is not formula (II): where X, R3? and R4? are defined in the claims.Type: ApplicationFiled: December 30, 2005Publication date: June 24, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Nicholas Gareth Morse Davies, Adrian Liam Gill, Eva Figueroa Navarro, Steven Howard, Gary Trewartha, Andrew James Woodhead, Alison Jo-Anne Woolford, Paul Graham Wyatt
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Publication number: 20100120874Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: ApplicationFiled: November 4, 2009Publication date: May 13, 2010Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Publication number: 20100113546Abstract: Imidazol-4-one or imidazole-4-thione compounds of formula (I): wherein X, R1, R2, R3, R4, R5, and R6 are defined herein. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.Type: ApplicationFiled: October 30, 2009Publication date: May 6, 2010Applicant: National Health Research InstitutesInventors: Kak-Shan Shia, Chien-Huang Wu, Teng-Kuang Yeh, Yu-Sheng Chao
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Patent number: 7705030Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: GrantFiled: July 28, 2008Date of Patent: April 27, 2010Assignee: Wyeth LLCInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Patent number: 7700602Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.Type: GrantFiled: December 10, 2008Date of Patent: April 20, 2010Assignee: Wyeth LLCInventors: Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Ping Zhou, Yinfa Yan, Dominic A. Quagliato
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Patent number: 7678923Abstract: Method for synthesising 1-aryl-4-(imidazol-2-yl)-3-alkyl-1H-pyrazole derivatives from 1-aryl-3-alkyl-1H-pyrazo-line-5-one derivatives.Type: GrantFiled: April 9, 2004Date of Patent: March 16, 2010Assignee: EVULTISInventors: Alessandro Mazzola, Giovanni Sanso
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Publication number: 20100063063Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: September 9, 2009Publication date: March 11, 2010Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Patent number: 7662827Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: July 24, 2006Date of Patent: February 16, 2010Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Wilfried Rautenberg
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Publication number: 20100022598Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: ApplicationFiled: October 16, 2007Publication date: January 28, 2010Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Michael M.C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Publication number: 20100004280Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: ApplicationFiled: October 16, 2007Publication date: January 7, 2010Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Jian Liu, Michael M.-C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 7553988Abstract: A method is provided for producing a specific crosscoupling compound and a specific catalyst for producing the compound. The method includes reacting in the presence of a base and a nickel compound catalyst organic halide of the formula n?(R1X1n), wherein R1 is a hydrocarbon group and the ? and ? carbons to X? are sp3 carbon atoms; X1 is a chlorine, bromine, or iodine atoms, and n and n1 are 1 or 2 but not both 2, with a compound having the formula m{R2(BX22)n?} where an R2 is an aryl, heteroaryl, or alkenyl group, and n? is 1 or 2, X2 is independently a hydroxyl group, an alkoxy or arylalkoxy group or X22 together form an alkylenedioxy or arylenedioxy group, and m represents 1 or 2 but m?n, and the boron atom is bonded to a sp2 carbon atom of R2 group or a boronic acid trimer anhydride.Type: GrantFiled: August 17, 2006Date of Patent: June 30, 2009Assignee: Sumitomo Chemical Company, LimtedInventors: Tamon Itahashi, Takashi Kamikawa
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Publication number: 20090149471Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: May 8, 2007Publication date: June 11, 2009Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Matthew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi k. Sawyer, Jan Antoinette C. Romero
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Publication number: 20090099209Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treatiType: ApplicationFiled: December 12, 2008Publication date: April 16, 2009Inventors: Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
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Publication number: 20090093498Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.Type: ApplicationFiled: December 10, 2008Publication date: April 9, 2009Applicant: WyethInventors: Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Ping Zhou, Yinfa Yan, Dominic A. Quagliato
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Patent number: 7514459Abstract: Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of ?-amyloid.Type: GrantFiled: September 16, 2004Date of Patent: April 7, 2009Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian James Collins, Joanne Clare Hannam, Andrew Madin, Mark Peter Ridgill
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Patent number: 7482349Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.Type: GrantFiled: June 15, 2005Date of Patent: January 27, 2009Assignee: WyethInventors: Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Ping Zhou, Yinfa Yan, Dominic A. Quagliato
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Publication number: 20080293936Abstract: The present invention concerns novel pyridazine-3-on- and pyrazol-3-on derivatives, methods of synthesizing such, a pharmaceutical agent containing pyridazine-3-on- and pyrazol-3-on derivatives as well as the use of the compounds for the prophylaxis or treatment of fibrotic diseases and/or pathologic remodelling and the use of said compounds for the expansion of stem cells.Type: ApplicationFiled: May 23, 2007Publication date: November 27, 2008Inventor: Elmar Reinhold Burchardt
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Publication number: 20080287681Abstract: The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R1 is optionally substituted amino or hydroxy, and the substituents R2 to R6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.Type: ApplicationFiled: July 16, 2008Publication date: November 20, 2008Inventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Sudhir Srivastava, Goutam Saha
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Patent number: 7429581Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: GrantFiled: December 23, 2003Date of Patent: September 30, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20080207647Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 24, 2006Publication date: August 28, 2008Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Wilfried Rautenberg
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Patent number: 7417152Abstract: Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.Type: GrantFiled: April 30, 2004Date of Patent: August 26, 2008Assignee: Elan Pharmaceuticals, Inc.Inventors: Jay S. Tung, Albert W. Garofalo, Michael A. Pleiss, Jing Wu, David W. G. Wone, Ashley C. Guinn, Darren B. Dressen, R. Jeffrey Neitz, Jennifer Marugg, Martin Neitzel
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Publication number: 20080132524Abstract: This invention pertains to compounds of Formula I, their N-oxides and suitable salts wherein A is O or S; G is a 5- or 6-membered heteroaromatic ring or a 5- or 6-membered nonaromatic heterocyclic ring optionally including one or two ring members selected from the group consisting of C(?O), SO or S(O)2, each ring optionally substituted with from one to four R2; each J is independently a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system, wherein each ring or ring system is optionally substituted with from one to four R3; and R1, R2, R3, R4 and n are as defined in the disclosure. A composition comprising a compound of Formula I, and a method for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I are also disclosed.Type: ApplicationFiled: December 19, 2007Publication date: June 5, 2008Inventors: David Alan Clark, Bruce Lawrence Finkelstein, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20080113998Abstract: The invention relates to 5-diazacycloalkylpyrazole derivatives of the formula (I) or salts thereof a process for their preparation, to compositions thereof and to their use for the control of pests, including arthropods and helminths.Type: ApplicationFiled: June 7, 2007Publication date: May 15, 2008Inventors: Stefan SCHNATTERER, Michael MAIER, Friederike PETRY, Werner KNAUF, Karl SEEGER
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Patent number: 7291642Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.Type: GrantFiled: October 21, 2005Date of Patent: November 6, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Norbert Hauel, Henri Doods, Angelo Ceci, Stefan Peters
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Patent number: 7285554Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substiType: GrantFiled: April 7, 2006Date of Patent: October 23, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Publication number: 20070238765Abstract: The present invention provides a compound of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Y, Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Inventors: Xiao-Fa Lin, David Garrett Loughhead, Jason Manka, Counde O'Yang, Michael Soth, Dennis M. Yasuda
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Patent number: 7253169Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.Type: GrantFiled: April 17, 2001Date of Patent: August 7, 2007Assignee: Gliamed, Inc.Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
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Patent number: 7247635Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more sType: GrantFiled: June 17, 2005Date of Patent: July 24, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Patent number: 7217677Abstract: A method is provided for producing a specific crosscoupling compound and a specific catalyst for producing the compound. The method includes reacting in the presence of a base and a nickel compound catalyst organic halide of the formula n?(R1X1n), wherein R1 is a hydrocarbon group and the ? and ? carbons to X? are sp3 carbon atoms; X1 is a chlorine, bromine, or iodine atoms, and n and n1 and 1 or 2 but not both 2, with a compound having the formula m{R2(BX22)n?} where an R2 is an aryl, heteroaryl, or alkenyl group, and n? is 1 or 2, X2 is independently a hydroxyl group, an alkoxy or arylalkoxy group or X22 together form an alkylenedioxy or arylenedioxy group, and m represents 1 or 2 but m?n, and the boron atom is bonded to a sp2 carbon atom of R2 group or a boronic acid trimer anhydride.Type: GrantFiled: January 14, 2004Date of Patent: May 15, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Tamon Itahashi, Takashi Kamikawa
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Patent number: 7214802Abstract: Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 7, 2005Date of Patent: May 8, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Ming-Hong Hao, Victor Marc Kamhi, Craig Andrew Miller, Matthew Russell Netherton, Alan David Swinamer
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Patent number: 7141581Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: August 12, 2003Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Bender, Dana Hu-Lowe, David Ray Shalinsky
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Patent number: 7091350Abstract: The invention relates to diaminopyrazole derivatives having the following structure (I), wherein R1 represents an alkyl or alkenyl radical bearing at least one substituent selected from among OR, NRR?, SR, SOR, SO2R, COOR, CONRR?, PO(OH)2, SO3X, NHCONRR, a non-cationic heterocycle, an aryl, a halogen. R2 and R3 are different from H and represent, independently of each other, an alkyl or alkenyl group; R2 and R3, together with the nitrogen atom to which they are attached, can form a heterocycle possibly comprising at least one other heteroatom selected from among N, O and S; R2 and R3 or the heterocycle that they form with the nitrogen to which they are attached can be substituted by at least one substituent defined above.Type: GrantFiled: February 14, 2002Date of Patent: August 15, 2006Assignee: L'OrealInventors: Thilo Fessmann, Eric Terranova
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Patent number: 7041669Abstract: Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): wherein Ar, X, A, L, and Q of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: February 19, 2003Date of Patent: May 9, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John Robinson Regan
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Patent number: 6958339Abstract: The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.Type: GrantFiled: February 2, 2001Date of Patent: October 25, 2005Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Jun Ishikawa, Makoto Takeuchi
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Patent number: 6906199Abstract: It is described a process for preparing, in high yields and purity and without the need of carrying out several steps and/or isolating many intermediates which could lead to undesired by-products, a distamycin derivative of formula wherein R is a bromine or chlorine atom; or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are useful in therapy as antitumor agents.Type: GrantFiled: November 7, 2001Date of Patent: June 14, 2005Assignee: Pharmacia Italia S.p.A.Inventors: Francensco Caldarelli, Lucio Ceriani, Ilaria Candiani
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Publication number: 20040224945Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) 1Type: ApplicationFiled: May 28, 2004Publication date: November 11, 2004Applicant: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hutter, Klaus Dembowsky, Elke Stahl
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Publication number: 20040204406Abstract: The present invention is directed to a compound of formula I, 1Type: ApplicationFiled: December 23, 2003Publication date: October 14, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Patent number: 6794518Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: December 17, 1999Date of Patent: September 21, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
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Patent number: 6753316Abstract: Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R1 and R2, which are the same or different, are selected from hydrogen, halogen, and C1-C4 alkyl; R3 is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and —C≡N; wherein R4, R5, R6, R7, R8, R10, R11, and R12 are, independently from each other, hydrogen or C1-C4 alkyl; and R9 is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R4, R5 and R6 is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.Type: GrantFiled: September 19, 2000Date of Patent: June 22, 2004Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Cozzi, Pier Giovanni Baraldi, Italo Beria, Marina Caldarelli, Laura Capolongo, Romeo Romagnoli
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Patent number: 6746989Abstract: The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), R1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkoxycarbonyl or cycloalkyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, Y represents hydrogen or represents in each case optionally substitutedType: GrantFiled: September 26, 2001Date of Patent: June 8, 2004Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Patent number: 6723743Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably atType: GrantFiled: September 28, 2000Date of Patent: April 20, 2004Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Xiao-shu He, He Zhao, John Peterson, Xiaoyan Zhang, Robbin Brodbeck, James Krause, George Maynard, Alan Hutchison