Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding [e.g., 1-(2-hydroxyethyl)-3-amino-4(para-chlorophenyl)-pyrazole, Etc.] Patents (Class 548/372.5)
-
Publication number: 20110130431Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Renee M. ZINDELL, Nigel BLUMIRE, Chandana CHOWDHURY, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Christopher Francis PALMER, Malcolm TAYLOR
-
Publication number: 20110112073Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Applicant: DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
-
Patent number: 7935699Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I) useful for the treatment of metabolic diseases and disorders, preferably diabetes mellitus.Type: GrantFiled: July 19, 2007Date of Patent: May 3, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Ramakanth Sarabu, Chinh Viet Tran, Dionisios Vourloumis
-
Patent number: 7928123Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 13, 2007Date of Patent: April 19, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
-
Publication number: 20110046195Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.Type: ApplicationFiled: June 24, 2010Publication date: February 24, 2011Inventors: Helen E. BLACKWELL, Christine E. McInnis
-
Publication number: 20110034521Abstract: The present invention provides compounds and methods for treating zinc matrix metalloprotease dependent diseases.Type: ApplicationFiled: September 19, 2008Publication date: February 10, 2011Inventors: Alan Jacobson, Scott Moe
-
Publication number: 20100310493Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: October 7, 2008Publication date: December 9, 2010Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITEDInventors: Debnath Bhuniya, Sandeep Bhausaheb Bhosale, Gobind Sing Kapkoti, Venkata Poornapragnacharyulu Palle, Siddhartha De, Kasim A. Mookhtiar, Bhavesh Dave, Anil Deshpande, Santosh Kurhade, Balasaheb Kobal, Keshav Naik, Sachin Kandalkar
-
Publication number: 20100292274Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Inventors: Jean-Francois Rossignol, J. Edward Semple
-
Publication number: 20100286171Abstract: A phenylacetamide derivative having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide has an excellent GK activation action, thereby completing the present invention. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, since it has an excellent GK activation action.Type: ApplicationFiled: January 16, 2009Publication date: November 11, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Yoshiyuki Kido, Takahiro Nigawara, Mitsuaki Okumura, Akira Kanai, Keisuke Maki, Nobuaki Amino
-
Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
-
Publication number: 20100273744Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.Type: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Inventors: Paul Martin Gore, Steven Leslie Sollis
-
Publication number: 20100249087Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: Xueqing Wang, Jennifer M. Frost, Michael J. Dart, Bo Liu
-
Publication number: 20100249086Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: Xueqing Wang, Michael J. Dart, Bo Liu
-
Publication number: 20100222217Abstract: N-[2-(Haloalkoxy)phenyl]heteroarylcarboxamides of the formula I, where n=0 or 1, Hal=halogen, X=C2-C4-haloalkyl, Het=a pyrazole, thiazole or pyridine radical (a), (b) or (c), where R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, R3=C1-C4-alkyl or C1-C4-haloalkyl and R5=halogen, C1-C4-alkyl or C1-C4-haloalkyl; except for N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-1,3-dimethylpyrazol-4-yl-carboxamide, N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-trifluoromethyl-1-methylpyrazol-4-yl-carboxamide and N-[2-(2,2,2-trifluorethoxy)phenyl]-3-trifluormethyl-1-methylpyrazol-4-yl-carboxamide. A fungicidal composition comprising at least one compound I, the use of the compounds I for preparing a composition suitable for controlling harmful fungi, a method for controlling harmful fungi using the compounds I and also seed comprising at least one compound I.Type: ApplicationFiled: August 2, 2006Publication date: September 2, 2010Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann
-
Publication number: 20100210690Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, Alk and D have the meanings indicated in claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: September 9, 2008Publication date: August 19, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Lars Thore Burgdorf, Norbert Beier, Johannes Gleitz, Ulrich Emde, Christine Charon, Denis Carniato
-
Publication number: 20100099671Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).Type: ApplicationFiled: March 6, 2008Publication date: April 22, 2010Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Kohei Ohata, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
-
Patent number: 7700640Abstract: A process for making a compound of formula (I), said process comprising a) reacting a compound of formula (II) with: i) a compound of formula (III) by nucleophilic aromatic substitution of X2 and ii) a compound of formula (IV) for example by nucleophilic aromatic substitution b) where necessary, converting X1 to a carboxylic acid; and c) coupling of the carboxylic acid group to an appropriate heterocyclic amine; wherein all variables are as defined in the description.Type: GrantFiled: October 11, 2005Date of Patent: April 20, 2010Assignee: AstraZeneca ABInventors: Philip Cornwall, David Simon Ennis, Melvyn Edward Giles, Jacob Robert James Perkins, Shelly Louise Jenkin, Jeremy Stephen Parker, Bharti Patel
-
Publication number: 20100063106Abstract: Provided are aminopyrazole derivatives, a process for the preparation thereof, and a composition for preventing or treating an ischemic disease containing the same. Since the aminopyrazole derivatives of the present invention can reduce an ischemic cell death significantly, they can be effectively used for the prevention and treatment of ischemic diseases mediated by ischemic cell death, or protection of organs.Type: ApplicationFiled: October 26, 2007Publication date: March 11, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Yong-Sam JUNG, Eunhee Kim, Nakjeong Kim, Yun-Sun Lee, Jeehee Suh, Haeyoung Suh, Kyu Yang Yi, Sung-eun Yoo
-
Publication number: 20090326241Abstract: A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed, wherein the pyrimidine ring is cyclized using a cyanating agent.Type: ApplicationFiled: September 2, 2009Publication date: December 31, 2009Inventors: Shen-Chun Kuo, David Jieh-Shyh Tsai, Loc Thanh Tran, Pengyi Zhang, Andrew D. Jones
-
Publication number: 20090291965Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.Type: ApplicationFiled: October 30, 2006Publication date: November 26, 2009Inventors: Joshua Close, Richard W. Heidebrecht, Solomon Kattar, Thomas A. Miller, David Sloman, Matthew G. Stanton, Paul Tempest, David J. Witter
-
Publication number: 20090291984Abstract: The disclosure relates to a compound of formula (1): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.Type: ApplicationFiled: May 8, 2009Publication date: November 26, 2009Applicant: sanofi-aventisInventors: Kirsten Bjergarde, Mark Dodson, Jacques Mauger, Anil Nair, Marcel Patek, Michel Tabart
-
Publication number: 20090239845Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein Z, R1, R2a, R2b, R10, R11 and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: April 24, 2006Publication date: September 24, 2009Inventors: Elizabeth Ann Conway, Gerard Martin Paul Giblin, Mairi Gibson, Adrian Hall, Thomas George Christopher Hayhow, Mark Patrick Healy, David Nigel Hurst, Ian Reginald Kilford, Stephen Carl McKeown, Alan Naylor, Helen Susanne Price, Derek Anthony Rawlings
-
Patent number: 7538135Abstract: Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.Type: GrantFiled: July 7, 2004Date of Patent: May 26, 2009Assignee: Novartis AGInventor: Thalaththani Ralalage Vedananda
-
Publication number: 20090131662Abstract: This invention is related to compositions and methods pertaining to PNA synthons, PNA oligomers and/or PNA/DNA Chimeras comprising a universal base.Type: ApplicationFiled: January 23, 2009Publication date: May 21, 2009Applicant: LIFE TECHNOLOGIES CORPORATION, a Delaware CorporationInventors: Birenda K. Bhattacharya, James M. Coull
-
Publication number: 20090062365Abstract: The present invention relates to novel pyrazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and Y are as defined in the description. For example, R1 may be hydrogen or alkyl, R2 may be hydrogen or alkyl, R3 may be alkoxy and Y may be a carbonylamino linked substituent containing an aryl group.Type: ApplicationFiled: December 21, 2006Publication date: March 5, 2009Inventor: Udo Bauer
-
Publication number: 20090054444Abstract: Compounds of Formula (I) wherein R1 is a cycloalkylsulphonyl group, or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: August 9, 2005Publication date: February 26, 2009Inventors: Matthew Colin Thor Fyfe, Vilasben Kanji Shah
-
Publication number: 20090005559Abstract: A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed, wherein the pyrimidine ring is cyclized using a cyanating agent.Type: ApplicationFiled: September 11, 2008Publication date: January 1, 2009Inventors: Shen-Chun Kuo, David Jieh-Shyh Tsai, Loc Thanh Tran, Pengyi Zhang, Andrew D. Jones
-
Publication number: 20080312435Abstract: An imine compound represented by the formula: wherein A represents a heterocyclic group; R1, R2, an R3 each represent a hydrogen atom, a halogen atom, a C1-10 alkyl group optionally substituted with an aryl group(s) substituted with a halogen atom(s), a C3-10 cycloalkyl group, a C1-6 haloalkyl group, a C1-10 alkoxy group, etc.; R4 represents an optionally substituted C1-10 alkyl, C2-6 alkenyl, or aryl group; R5 represents a hydrogen atom, a C1-10 alkoxy group, a C1-6 haloalkyl group, an optionally substituted C1-10 alkyl or C2-6 alkenyl group, an optionally substituted aryl or heterocyclic group, etc.; W represents —CO—, —CO—CO—, —CO—NH—, —CS—NH—, or —SO2—, or a cannabinoid-receptor agonist comprising said imine compound as an active ingredient. The imine compound of the present invention has a cannabinoid-receptor agonist effect, and is useful as a therapeutic or prophylactic drug for pains and autoimmune diseases.Type: ApplicationFiled: October 31, 2005Publication date: December 18, 2008Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Shiuji Saito, Hiroshi Ohta, Tomoko Ishizaki, Mitsukane Yoshinaga, Makoto Tatsuzuki, Yuji Yokobori, Yasumitsu Tomishima, Aki Morita, Yoshihisa Toda, Kimiko Tokugawa, Ayaka Kaku, Tomomi Murakami, Hiromitsu Yoshimura, Shingo Sekine, Takao Yoshimizu
-
Publication number: 20080275092Abstract: The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, or pyrazinyl ring; R2 is alkyl or an amino group as defined herein; and Z is optionally-substituted oxadiazolyl or —C(?O)NR6, wherein R6 is lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing pharmaceutical compositions for treating p38 kinase related conditions and/or in methods of treating conditions associated with the activity of p38 kinase in a patient.Type: ApplicationFiled: May 12, 2008Publication date: November 6, 2008Inventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Rulin Zhao, Bank-Chi Chen, Stephen T. Wrobleski
-
Publication number: 20080269207Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, 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; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: October 19, 2007Publication date: October 30, 2008Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
-
Publication number: 20080269500Abstract: Processes for the preparation of 4-aminopyrazole and derivatives thereof, such as those of formula (C), which are useful as intermediates in the preparation of pharmaceutical compounds; to certain compounds used in these processes; and to processes for the preparation of said compounds.Type: ApplicationFiled: September 20, 2006Publication date: October 30, 2008Applicant: ASTRAZENECA ABInventor: George Beresford Hill
-
Publication number: 20080234273Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: June 3, 2006Publication date: September 25, 2008Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
-
Publication number: 20080200694Abstract: A process for making a compound of formula (I), said process comprising a) reacting a compound of formula (II) with: i) a compound of formula (III) by nucleophilic aromatic substitution of X2 and ii) a compound of formula (IV) for example by nucleophilic aromatic substitution b) where necessary, converting X1 to a carboxylic acid; and c) coupling of the carboxylic acid group to an appropriate heterocyclic amine; wherein all variables are as defined in the description.Type: ApplicationFiled: October 11, 2005Publication date: August 21, 2008Inventors: Philip Cornwall, David Simon Ennis, Melvyn Edward Giles, Jacob Robert James Perkins, Shelly Louise Jenkin, Jeremy Stephen Parker, Bharti Patel
-
Publication number: 20080188536Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: August 7, 2008Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
-
Publication number: 20080153812Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: December 18, 2007Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: David Buttar, Kevin Micheal Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
-
Publication number: 20080146625Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.Type: ApplicationFiled: December 6, 2007Publication date: June 19, 2008Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
-
Publication number: 20080132495Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 30, 2005Publication date: June 5, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Maria Grazia Carr, Adrian Liam Gill, Steven Howard, Eva Figueroa Navarro, Gary Trewartha, David Charles Rees, Mladen Vinkovic, Paul Graham Wyatt
-
Publication number: 20080021032Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I) useful for the treatment of metabolic diseases and disorders, preferably diabetes mellitus.Type: ApplicationFiled: July 19, 2007Publication date: January 24, 2008Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Ramakanth Sarabu, Chinh Viet Tran, Dionisios Vourloumis
-
Patent number: 7208514Abstract: A compound having a xanthine oxidase inhibitory activity, such as 1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid and the like, can be a drug for preventing cancer including colon cancer and the like, as an agent for suppressing tumorigenesis.Type: GrantFiled: March 12, 2004Date of Patent: April 24, 2007Assignee: Mitsubishi Pharma CorporationInventor: Norihisa Kato
-
Patent number: 7183306Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.Type: GrantFiled: November 14, 2003Date of Patent: February 27, 2007Assignee: Astellas Pharma Inc.Inventors: Fumiyuki Shirai, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
-
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
-
Patent number: 7070629Abstract: The invention relates to a dye composition comprising a first oxidation base of the diaminopyrazole type, a second oxidation base of the para-phenylenediamine type containing a cyclic amino group, and a coupler. The invention also relates to the use of this composition for dyeing keratin fibers and also to the dyeing process using this composition.Type: GrantFiled: September 27, 2002Date of Patent: July 4, 2006Assignee: L'Oreal, S.A.Inventors: Sylvain Kravtchenko, Alain Lagrange
-
Patent number: 7037880Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.Type: GrantFiled: August 8, 2002Date of Patent: May 2, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
-
Patent number: 7034049Abstract: Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3–C6 cycloalkyl group optionally substituted by a straight or branched C1–C6 alkyl or arylalkyl group; R1 is a straight or branched C1–C6 alkyl, C2–C4 alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl or arylalkenyl group, each of which may be optionally further substituted as indicated in the description; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.Type: GrantFiled: May 5, 2000Date of Patent: April 25, 2006Assignees: Pharmacia Italia S.p.A., Pharmacia & Upjohn Company LLCInventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce, Maria Grabriella Brasca
-
Patent number: 7004979Abstract: The invention relates to a dye composition comprising an oxidation base of the diaminopyrazole type and a pyrazolo-azole coupler. The invention also relates to the use of this composition for dyeing keratin fibres and also to the dyeing process using this composition.Type: GrantFiled: September 27, 2002Date of Patent: February 28, 2006Assignee: L'Oreal S.A.Inventors: Sylvain Kravtchenko, Alain Lagrange
-
Patent number: 6979693Abstract: The present invention relates to certain pyrazole derivatives of Formula (I): that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: February 1, 2002Date of Patent: December 27, 2005Assignee: Syntex (U.S.A.) LLCInventors: David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjogren, Francisco Xavier Talamas
-
Patent number: 6905522Abstract: Dye compositions comprising, in a medium suitable for dyeing: at least one first oxidation base chosen from 4,5-diaminopyrazole derivatives of formula (I) and addition salts thereof, at least one second cationic oxidation base chosen from monobenzenic, dibenzenic and heterocyclic oxidation bases, and the addition salts thereof, comprising at least one cationic group Z chosen from aliphatic chains optionally bearing at least one ring chosen from saturated and unsaturated rings; wherein said at least one cationic group Z is linked directly to at least one benzenic ring or to at least one heterocycle of said at least one second cationic oxidation base or linked to at least one amine functional group borne by said at least one benzenic ring or said at least one heterocycle; and at least one coupler; as well as the use of this composition for dyeing keratin fibers and the dying process using this composition.Type: GrantFiled: February 11, 2003Date of Patent: June 14, 2005Assignee: L'Oreal S.A.Inventors: Sylvain Kravtchenko, Alain Lagrange
-
Patent number: 6838458Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, ring G, R1 through R7 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: January 4, 2005Assignee: Pfizer, Inc.Inventor: Subas M. Sakya
-
Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
-
Patent number: 6677335Abstract: Compounds of the formula (I): wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).Type: GrantFiled: October 6, 2000Date of Patent: January 13, 2004Assignee: Pfizer IncInventors: Mark Edward Bunnage, Keith Michael DeVries, Laurence James Harris, Philip Charles Levett, John Paul Mathias, Joanna Teresa Negri, Stephen Derek Albert Street, Albert Shaw Wood