1,2,4-triazoles (including Hydrogenated) Patents (Class 548/262.2)
  • Publication number: 20100086915
    Abstract: The present invention relates to an in-vitro method of identifying a tumor resulting from a proliferative breast disease as responsive to anti-estrogen treatment. Further, the invention relates to an in-vitro method of identifying a candidate patient with a proliferative breast disease as suitable for anti-estrogen treatment. In a further aspect, the invention provides an in-vitro method of identifying an individual with a non-cancerous proliferative breast disease who is at risk of developing breast cancer. The invention also provides kits for performing the above methods.
    Type: Application
    Filed: June 26, 2007
    Publication date: April 8, 2010
    Applicant: UNIVERSITÄTSKLINIKUM HAMBURGEPPENDORF
    Inventors: Guido Sauter, Ronald Simon, Philip Stahl, Frederik Holst, Khawla A-Kuraya, Christian Ruiz
  • Patent number: 7691892
    Abstract: The present invention relates to new compounds of formula I, wherein P, Q, X1, X2, X3, X4, R1, R2, m and p, are as defined as in formula I, or, salts, solvates or solvated salts thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
    Type: Grant
    Filed: February 18, 2005
    Date of Patent: April 6, 2010
    Assignee: AstraZeneca AB
    Inventors: Martin Johansson, Alexander Minidis, Karin Staaf, David Wensbo, Donald McLeod, Louise Edwards, Methvin Isaac, Anne O'Brien, Abdelmalik Slassi, Tao Xin, Tomislav Stefanac
  • Patent number: 7692025
    Abstract: A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis(2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2?-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidinone, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K2CO3, and Na2CO3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-?,?,{acute over (?)},{acute over (?)}-tetramethyl, at a temperature below ?20° C. are performed.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: April 6, 2010
    Assignee: Sicor, Inc.
    Inventors: Marco Villa, Roberta Fretta, Nicola Diulgheroff, Alessandro Pontiroli
  • Publication number: 20100075500
    Abstract: The invention provides a metal polishing slurry containing a compound represented by the general formula (1): (X1)n-L wherein X1 represents a heterocycle containing at least one nitrogen atom, n represents an integer of 2 or more, and L represents a linking group having a valence of 2 or more, provided that X1s whose number is n may be the same or different, an oxidizer and an organic acid; and a method of chemical mechanical polishing using such slurry. The metal polishing slurry and the chemical mechanical polishing method are used in chemical mechanical polishing in the step of manufacturing semiconductor devices and enable a high polishing rate to be achieved while causing minimal dishing in polishing an object (wafer).
    Type: Application
    Filed: March 17, 2009
    Publication date: March 25, 2010
    Applicant: FUJIFILM Corporation
    Inventors: Masaru Yoshikawa, Tadashi Inaba, Hiroshi Inada, Takamitsu Tomiga
  • Patent number: 7683059
    Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome.
    Type: Grant
    Filed: September 5, 2006
    Date of Patent: March 23, 2010
    Assignee: Amgen Inc.
    Inventors: Mario G. Cardozo, Jay P. Powers, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
  • Patent number: 7683087
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: March 23, 2010
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Martha de la Rosa, Zhi Hong, Stanley Lang
  • Patent number: 7674811
    Abstract: The present invention relates to 5-lipoxygenase inhibitors. Compounds disclosed herein can be useful in the treatment of bronchial asthma, chronic obstructive pulmonary disorder, arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, urticaria, atopic dermatitis, allergic rhinitis, other inflammatory, and autoimmune diseases. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as 5-lipoxygenase inhibitors are also provided.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: March 9, 2010
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Ashwani Kumar Verma, Sanjay Malhotra, Abhijit Ray, Shirumalla Raj Kumar
  • Patent number: 7674807
    Abstract: Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: March 9, 2010
    Assignee: Bayer CropScience AG
    Inventors: Katsuaki Wada, Takuya Gombuchi, Yasushi Yoneta, Yuichi Otsu, Katsuhiko Shibuya, Norihiko Nakakura, Rüdiger Fischer, Tetsuya Murata, Eiichi Shimojo
  • Publication number: 20100055056
    Abstract: The present invention herein provides a compound which promotes drug-permeation into nails. A penetrating promoter comprises, for instance, the following formulas. R1, R2 and R3 are alkyl groups having a carbon number of 1 to 15 and have OH groups at their ends.
    Type: Application
    Filed: September 4, 2008
    Publication date: March 4, 2010
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Masatoshi KATO, Hiroyuki KUSAKABE, Kazuhiro NIMURA, Hiroaki KIMURA, Koh NAGASAWA, Akihiro HASHIGUCHI, Chisato HIROSAWA, Tomohiro TADA
  • Patent number: 7666890
    Abstract: Synthesis and herbicidal activity of novel 1-(2-substituted benzo[d]thiazol-5-yl)-1H-1,2,4-triazol-5(4H)-one derivatives. Using a dose of 300 gai./h, the compounds of the invention possess significant herbicidal activity for Echinochloa crusgalli, Digiatria sanguinalis, Setaria viridis, Brassica juncea, Amaranthus retroflexus and Chenopodium album.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: February 23, 2010
    Assignee: Huazhong Normal University
    Inventors: Guangfu Yang, Yanping Luo, Zuming Liu
  • Publication number: 20100041655
    Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2— or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).
    Type: Application
    Filed: February 5, 2007
    Publication date: February 18, 2010
    Inventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato
  • Patent number: 7662813
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: August 17, 2006
    Date of Patent: February 16, 2010
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, David James, Shijie Zhang, Teresa Przewloka, Elena Kostik, Junghyun Chae, Howard P Ng, Zhenjian Du, James Barsoum, Dinesh Chimmanamada, Chi-Wan Lee, Kevin Foley
  • Patent number: 7655806
    Abstract: Anastrozole can be purified by crystallization from an aqueous-based solvent system. The aqueous-based solvent system can contain dilute acid, or an alcohol or both.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: February 2, 2010
    Assignee: Synthon BV
    Inventors: Jaroslav Pis, Rudolf Smrz
  • Patent number: 7652051
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: January 26, 2010
    Assignee: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • Patent number: 7652145
    Abstract: The invention relates to a complex compound of ruthenium of the general structural formula I in which X1 and X2 may be identical or different and represent an anionic ligand, in which R1 and R2 are identical or different, but may also have a ring, in which R1 and R2 represent hydrogen or/and a hydrocarbon group, in which the ligand L1 is a N-heterocyclic carbene and in which the ligand L2 is a neutral electron donor, especially a N-heterocyclic carbene or an amine, imine, phosphane, phosphite, stibine, arsine, carbonyl compound, carboxyl compound, nitrile, alcohol, ether, thiol or thioether, wherein R1, R2, R3 and R4 represent hydrogen or/and hydrocarbon groups.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: January 26, 2010
    Assignee: Degussa AG
    Inventors: Wolfgang Anton Herrmann, Wolfgang Schattenmann, Thomas Weskamp
  • Patent number: 7642264
    Abstract: The present invention relates to compounds of formula (Ia), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, R1, R2, R3 and R4 are as defined in the description and claims.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: January 5, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 7625841
    Abstract: The invention relates to novel substituted thiene-3-ylsulphonylamino(thio)carbonyl-triazolin(ethi)ones of the formula (I) in which Q1, Q2, R1, R2, R3 and R4 are as defined in the disclosure, except for prior-art compounds. The invention further relates to the preparation of the compounds, to their use as herbicides, and to herbicidal compositions comprising the novel compounds.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: December 1, 2009
    Assignee: Bayer CropScience AG
    Inventors: Ernst Rudolf F. Gesing, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Publication number: 20090291967
    Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.
    Type: Application
    Filed: March 5, 2009
    Publication date: November 26, 2009
    Applicant: ADHEREX TECHNOLOGIES, INC.
    Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
  • Publication number: 20090286989
    Abstract: The present invention relates to an improved process for the preparation of anastrozole having enhanced purity from crude anastrozole having isomeric impurity content up to less than 1%. The invention also relates to a process comprising steps of converting (3-cyanomethyl-5-methylphenyl) acetonitrile to 2-[(3-cyanodimethylmethyl)-5-methyl phenyl]- meiliyl propiononitrile (II) by C-alkylation, which is further converted into 2-[3-halomethyl-5-cyanodimethyl methyl)phenyl] methyl propiononitrile (ill) by radical bromination and further to crude anastrozole by reacting (III) with sodium salt of 1,2,4-triazole, purification of the crude anastrozole by preparing its acid addition salt, generating required final anaslrozole from the acid addition salt.
    Type: Application
    Filed: March 8, 2007
    Publication date: November 19, 2009
    Inventors: B. Vishnukant, Prashant Purohit, K. Paparao, Veereshappa Veereshappa
  • Patent number: 7615555
    Abstract: Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
    Type: Grant
    Filed: April 20, 2005
    Date of Patent: November 10, 2009
    Assignee: AstraZeneca AB
    Inventors: Alan Faull, Howard Tucker
  • Patent number: 7612059
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: November 3, 2009
    Assignee: Vicuron Pharmaceuticals, Inc.
    Inventors: Jeffrey Jacobs, Rakesh K Patel, Jason G Lewis, Dinesh V Patel, Zhengyu Yuan
  • Publication number: 20090270633
    Abstract: The present invention relates to a process for the preparation of 4-[1-(4-cyano phenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile (letrozole), substantially free from its isomeric impurity. The preparation involves reaction of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile with 4-fluorobenzonitrile in the presence of an organic solvent and a silicon amine. The present invention also relates to a process for the preparation of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile which involves: (a) the reaction of a 4-halomethyl benzonitrile with 1,2,4-triazole in the presence of cesium carbonate and an organic solvent to obtain a reaction mass comprising 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile of formula II; and (b) precipitation of 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile (II) from the reaction mass using a suitable organic solvent.
    Type: Application
    Filed: March 19, 2007
    Publication date: October 29, 2009
    Inventors: Srinivas Laxminarayan Pathi, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Sandip Vasant Chikhalikar
  • Publication number: 20090253905
    Abstract: The invention relates to a method for producing onium salts comprising alkyl anions or aryl sulfonate anions or alkyl carboxylate anions or acryl carboxylate anions by reacting an onium halide with an alkyl silyl ester or trialkyl silyl ester of an alkyl sulfonic acid or aryl sulfonic acid or an alkyl carboxylic acid or aryl carboxylic acid or the anhydrides thereof.
    Type: Application
    Filed: November 18, 2005
    Publication date: October 8, 2009
    Inventors: Nikolai (Mykola) Ignatyev, Urs Weiz-Biermann, Andriy Kucheryna, Helge Willner
  • Patent number: 7598279
    Abstract: Azole compounds containing carbamoyl group and pharmaceutically useful salts thereof are described. The compounds are effective anticonvulsants which are used in the treatment of disorders of the central nervous system, especially as anxiety, depression, convulsion, epilepsy, migraine, bipolar disorder, drug abuse, smoking, ADHD, obesity, sleep disorder, neuropathic pain, stroke, cognitive impairment, neurodegeneration, stroke and muscle spasm.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: October 6, 2009
    Assignee: SK Holdings Co., Ltd.
    Inventors: Yong Moon Choi, Choon-Gil Kim, Han-Ju Yi, Young-Sun Kang, Hyun-Seok Lee
  • Publication number: 20090247765
    Abstract: The present invention discloses two new related substances (6) and (7) of Anastrozole synthesis from Q. A. Salt (5) as in Scheme—1 and purification procedures to get Anastrozole (1) free from (6) and (7).
    Type: Application
    Filed: September 4, 2006
    Publication date: October 1, 2009
    Applicant: Cadila Healthcare Limited
    Inventors: Kirtipalsinh Sajjansinh Solanki, Manoj Kumar Singh, Jay Shantilal Kothari, Virenda Kumar Agarwal
  • Patent number: 7592356
    Abstract: a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ?Z1—Z2?Z3— represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2), wherein n is 1 to 4, C(?O), C(?S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: September 22, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ashis Kumar Saha, David William End, Bart Lieven Daniel De Corte, Henry Joseph Breslin, Li Liu
  • Publication number: 20090234134
    Abstract: The present invention relates to compositions of matter that are ionic liquids, the compositions comprising any of eleven cations combined with any of three fluorinated sulfonated anions. Compositions of the invention should be useful as solvents and, perhaps, as catalysts for many reactions, including aromatic electrophilic substitution, nitration, acylation, esterification, etherification, oligomerization, transesterification, isomerization and hydration.
    Type: Application
    Filed: May 27, 2009
    Publication date: September 17, 2009
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Mark Andrew Harmer, Christopher P. Junk, Jemma Vickery
  • Patent number: 7579352
    Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: August 25, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
  • Patent number: 7576098
    Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: August 18, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter W. Glunz, Nicolas Wurtz, Xuhong Cheng
  • Patent number: 7572822
    Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: August 11, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Prasun K. Chakravarty, Louis L. Zuegner, III, legal representative, William H. Parsons, Brenda Palucki, Bishan Zhou, Min K. Park, Michael H. Fisher
  • Patent number: 7572816
    Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Publication number: 20090197929
    Abstract: The present invention relates to azolylmethyloxiranes of the general formula I in which A or B is a 5-membered heteroaryl selected from the group consisting of thienyl, furyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl and isothiazolyl which is substituted by one to three of the following substituents: halogen, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and the respective other substituent A or B is phenyl which is optionally substituted by one to three of the following substituents: halogen, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and to the plant-compatible acid addition salts or metal salts thereof, to the use of the compounds of the formula I for controlling phytopathogenic fungi and to compositions comprising these compounds.
    Type: Application
    Filed: June 25, 2007
    Publication date: August 6, 2009
    Applicant: BASF SE
    Inventors: Jochen Dietz, Thomas Grote, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glättli
  • Patent number: 7569699
    Abstract: This invention provides a process for producing an epoxytriazole derivative represented by formula (2): (wherein R and Ar are defined below), which comprises a step including a reaction of an epoxy derivative represented by formula (1?): (wherein R represents a hydrogen atom or C1-12 alkyl group and Ar represents an aromatic group optionally substituted by a halogen atom(s) or trifluoromethyl group(s), and X? represents a hydroxy group or leaving group), with 1,2,4-triazole in the presence of a base and water.
    Type: Grant
    Filed: November 29, 2005
    Date of Patent: August 4, 2009
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Taro Ishibahsi, Hideo Muraoka, Tadashi Mizuno
  • Publication number: 20090186928
    Abstract: Novel crystalline salts of 3-[1-(4-chlorophenyl)-trans-3-fluorocyclobutyl]-4,5-dicyclopropyl-r-4H-1,2,4-triazole are potent inhibitors of 11?-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.
    Type: Application
    Filed: January 21, 2005
    Publication date: July 23, 2009
    Inventors: Yuri Bereznitski, Mark A. Huffman, Joseph E. Lynch, Matthew Zhao
  • Patent number: 7563905
    Abstract: The present invention is directed to compounds of formula (I): wherein R1, R2 and R3 are independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl and X1 and X2 are independently a bond or an linker group of 1 to 6 atoms and may be optional substituted or oxidized, or a prodrug, a pharmaceutically acceptable salt or a pharmaceutically active metabolite thereof. The invention is also directed to methods of using the same for treating HIV infections, or AIDs or preventing viral replication.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: July 21, 2009
    Assignee: Wyeth
    Inventors: Matthew Olson, Martin Di Grandi
  • Patent number: 7538230
    Abstract: Provided is a method for preparing letrozole, which includes reacting an activated bis-(4-cyanophenyl)-methane with a triazole to produce letrozole, and, optionally, purifying the letrozole. Also provided are highly pure letrozole, and a method of purifying letrozole, which method includes precipitating letrozole, e.g., by selective precipitation from a reaction mixture and/or by subjecting the letrozole to one or more crystallizations.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: May 26, 2009
    Assignee: Chemagis Ltd.
    Inventors: Oded Friedman, Boris Freger, Olga Etlin, Julia Ditkovitch, Edna Danon, Yana Seryi, Guy Davidi, Oded Arad, Joseph Kaspi
  • Patent number: 7531560
    Abstract: Disclosed are 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: Grant
    Filed: November 9, 2005
    Date of Patent: May 12, 2009
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Derek Cogan, Matthew Russell Netherton
  • Publication number: 20090118517
    Abstract: The invention is directed to processes for purifying the Anastrozole intermediate, 3,5-bis(2-cyanoisopropyl)toluene, processes for producing Anastrozole, processes for preparing Anastrozole pharmaceutical compositions, and Anastrozole and Anastrozole pharmaceutical compositions prepared with the processes of the invention.
    Type: Application
    Filed: December 22, 2008
    Publication date: May 7, 2009
    Inventors: Alessandro Pontiroli, Roberto Casalone
  • Publication number: 20090093472
    Abstract: Compounds of the formula are disclosed. The compounds are CCR1 antagonists which are useful for the treatment and prevention of inflammatory and autoimmune diseases. Other embodiments are also disclosed.
    Type: Application
    Filed: October 3, 2008
    Publication date: April 9, 2009
    Applicant: PHARMACOPEIA, INC.
    Inventors: Vidyadhar M. Paradkar, Marc Brescia, Ray James, Jinqi Liu, Ruiyan Liu, James Robert Merritt, Michelle Morris, Michael J. Ohlmeyer, Chongwu Zhang, Rui Zhang
  • Patent number: 7511061
    Abstract: A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(?O), C(?S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hy
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: March 31, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ashis Kumar Saha, David William End, Bart Lieven Daniel De Corte, Henry Joseph Breslin, Li Liu
  • Publication number: 20090082413
    Abstract: The present application describes deuterium-enriched letrozole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 26, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7507755
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: March 24, 2009
    Assignee: IRM LLC
    Inventors: Hong Liu, Phillip B. Alper, Donald S. Karanewsky
  • Publication number: 20090062550
    Abstract: The present invention provides a method for preparing pure Rizatriptan benzoate having purity more than 99.5% and dimer impurity less than 0.1% comprises, i) Condensation of 1,2,4-Triazole with 4-Nitro benzyl bromide to yield 1-(4-nitrophenyl)methyl-1,2,4-triazole ii) Reducing the 1-(4-nitrophenyl)methyl-1,2,4-triazole to give 1-(4-aminophenyl)methyl-1,2,4-triazole iii) Converting 1-(4-aminophenyl)methyl-1,2,4-triazole to 1-(4-hydrazinophenyl)methyl-1,2,4-triazole hydrochloride iv) Condensing the hydrazine derivative with 4-(Dimethylamino) butanal diethylacetal to get Rizatriptan and v) Salification of Rizatriptan to Rizatriptan benzoate.
    Type: Application
    Filed: November 14, 2006
    Publication date: March 5, 2009
    Applicant: MATRIX LABORATORIES LTD
    Inventors: Purna Chandra Ray, Mohan Bandari, Mohammed Qadeeruddin, Seeta Ramanjaneyulu Gorantla
  • Patent number: 7473705
    Abstract: The invention is concerned with novel hexafluoroisopropanol substituted ether derivatives of formula (I): wherein R1 to R3 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
    Type: Grant
    Filed: September 28, 2005
    Date of Patent: January 6, 2009
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Henrietta Dehmlow, Bernd Kuhn, Narendra Panday, Hasane Ratni, Matthew Blake Wright
  • Patent number: 7473700
    Abstract: A 1,2,4-triazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided.
    Type: Grant
    Filed: November 26, 2003
    Date of Patent: January 6, 2009
    Assignee: CJ Corporation
    Inventors: Il Hwan Cho, Dong Hyun Ko, Myeong Yun Chae, In Ki Min, Young Hoon Kim, Kyu Jeong Yeon, Jong Hoon Kim, Sung Hak Jung, Sang Wook Park, Il Hwan Kim, Hyung Chul Ryu, Ji Young Noh, Hyun Jung Park, Jie Eun Park, Young Mee Chung
  • Patent number: 7470716
    Abstract: The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: June 24, 2005
    Date of Patent: December 30, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Leo Thomas, Mohammad Tadayyon
  • Publication number: 20080319037
    Abstract: There is provided a compound of Formula I wherein R3, R4, R5, R6 and R7 are independently selected from H and —Y—R8; wherein each R8 is independently selected from —OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2), H-bond acceptors, and halogens; wherein at least one of R3, R4, R5, R6 and R7 is —Y—R8 wherein R8 is selected from substituted and unsubstituted heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further substituted; wherein R9 is selected from H, —OH and —OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R3, R4, R5, R6 and R7 is —Y—R8; OR (b) R9 is —OSO2NR1R2 or —OH and four of R3, R4, R5, R6 and R7 are H and one of R3, R4, R5, R6 and R7 is —Y—R8. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.
    Type: Application
    Filed: June 13, 2008
    Publication date: December 25, 2008
    Inventors: Lok Wai Lawrence Woo, Toby Jackson, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
  • Patent number: 7468385
    Abstract: The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: December 23, 2008
    Assignee: Laboratoires Serono SA
    Inventors: Anna Quattropani, Matthias Schwarz, Russell J. Thomas, Thomas Coulter
  • Patent number: 7465749
    Abstract: Provided is a process for purifying a letrozole product that contains an isoletrozole impurity, which process preferably includes converting at least a portion of the isoletrozole impurity into 4,4?-dicyanobenzophenone and removing 4,4?-dicyanobenzophenone, to produce a purified letrozole product.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: December 16, 2008
    Assignee: Chemagis, Ltd.
    Inventors: Michal Hasson, Hila Isenberg, Efrat Manoff, Moshe Bentolila, Oded Friedman, Lior Zelikovitch
  • Patent number: 7459475
    Abstract: Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: November 10, 2004
    Date of Patent: December 2, 2008
    Assignee: Merck & Co. Inc.
    Inventors: Min K. Park, Prasun K. Chakravarty, Bishan Zhou, Edward Gonzalez, Hyun Ok, Brenda Palucki, William H. Parsons, Rosemary Sisco, Louis L. Zuegner, III, legal representative, Michael H. Fisher