The Chalcogen Is Bonded Directly To A Ring Carbon Of The Five-membered Hetero Ring Which Is Adjacent To The Ring Nitrogen (e.g., 2-indolinones, Etc.) Patents (Class 548/486)
-
Publication number: 20110263670Abstract: The present invention relates to novel polymorphs of sunitinib free base designated form II and form III and to processes for their preparation. The invention also relates to their use as APIs and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising said novel polymorphs and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.Type: ApplicationFiled: August 24, 2009Publication date: October 27, 2011Inventors: Vinayak Gore, Bharati Choudhari, Mahesh Hublikar, Prakash Bansode
-
Publication number: 20110251200Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.Type: ApplicationFiled: September 11, 2009Publication date: October 13, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Peter Toogood, Gina Ney
-
Publication number: 20110251193Abstract: Novel classes of 1,2-benzisothiazolinone and isoindolinone compounds and compositions are disclosed. These compounds and compositions are useful in treating, preventing, and/or ameliorating viral, yeast, and fungal infections such as, for example, Hepatitis C Virus, Flavivirus infections, Aspergillus fumigatus, and candidiasis.Type: ApplicationFiled: September 23, 2009Publication date: October 13, 2011Applicants: WICHITA STATE UNIVERSITY, GEORGETOWN UNIVERSITYInventors: Richard A. Calderone, William C. Groutas, Brent E. Korba
-
Publication number: 20110207941Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Inventors: ULRICH BERENS, OLIVER DOSENBACH, DANIEL SPRENGER
-
Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
-
Publication number: 20110190294Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: ApplicationFiled: April 16, 2009Publication date: August 4, 2011Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
-
Patent number: 7981880Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: April 23, 2007Date of Patent: July 19, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Treu, Andreas Mantoulidis, Ulrike Tontsch-Grunt
-
Patent number: 7968731Abstract: An improved process is described for the purification of ropinirole hydrochloride. The process includes (i) dissolving ropinirole hydrochloride in water; (ii) treating the solution obtained in step (i) with sodium dithionate and charcoal; (iii) treating the filtrate obtained in step (ii) with water immiscible solvent and base and isolating the free base; and (iv) treating the free base obtained in step (iii) with ethanolic HCl to give ropinirole hydrochloride.Type: GrantFiled: March 21, 2007Date of Patent: June 28, 2011Assignee: Alembic LimitedInventors: Pandurang Balwant Deshpande, Ashok Prataprai Shanishchara, Trushar Rajanikant Shah, Hitarth Harshendu Acharya, Parven Kumar Luthra
-
Publication number: 20110135594Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: July 14, 2009Publication date: June 9, 2011Inventors: Michael Graupe, Chandrasekar Venkataramani
-
Publication number: 20110130437Abstract: The present invention relates to salt forms of the compound 4-[(Z)-[[4-[(dimethylaminoJmethyllphenyllaminolCe-fluoro-1,2-dihydro2-oxo-3H-indol-3-ylidene)methyl]-benzenepropanoic acid which are suitable for pharmaceutical development and to a process for their manufacture.Type: ApplicationFiled: January 22, 2009Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrike Werthmann, Christian Kulinna, Waldemar Pfrengle, Werner Rall
-
Publication number: 20110071195Abstract: The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.Type: ApplicationFiled: September 14, 2010Publication date: March 24, 2011Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajung Nan, Tao Pang, Lifang Yu, Mei Zhang
-
Publication number: 20110071132Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.Type: ApplicationFiled: July 30, 2010Publication date: March 24, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Andrea Hager-Wernet, Wilfried Hornberger, Liliane Unger
-
Publication number: 20110046395Abstract: The present invention relates to a process for the manufacture of the compound 4-[(Z)-[[4-[(dimethylamino)methyl]phenyl]amino](6-fluoro-1,2-dihydro-2-oxo-3H-in-dol-3-ylidene)methyl]-benzenepropanoic acid and to a new intermediate for the synthesis.Type: ApplicationFiled: January 22, 2009Publication date: February 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Werner Rall, Waldemar Pfrengle, Juergen Schnaubelt
-
Patent number: 7868034Abstract: This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: June 17, 2008Date of Patent: January 11, 2011Assignee: H. Lundbeck A/SInventors: Michael Konkel, John M. Werzel, Jamie Talisman
-
Patent number: 7863462Abstract: The present invention provides an improved process for the purification of ropinirole hydrochloride. The process includes (i) treating ropinirole hydrochloride with sodium dithionate and charcoal in suitable alcoholic solvent; (ii) triturating the ropinirole hydrochloride obtained in step (i) with ethanol; (iii) reacting the triturated solid with base in water immiscible solvent and isolating the free base; and (iv) treating the free base obtained in step (iii) with ethanolic HCl to give ropinirole hydrochloride.Type: GrantFiled: March 21, 2007Date of Patent: January 4, 2011Assignee: Alembic LimitedInventors: Pandurang Balwant Deshpande, Parven Kumar Luthra, Hitarth Harshendu Acharya
-
Publication number: 20100311715Abstract: This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.Type: ApplicationFiled: August 19, 2010Publication date: December 9, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, R. Scott Rowland, Dilrukshi Vitharana
-
Publication number: 20100311985Abstract: The present invention relates to specific indolinone derivatives, namely the compounds of formula, in which R1 represents an hydrogen atom or a group, and R2 and R3 each represent an hydrogen atom or R2 and R3 taken together represent a group, with the proviso that when R1 represents an hydrogen atom R2 and R3 taken together represent a group, and to a process for their manufacture.Type: ApplicationFiled: December 2, 2008Publication date: December 9, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joern Mertten, Svenja Renner, Carsten Reichel
-
Patent number: 7846962Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: GrantFiled: February 10, 2009Date of Patent: December 7, 2010Assignee: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
-
Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
-
Publication number: 20100249433Abstract: An improved process is described for the purification of ropinirole hydrochloride. The process includes (i) dissolving ropinirole hydrochloride in water; (ii) treating the solution obtained in step (i) with sodium dithionate and charcoal; (iii) treating the filtrate obtained in step (ii) with water immiscible solvent and base and isolating the free base; and (iv) treating the free base obtained in step (iii) with ethanolic HCl to give ropinirole hydrochloride.Type: ApplicationFiled: March 21, 2007Publication date: September 30, 2010Applicant: ALEMBIC LIMITEDInventors: Pandurang Balwant Deshpande, Ashok Prataprai Shanishchara, Trushar Rajanikant Shah, Hitarth Harshendu Acharya, Parven Kumar Luthra
-
Patent number: 7803834Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.Type: GrantFiled: March 23, 2006Date of Patent: September 28, 2010Assignee: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger
-
Publication number: 20100227863Abstract: The present application discloses substituted 3-(4-hydroxyphenyl)-indolin-2-one compounds (oxindole compounds) of the formula and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal, in particular in humans.Type: ApplicationFiled: April 28, 2008Publication date: September 9, 2010Applicant: TOPOTARGET A/SInventors: Mette Knak Christensen, Fredrik Bjoerkling
-
Publication number: 20100179332Abstract: The present invention provides an improved process for the purification of ropinirole hydrochloride. The process includes (i) treating ropinirole hydrochloride with sodium dithionate and charcoal in suitable alcoholic solvent; (ii) triturating the ropinirole hydrochloride obtained in step (i) with ethanol; (iii) reacting the triturated solid with base in water immiscible solvent and isolating the free base; and (iv) treating the free base obtained in step (iii) with ethanolic HCl to give ropinirole hydrochloride.Type: ApplicationFiled: March 21, 2007Publication date: July 15, 2010Applicant: Alembic LimitedInventors: Pandurang Balwant Deshpande, Parven Kumar Luthra, Hitarth Harshendu Acharya
-
Patent number: 7754895Abstract: Processes for preparing oxindoles, which can be utilized in the preparation of a variety of useful compounds, and methods for minimizing or preventing N-alkylation of amide containing compounds, including oxindoles, are provided.Type: GrantFiled: July 27, 2006Date of Patent: July 13, 2010Assignee: Wyeth LLCInventors: Yanzhong Wu, Bogdan Kazimierz Wilk, Zhixian Ding, Xinxu Shi, Charles Chao Wu, Panolil Raveendranath, Haris Durutlic
-
Publication number: 20100158842Abstract: A cosmetic and dermatological composition comprises 2, 3-dihydro-4-hydroxy-2-oxo-1-H-indole-3-acetic acid (4-hydroxy-1-oxindole-3-acetic acid) as an active ingredient for use as a melanin inhibitor and as an anti-tyrosinase enzyme inhibitor. This composition is excellent as a skin whitening agent. Since it also has potent antioxidant and anti-irritant activities it is useful in a cosmetic composition for improving hyperpigmentation disorders of the skin.Type: ApplicationFiled: October 9, 2009Publication date: June 24, 2010Inventor: John Jacob WILLE, Jr.
-
Patent number: 7737174Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: GrantFiled: August 30, 2007Date of Patent: June 15, 2010Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Dongguang Qin, Jiangyong Chen, Shanghai Yu
-
Publication number: 20100137291Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: ApplicationFiled: December 11, 2009Publication date: June 3, 2010Inventors: Richard A. EARL, Maiko EZAWA, Xinqin FANG, David S. GARVEY, Ricky D. GASTON, Subhash P. KHANAPURE, L. Gordon LETTS, Chia-En LIN, Ramani R. RANATUNGA, Stewart K. RICHARDSON, Joseph D. SCHROEDER, Cheri A. STEVENSON, Shiow-Jyi WEY
-
Publication number: 20100130582Abstract: The present invention relates to new indolinone modulators of dopamine receptor, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 24, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Patent number: 7714146Abstract: The invention is related to novel azulene-oxindole compounds having formula (I) shown below, wherein one of R1, R2 and R3 represents a moiety of formula (II), each of A1 and A2 independently is nitrogen, oxygen or sulfur, each of the others of R1, R2, R3, R1, R5, R6, R7, R8, R9, R10, R11, R12, R13, and R14 is as recited in the specification. The novel compound potentially inhibits multiple kinases and thus can be used to treat some disease like cancer or inflammatory.Type: GrantFiled: October 31, 2007Date of Patent: May 11, 2010Assignee: Industrial Technology Research InstituteInventors: On Lee, Chrong-Shiong Hwang, Chih-Hung Chen, Yuan-Jang Tsai, Chih-Peng Liu, Ching-Huai Ko, Hsin-Hsin Shen, Ling-Mei Wang, Kuei-Tai Lai, Ying-Chu Shih, Ting-Shou Chen, Yen-Chun Chen, Lain-Tze Lee
-
Publication number: 20100098634Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.Type: ApplicationFiled: July 24, 2009Publication date: April 22, 2010Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
-
Publication number: 20100069384Abstract: The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V2 receptors of vasopressin (“V2 receptors”) and can therefore constitute active principles of pharmaceutical compositions.Type: ApplicationFiled: June 12, 2009Publication date: March 18, 2010Applicant: SANOFI-AVENTISInventors: Loic FOULON, Pierrick ROCHARD, Claudine SERRADEIL-LE GAL, Gerard VALETTE
-
Publication number: 20100069375Abstract: The present invention relates to indolone-acetamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as for the treatment of epilepsy, epileptogenesis, seizure disorders and convulsion.Type: ApplicationFiled: November 20, 2009Publication date: March 18, 2010Applicant: UCB PHARMA, S.A.Inventors: Jean-Philippe Starck, Benoit Kenda
-
Publication number: 20100041635Abstract: The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.Type: ApplicationFiled: June 30, 2009Publication date: February 18, 2010Inventors: Mustapha HADDACH, Johnny Yasuo NAGASAWA
-
Patent number: 7645887Abstract: The present invention relates to indolone-acetamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as for the treatment of epilepsy, epileptogenesis, seizure disorders and convulsion.Type: GrantFiled: March 16, 2004Date of Patent: January 12, 2010Assignee: UCB Pharma, S.A.Inventors: Jean-Philippe Starck, Benoît Kenda
-
Publication number: 20090281137Abstract: The present invention is related to new 3,3-disubstituted indol-2-one derivatives of the general Formula (I) The new compounds are useful for the treatment or prophylaxis of the central nervous system, the gastrointestinal system or the cardiovascular system.Type: ApplicationFiled: July 9, 2009Publication date: November 12, 2009Inventors: Balázs Volk, József Barkóczy, Gyula Simig, Tibor Mezei, Rita Kapillerné Dezsófi, István Gacsályi, Katalin Pallagi, Gábor Gigler, Gyôrgy Lévay, Krisztina Móricz, Csilla Leveleki, Nóra Sziray, Gábor Szénási, András Egyed, László Gábor Hársing
-
Publication number: 20090275578Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: August 12, 2005Publication date: November 5, 2009Applicants: AstraZeneca AB, NPS PHARMACEUTICALS, INCInventors: Joshua Clayton, Fupeng Ma, Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Ian Egle, James Empfield, Methvin Isaac, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
-
Publication number: 20090275758Abstract: A process for the production of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable prodrug ester thereof, comprising cleaving a lactam of formula II wherein the symbols are as defined, with a base; and precursors therefor and processes for the preparation of the precursors. The compounds of Formula I are pharmaceutically active compounds which are selective inhibitors of Cyclooxygenase II.Type: ApplicationFiled: May 7, 2009Publication date: November 5, 2009Inventors: Murat Acemoglu, Thomas Allmendinger, John Vincent Calienni, Jacques Cercus, Olivier Loiseleur, Gottfried Sedelmeier, David Xu
-
Patent number: 7612065Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: March 28, 2007Date of Patent: November 3, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Susanne Wilke, Francesco Salituro, Edmund Harrington, Jingrong Cao, Guy Bemis, Huai Gao
-
Patent number: 7608711Abstract: A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.Type: GrantFiled: November 13, 2006Date of Patent: October 27, 2009Assignee: Dipharma Francis SrlInventors: Jacopo Zanon, Oscar Martini, Francesco Ciardella, Luca Gregori, Federico Sbrogio, Andrea Castellin
-
Patent number: 7595338Abstract: Methods for preparing oxindole and thio-oxindole compounds are provided, which compounds are useful as precursors to useful pharmaceutical compounds. Specifically provided are methods for preparing 5-pyrrole-3,3-oxindole compounds and 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile. Also provided are methods for preparing iminobenzo[b]thiophene and benzo[b]thiophenone compounds.Type: GrantFiled: April 27, 2006Date of Patent: September 29, 2009Assignee: WyethInventor: Bogdan Kazimierz Wilk
-
Patent number: 7560480Abstract: The present invention relates to alkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).Type: GrantFiled: March 10, 2005Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Gerald Juergen Roth, Joerg Kley, Stefan Hoerer, Ingo Uphues
-
Publication number: 20090162432Abstract: The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido)benzoic acid,1H,3H-spiro[5-chloro-1-methylquinoline-2,4-dione-3,3?-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4-tetrahydro-quinoline-3-carboxamide.Type: ApplicationFiled: December 19, 2008Publication date: June 25, 2009Inventors: Muhammad Safadi, Daniella Licht, Ioana Lovinger, Aharon M. Eyal, Tomas Fristedt, Karl Jansson
-
Publication number: 20090131599Abstract: Disclosed herein is a method for producing a 2-hydrocarbyl-3,3-bis(4-hydroxyaryl)phthalimidine. The method comprises forming a reaction mixture comprising at least one substituted or unsubstituted phenolphthalein compound, at least one substituted or unsubstituted primary hydrocarbyl amine, and an acid catalyst; and heating the reaction mixture to form 2-hydrocarbyl-3,3-bis(4-hydroxyaryl)phthalimidine. An adduct of the 2-hydrocarbyl-3,3-bis(4-hydroxyaryl) phthalimidine is formed either by using an excess of the primary hydrocarbyl amine in the first heating step, or by isolating crude 2-hydrocarbyl-3,3-bis(4-hydroxyaryl)phthalimidine after the heating step and then reacting with a further amount of the primary hydrocarbyl amine. The 2-hydrocarbyl-3,3-bis(4-hydroxyaryl)phthalimidine has a formula: where R1 is selected from the group consisting of a hydrogen and a hydrocarbyl group, and R2 is selected from the group consisting of a hydrogen, a hydrocarbyl group, and a halogen.Type: ApplicationFiled: November 21, 2008Publication date: May 21, 2009Inventors: Vinod Kumar RAI, Radhakrishna Srinivasarao ARAKALI
-
Publication number: 20090131506Abstract: The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition.Type: ApplicationFiled: May 11, 2006Publication date: May 21, 2009Inventors: Lars Thore Burgdorf, David Bruge, Hartmut Greiner, Maria Kordowicz, Christian Sirrenberg, Frank Zenke
-
Publication number: 20090111988Abstract: The present invention provides a novel, industrially easily realisable and economically preferable process for production of pure 5-{2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one i.e., ziprasidone hydrochloride shown in the reaction scheme (II), (III), (IV), (V) and (VI). According to the invention the intermediate compound 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) is produced from 5-(2-bromoacethyl)-6-chloro-1,3-dihydro-2H-indole-2-one of Formula (IV). The highly pure ziprasidone base of Formula (II) is obtained in the reaction of 3-piperazinyl-1,2-benzisothiazol of Formula (VI) with 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) in an organic solvent or organic solvent mixture.Type: ApplicationFiled: May 2, 2007Publication date: April 30, 2009Inventors: Jozsef Neu, Jozsef Torley, Sandor Garadnay
-
Publication number: 20090111830Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: February 15, 2006Publication date: April 30, 2009Applicant: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
-
Publication number: 20090105216Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: April 23, 2007Publication date: April 23, 2009Inventors: Matthias Treu, Andreas Mantoulidis, Ulrike Tontsch-Grunt
-
Patent number: 7514457Abstract: Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.Type: GrantFiled: May 31, 2006Date of Patent: April 7, 2009Assignee: Pfizer Inc.Inventors: Tadashi Inoue, Satoshi Nagayama, Yuji Shishido
-
Patent number: 7507836Abstract: The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: March 22, 2004Date of Patent: March 24, 2009Assignee: Merck & Co. Inc.Inventors: Mark E. Duggan, Craig W. Lindsley, David D. Wisnoski
-
Patent number: RE41151Abstract: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.Type: GrantFiled: August 20, 2008Date of Patent: February 23, 2010Assignee: Medinox, Inc.Inventors: Ching-San Lai, Tingmin Wang