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)
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Publication number: 20090069313Abstract: The present invention provides a new medical use for the compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, as MAO-A inhibitors. Also included is a method for prophylaxis and treatment of mental disorders such as depression, in a mammal, comprising administering an effective amount of a compound of formula (I). These compounds are also effective in treating a disease, condition or disorder such as weight loss, obesity, bulimia, depression, bipolar disorders, psychoses, schizophrenia, behaviors, alcoholism, tobacco abuse, memory loss, Alzheimer's disease, dementia of aging, seizure disorders, epilepsy, attention deficit disorder, and Parkinson's disease, which is modulated by a cannabinoid receptor antagonist.Type: ApplicationFiled: September 6, 2007Publication date: March 12, 2009Applicant: ORCHID RESEARCH LABORATORIES LTD.Inventors: Debendranath Dey, Gajendra Singh, Partha Neogi, Uma Ramachandran, Chithra Santhanagopalan
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Publication number: 20090069565Abstract: The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.Type: ApplicationFiled: May 12, 2008Publication date: March 12, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Mark NAZARE, Melanie Essrich, David William WILL, Hans MATTER, Kurt RITTER, Volkmar WEHNER
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Publication number: 20090047354Abstract: The present invention relates to improved processes for the preparation of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one and its hydrochloride, which is known as Ziprasidone hydrochloride of Formula (I) and 5-(2-Chloro acetyl)-6-chloro oxindole of Formula (IV), which is an intermediate for the preparation of 5-(2-chloro ethyl)-6-chloro oxindole of Formula (V). Ziprasidone hydrochloride of Formula (I) of the present invention is depicted by the following structure.Type: ApplicationFiled: April 24, 2008Publication date: February 19, 2009Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.Inventors: Manne Satyanarayana Reddy, Sundaram Venkatraman, Srinivasan Thirumalai Rajan, Sharat Pandurang Narsapur, Manoj Ramesh Kharkar, Surya Narayana Devarkonda, Yarraguntla Sesha Reddy, Rangineni Srinivasulu, Deepak K. Shukla, Pushkar B. Lakhekar, Uppala Venkata Bhaskar Rao, Mummadi Venkatesh
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Publication number: 20090043111Abstract: A method for producing compounds of the formula: Wherein R2 is selected from the group consisting of amino, lower alkylamino, di-lower alkylamino, allylamino, diallylamino, N-lower alkyl-N-allylamino, benzylamino, dibenzylamino, phenethylamino, diphenethylamino, 4-hydroxyphenethylamino or di-(4-hydroxyphenethylamino); comprising: a) reacting with Wittig Reagent to produce wherein R1 is alkoxyl; f) hydrolyzing compound II under acidic conditions to produce g) subjecting compound III to reduction and amination to produce the tertiary amine wherein R2 is as defined above; h) reacting compound IV with 4-chlorophenoxyacetonitrile to create nucleophilic substitution to produce the nitrile compound wherein R2 is as defined above; and i) effecting reduction and hydrolysis in the same step with palladium/C and sodium hydroxide to produce wherein R2 is as defined above.Type: ApplicationFiled: August 6, 2007Publication date: February 12, 2009Inventor: Meizheng Liu
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Publication number: 20090012147Abstract: The present invention relates to indolone derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 14, 2005Publication date: January 8, 2009Applicant: UCB PHARMA, S.A.Inventors: Benoit Kenda, Jean-Philippe Starck
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Publication number: 20080319031Abstract: The present invention relates to novel tyrosine derivatives of formula (I), their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel tyrosine derivatives of the general formula (I).Type: ApplicationFiled: March 10, 2006Publication date: December 25, 2008Inventors: Surendrakumar Satyanarayan Pandey, Shiv Kumar Agarwal, Gajendra Singh, Santhanagopalan Chithra, Sangmesh Badiger, Bishwajit Nag, Debendranath Dey, Abhijeet Nag, Partha Neogi
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Publication number: 20080275041Abstract: Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.Type: ApplicationFiled: September 21, 2004Publication date: November 6, 2008Applicant: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg
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Publication number: 20080262244Abstract: A process for the preparation of 4-[2-(Di-n-propylamino)ethyl]-2,3-dihydro-1H-indol-2-one of formula (I) and its pharmaceutically acceptable salts, solvates Formula I involving new intermediates of compound of formula (A) and (B) wherein R represents (i) a halogen atom selected from fluorine, chlorine atom, bromine atom and iodine atom; (ii) lower alkanesulfonyloxy group selected from methanesulfonyloxy, ethanesulfonyloxy, isopropanesulfonyloxy, propanesulfonyloxy, butanesulfonyloxy, tert-butanesulfonyloxy, pentanesulfonyloxy, hexanesulfonyloxy; (iii) substituted or unsubstantiated arylsulfonyloxy group selected from phenylsulfonyloxy, 4-methylphenylsulfonyloxy, 2-methylphenylsulfonyloxy, 4-nitrophenylsulfonyloxy, 4-methoxyphenylsulfonyloxy, 3-chlorophenylsulfonyloxy; (iv) arylalkylsulfonyloxy group selected from benzylsulfonyloxy, 2-phenylethylsulfonyloxy, 4-phenylbutylsulfonyloxy, 4- methylbenzylsulfonyloxy, 2-methylbenzylsulfonyloxy, 4-nitrobenzylsulfonyloxy, 4-methoxybenzylsulfonyloxy, 3-chlorobenzylsulfoType: ApplicationFiled: February 15, 2006Publication date: October 23, 2008Applicant: Alembic LimitedInventors: Rohit Ravikant Soni, Hitarth Harshendu Acharya, Hetal Rameshchandra Shah, Trushar Rajnikant Shah, Buchi Reguri Reddy
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Patent number: 7439371Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 11, 2006Date of Patent: October 21, 2008Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Richard C. Yee
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Publication number: 20080249318Abstract: 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: August 16, 2007Publication date: October 9, 2008Inventors: Murat Acemoglu, Thomas Allmendinger, John Vincent Calienni, Jacques Cercus, Olivier Loiseleur, Gottfried Sedelmeier, David Xu
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Publication number: 20080227794Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: ApplicationFiled: February 15, 2006Publication date: September 18, 2008Inventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Patent number: 7414054Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: November 15, 2005Date of Patent: August 19, 2008Assignee: Allergan, Inc.Inventors: Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
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Publication number: 20080188532Abstract: The present invention relates to a compound represented by the formula (I), wherein all symbols are as defined in the description, a salt thereof, a solvate thereof, or a prodrug thereof, which has a leukotriene receptor antagonistic activity which is expected to be more effective than those of the leukotriene receptor antagonists currently used in clinical trials. Therefore, it is useful as an agent for the prevention and/or treatment of a leukotriene-mediated disease such as a respiratory diseases such as bronchial asthma, chronic obstructive pulmonary disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g. interstitial pneumonia etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), or the like, or as an expectorant or an antiitussive.Type: ApplicationFiled: February 24, 2006Publication date: August 7, 2008Inventors: Jun Takeuchi, Yoshisuke Nakayama, Manabu Fujita
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Publication number: 20080146645Abstract: Processes are disclosed for preparing indolinone phenylaminopropanol derivatives, particularly chiral indolinone phenylaminopropanol derivatives of the general formula: The processes disclosed may be used to prepare, inter alia, 7-fluoro-1-[(1S, 2R)-1-(3-fluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one and 7-fluoro-1-[(1S, 2R)-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one. Intermediates of the processes are also disclosed.Type: ApplicationFiled: August 22, 2007Publication date: June 19, 2008Applicant: WyethInventors: Anita Wai-Yin Chan, Zhixian Ding, Mousumi Ghosh, Mahmut Levent, Panolil Raveendranath, Jianxin Ren, Maotang Zhou, Asaf Alimardanov, Alexander V. Gontcharov, Antonia A. Nikitenko, John R. Potoski, Girija Raveendranath, Vijay Raveendranath, Sanjay Raveendranath
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Publication number: 20080125590Abstract: An azulene compound is provided. The azulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. One of R1, R2, R3, R4, R5, R6, R7, and R8 in formula (I) is a moiety of formula (II). The compound can be used to treat cancer.Type: ApplicationFiled: October 31, 2007Publication date: May 29, 2008Applicant: 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
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Patent number: 7378439Abstract: The present invention discloses a novel process and novel intermediates for the Preparation of 4-[2-(di-n-propyl amino) ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole (I) and pharmaceutical composition comprising the same. Further the present invention also discloses a method of treatment for cardiovascular disorders and Parkinson's disease.Type: GrantFiled: July 9, 2004Date of Patent: May 27, 2008Assignee: USV, Ltd.Inventors: Venkatasubramanian Radhakrishna Tarur, Dhananjay Govind Sathe, Harish Kashinath Mondkar, Rajesh Ganpat Bhopalkar, Samadhan Daulat Patil
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Patent number: 7374857Abstract: The present invention relates to a novel bisimide compound useful as an acid generator for a chemically amplified resist composition used in manufacturing of semiconductor element and the like or a raw material for synthesizing heat resistant polymers, an acid generator and a resist composition using said compound and a method for pattern formation using said composition, and further relates to a synthetic n intermediate for a bisimide compound and a bis(N-hydroxy)phthalimide compound useful as an intermediate for a functional compound such as a heat resistant polymer or photosensitive material, and provides a bisimide compound shown by the general formula [1]: (wherein R and A1 are as defined in claim 1).Type: GrantFiled: November 28, 2002Date of Patent: May 20, 2008Assignees: Wako Pure Chemical Industries Ltd., Matsushita Electric Industrial Co., Ltd.Inventors: Tsuneaki Maesawa, Fumiyoshi Urano, Masayuki Endo, Masaru Sasago
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Patent number: 7342040Abstract: A 5-fluorooxindole-3-carboxylic acid ester represented by a formula (2): wherein R1 is a group selected from the group consisting of an unsubstituted or substituted alkyl group having 1 to 10 carbon atoms, an unsubstituted or substituted cycloalkyl group having 3 to 7 carbon atoms, an aralkyl group having 7 to 10 carbon atoms or an aryl group having 6 to 14 carbon atoms.Type: GrantFiled: March 30, 2005Date of Patent: March 11, 2008Assignee: UBE Industries, Ltd.Inventors: Katsumasa Harada, Shigeyoshi Nishino, Kenji Hirotsu, Shuji Yokoyama, Takeshi Takahashi, Hiroyuki Oda
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Patent number: 7262206Abstract: The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, 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: August 28, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Gerald Jürgen Roth, Jörg Kley, Stefan Hoerer, Ingo Uphues
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Patent number: 7250442Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation, particularly congestive heart failure, comprising administering to a patient in need thereof an effective amount of a compound of the formula: I or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 11, 2003Date of Patent: July 31, 2007Assignee: Eli Lilly and CompanyInventors: Matthew Lee Brown, Timothy Alan Grese, Prabhakar Kondaji Jadhav, David Andrew Neel, Mitchell Irvin Steinberg, Peter Ambrose Lander
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Patent number: 7250440Abstract: This invention provides estrogen receptor modulators of formula I, having the structure where R1, R2, R3, and R4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 9, 2004Date of Patent: July 31, 2007Assignee: WyethInventors: Richard Eric Mewshaw, Stephen Marc Bowen, Eric Steven Manas
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Patent number: 7230118Abstract: A new process for the preparation of Ropinirole (1) and pharmaceutically acceptable hydrochloride salt thereof comprising reacting the compound (V) with nitromethane to obtain the compound of formula (II), which is reduced to compound (III) and alkylated to obtain compound (IV).Type: GrantFiled: October 13, 2004Date of Patent: June 12, 2007Assignee: Urquima S.A.Inventors: Joan Bosch Cartés, Xavier Pujol Ollé, José Luis Del Rio Pericacho, Yolanda Alonso Marin, Mercè Bessa Sanchez
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Patent number: 7217732Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, L1, L2, M, n, p, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.Type: GrantFiled: June 17, 2003Date of Patent: May 15, 2007Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Bandarpalle B. Shankar, Neng-Yang Shih, Ling Tong
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Patent number: 7199265Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.Type: GrantFiled: June 15, 2001Date of Patent: April 3, 2007Assignee: Karo Bio ABInventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
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Patent number: 7176231Abstract: The present invention relates to aryl-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: February 13, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Gerald Juergen Roth, Joerg Kley, Stefan Hoerer, Ingo Uphues
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Patent number: 7169803Abstract: The present invention provides novel N-substituted fluorooxindoles having the general Formula I wherein the wavy bond represents the racemate, the (R)-enantiomer or the (S)-enantiomer and m, n, p, q, A, B, D, Q, X, and Z are as defined below, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.Type: GrantFiled: March 7, 2005Date of Patent: January 30, 2007Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Omar D. Lopez, Piyasena Hewawasam, Min Ding
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Patent number: 7112603Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: February 10, 2004Date of Patent: September 26, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Marcel Koenig
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Patent number: 7098234Abstract: Indole derivatives represented by formula (I): (wherein all symbols are described in the description), a process for the preparation of the same and a DP receptor antagonist comprising it as an active ingredient. Since the compounds of formula (I) binds to and are antagonistic to a DP receptor, they are useful in for the prevention and/or treatment of diseases, for example, allergic diseases (allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma, food allergy, etc., systemic mastocytosis; disorders due to systemic mastocyte activation, anaphylactic shock, bronchoconstriction, urticaria, eczema, etc.), diseases accompanied with itching (atopic dermatitis, urticaria, etc.), secondary diseases caused by behaviors (scratching behaviors, beating, etc.) (cataract, retinal detachment, inflammation, infection, sleep disorder, etc.Type: GrantFiled: March 8, 2004Date of Patent: August 29, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuhiko Torisu, Kaoru Kobayashi, Fumio Nambu
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Patent number: 7098236Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 6, 2004Date of Patent: August 29, 2006Assignee: Allergan, Inc.Inventors: Steven W. Andrews, Julie A. Wurster, Clarence E. Hull, III
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Patent number: 7087611Abstract: The present invention relates to new and useful processes for the preparation of the anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride.Type: GrantFiled: August 30, 2004Date of Patent: August 8, 2006Assignee: Apotex Pharmachem Inc.Inventors: Carlos Zetina-Rocha, Allan W. Rey, Stephen E. Horne
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Patent number: 7084168Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: June 6, 2003Date of Patent: August 1, 2006Assignee: WyethInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H.W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 7081470Abstract: This invention is directed to indolone derivatives which are antagonists for 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: April 16, 2003Date of Patent: July 25, 2006Assignee: H. Lundbeck A/SInventors: Michael Konkel, John M. Werzel, Jamie Talisman
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Patent number: 7078429Abstract: Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.Type: GrantFiled: December 9, 2003Date of Patent: July 18, 2006Assignee: WyethInventor: Lee D. Jennings
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Patent number: 7057052Abstract: Pyrrolylquinones and indolylquinones useful for treating diseases such as neurodegenerative disease, viral infections and proliferative disease are described, along with methods of making such compounds and pharmaceutical formulations containing such compounds.Type: GrantFiled: September 26, 2002Date of Patent: June 6, 2006Assignee: Duke UniversityInventors: Michael C. Pirrung, Johannes Rudolph
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Patent number: 7015220Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: February 20, 2004Date of Patent: March 21, 2006Assignee: Allergan, Inc.Inventors: Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
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Patent number: 6982275Abstract: The present invention relates to a production method of an optically active form of a compound represented by formula (II) wherein ring A is a benzene ring optionally having substituent(s); R1 is H, a hydrocarbon group optionally having substituent(s), an acyl group or an acyloxy group; R2, R3 and R4 are each H, an alkyl group optionally having substituent(s), an alkoxy group optionally having substituent(s) or an amino group optionally having substituent(s); X is N or CH; Y is N or CH; and * shows an asymmetric center, or a salt thereof, which includes reacting a compound represented by the formula (I) wherein each symbol is as defined above, or a salt thereof, with an excess amount of an oxidizing agent in the presence of a catalyst for asymmetric induction, and provides an efficient production method of an optically active sulfoxide derivative in high yield on an industrial large scale by a convenient method, while achieving an extremely high enantiomer excess.Type: GrantFiled: April 26, 2001Date of Patent: January 3, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Hideo Hashimoto, Tadashi Urai
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Patent number: 6964977Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: November 15, 2005Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Robert N Hunter, Robert Walton McNutt, Jr., Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Robert Peel, Edgar Raymond Wood, III
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Patent number: 6930124Abstract: The invention relates to compounds of formula (I) in which R5 is chosen from the group consisting of: in which R2 is a C1-C3 alkyl group in which X may be Cl, Br, or F in which n is between 1 and 3, in the E or Z form, or a mixture of the two isomeric forms, possessing antimitotic, antiproliferative and antivascular properties through inhibition of the polymerization of tubulin into microtubulesType: GrantFiled: September 10, 2003Date of Patent: August 16, 2005Assignee: Aventis Pharma S. A.Inventors: Cécile Combeau, Patrick Mailliet, Marielle Chiron
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Patent number: 6924304Abstract: Compounds having formula (I) inhibit cellular proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.Type: GrantFiled: November 21, 2002Date of Patent: August 2, 2005Assignee: Abbott LaboratoriesInventors: Qun Li, Hing Sham, Keith W. Woods, Beth A. Steiner, Stephen L. Gwaltney, II, Kenneth J. Barr, Hovis M. Imade, Saul Rosenberg
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Patent number: 6906090Abstract: The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.Type: GrantFiled: March 4, 1999Date of Patent: June 14, 2005Assignee: AstraZeneca ABInventor: Ramachandran Janakiraman
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Patent number: 6900335Abstract: The present invention discloses a process for preparing 5-fluorooxindole represented by the formula (3): which comprises (A) a first step of cyclizing 2-(5-fluoro-2-nitrophenyl)malonic acid diester represented by the formula (1): wherein R1 and R2 may be the same or different from each other and each represents a group which does not participate in the reaction, under reductive conditions to form 5-fluorooxindole-3-carboxylic acid ester represented by the formula (2): wherein R1 has he same meaning as defined above, and (B) then, a second step of decarboxylating the 5-fluorooxindole-3-carboxylic acid ester, and a process for preparing its synthetic intermediates.Type: GrantFiled: July 19, 2001Date of Patent: May 31, 2005Assignee: Ube Industries, Ltd.Inventors: Katsumasa Harada, Shigeyoshi Nishino, Kenji Hirotsu, Shuji Yokoyama, Takeshi Takahashi, Hiroyuki Oda
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Patent number: 6884895Abstract: The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2?[1?H]-one derivatives of the general formula I wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of the general formula II wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group—with an acrylic acid C1-4ester, cyclizing the resulting compound of the general formula IV wherein R1, R2 and A are as defined above, R3 stands for C1-4 alkyl grouType: GrantFiled: April 8, 2003Date of Patent: April 26, 2005Assignee: sanofi-aventisInventors: Csaba Gönczi, Éva Csikós, István Hermecz, Gergely Héja, Árpád Illár, Lajos Nagy, Andrea Sántáné Csutor, Attila Simon, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
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Patent number: 6864277Abstract: The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the Vreceptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.Type: GrantFiled: June 19, 2001Date of Patent: March 8, 2005Assignee: Sanofi-SynthelaboInventors: Richard Roux, Claudine Serradeil-Le Gal, Jean Wagnon
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Patent number: 6861418Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.Type: GrantFiled: December 16, 2003Date of Patent: March 1, 2005Assignee: Sugen, Inc.Inventors: Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
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Patent number: 6858641Abstract: The present invention relates to indolinones substituted in the 6-position of general formula wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: April 4, 2002Date of Patent: February 22, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Gerald Juergen Roth, Armin Heckel, Thorsten Lehmann-Lintz, Joerg Kley, Frank Hilberg, Jacobus Van Meel
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Patent number: 6858623Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: May 29, 2003Date of Patent: February 22, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Eugene R. Hickey, Weimin Liu, Usha R. Patel, Denice M. Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young
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Patent number: 6855710Abstract: The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.Type: GrantFiled: September 19, 2003Date of Patent: February 15, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Rainer Walter, Wolfgang Grell, Armin Heckel, Frank Himmelsbach, Wolfgang Eberlein, Gerald Roth, Jacobus C.A. van Meel, Norbert Redemann, Walter Spevak, Ulrike Tontsch-Grunt, Thomas von Rueden
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Patent number: 6855829Abstract: Compounds which function as modulators, particularly, openers, of human KCNQ potassium channel proteins or polypeptides, particularly, central nervous system (CNS)-located KCNQ potassium channels, and heteromultimers thereof, and their use in the treatment of migraine are provided by the present invention. One novel type of potassium channel polypeptide openers provided by the present invention is the fluorooxindole compounds, described for the first time as therapeutics for the treatment of migraine by preventing the asynchronous firing of neurons. Other KCNQ potassium channel opener compounds that are also useful in the treatments of the invention include 2,4-disubstituted pyrimidine-5-carboxamide derivatives. One or more of the compounds according to the present invention may be utilized alone, in combination, or in conjunction with other treatment modalities for reducing, ameliorating and/or alleviating migraine or diseases similar to, or mechanistically related to, migraine, e.g., cluster headache.Type: GrantFiled: February 14, 2002Date of Patent: February 15, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Steven I. Dworetzky, Valentin K. Gribkoff, Gene G. Kinney, Piyasena Hewawasam
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Patent number: 6855730Abstract: The present invention relates to novel 3-methylidenyl-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: March 10, 2003Date of Patent: February 15, 2005Assignee: Sugen, Inc.Inventors: Pen Cho Tang, Li Sun, Todd Anthony Miller, Congxin Liang, Ngoc My Tran, Anh Thi Nguyen, Asaad Nematalla
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Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors
Patent number: 6825352Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: August 30, 2002Date of Patent: November 30, 2004Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan