Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
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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: 7087627Abstract: Compositions for the inhibition of the formation of new vasculature by angiogenesis are provided comprising the combination of a vasculature damaging agent and an inhibitor of the formation or action of nitric oxide in mammalian systems. There are also provided the use of said combinations in medicaments and kits of said compounds and treatment employing said materials.Type: GrantFiled: February 15, 2000Date of Patent: August 8, 2006Assignee: Angiogene Pharmaceuticals Ltd.Inventor: Peter David Davis
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Patent number: 7084169Abstract: The invention provides compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein R1, R2, R3, R4, m and n are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: GrantFiled: December 1, 2003Date of Patent: August 1, 2006Assignee: Roche Palo Alto LLCInventor: Shu-Hai Zhao
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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: 7084167Abstract: The invention concerns compounds of general formula (I) wherein: the group X represents a —NR4, —CH?N or —CHR5-NR4-group; the group Y represents an oxygen or sulphur atom or a NR, —CR5, —CHR5-, —CR5=CR6- or —CHR5-CHR6 group provided that when group X represents the —CH?N— or —CHR5-NR4-group, group Y represents an oxygen or a sulphur atom or a Nr, —CR5 or —CHR group; the group R represents a hydrogen atom or an alkyl, aryl or aralkyl group; the groups R1, R5 and R6, identical or different, represent each a hydrogen or halogen atom or an alkyl or alkoxy group; the group R2 represents a hydrogen atom or an alkyl group; the group R3 represents an aryl group; and the group R4 represents a hydrogen atom, an alkyl, aryl, aralkyl, alkylsulphonamide, arylsulphonamide or aralkylsulphonamide group; and their salt with a pharmaceutically acceptable acid, in the form of a racemic mixture and their optically pure isomer.Type: GrantFiled: May 23, 2001Date of Patent: August 1, 2006Assignee: Centre National de la Rechereche Scientifique (CNRS)Inventors: Martial Ruat, Robert Dodd, Hélène Véronique Faure, Philippe Marcel Dauban, Albane Kessler, Pierre Jean-Paul Potier
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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: 7074814Abstract: The present invention provides indoles of Formula I: wherein R1 and R2 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: GrantFiled: June 3, 2004Date of Patent: July 11, 2006Assignee: Warner-Lambert Company LLCInventors: Kimberly Suzanne Para, Charles John Stankovic, Melean Visnick
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Patent number: 7071217Abstract: 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: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio, Edgar Raymond Wood, III
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Patent number: 7026358Abstract: The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents.Type: GrantFiled: April 15, 2002Date of Patent: April 11, 2006Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Patent number: 7015242Abstract: This invention provides methods for the treatment or inhibition of hyperactive gastrointestinal motility in a mammal utilizing compounds having the formula: where R, and R1 to R6 are described herein.Type: GrantFiled: August 6, 2003Date of Patent: March 21, 2006Assignee: WyethInventor: Thomas M. Argentieri
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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: 6989401Abstract: The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.Type: GrantFiled: July 19, 2001Date of Patent: January 24, 2006Assignee: Mitsubishi Pharma CorporationInventors: Kazuhiro Maeda, Shuji Sonda, Tadahiro Takemoto, Tomokazu Goto, Fujio Kobayashi, Masahiko Kajii, Naruyasu Komorita, Fumihiro Hirayama
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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: 6969729Abstract: The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents.Type: GrantFiled: October 16, 2002Date of Patent: November 29, 2005Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Tino Dyhring Jørgensen, Philip K. Ahring, Palle Christophersen, Dorte Strøbaek, Lene Teuber, Søren Peter Olesen
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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: 6946454Abstract: This invention relates to methods of co-administering compounds of formula 1 which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, with estrogen, an estrogen, or an estrogen receptor agonist for contraception, hormone replacement therapy, or treating progesterone-related carcinomas and adenocarcinomas.Type: GrantFiled: April 5, 2002Date of Patent: September 20, 2005Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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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: 6921756Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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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: 6884791Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6878733Abstract: The present invention features formulations of indolinones which compounds are ionizable as free acids or free bases. The formulation is suitable for parenteral or oral administration, wherein the formulation comprises an ionizable substituted indolinone, and a pharmaceutically acceptable carrier therefor. The term “ionizable substituted indolinone” includes pyrrole substituted 2-indolinones which, in addition to being otherwise optionally substituted on both the pyrrole and 2-indolinone portions of the compound, are necessarily substituted on the pyrrole moiety with one or more hydrocarbon chains which themselves are substituted with at least one polar group. The formulations and the compounds themselves are useful for the treatment of protein kinase related disorders as discussed herein.Type: GrantFiled: November 21, 2000Date of Patent: April 12, 2005Assignee: Sugen, Inc.Inventors: Narmada Shenoy, Waranush Sorasuchart, Arun Koparkar
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Patent number: 6872744Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: September 26, 2002Date of Patent: March 29, 2005Assignee: Syntex (U.S.A.) LLCInventors: Chris Allen Broka, Jeffrey Allen Campbell
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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: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6861442Abstract: The present invention relates generally to the fields of immunology and medicine, and more specifically to the field of cellular signal transduction. The present invention relates, inter alia, to methods for diagnosis, treatment, and identification of therapeutics for particular inflammation-related diseases or disorders characterized by an interaction between a PYK2 polypeptide and a natural binding partner.Type: GrantFiled: December 30, 1999Date of Patent: March 1, 2005Assignees: Sugen, Inc., New York UniversityInventors: Joseph Schlessinger, Mitsuhiko Okigaki, Mikhail Gishizky
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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: 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: 6855729Abstract: The present invention provides a method for treating fibromyalgia and/or chronic fatigue syndrome by administering an antagonist or partial agonist of 5HT1a receptors.Type: GrantFiled: February 20, 2002Date of Patent: February 15, 2005Inventors: Timothy G. Dinan, Paul W. N. Keeling
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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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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: 6849654Abstract: Compositions comprising 5-methoxy-carbonylamino-N-acetyltryptamine compounds and derivatives thereof for the treatment of depression are disclosed.Type: GrantFiled: March 18, 2003Date of Patent: February 1, 2005Assignee: Caritas St. Elizabeth's Medical Center of Boston, Inc.Inventors: Gregory F. Oxenkrug, Nikolai S. Zefirov, Sergey O. Bachurin
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Patent number: 6846839Abstract: The present invention relates to methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis. More specifically, this invention relates to methods for treating diseases and disorders, such as rheumatoid arthritis, endometriosis, ocular neovascularization, solid tumor growth and metastases, and excessive scarring during wound healing, with indolinone compounds.Type: GrantFiled: June 16, 1999Date of Patent: January 25, 2005Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Laura Kay Shawver, Klaus Peter Hirth, Annie Fong
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Patent number: 6844423Abstract: The production of a purified extracellular bacterial signal called autoinducer-2 is regulated by changes in environmental conditions associated with a shift from a free-living existence to a colonizing or pathogenic existence in a host organism. Autoinducer-2 stimulates LuxQ luminescence genes, and is believed also to stimulate a variety of pathogenesis related genes in the bacterial species that produce it. A new class of bacterial genes is involved in the biosynthesis of autoinducer-2.Type: GrantFiled: September 21, 2001Date of Patent: January 18, 2005Assignees: Princeton University, University Technologies Transfer InternationalInventors: Bonnie L. Bassler, Michael G. Surette
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Publication number: 20040259158Abstract: The present invention relates generally to the fields of immunology and medicine, and more specifically to the field of cellular signal transduction. The present invention relates, inter alia, to methods for diagnosis, treatment, and identification of therapeutics for particular inflammation-related diseases or disorders characterized by an interaction between a PYK2 polypeptide and a natural binding partner.Type: ApplicationFiled: February 27, 2004Publication date: December 23, 2004Applicants: Sugen, Inc., New York UniversityInventors: Joseph Schlessinger, Mitsuhiko Okigaki, Mikhail Gishizky
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Publication number: 20040259877Abstract: A medicament having inhibitory activity against NF-&kgr;B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: 1Type: ApplicationFiled: February 19, 2004Publication date: December 23, 2004Inventors: Susumu Muto, Tatsuo Nagano, Tomomi Sotome, Akiko Itai
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Publication number: 20040248965Abstract: The present invention relates to protein kinase inhibitors and to the use thereof for the treatment of diseases induced by pathological signal transduction cascades.Type: ApplicationFiled: July 6, 2004Publication date: December 9, 2004Inventors: Vladimir Chirchin, Giannis Athanassios, Ralph Mazitschek, Jonathan Sleemann
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Patent number: 6828106Abstract: The present invention relates to a polypeptide multimer comprising a first polypeptide having associated therewith a label and a second polypeptide, wherein a) at least one of the polypeptides is susceptible to protease digestion; b) association of the polypeptides to form a multimer is detectable via a signal emitted by the label; and c) digestion of at least one polypeptide results in dissociation of the multimer and modulation of the signal emitted by the label, and The method of detecting or monitoring the activity of a protease enzyme based on such a multimer.Type: GrantFiled: January 26, 2000Date of Patent: December 7, 2004Assignee: Cyclacel LimitedInventors: John Colyer, Joanne Lightowler
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Publication number: 20040242669Abstract: The present invention is directed to a method for treating the motor, behavioral, and cognitive deficits resulting from brain injury comprising administering a safe and effective amount of a dopamine agonist to a patient in need thereof.Type: ApplicationFiled: May 27, 2004Publication date: December 2, 2004Inventor: Filippo Drago
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Publication number: 20040242601Abstract: The present invention relates to a method for treating interstitial cystitis, comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, potent and selective c-kit inhibitor, wherein said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.Type: ApplicationFiled: March 22, 2004Publication date: December 2, 2004Inventors: Alain Moussy, Jean-Pierre Kinet
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Publication number: 20040225003Abstract: The invention relates to substituted indoles, method for production thereof, medicaments containing said compounds and use of said compounds for the production of medicaments.Type: ApplicationFiled: April 26, 2004Publication date: November 11, 2004Inventors: Michael Sattlegger, Helmut Buschmann, Michael Przewosny, Werner Englberger, Babette-Yvonne Koegel, Hans Schick
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Patent number: 6815439Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase II inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.Type: GrantFiled: September 23, 2003Date of Patent: November 9, 2004Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
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Patent number: 6815440Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.Type: GrantFiled: March 3, 2003Date of Patent: November 9, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Publication number: 20040198802Abstract: 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: ApplicationFiled: April 20, 2004Publication date: October 7, 2004Applicant: Allergan, Inc.Inventors: Steven W. Andrews, Michael E. Garst, Xialing Guo, Jonathan J. Hebert, Thomas Malone, Julie A. Wurster, Clarence Eugene Hull
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Patent number: 6800649Abstract: The invention provides a method for inhibiting c-jun activation in mammalian or avian cells comprising contacting the cells with a substance that inhibits the activity of Janus family kinase 3 (JAK-3). The invention also provides a therapeutic method for preventing or treating a pathological condition in a mammal wherein c-jun activation is implicated and inhibition of its activation is desired comprising administering to a mammal in need of such therapy, an effective amount of a substance that inhibits the activity of JAK-3. Novel compounds that are JAK-3 inhibitors, as well as pharmaceutical compositions comprising the compounds are also provided.Type: GrantFiled: June 30, 1999Date of Patent: October 5, 2004Assignee: Parker Hughes InstituteInventor: Fatih M. Uckun
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Publication number: 20040192753Abstract: A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas: 1Type: ApplicationFiled: November 10, 2003Publication date: September 30, 2004Inventors: Samuel Chackalamannil, Yan Xia, Enrico P. Veltri, Mariappan V. Chelliah, Wenxue Wu, Michael P. Graziano, Teddy Kosoglou, Madhu Chintala
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Patent number: 6794407Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shift-work sleep disturbance are provided.Type: GrantFiled: July 23, 2002Date of Patent: September 21, 2004Assignee: Oregon Health and Sciences UniversityInventors: Alfred J. Lewy, Robert L. Sack
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Patent number: 6794395Abstract: The present invention relates to substituted indolinones of general formula wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, in particular the physiologically acceptable salts thereof which have valuable pharmacological properties, especially an inhibitory effect on various receptor-tyrosine kinases, and cycline/CDK complexes as well as on the proliferation of endothelial cells and various tumor cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: July 22, 2002Date of Patent: September 21, 2004Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Gerald Juergen Roth, Armin Heckel, Rainer Walter, Ulrike Tontsch-Grunt, Walter Spevak, Jacobus C. A. Van Meel
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Patent number: RE38761Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, which is a substituted styrene compound which can also be a naphthalene, an indane or a benzoxazine; including nitrile and molononitrile compounds, and pharmaceutical compositions comprising, in admixture with a pharmaceutically acceptable carrier, a pharmaceutically-effective amount of such compound.Type: GrantFiled: October 14, 1994Date of Patent: July 19, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Alexander Levitzki, Chaim Gilon, Michael Chorev, Aviv Gazit