Plural 1,3-diazine Rings Patents (Class 544/296)
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Publication number: 20080293940Abstract: The present invention is directed to an amide derivative having excellent BCR-ABL tyrosine kinase inhibitory activity, or a salt thereof. The present invention provides an amide derivative represented by the following general formula (1): [Chemical 23] (wherein R1 represents —CH2—R11, etc.; R2 represents alkyl, halogen, haloalkyl, etc.; R3 represents hydrogen, etc.; Het1 represents a group of the formula [6] as above, etc.; and Het2 represents pyrimidinyl, etc.), or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.Type: ApplicationFiled: December 27, 2004Publication date: November 27, 2008Inventors: Tetsuo Asaki, Yukiteru Sugiyama, Jun Segawa
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Publication number: 20080287475Abstract: This invention relates to novel compounds having the formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: ApplicationFiled: October 26, 2006Publication date: November 20, 2008Applicant: ASTRAZENECA ABInventors: Xiaomei Feng, Huiping Guan, Ying Kan, Stephanos Ioannidis, Bo Peng, Mei Su, Bin Wang, Tao Wang, Hai-Jun Zhang
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Patent number: 7452896Abstract: The invention relates to novel sulfamic acid amides of General Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: November 10, 2003Date of Patent: November 18, 2008Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller
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Publication number: 20080269266Abstract: There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: March 26, 2008Publication date: October 30, 2008Applicant: ASTRAZENECA ABInventors: Thorsten Nowak, Andrew Peter Thomas, Stuart Charles Purkiss
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Patent number: 7442699Abstract: Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.Type: GrantFiled: August 24, 2005Date of Patent: October 28, 2008Assignee: Signal Pharmaceuticals, LLCInventors: Adam Kois, Karen J. MacFarlane, Yoshitaka Satoh, Shripad S. Bhagwat, Jason S. Parnes, Moorthy S. S. Palanki, Paul E. Erdman
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Publication number: 20080242687Abstract: Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 1, 2008Publication date: October 2, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20080234223Abstract: The present invention relates to N4 carboxylester or ester derivatives of pyrimidine analogs with increased stability, solubility, and bioavailability. Also disclosed are methods of using these compounds for targeted drug delivery and combination therapy.Type: ApplicationFiled: October 30, 2007Publication date: September 25, 2008Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Allen S. Yang, Victor Marquez, Hyang-Min Byun, Jean-Pierre Issa
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Publication number: 20080227782Abstract: This invention is directed to a compound of formula (I): wherein R1, R2, R3 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: April 4, 2008Publication date: September 18, 2008Applicant: AVENTIS PHARMACEUTICALS INCInventors: Suzanne C. Aldous, John Ziqi Jiang, Jinqi Lu, Liang Ma, Lan Mu, Harry Randall Munson, Jeffrey Stephen Sabol, Sukanthini Thurairatnam, Christopher Loren Vandeusen
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Publication number: 20080220286Abstract: The present invention relates to a dinaphthyl ethylene derivative of formula (I), a process for preparing it, a film prepared from it useful in the manufacure of an organic light emitting device (OLED), an OLED including the film, and the use of the dinaphthyl ethylene derivative in the manufacture of an OLED. Wherein R1 to R16 are defined as in the specification.Type: ApplicationFiled: January 30, 2008Publication date: September 11, 2008Applicants: Tsinghua University, Beijing Visionox Technology Co., LTDInventors: Yong Qiu, Han Chen, Yinkui Li
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Publication number: 20080214544Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as c-met mediated diseases and/or HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: December 19, 2007Publication date: September 4, 2008Applicant: Amgen Inc.Inventors: Steven Bellon, Shon Booker, Noel D'Angelo, Ingrid M. Fellows, Jean-Christophe Harmange, Tae-Seong Kim, Matthew Lee, Longbin Liu, Mark H. Norman
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Publication number: 20080194545Abstract: The present invention is directed to compounds of formula I, pharmaceutical compositions comprising the compounds, and methods for making and using the inventive compounds.Type: ApplicationFiled: February 7, 2008Publication date: August 14, 2008Applicant: TRIUS THERAPEUTICSInventors: Xiaoming Li, John M. Finn, Mark T. Hilgers
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Publication number: 20080160244Abstract: The invention provides dyes for optical disc recoding media, having the general formula: wherein m, n is independently selected from integers 0-3; X represents oxygen, sulfur, C—R1, or N—R2R3; Y is oxygen or sulfur; each of R1, R2, and R3 can be the same or different; and Z? is a cation. The dyes have a maximum absorption in wavelength of 300-500 nm and can be used in recording layers of high density optical disc recording media.Type: ApplicationFiled: December 27, 2006Publication date: July 3, 2008Inventors: Shin-Shin Wang, Wen-Ping Chu, Chien-Liang Huang, Wen-Yih Liao, Hui-Ping Tsai, Jong-Lieh Yang, An-Tse Lee
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Publication number: 20080146571Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: ApplicationFiled: December 12, 2007Publication date: June 19, 2008Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu
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Publication number: 20080139534Abstract: Disclosed are bisbenzamidine and bisbenzamidoxime compounds useful for treatment of treatment of trypanosomiasis. The compounds disclosed are useful for treating mammals infected with parasitic hemoflagellates, in particular Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense.Type: ApplicationFiled: December 7, 2007Publication date: June 12, 2008Applicant: XAVIER UNIVERSITY OF LOUISIANAInventors: Tien L. HUANG, Jean Jacques VANDEN EYNDE, Annie MAYENCE, Cyrus BACCHI, Isaac O. DONKOR, Nageswara R. KODE
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Publication number: 20080125440Abstract: The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2007Publication date: May 29, 2008Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Patent number: 7371858Abstract: Compounds of the formulae wherein, provided that at least one of R1, R2, and R3 is not a hydrogen atom, R1, R2, and R3 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R1 and R2 can also be alkoxy aryloxy, arylalkyloxy, alkylaryloxy, polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silyl, siloxane, polysilylene, polysiloxane, or a group of the formula wherein r and s are integers representing a number of repeat —CH2— groups, and wherein X is a direct bond, oxygen, sulfur, —NR40— wherein R40 is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, or —CR50R60— wherein R50 and R60 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and R10 and R11 each, independently of the other, is alkylene, arylene, arylalkylene, or alkylarylene, and wherein R10 can also be polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silylene, siloxane, polysilylene, or polysiloxane.Type: GrantFiled: March 5, 2004Date of Patent: May 13, 2008Assignee: Xerox CorporationInventors: Danielle C Boils-Boissier, Marcel P Breton, Jule W Thomas, Jr., Donald R Titterington, Jeffrey H Banning, H Bruce Goodbrand, James D Wuest, Marie-Eve Perron, Hugues Duval
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Publication number: 20080070093Abstract: Featured are novel heterocycle substituted hydroquinones, aromatic copolymers and homopolymers bearing main and side chain polar pyridine units. These polymers exhibit good mechanical properties, high thermal and oxidative stability, high doping ability and high conductivity values. These novel polymers can be used in the preparation and application of MEA on PEMFC type single cells. The combination of the above mentioned properties indicate the potential of the newly prepared materials to be used as electrolytes in high temperature PEM fuel cells.Type: ApplicationFiled: May 23, 2007Publication date: March 20, 2008Applicant: Advent TechnologiesInventors: Maria Geormezi, Nora Gourdoupi
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Patent number: 7329749Abstract: Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).Type: GrantFiled: December 24, 2001Date of Patent: February 12, 2008Assignee: Merck Patent GesellschaftInventors: Henning Boettcher, Gerd Bartoszyk, Juergen Harting, Christoph van Amsterdam, Christoph Seyfried
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Patent number: 7326793Abstract: The present invention relates to a process for the preparation of diketopyrrolopyrroles of the formula (I), wherein A1, A2, A3 and A4 are as defined in the description of the present invention, to new diketopyrrolopyrroles of the general formula I obtainable by the process, and the use of the new diketopyrrolopyrroles of the general formula I for the preparation of inks, colorants, pigmented plastics for coatings, non-impact-printing material, color filters, cosmetics, polymeric ink particles, toners, dye lasers and electroluminescent devices, or as fluorescent markers for immunoassays and fluorescent tracers for leak detection of fluids.Type: GrantFiled: September 3, 2002Date of Patent: February 5, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Colin Morton, David Macdonald Smith, Vincent Ruffieux
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Publication number: 20080025904Abstract: A compound of formula I and a corresponding method for the extraction of high-order fullerenes from a carbonaceous mixture including at least one solid-liquid extraction.Type: ApplicationFiled: July 24, 2007Publication date: January 31, 2008Applicant: INSTITUT CATALA D'INVESTIGACIO QUIMICAInventors: Javier de Mendoza, Elisa Huerta Martinez, Gerald Metselaar
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Patent number: 7323465Abstract: The invention relates to novel alkansulfonamides of structure (I), wherein R1 is a lowel alzyl group and the other variables are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions.Type: GrantFiled: December 10, 2002Date of Patent: January 29, 2008Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller
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Patent number: 7285549Abstract: The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: April 7, 2006Date of Patent: October 23, 2007Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Walter Fischli, Martine Clozel, Thomas Weller
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Patent number: 7285560Abstract: The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of I?B kinase comprising administering such compounds.Type: GrantFiled: August 18, 2003Date of Patent: October 23, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Olaf Ritzeler, Gerhard Jaehne
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Patent number: 7285663Abstract: The invention relates to a compound of general formula (I) in which C represents an alicyclic or heterocyclic group having C2v symmetry, and B represents ortho-C6-C18-arylene. The invention also relates to a method for producing this compound and to the use thereof as a coloring agent for coloring or pigmenting organic or inorganic high-molecular or low-molecular, particularly high-molecular, organic materials.Type: GrantFiled: December 13, 2003Date of Patent: October 23, 2007Assignee: Clariant Produkte (Deutschland) GmbHInventors: Heino Heckmann, Hans Joachim Metz
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Patent number: 7259162Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl; G is an unsubstituted or substituted pyrimidinyl group.Type: GrantFiled: December 20, 2000Date of Patent: August 21, 2007Assignee: Applied Research Systems Ars Holding N.V.Inventors: Serge Halazy, Dennis Church, Montserrat Camps, Pascale Gaillard, Jean-Pierre Gotteland
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Patent number: 7232904Abstract: Novel crystals of a potassium salt of (E)-N-[6-methoxy-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]-2-phenylethenesulfonamide, a preparation process thereof, and novel solvates of (E)-N-[6-methoxy-5-(2-ethoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]-2-phenylethenesulfonamide.Type: GrantFiled: July 25, 2002Date of Patent: June 19, 2007Assignee: Astellas Pharma Inc.Inventors: Yoshinori Kato, Hironori Harada, Masahiro Kurotani, Haruhiko Toda, Kenichirou Sakamoto
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Patent number: 7226919Abstract: The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3, JAK-3, FLT-3, PIM-1, SYK, or PDK-1 mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: December 17, 2003Date of Patent: June 5, 2007Assignee: Vertex Pharmaceuticals Inc.Inventors: Mark Ledeboer, Robert Davies, David Messersmith, Young-Choon Moon, Michael Mullican
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Patent number: 7220736Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ?CH— or ?N—, Y is —NH—, —NR4—, —S—, —O—, —CH?N—, —N?CH—, —N?N—, —CH?CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring.Type: GrantFiled: March 15, 2001Date of Patent: May 22, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 7196089Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: January 29, 2004Date of Patent: March 27, 2007Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Patent number: 7173130Abstract: Methods and compositions are provided for detecting changes in membrane potential in membranes biological systems. In one aspect, the method comprises; a) providing a living cell with a first reagent comprising a charged hydrophobic molecule which is typically a fluorescence resonance energy transfer (FRET) acceptor or donor, or is a quencher and is capable of redistributing within the membrane of a biological membrane in response to changes in the potential across the membrane; b) providing the cell with a second reagent that can label the first face or the second face of a biological membrane within the cell; c) detecting light emission from the first reagent or the second reagent. One aspect of this method involves monitoring membrane potential changes in subcellular organelle membranes in a living cells. Another aspect of the invention is the use of certain embodiments of the method for the screening of test chemicals for activity to modulate the activity of a target ion channel.Type: GrantFiled: September 28, 2001Date of Patent: February 6, 2007Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Jesus E. Gonzalez, III
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Patent number: 7163951Abstract: N-Biarylmethylaminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: August 25, 2003Date of Patent: January 16, 2007Assignee: Merck & Co., Inc.Inventors: Scott D. Kuduk, Michael R. Wood, Mark G. Bock
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Patent number: 7122551Abstract: Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: GrantFiled: February 26, 2004Date of Patent: October 17, 2006Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Robert Ian Dowell, Maurice Raymond Verschoyle Finlay, Nicholas John Newcombe, Howard Tucker, David Waterson
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Patent number: 7122544Abstract: Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.Type: GrantFiled: December 4, 2001Date of Patent: October 17, 2006Assignee: Signal Pharmaceuticals, LLCInventors: Adam Kois, Karen J. MacFarlane, Yoshitaka Satoh, Shripad S. Bhagwat, Jason S. Parnes, Moorthy S. S. Palanki, Paul E. Erdman
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Patent number: 7115616Abstract: Pyrimidinone compounds of formula (10 are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.Type: GrantFiled: February 11, 2004Date of Patent: October 3, 2006Assignee: SmithKline Beecham PlcInventors: Ashley Edward Fenwick, Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith
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Patent number: 7112674Abstract: The invention relates to an organic electroluminescent device which contains 2,5-diaminoterephthalic acid derivatives of formula 1a as emitter substances in one or several emitter layers in a pure or doped manner. The ring A is a triple unsaturated benzene ring wherein R4? and R8? are zero or ring A is a double unsaturated ring respectively provided with a double bond in the 1,2 position and 4,5 position, and wherein R10 is a nitrile radical —CN or a radical C(?X1)—X2R1, R11 is a nitrile radical —CN or a radical —C(?X3)—X4R5, X1 and X3 are oxygen, sulfur or imino, X2 and X4 are oxygen, sulfur or optionally substituted amino, R1–R8, R4? and R8? are H, C1–20-alkyl, aryl, heteroaryl, R4 and R8 can be halogen, nitro, cyanogen or amino, R2–R4, R6–R8, R4? and R8? can be trifluoromethyl or pentafluorophenyl, and wherein certain radicals can form a saturated or unsaturated ring.Type: GrantFiled: August 21, 2002Date of Patent: September 26, 2006Assignee: Sensient Imaging Technologies GmbHInventors: Andreas Richter, Jens Schoenewerk, Gerhard Diener
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Patent number: 7112585Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: March 12, 2004Date of Patent: September 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Richard A. Hartz, Argyrios G. Arvanitis
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Patent number: 7101873Abstract: Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the treatment of inflammation and immunological diseasesType: GrantFiled: April 9, 2003Date of Patent: September 5, 2006Assignee: Bexel Pharmaceuticals Inc.Inventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
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Patent number: 7094781Abstract: The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: December 4, 2001Date of Patent: August 22, 2006Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Walter Fischli, Martine Clozel, Thomas Weller
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Patent number: 7091202Abstract: The invention encompasses compounds of Formula I, which are blockers of KCNQ channels. Blockers of KCNQ channels are known to enchance cognition in laboratory animals.Type: GrantFiled: September 8, 2005Date of Patent: August 15, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Kevin W. Gillman, Dharmpal S. Dodd, John E. Starrett, Jr., Danielle Bocchino
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Patent number: 7091201Abstract: The invention relates to novel aryl-alkane-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: August 28, 2001Date of Patent: August 15, 2006Assignee: Actelion Pharmaceuticals Ltd.Inventors: Thomas Weller, Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli
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Patent number: 7045519Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: September 6, 2001Date of Patent: May 16, 2006Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Kirk Johnson, Keith B. Pfister, Savithri Ramurthy, Lynn Seely, Allan S. Wagman, Manoj C. Desai, Barry H. Levine
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Patent number: 6995148Abstract: The present invention relates to novel compounds that are novel adenosine receptor analogues. Specifically, the compounds of the present invention preferably function as both adenosine receptor agonists and ganglionic blocking agents. To achieve this functionality, the compounds of the present invention, preferably contain a ganglionic blocking motif, is inserted into the adenosine molecule. The ganglionic blocking motif preferably includes an elongated carbon chain that, in a particularly preferred embodiment, contains two terminal amino groups. The ganglionic blocking motif preferably includes a carbon along the elongated carbon chain that is integral to a cyclic ketal that is part of the adenosine molecule. In presently-preferred embodiments, the elongated carbon chain ranges from two to sixteen carbons in length. The compounds of the present invention will be useful for treatment of a variety of conditions including, but not limited to, hypertension, vasodilation, and ischemia.Type: GrantFiled: April 5, 2001Date of Patent: February 7, 2006Assignee: University of PittsburghInventors: Garth S. Jones, Edwin K. Jackson
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Patent number: 6992044Abstract: The invention relates to novel substituted phenyl uracils of the formula (I) in which R1 represents hydrogen, amino or in each case optionally substituted alkyl, alkenyl or alkynyl, R2 represents cyano, carboxy, carbamoyl, thiocarbamoyl or optionally substituted alkyl or alkoxycarbonyl, R3 represents hydrogen, halogen or optionally substituted alkyl, R4 represents hydrogen, nitro, cyano, alkoxy or halogen, R5 represents cyano, thiocarbamoyl, halogen or optionally substituted alkyl or alkoxy and R6 represents an optionally substituted nitrogen-containing heterocyclic group which is attached to R6 via N, to processes for their preparation, to their use as crop treatment agents, and to intermediates and processes for their preparation.Type: GrantFiled: October 8, 2001Date of Patent: January 31, 2006Assignee: Bayer CropScience AGInventors: Roland Andree, Hans-Georg Schwarz, Udo Schneider, Ralf Wischnat, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Patent number: 6953803Abstract: Pyrmidinone compounds of formula (I) are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.Type: GrantFiled: April 25, 2000Date of Patent: October 11, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Deirdre Mary Bernadette Hickey, Colin Andrew Leach, Stephen Allan Smith
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Patent number: 6951856Abstract: The invention relates to novel aryl-ethene-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: July 10, 2001Date of Patent: October 4, 2005Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christoph Boss, Martin Bolli, Martine Clozel, Walter Fischli, Thomas Weller
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Patent number: 6949567Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.Type: GrantFiled: February 26, 2002Date of Patent: September 27, 2005Assignee: 4SC AGInventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
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Patent number: 6949544Abstract: The present invention provide a compound of formula I or II: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; and Src-family kinases, especially Src and Lck kinases. These compounds are also inhibitors of GSK3 and CDK2 kinases. 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, 2002Date of Patent: September 27, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Randy S. Bethiel, John Cochran, Young-Choon Moon, Suganthini Nanthakumar
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Patent number: 6936607Abstract: This invention is directed to pyrimidine derivatives which are selective 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. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.Type: GrantFiled: August 7, 2003Date of Patent: August 30, 2005Assignee: H. Lunobeck A/SInventor: Mathivanan Packiarajan
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Patent number: 6919332Abstract: The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 28, 2003Date of Patent: July 19, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Lilli Ann Wolf-Gouveia
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Patent number: 6916804Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl mType: GrantFiled: December 20, 2002Date of Patent: July 12, 2005Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington