Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
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Patent number: 7728131Abstract: 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: GrantFiled: December 27, 2004Date of Patent: June 1, 2010Assignee: Nippon Shinyaku Co., Ltd.Inventors: Tetsuo Asaki, Yukiteru Sugiyama, Jun Segawa
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Patent number: 7713970Abstract: Certain novel phenyl substituted cyclic urea derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B a, D, b, E, G, c, d, J, X and R through R10, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: May 18, 2005Date of Patent: May 11, 2010Assignee: FMC CorporationInventors: Edward J. Barron, Larry Y. Zhang, John W. Lyga, Matthew P. Whiteside
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Patent number: 7713971Abstract: The invention relates to 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I in which the variables are defined herein, as well as additive salts with pharmaceutically acceptable bases and the various enantiomers of compounds having asymmetrical carbons, as well as their mixtures in all proportions, including racemic mixtures in particular.Type: GrantFiled: March 2, 2006Date of Patent: May 11, 2010Assignee: Pierre Fabre MedicamentInventors: Elisabeth Dupont-Passelaigue, Isabelle Leroy, Jean-François Patoiseau, Didier Junquero, Yves Rival, André Delhon
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Publication number: 20100093737Abstract: The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3? position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.Type: ApplicationFiled: January 17, 2008Publication date: April 15, 2010Applicant: INSTITUT DE RECHERCHES CLINIQUES DE MONTREALInventor: Yvan Guindon
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Publication number: 20100087638Abstract: A novel process for the preparation of lamotrigine and its intermediates is devised.Type: ApplicationFiled: August 9, 2007Publication date: April 8, 2010Inventors: Jean-Paul Roduit, Francis Djojo
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Patent number: 7687500Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: GrantFiled: January 24, 2008Date of Patent: March 30, 2010Assignee: The University of ConnecticutInventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Patent number: 7683097Abstract: The present invention provides compounds that are effective against inhibiting topoisomerase (i.e., topoisomerase I and/or topoisomerase II). These compounds are used for treating cell-proliferative disorders. In some instances, these compounds have anticancer activity, e.g., against multi-drug resistant cancers.Type: GrantFiled: May 25, 2005Date of Patent: March 23, 2010Assignee: Propharmacon Inc.Inventors: Martin A. Murphy, John Robert Schullek, John S. Ward, Gary C. Look, Brian Siesel
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Patent number: 7671053Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: June 26, 2008Date of Patent: March 2, 2010Assignee: Pfizer, Inc.Inventors: Mark A. Dombrowski, Allen J. Duplantier
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Publication number: 20100048574Abstract: The present invention relates to compounds of the general formula (II): or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof.Type: ApplicationFiled: October 9, 2009Publication date: February 25, 2010Applicant: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20100048568Abstract: This invention is directed to a compound of formula (I): wherein R1, R2, R3, R4 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: September 30, 2009Publication date: February 25, 2010Applicant: SANOFI-AVENTISInventors: Suzanne C. Aldous, Michael W. Fennie, John Z. Jiang, Stanly John, Lan Mu, Brian Pedgrift, James R. Pribish, Barbara Rauckman, Jeffrey S. Sabol, Grzegorz T. Stoklosa, Sukanthini Thurairatnam, Christopher L. Vandeusen
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Publication number: 20100041660Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 23, 2009Publication date: February 18, 2010Inventors: MORIHIRO MITSUYA, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20100016545Abstract: The present invention relates to a process for linking two molecules by means of a Diels Alder reaction with inverse electron requirement (DARinv), comprising the following steps: reaction of a (a) triazine or tetrazine with one or more electron-attracting substituents on the ring as a diene component, the electron-attracting substituents being selected from: COOR C(O)NR2 CX3 (X=halogen) halogen CN SO2—R or SO3—R PR2 wherein R?H, alkyl, aryl, heterocycle, which in turn may be substituted, where appropriate, with alkyl, OH, SH, halogen, aryl, heterocycle, nitro, carboxyamido or amine group.Type: ApplicationFiled: June 18, 2007Publication date: January 21, 2010Applicant: DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OFFENTLICHEN RECHTSInventors: Manfred Wiessler, Eduard Müller, Peter Lorenz, Christian Kliem, Heinz Fleischhacker
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Publication number: 20100009990Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: July 14, 2009Publication date: January 14, 2010Inventor: Chandrasekar Venkataramani
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Publication number: 20100004245Abstract: Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: October 18, 2007Publication date: January 7, 2010Applicant: MERCK FROSST CANADA LTD.Inventors: Renata M. Oballa, Denis Deschenes, Marc Gagnon, Yves Leblanc, David Powell, Yeeman K. Ramtohul
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Publication number: 20100004246Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.Type: ApplicationFiled: November 9, 2007Publication date: January 7, 2010Applicant: ADDEX PHARMA SAInventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
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Publication number: 20090318429Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-14 or encompassed by formulas I-XII) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: April 27, 2009Publication date: December 24, 2009Inventors: Kevin James Doyle, Graham Peter Jones, Michael Geoffrey Neil Russell, Sebastian Bruckner, Jacqueline Anne Macritchie, Joanne Peach
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Publication number: 20090318454Abstract: Formula 1 is an antioxidant compound, wherein R, R1, or D is an antioxidant substituent; R and D are each independently selected from hydrogen or groups containing cysteine, thiols, disulfides, amino acids, amines, amides, or carboxylic acids; when one of R or D is hydrogen, the other includes a thiol, disulfide, or carboxylic acid; A is CO, SO, SO2, or C?S; E is one or more ring groups which are aromatic, carbocyclic, and/or heterocyclic 5, 6 and 7 membered rings being mono, bi, tri, tetra, penta, hexa, hepta or octa cyclic fused rings that are substituted or unsubstituted, each heterocyclic ring can include hetero atoms chosen from to O, S, N, Se, or P; each R1 is at a para, meta, and/or ortho position; n is 1, 2, 3, 4, or 5 for each ring; and each R1 is hydrogen or an antioxidant substituent.Type: ApplicationFiled: March 24, 2009Publication date: December 24, 2009Inventors: Carl P. Weiner, Peter Swaan, Jeffrey Aube, Abhijit Ray
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Publication number: 20090312544Abstract: A method for preparing 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine, commonly known as lamotrigine, is disclosed. A method of preparing the intermediate, 2,3-dichlorobenzoyl chloride, by photochlorination of 2,3-dichlorobenzotrichloride followed by hydrolysis is also disclosed. The intermediate may then be used in the preparation of lamotrigine.Type: ApplicationFiled: May 30, 2007Publication date: December 17, 2009Applicant: Calaire Chimie SASInventors: Dirk Van Deynse, Marc Belmans, Frank Boers, Michel Dumur, Alain Laconi
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Patent number: 7625897Abstract: The present invention provides compounds of formula I where R1 to R4 are as defined herein which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides for methods of treating or preventing HIV infection with compounds according to formula I and compositions containing the same. The invention still further provides process for the preparation of compounds of formula I wherein R4 is A1 and X1 is NH or O.Type: GrantFiled: September 29, 2006Date of Patent: December 1, 2009Assignee: Roche Palo Alto LLCInventors: Yoshihito David Saito, Mark Smith, Zachary Kevin Sweeney
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Publication number: 20090291954Abstract: Compounds of formula (I) especially where R1 is an optionally substituted alkyl, aralkyl or heterocyclyl-alkyl group, are shown to have activity as sodium channel blockers or as antifolates. Some novel compounds where R1 is an aralkyl or hetero-cyclyl-alkyl are disclosed.Type: ApplicationFiled: July 13, 2007Publication date: November 26, 2009Applicant: University of GreenwichInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Paul Barraclough
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Publication number: 20090291956Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.Type: ApplicationFiled: May 20, 2009Publication date: November 26, 2009Inventors: Lingkai Weng, Lei Qiao, Jiacheng Zhou, Pingli Liu, Yongchun Pan
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Publication number: 20090286976Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.Type: ApplicationFiled: August 15, 2008Publication date: November 19, 2009Inventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
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Patent number: 7608618Abstract: Compounds of the formula wherein: Y? is O or S, W? is optionally substituted, Z? is selected from the group consisting of wherein Q? is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.Type: GrantFiled: April 27, 2005Date of Patent: October 27, 2009Assignee: Icos CorporationInventors: Edward A. Kesicki, John Joseph Gaudino, Adam Wade Cook, Scott Douglas Cowen, Laurence Edward Burgess
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Publication number: 20090264433Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: April 20, 2009Publication date: October 22, 2009Inventors: Michael Geoffrey Neil Russell, Joanne Peach, Jacqueline Anne Macritchie, Sebastian Bruckner, Kevin James Doyle
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Publication number: 20090253906Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: April 2, 2009Publication date: October 8, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Patent number: 7585861Abstract: The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.Type: GrantFiled: February 5, 2004Date of Patent: September 8, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Jozef Herwig Arts, legal representative, Marc René de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Ruben Gerardus George Leenders, Georges Joseph Cornelius Hoomaert, Amuri Kilonda, Donald William Ludovici
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Publication number: 20090182140Abstract: An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is —NH—, —O—, —CH2—, etc., Y is —CH2—, —CO—, —SO2—, etc., Z is —CO—, —SO2—, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.Type: ApplicationFiled: November 30, 2006Publication date: July 16, 2009Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shigeru Furukubo, Hiroshi Miyazaki
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Patent number: 7560450Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
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Publication number: 20090176787Abstract: The invention is directed to novel crystalline forms of lamotrigine. These novel crystalline forms of lamotrigine have improved dissolution and in-vivo absorption profile, as compared to pure lamotrigine. These novel crystalline forms of lamotrigine provide a substantial increase in the blood concentration of lamotrigine, as compared to pure lamotrigine when administered to a subject. These novel crystalline forms of lamotrigine also provide a slower, steady build up of lamotrigine blood concentration suitable for sustained release of lamotrigine in-vivo, as compared to pure lamotrigine.Type: ApplicationFiled: November 10, 2008Publication date: July 9, 2009Applicant: Thar PharmaceuticalsInventors: Mazen Hanna, Ning Shan, Miranda L. Cheney
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Publication number: 20090163468Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: ApplicationFiled: December 2, 2008Publication date: June 25, 2009Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joesph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
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Publication number: 20090156592Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 27, 2007Publication date: June 18, 2009Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
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Patent number: 7528132Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease.Type: GrantFiled: January 24, 2006Date of Patent: May 5, 2009Assignee: Schering CorporationInventors: Tin-Yau Chan, Thierry O. Fischmann, Mark A. McCoy, Brian A. McKittrick, Andrew J. Prongay, Haiyan Pu, Li Wang, Li Xiao
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Publication number: 20090111815Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, two or more ring constitutional atoms of the heterocyclic group are a nitrogen atom, and the heterocyclic group may be substituted with at least one group selected from the group consisting of a C1-C3 alkyl group etc.], and a plant disease controlling agent comprising this as an active ingredient.Type: ApplicationFiled: July 12, 2006Publication date: April 30, 2009Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Sadayuki Arimori, Yoshiharu Kinoshita
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Publication number: 20090111692Abstract: The invention relates to 3-(pyridin-2-yl)-[1,2,4]-triazines of formula (I) and their use in the control of parasitic fungi and to herbicides that contain said compounds as an effective ingredient thereof.Type: ApplicationFiled: April 11, 2007Publication date: April 30, 2009Inventors: Wassilios Grammenos, Thomas Grote, Jochen Dietz, Jan Klaas Lohmann, Jens Renner, Bernd Muller, Sarah Ulmschneider
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Patent number: 7521553Abstract: The present invention relates to novel crystalline forms of lamotrigine, to processes for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: March 17, 2003Date of Patent: April 21, 2009Assignee: Hetero Drugs LimitedInventors: Reddy Bandi Parthasaradhi, Reddy Kura Rathnakar, Reddy Rapolu Raji, Reddy Dasari Muralidhara, Reddy Kesireddy Subash Chander
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Publication number: 20090099189Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.Type: ApplicationFiled: May 30, 2005Publication date: April 16, 2009Applicant: 7TM PHARMA A/SInventors: Trond Ulven, Thomas Frimurer, Oystein Rist, Evi Kostenis, Thomas Hogberg, Jean-Marie Receveur, Marie Grimstrup
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Patent number: 7517881Abstract: The invention relates to triazine derivatives of general formula (I): Wherein R1, R2 and R3 are as defined herein. The invention also relates to a method for preparing these triazine derivatives and to the therapeutic application thereof.Type: GrantFiled: October 9, 2007Date of Patent: April 14, 2009Assignee: Aventis Pharma S.A.Inventors: Yannick Benedetti, Andrees Bohme, Arielle Genevois-Borella, Gaetan Touyer, Jidong Zhang
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Publication number: 20090082310Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.Type: ApplicationFiled: September 2, 2008Publication date: March 26, 2009Inventors: NANCY-ELLEN HAYNES, Nathan R. Scott, Jefferson Wright Tilley
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Patent number: 7504501Abstract: Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidial agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).Type: GrantFiled: March 2, 2004Date of Patent: March 17, 2009Assignee: Merial LimitedInventors: Matthew J. Wyvratt, Tesfaye Biftu, Michael H. Fisher, Dennis M. Schmatz
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Publication number: 20090069303Abstract: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C?O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(?O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2.Type: ApplicationFiled: November 14, 2008Publication date: March 12, 2009Applicant: MAYBRIDGE LIMITEDInventors: Muhammad Hashim Javaid, Keith Allan Menear, Sylvie Gomez, Marc Geoffrey Hummersone, Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Xiao-Ling Fan Cockcroft, Frank Kerrigan
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Patent number: 7501415Abstract: Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such as cancer.Type: GrantFiled: December 20, 2005Date of Patent: March 10, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alexander Aronov, Michael Hale, Francois Maltais, Gabriel Martinez-Botella, Judith Straub, Qing Tang
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Patent number: 7498337Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.Type: GrantFiled: August 29, 2006Date of Patent: March 3, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
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Patent number: 7494997Abstract: The present invention provides an amide derivative represented by the following general formula (1): wherein R1 represents a saturated cyclic amino group, R2 represents alkyl, halogen or haloalkyl, R3 represents hydrogen or halogen, Het 2 represents pyridyl or pyrimidinyl, and Het 1 represents a group of the formula [6], or a 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: GrantFiled: June 27, 2003Date of Patent: February 24, 2009Assignee: Nippon Shinyaku Co., Ltd.Inventors: Tetsuo Asaki, Taisuke Hamamoto, Yukiteru Sugiyama
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Patent number: 7494996Abstract: This invention relates to dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad spectrum fungicides and insecticides. This invention also teaches methods of preparing these compounds as well as methods of using the compounds as fungicides and insecticides.Type: GrantFiled: October 26, 2001Date of Patent: February 24, 2009Assignee: Dow AgroSciences LLCInventors: Martha Jean Kelly, Karen Anderson Evans, James Joseph Gallagher, Mark Joseph Mulvihill
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Publication number: 20090048250Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: ApplicationFiled: August 20, 2007Publication date: February 19, 2009Inventors: Alex Aronov, David J. Lauffer, Huan Qiu Li, Ronald Charles Tomlinson, Pan Li
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Publication number: 20090048443Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: October 16, 2008Publication date: February 19, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Publication number: 20090042886Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: ApplicationFiled: June 26, 2008Publication date: February 12, 2009Applicant: Pfizer, Inc.Inventors: MARK A. DOMBROSKI, ALLEN J. DUPLANTIER
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Patent number: 7485639Abstract: Triazine derivatives of the formula (I) and physiologically acceptable salts and solvates thereof, in which R1, R2, A and R5 are as defined in Claim 1, exhibit phosphodiesterase IV inhibition and can be employed for the treatment of allergic diseases, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin diseases, inflammatory diseases, autoimmune diseases, such as, for example, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumour growth or tumour metastases, sepsis, memory disorders, atherosclerosis and AIDS, furthermore for inhibiting the formation of TNF?.Type: GrantFiled: June 19, 2002Date of Patent: February 3, 2009Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf, Norbert Beier, Joachim Leibrock, Pierre Schelling, Michael Gassen, Thomas Ehring
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Publication number: 20090030000Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: ApplicationFiled: May 1, 2008Publication date: January 29, 2009Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY. LTD.Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Patent number: 7482449Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.Type: GrantFiled: March 19, 2008Date of Patent: January 27, 2009Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa