Chalcogen Bonded Directly To Ring Carbon Of A 1,2-diazine Ring Patents (Class 544/239)
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Patent number: 11512056Abstract: A P2Y12 receptor antagonist containing a guanidyl, and a preparation method and the use thereof. In particular, the present disclosure provides a pyridazinone-guanidine compound that is a compound of structural formula (I), or a stereoisomer of the above-mentioned compound, a pro-drug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof. Such a compound has multiple pharmacological activities, especially has an inhibitory effect on platelet aggregation, and can be used for preparing an anti-platelet aggregation pharmaceutical composition.Type: GrantFiled: November 25, 2020Date of Patent: November 29, 2022Assignee: Anhui New Star Pharmaceutical Development Co., LtdInventors: Xiaoxiang Li, Ziao Xu, Degang Li, Yumei Xu, Yonghai Zhao, Genling Jiang
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Patent number: 10696658Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.Type: GrantFiled: August 13, 2019Date of Patent: June 30, 2020Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
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Patent number: 9902701Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, X and a are as described in the description and in the claims, as well as or pharmaceutically acceptable salts thereof. The invention also contains compositions including the compounds and methods of using the compounds.Type: GrantFiled: February 14, 2017Date of Patent: February 27, 2018Assignee: Hoffman-La Roche Inc.Inventors: Song Yang, Chungen Liang, Jianping Wang, Song Pan
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Patent number: 9861640Abstract: A medicament for therapeutic and/or preventive treatment of Alzheimer's disease, which comprises a combination of a retinoic acid receptor (RAR) agonist such as Am80 and a retinoid X receptor (RXR) agonist such as HX630.Type: GrantFiled: May 30, 2014Date of Patent: January 9, 2018Assignee: KEMPHYS LTD.Inventors: Kohichi Kawahara, Michita Suenobu, Koichi Shudo
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Patent number: 9000158Abstract: In an embodiment, the present invention provides a process for preparing (?)-6-(4-aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula II with a chiral tartaric acid derivative to obtain a diastereomeric salt of (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone and the chiral tartaric acid derivative; and b) reacting the diastereomeric salt with a base to obtain (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone. The (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone may be used to prepare levosimendan.Type: GrantFiled: July 12, 2010Date of Patent: April 7, 2015Assignee: Cipla LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Ashwini Amol Sawant
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Patent number: 8993569Abstract: The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.Type: GrantFiled: December 20, 2011Date of Patent: March 31, 2015Assignee: Pierre Fabre MedicamentInventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Samuel Mialhe, Christophe Pignier
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Patent number: 8987272Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N?O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.Type: GrantFiled: April 1, 2011Date of Patent: March 24, 2015Assignee: Critical Outcome Technologies Inc.Inventors: Wayne Danter, Clinton Threlfall, Sylvain Guizzetti, Julien Marin
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Patent number: 8975260Abstract: Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: August 31, 2011Date of Patent: March 10, 2015Assignees: Genetech, Inc, Gilead Connecticut, Inc.Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
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Patent number: 8969347Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: GrantFiled: October 15, 2012Date of Patent: March 3, 2015Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
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Publication number: 20140364606Abstract: Phosphodiesterase 4 inhibitors without vomiting of the present invention are compounds or prodrugs or solvates represented by formula (I) wherein R1 is an independent methoxy, bromine and substituted aryl; X is an optionally substituted six-membered heterocyclic ring; Y is —(CH2)n—, —NH(CH2)n—, and —NH(CH2)n—O—, wherein n is any value among 0, 1, 2 and 3; Z is an optionally substituted aromatic ring or an optionally substituted heteroaromatic ring. Phosphodiesterase 4 inhibitor without vomiting of the present invention are novel biphenyl series PDE4D inhibitors, and can be applied to treat depression and Alzheimer's disease, improve cognitive ability and avoid vomiting.Type: ApplicationFiled: August 25, 2012Publication date: December 11, 2014Applicant: Ningo Tiangsheg Patent AttorneysInventors: Jiangping Xu, Zhongzhen Zhou
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Patent number: 8889682Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: GrantFiled: August 16, 2012Date of Patent: November 18, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Christine E. Brotherton-Pleiss, Saul Jaime-Figueroa, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens
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Patent number: 8871765Abstract: Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly(ADP-ribose)polymerase-1 inhibitors (PARP-1 inhibitors).Type: GrantFiled: July 7, 2011Date of Patent: October 28, 2014Assignee: Cadila Healthcare LimitedInventor: Brijesh Kumar Shrivastava
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Publication number: 20140303174Abstract: Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods of use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.Type: ApplicationFiled: August 2, 2012Publication date: October 9, 2014Applicant: THE BRIGHAM AND WOMEN S HOSPITAL, INC.Inventors: Gregory D. Cuny, Marcie Glicksman, Xeuchao Xing, Chien-Liang Glenn Lin
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Patent number: 8853211Abstract: Compounds of the formula (I) in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: December 10, 2009Date of Patent: October 7, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8841310Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.Type: GrantFiled: October 7, 2009Date of Patent: September 23, 2014Assignee: Janssen R & D IrelandInventor: Paul Stoffels
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Publication number: 20140228219Abstract: The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH2, O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, a C1-6 alkyl group and the like; R4 represents a C6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C1-6 alkyl group and the like; is useful as an active ingredient for herbicides.Type: ApplicationFiled: May 29, 2012Publication date: August 14, 2014Inventors: Yosuke Nakashima, Yoshinobu Jin, Masato Konobe
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Publication number: 20140221376Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: April 9, 2014Publication date: August 7, 2014Applicant: Xcovery Holding Company, LLCInventors: Congxin Liang, Zhigang Li
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Publication number: 20140148468Abstract: The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.Type: ApplicationFiled: November 27, 2013Publication date: May 29, 2014Applicant: GRÜNENTHAL GMBHInventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
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Patent number: 8697866Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: GrantFiled: June 18, 2009Date of Patent: April 15, 2014Assignee: Xcovery Holding Company LLCInventors: Congxin Liang, Zhigang Li
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Patent number: 8686155Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
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Publication number: 20140073651Abstract: The invention relates to benzamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: February 21, 2012Publication date: March 13, 2014Applicant: Actelion Pharmaceuticals Ltd.Inventors: Kurt Hilpert, Francis Hubler, Mark Murphy, Dorte Renneberg
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Patent number: 8669254Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: GrantFiled: December 8, 2011Date of Patent: March 11, 2014Assignee: Hoffman-La Roche Inc.Inventors: Paul Hebeisen, Stephan Roever
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Patent number: 8658644Abstract: The present invention relates to novel pyridazine derivatives of formula (I) wherein R1 is methyl or ethyl; R2 is H or chloro; R3 is fluoro or chloro; R4 is fluoro or methoxy; and R5 is chloro or methoxy or an agrochemically usable salt from thereof, as active ingredients which have microbiodidal activity, in particular fungicidal activity.Type: GrantFiled: February 1, 2011Date of Patent: February 25, 2014Assignee: Syngenta Crop Protection, LLCInventors: Stephan Trah, Clemens Lamberth
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Publication number: 20130331382Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, J, and X3 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, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.Type: ApplicationFiled: March 12, 2013Publication date: December 12, 2013Inventors: Robert D. HUBBARD, Le WANG, Chang H. PARK, Chaohong SUN, Keith F. McDANIEL, John K. PRATT, Todd N. SOLTWEDEL, Michael D. WENDT, John H. HOLMS, Dachun LIU, George S. SHEPPARD
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Publication number: 20130267520Abstract: The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 20, 2011Publication date: October 10, 2013Applicant: PIERRE FABRE MEDICAMENTInventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Samuel Mialhe, Christophe Pignier
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Publication number: 20130261125Abstract: The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Inventors: Gerald W. Shipps, JR., Xiaohua Huang, Yongqi Deng, Liang Zhu, Alan B. Cooper, Binyuan Sun, Abdelghani Achab, Sie-Mun Lo
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Patent number: 8524896Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.Type: GrantFiled: March 2, 2009Date of Patent: September 3, 2013Assignee: Syngenta Crop Protection LLCInventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
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Publication number: 20130225596Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 9, 2011Publication date: August 29, 2013Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
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Patent number: 8501731Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: GrantFiled: March 18, 2009Date of Patent: August 6, 2013Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Patent number: 8481537Abstract: The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.Type: GrantFiled: July 27, 2007Date of Patent: July 9, 2013Assignee: LG Life Sciences Ltd.Inventors: Hye Kyung Chang, Yeong Soo Oh, Yong Jin Jang
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Publication number: 20130158021Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.Type: ApplicationFiled: October 26, 2012Publication date: June 20, 2013Applicant: Massachusetts Institute of TechnologyInventor: Massachusetts Institute of Technology
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Publication number: 20130158041Abstract: The present invention relates to pyridazinthione derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: August 26, 2011Publication date: June 20, 2013Inventors: Kevin Wilson, Matthew Daniels
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Publication number: 20130137691Abstract: The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a —CH— group; X1 represents a nitrogen atom or a —CH?CH— group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1-C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a —(C3-C10)cycloalkyl- group; Y represents a —(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1-C6)alkoxy group; Z1 is absent or represents an —NH— function; Z2 and Z3 are as defined in the description.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: SANOFIInventor: Sanofi
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Patent number: 8435981Abstract: Compounds of the formula (I) in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1 are inhibitors of tyrosine kinases, in particular of met kinase and can be employed inter alia for the treatment of tumors.Type: GrantFiled: July 12, 2007Date of Patent: May 7, 2013Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
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Patent number: 8431574Abstract: Disclosed are compounds of the Formulas III and IV and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: January 20, 2009Date of Patent: April 30, 2013Assignee: Array BioPharma Inc.Inventors: James F. Blake, Joseph P. Lyssikatos, Hong-Woon Yang, Eli M. Wallace
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Patent number: 8367668Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: May 2, 2008Date of Patent: February 5, 2013Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Patent number: 8357689Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: GrantFiled: July 25, 2008Date of Patent: January 22, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Publication number: 20130012485Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.Type: ApplicationFiled: December 20, 2007Publication date: January 10, 2013Inventors: Daniel Kaspar Bäschlin, Richard Sedrani, Stefanie Flohr, Kenji Namoto, Nils Ostermann, Finton Sirockin, François Gessier, Garry Fenton, Mandy Christine Beswick, David Edward Clark, Bohdan Waszkowycz
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Patent number: 8318742Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.Type: GrantFiled: September 20, 2011Date of Patent: November 27, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef DeCleyn, Michel Surkyn
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Publication number: 20120295876Abstract: The present invention relates to novel pyridazine derivatives of formula (I) wherein R1 is methyl or ethyl; R2 is H or chloro; R3 is fluoro or chloro; R4 is fluoro or methoxy; and R5 is chloro or methoxy or an agrochemically usable salt from thereof, as active ingredients which have microbiodidal activity, in particular fungicidal activity.Type: ApplicationFiled: February 1, 2011Publication date: November 22, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Stephan Trah, Clemens Lamberth
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Patent number: 8304413Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: GrantFiled: June 3, 2009Date of Patent: November 6, 2012Assignee: Intermune, Inc.Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
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Patent number: 8258140Abstract: The invention concerns bicyclic compounds of Formula I wherein , R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.Type: GrantFiled: February 9, 2010Date of Patent: September 4, 2012Assignee: Astrazeneca ABInventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
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Publication number: 20120213806Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: February 16, 2012Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Patent number: 8226929Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.Type: GrantFiled: January 15, 2008Date of Patent: July 24, 2012Assignee: Lantheus Medical Imaging, Inc.Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
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Publication number: 20120183522Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: March 26, 2012Publication date: July 19, 2012Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Patent number: 8217043Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.Type: GrantFiled: August 20, 2009Date of Patent: July 10, 2012Assignee: Fibrogen, Inc.Inventors: Shaojiang Deng, Wen-Bin Ho, Lee A. Flippin
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Publication number: 20120165524Abstract: In an embodiment, the present invention provides a process for preparing (?)-6-(4-aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula II with a chiral tartaric acid derivative to obtain a diastereomeric salt of (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone and the chiral tartaric acid derivative; and b) reacting the diastereomeric salt with a base to obtain (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone. The (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone may be used to prepare levosimendan.Type: ApplicationFiled: July 12, 2010Publication date: June 28, 2012Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Ashwini Amol Sawant
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Publication number: 20120157476Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: December 8, 2011Publication date: June 21, 2012Inventors: Paul Hebeisen, Stephan Roever
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Patent number: RE43748Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.Type: GrantFiled: August 26, 2010Date of Patent: October 16, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura