Chalcogen Bonded Directly To Ring Carbon Of A 1,2-diazine Ring Patents (Class 544/239)
  • Patent number: 10696658
    Abstract: 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: Grant
    Filed: August 13, 2019
    Date of Patent: June 30, 2020
    Assignee: 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
  • Patent number: 9902701
    Abstract: 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: Grant
    Filed: February 14, 2017
    Date of Patent: February 27, 2018
    Assignee: Hoffman-La Roche Inc.
    Inventors: Song Yang, Chungen Liang, Jianping Wang, Song Pan
  • Patent number: 9861640
    Abstract: 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: Grant
    Filed: May 30, 2014
    Date of Patent: January 9, 2018
    Assignee: KEMPHYS LTD.
    Inventors: Kohichi Kawahara, Michita Suenobu, Koichi Shudo
  • Patent number: 9000158
    Abstract: 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: Grant
    Filed: July 12, 2010
    Date of Patent: April 7, 2015
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Ashwini Amol Sawant
  • Patent number: 8993569
    Abstract: 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: Grant
    Filed: December 20, 2011
    Date of Patent: March 31, 2015
    Assignee: Pierre Fabre Medicament
    Inventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Samuel Mialhe, Christophe Pignier
  • Patent number: 8987272
    Abstract: 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: Grant
    Filed: April 1, 2011
    Date of Patent: March 24, 2015
    Assignee: Critical Outcome Technologies Inc.
    Inventors: Wayne Danter, Clinton Threlfall, Sylvain Guizzetti, Julien Marin
  • Patent number: 8975260
    Abstract: 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: Grant
    Filed: August 31, 2011
    Date of Patent: March 10, 2015
    Assignees: Genetech, Inc, Gilead Connecticut, Inc.
    Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
  • Patent number: 8969347
    Abstract: 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: Grant
    Filed: October 15, 2012
    Date of Patent: March 3, 2015
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Publication number: 20140364606
    Abstract: 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: Application
    Filed: August 25, 2012
    Publication date: December 11, 2014
    Applicant: Ningo Tiangsheg Patent Attorneys
    Inventors: Jiangping Xu, Zhongzhen Zhou
  • Patent number: 8889682
    Abstract: 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: Grant
    Filed: August 16, 2012
    Date of Patent: November 18, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christine E. Brotherton-Pleiss, Saul Jaime-Figueroa, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens
  • Patent number: 8871765
    Abstract: 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: Grant
    Filed: July 7, 2011
    Date of Patent: October 28, 2014
    Assignee: Cadila Healthcare Limited
    Inventor: Brijesh Kumar Shrivastava
  • Publication number: 20140303174
    Abstract: 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: Application
    Filed: August 2, 2012
    Publication date: October 9, 2014
    Applicant: THE BRIGHAM AND WOMEN S HOSPITAL, INC.
    Inventors: Gregory D. Cuny, Marcie Glicksman, Xeuchao Xing, Chien-Liang Glenn Lin
  • Patent number: 8853211
    Abstract: 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: Grant
    Filed: December 10, 2009
    Date of Patent: October 7, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Patent number: 8841310
    Abstract: 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: Grant
    Filed: October 7, 2009
    Date of Patent: September 23, 2014
    Assignee: Janssen R & D Ireland
    Inventor: Paul Stoffels
  • Publication number: 20140228219
    Abstract: 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: Application
    Filed: May 29, 2012
    Publication date: August 14, 2014
    Inventors: Yosuke Nakashima, Yoshinobu Jin, Masato Konobe
  • Publication number: 20140221376
    Abstract: 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: Application
    Filed: April 9, 2014
    Publication date: August 7, 2014
    Applicant: Xcovery Holding Company, LLC
    Inventors: Congxin Liang, Zhigang Li
  • Publication number: 20140148468
    Abstract: 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: Application
    Filed: November 27, 2013
    Publication date: May 29, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
  • Patent number: 8697866
    Abstract: 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: Grant
    Filed: June 18, 2009
    Date of Patent: April 15, 2014
    Assignee: Xcovery Holding Company LLC
    Inventors: Congxin Liang, Zhigang Li
  • Patent number: 8686155
    Abstract: 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: Grant
    Filed: June 28, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
  • Publication number: 20140073651
    Abstract: 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: Application
    Filed: February 21, 2012
    Publication date: March 13, 2014
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Kurt Hilpert, Francis Hubler, Mark Murphy, Dorte Renneberg
  • Patent number: 8669254
    Abstract: 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: Grant
    Filed: December 8, 2011
    Date of Patent: March 11, 2014
    Assignee: Hoffman-La Roche Inc.
    Inventors: Paul Hebeisen, Stephan Roever
  • Patent number: 8658644
    Abstract: 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: Grant
    Filed: February 1, 2011
    Date of Patent: February 25, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Stephan Trah, Clemens Lamberth
  • Publication number: 20130331382
    Abstract: 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: Application
    Filed: March 12, 2013
    Publication date: December 12, 2013
    Inventors: 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
  • Publication number: 20130267520
    Abstract: 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: Application
    Filed: December 20, 2011
    Publication date: October 10, 2013
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Samuel Mialhe, Christophe Pignier
  • Publication number: 20130261125
    Abstract: 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: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Inventors: Gerald W. Shipps, JR., Xiaohua Huang, Yongqi Deng, Liang Zhu, Alan B. Cooper, Binyuan Sun, Abdelghani Achab, Sie-Mun Lo
  • Patent number: 8524896
    Abstract: 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: Grant
    Filed: March 2, 2009
    Date of Patent: September 3, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
  • Publication number: 20130225596
    Abstract: 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: Application
    Filed: August 9, 2011
    Publication date: August 29, 2013
    Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
  • Patent number: 8501731
    Abstract: 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: Grant
    Filed: March 18, 2009
    Date of Patent: August 6, 2013
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
  • Publication number: 20130184222
    Abstract: 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: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Patent number: 8481537
    Abstract: 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: Grant
    Filed: July 27, 2007
    Date of Patent: July 9, 2013
    Assignee: LG Life Sciences Ltd.
    Inventors: Hye Kyung Chang, Yeong Soo Oh, Yong Jin Jang
  • Publication number: 20130158041
    Abstract: 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: Application
    Filed: August 26, 2011
    Publication date: June 20, 2013
    Inventors: Kevin Wilson, Matthew Daniels
  • Publication number: 20130158021
    Abstract: 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: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • Publication number: 20130137691
    Abstract: 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: Application
    Filed: January 23, 2013
    Publication date: May 30, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Patent number: 8435981
    Abstract: 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: Grant
    Filed: July 12, 2007
    Date of Patent: May 7, 2013
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
  • Patent number: 8431574
    Abstract: 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: Grant
    Filed: January 20, 2009
    Date of Patent: April 30, 2013
    Assignee: Array BioPharma Inc.
    Inventors: James F. Blake, Joseph P. Lyssikatos, Hong-Woon Yang, Eli M. Wallace
  • Patent number: 8367668
    Abstract: 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: Grant
    Filed: May 2, 2008
    Date of Patent: February 5, 2013
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Patent number: 8357689
    Abstract: 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: Grant
    Filed: July 25, 2008
    Date of Patent: January 22, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Publication number: 20130012485
    Abstract: 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: Application
    Filed: December 20, 2007
    Publication date: January 10, 2013
    Inventors: 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
  • Patent number: 8318742
    Abstract: 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: Grant
    Filed: September 20, 2011
    Date of Patent: November 27, 2012
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef DeCleyn, Michel Surkyn
  • Publication number: 20120295876
    Abstract: 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: Application
    Filed: February 1, 2011
    Publication date: November 22, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Stephan Trah, Clemens Lamberth
  • Patent number: 8304413
    Abstract: 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: Grant
    Filed: June 3, 2009
    Date of Patent: November 6, 2012
    Assignee: Intermune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Patent number: 8258140
    Abstract: 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: Grant
    Filed: February 9, 2010
    Date of Patent: September 4, 2012
    Assignee: Astrazeneca AB
    Inventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
  • Publication number: 20120213806
    Abstract: 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: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Patent number: 8226929
    Abstract: 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: Grant
    Filed: January 15, 2008
    Date of Patent: July 24, 2012
    Assignee: Lantheus Medical Imaging, Inc.
    Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
  • Publication number: 20120183522
    Abstract: 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: Application
    Filed: March 26, 2012
    Publication date: July 19, 2012
    Applicant: DECODE GENETICS EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Patent number: 8217043
    Abstract: 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: Grant
    Filed: August 20, 2009
    Date of Patent: July 10, 2012
    Assignee: Fibrogen, Inc.
    Inventors: Shaojiang Deng, Wen-Bin Ho, Lee A. Flippin
  • Publication number: 20120165524
    Abstract: 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: Application
    Filed: July 12, 2010
    Publication date: June 28, 2012
    Applicant: CIPLA LIMITED
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Ashwini Amol Sawant
  • Publication number: 20120157476
    Abstract: 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: Application
    Filed: December 8, 2011
    Publication date: June 21, 2012
    Inventors: Paul Hebeisen, Stephan Roever
  • Publication number: 20120129858
    Abstract: 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 1-3 or encompassed by formula I-III) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: April 19, 2010
    Publication date: May 24, 2012
    Inventors: Stephen David Penrose, Kevin James Doyle
  • Patent number: RE43748
    Abstract: 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: Grant
    Filed: August 26, 2010
    Date of Patent: October 16, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura