The Additional Hetero Ring Is A Five-membered Nitrogen Hetero Ring Patents (Class 514/252.05)
  • Patent number: 8653260
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • Publication number: 20140045795
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: October 15, 2013
    Publication date: February 13, 2014
    Applicant: SYNTA PHARMACEUTICALS CORPORATION
    Inventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
  • Publication number: 20140045690
    Abstract: The present invention relates to novel pyrazoles of formula I wherein the variables are as defined in the description, a method for controlling invertebrate pests, a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, and to an agricultural composition.
    Type: Application
    Filed: May 16, 2012
    Publication date: February 13, 2014
    Applicant: BASF SE
    Inventors: Christian Defieber, Sebastian Soergel, Daniel Saelinger, Ronan Le Vezouet, Karsten Koerber, Steffen Gross, Deborah L. Culbertson, Koshi Gunjima
  • Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Publication number: 20140031354
    Abstract: The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
    Type: Application
    Filed: July 30, 2012
    Publication date: January 30, 2014
    Applicant: Astar Biotech LLC
    Inventors: Chunrong YU, Haihong Huang, Dongfeng Zhang, Peng Li
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20140024648
    Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Application
    Filed: March 6, 2012
    Publication date: January 23, 2014
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Marjo Pihlavisto, David Smith, Auni Juhakoski, Ferenc Fulop, Laszlo Lazar, Istvan Szatmari, Ferenc Miklos, Zsolt Szakonyi, Lorand Kiss, Marta Palko
  • Patent number: 8629144
    Abstract: The invention relates to novel polymorphic and hydrate forms and salts of 6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline, to methods for their preparation, to pharmaceutical compositions comprising at least one of said polymorphic or hydrate forms or salts, and to the therapeutic and/or prophylactic use of such compositions. The invention also provides new manners for preparing said compound.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: January 14, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Carina Leys, Julius Walter Jozef Dickens, Sigrid Carl Maria Stokbroekx
  • Patent number: 8624025
    Abstract: 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: Grant
    Filed: July 3, 2012
    Date of Patent: January 7, 2014
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Publication number: 20130338112
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: August 1, 2013
    Publication date: December 19, 2013
    Inventors: Zachary Demko, Christopher Borella, Shoujun Chen, Lijun Sun
  • Publication number: 20130338111
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 19, 2013
    Applicants: Icagen, Inc., Pfizer Limited
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • 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
  • Patent number: 8604016
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: December 10, 2013
    Assignee: Calithera Biosciences Inc.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Patent number: 8604038
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Publication number: 20130324544
    Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Application
    Filed: November 25, 2011
    Publication date: December 5, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
  • Patent number: 8598177
    Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, R9, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 3, 2013
    Assignee: Sanofi
    Inventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen
  • Patent number: 8592426
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: November 26, 2013
    Assignee: Hoffmann—La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
  • Patent number: 8586588
    Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds and/or their pharmaceutically acceptable salts may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: November 19, 2013
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
  • Publication number: 20130281426
    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: Application
    Filed: June 18, 2013
    Publication date: October 24, 2013
    Inventors: Youhong HU, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
  • Patent number: 8557813
    Abstract: Compounds of the formula I in which R1, R2, R3, R4? 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 tumors.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: October 15, 2013
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Publication number: 20130267476
    Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pyrazole compound I of formula I wherein the variables are as defined in the description; and 2) at least one active compound II as defined in the description in synergistically effective amounts, further to methods and use of these mixtures for combating insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests, especially also for protecting plant propagation material as like seeds.
    Type: Application
    Filed: December 15, 2011
    Publication date: October 10, 2013
    Applicant: BASF SE
    Inventors: Christian Defieber, Sebastian Soergel, Daniel Saelinger, Juergen Langewald
  • Patent number: 8551992
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: October 8, 2013
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Publication number: 20130261128
    Abstract: This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Osamu Sakurai, Kunio Saruta, Norimitsu Hayashi, Takashi Goi, Kenji Morokuma, Hidekazu Tsujishima, Hiroaki Sawamoto, Hiroaki Shitama, Ritsuo Imashiro
  • Patent number: 8541414
    Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.
    Type: Grant
    Filed: March 13, 2007
    Date of Patent: September 24, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Toshiyuki Kiji, Takafumi Fusaka
  • Publication number: 20130244994
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: February 15, 2013
    Publication date: September 19, 2013
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
  • Publication number: 20130243754
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Application
    Filed: December 20, 2012
    Publication date: September 19, 2013
    Applicant: TARGEGEN, INC.
    Inventors: Wolfgang WRASIDLO, Elena DNEPROVSKAIA
  • Publication number: 20130237545
    Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: AGENEBIO, INC.
    Inventor: John A. Lowe, III
  • Publication number: 20130231344
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 4, 2013
    Publication date: September 5, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • 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
  • Publication number: 20130225582
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: April 4, 2013
    Publication date: August 29, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • Patent number: 8518943
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: August 27, 2013
    Assignee: UCB Pharma, S.A.
    Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
  • Patent number: 8513251
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: August 20, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo
  • 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: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • Publication number: 20130190298
    Abstract: The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against ALK and are useful in treating disorders related to abnormal protein kinase activities such as cancer, neurological and psychiatric diseases.
    Type: Application
    Filed: October 7, 2011
    Publication date: July 25, 2013
    Applicant: Xcovery Holding Company, LLC.
    Inventor: Congxin Liang
  • Publication number: 20130190312
    Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.
    Type: Application
    Filed: November 29, 2012
    Publication date: July 25, 2013
    Inventors: Jiann-Jyh HUANG, Shih-Hsien CHUANG, Ying-Shuan Eda LEE, Yu-Ling HUANG, Johnson LAU
  • Patent number: 8492111
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: July 23, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
  • Patent number: 8486946
    Abstract: The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: July 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk
  • Patent number: 8486979
    Abstract: The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: July 16, 2013
    Assignee: AbbVie Inc.
    Inventors: Jianguo Ji, Chih-Hung Lee, Kevin B. Sippy, Tao Li, Murali Gopalakrishnan
  • 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: 20130157998
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: November 19, 2012
    Publication date: June 20, 2013
    Applicant: CALITHERA BIOSCIENCES INC.
    Inventor: Calithera Biosciences Inc.
  • Publication number: 20130150344
    Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 13, 2013
    Inventors: Masato Yoshikawa, Shinkichi Suzuki, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo, Haruhi Kamisaki, Takahiko Taniguchi
  • Publication number: 20130150374
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Application
    Filed: December 17, 2012
    Publication date: June 13, 2013
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventor: Mitsubishi Tanabe Pharma Corporation
  • Publication number: 20130137675
    Abstract: The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W1—W2??(1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: May 30, 2013
    Inventors: Takahiko Taniguchi, Shinkichi Suzuki, Masato Yoshikawa, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo
  • Publication number: 20130131062
    Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.
    Type: Application
    Filed: December 21, 2007
    Publication date: May 23, 2013
    Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
  • Patent number: 8445494
    Abstract: The present disclosure generally relates to a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: May 21, 2013
    Assignees: Bristol-Myers Squibb Company, Albany Molecular Research, Inc.
    Inventors: Jun Qiu, Qi Gao, Shuang Liu, Matthew Isherwood
  • Publication number: 20130116231
    Abstract: The present invention relates to 1,4-dihydropyridazinone 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 related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: July 7, 2011
    Publication date: May 9, 2013
    Inventors: Kevin Wilson, Michael Altman, Kathryn Lipford, Catherine White, Matthew Daniels
  • Publication number: 20130116264
    Abstract: The present invention relates to hetaryl (thio)carboxamide compounds of formula I, to the tautomers and N-oxides thereof and to the salts thereof: wherein X, R1 and A are as defined in the description. The present invention further relates to a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one hetaryl (thio)carboxamide compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.
    Type: Application
    Filed: July 18, 2011
    Publication date: May 9, 2013
    Applicant: BASF SE
    Inventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Deborah L. Culbertson, Douglas D. Anspaugh