JP2008540636A - 代謝型グルタミン酸受容体の陽性アロステリック調節因子としての新規複素環式化合物 - Google Patents

代謝型グルタミン酸受容体の陽性アロステリック調節因子としての新規複素環式化合物 Download PDF

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JP2008540636A
JP2008540636A JP2008511822A JP2008511822A JP2008540636A JP 2008540636 A JP2008540636 A JP 2008540636A JP 2008511822 A JP2008511822 A JP 2008511822A JP 2008511822 A JP2008511822 A JP 2008511822A JP 2008540636 A JP2008540636 A JP 2008540636A
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alkyl
cycloalkyl
alkenyl
alkynyl
heteroaryl
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JP2008540636A5 (enExample
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ファリナ,マルコ
ガグリアルディ,ステファニア
ポール,エマニュエル ル
パロンビ,ジョバンニ
ロシェル,ジャン−フィリップ
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Addex Pharmaceuticals SA
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/16Anti-Parkinson drugs
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    • A61P25/22Anxiolytics
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P3/00Drugs for disorders of the metabolism
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2008511822A 2005-05-18 2006-05-17 代謝型グルタミン酸受容体の陽性アロステリック調節因子としての新規複素環式化合物 Pending JP2008540636A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0510139.9A GB0510139D0 (en) 2005-05-18 2005-05-18 Novel compounds B1
PCT/IB2006/001882 WO2006129199A1 (en) 2005-05-18 2006-05-17 Novel heterocyclic compounds as positive allosteric modulators of metabotropic glutamate receptors

Publications (2)

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JP2008540636A true JP2008540636A (ja) 2008-11-20
JP2008540636A5 JP2008540636A5 (enExample) 2009-07-02

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JP2008511822A Pending JP2008540636A (ja) 2005-05-18 2006-05-17 代謝型グルタミン酸受容体の陽性アロステリック調節因子としての新規複素環式化合物

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Country Link
US (1) US20100004284A1 (enExample)
EP (1) EP1896464A1 (enExample)
JP (1) JP2008540636A (enExample)
KR (1) KR20080017040A (enExample)
CN (1) CN101218231B (enExample)
AU (1) AU2006253863A1 (enExample)
BR (1) BRPI0610067A2 (enExample)
CA (1) CA2609513A1 (enExample)
EA (1) EA014904B1 (enExample)
GB (1) GB0510139D0 (enExample)
IL (1) IL187189A0 (enExample)
MX (1) MX2007014400A (enExample)
NO (1) NO20076477L (enExample)
NZ (1) NZ564255A (enExample)
UA (1) UA92914C2 (enExample)
WO (1) WO2006129199A1 (enExample)
ZA (1) ZA200710280B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011236157A (ja) * 2010-05-11 2011-11-24 Toray Fine Chemicals Co Ltd 光学活性ニペコチン酸誘導体の製造方法
JP2012524798A (ja) * 2009-04-23 2012-10-18 メルク・シャープ・エンド・ドーム・コーポレイション 2−アルキルピペリジンmglur5受容体モジュレーター

Families Citing this family (142)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0510140D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B2
MX2007014444A (es) * 2005-05-18 2008-04-21 Addex Pharmaceuticals Sa Derivados de oxadiazol sustituido como moduladores aloestericos positivos de los receptores de glutamato metabotropicos.
GB0510142D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds A1
GB0510141D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
IL169855A (en) * 2005-07-25 2014-05-28 Elta Systems Ltd A system and method for locating a receiver location
AR058439A1 (es) 2005-07-26 2008-02-06 Portela & Ca Sa Derivados de nitrocatecol como inhibidores de comt. procesos de obtencion y composiciones farmaceuticas.
ES2778846T3 (es) 2005-11-08 2020-08-12 Vertex Pharma Moduladores heterocíclicos de transportadores de casete de unión a ATP
SI2455382T1 (sl) 2005-12-13 2017-03-31 Incyte Holdings Corporation S heteroarilom substituirani pirolo(2,3b)piridini in pirolo(2,3-b)pirimidini kot zaviralci janus kinaze
US7671221B2 (en) 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
EP1845097A1 (en) 2006-04-10 2007-10-17 Portela & Ca., S.A. Oxadiazole derivatives as COMT inhibitors
US7943622B2 (en) 2006-06-06 2011-05-17 Cornerstone Therapeutics, Inc. Piperazines, pharmaceutical compositions and methods of use thereof
GEP20125425B (en) 2006-10-18 2012-03-26 Pfizer Prod Inc Biaryl ether urea compounds
GB0622202D0 (en) * 2006-11-07 2006-12-20 Addex Pharmaceuticals Sa Novel compounds
US7754739B2 (en) 2007-05-09 2010-07-13 Vertex Pharmaceuticals Incorporated Modulators of CFTR
CN101657471B (zh) 2006-12-06 2013-07-03 史密丝克莱恩比彻姆公司 二环化合物及其作为抗糖尿病药的用途
CA2678391C (en) 2007-01-31 2017-01-17 David Alexander Learmonth Dosage regimen for comt inhibitors
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
JP4891111B2 (ja) * 2007-02-16 2012-03-07 富士フイルム株式会社 ズームレンズ
JP5265513B2 (ja) * 2007-02-19 2013-08-14 株式会社カネカ 光学活性3−アミノピペリジン又はその塩の製造方法
CA2681572C (en) 2007-03-23 2014-02-11 Icagen, Inc. Inhibitors of ion channels
CA2686838C (en) 2007-05-09 2017-03-14 Vertex Pharmaceuticals Incorporated Modulators of cftr
ES2467665T5 (es) 2007-06-13 2022-11-03 Incyte Holdings Corp Sales del inhibidor de cinasas Janus (R)-3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
CN101910156B (zh) 2007-12-07 2013-12-04 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的固体形式
MX364936B (es) 2007-12-07 2019-05-15 Vertex Pharma Procesos para producir acidos cicloalquilcarboxamido-piridin benzoicos.
NZ703814A (en) 2008-02-28 2016-06-24 Vertex Pharma Heteroaryl derivatives as cftr modulators
AU2009217865A1 (en) * 2008-02-28 2009-09-03 Bial - Portela & Ca., S.A. Pharmaceutical composition for poorly soluble drugs
EP2288610B8 (en) 2008-03-11 2016-10-12 Incyte Holdings Corporation Azetidine and cyclobutane derivatives as jak inhibitors
MX2010009610A (es) 2008-03-17 2010-09-30 Bial Portela & Ca Sa Formas de cristal de 5-[3-(2,5-dicloro-4,6-dimetil-1-oxi-piridin-3 -il)-[1,2,4]oxadiazol-5-il]-3-nitrobenceno-1,2-diol.
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
TWI434842B (zh) 2008-07-14 2014-04-21 Astellas Pharma Inc Azole compounds
GB0813142D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
US8273900B2 (en) 2008-08-07 2012-09-25 Novartis Ag Organic compounds
JP5683489B2 (ja) 2009-01-12 2015-03-11 アレイ バイオファーマ、インコーポレイテッド ピペリジン含有化合物およびその用途
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
EA018907B1 (ru) 2009-01-30 2013-11-29 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Кристаллический гидрохлорид n-{(1s)-2-амино-1-[(3-фторфенил)метил]этил}-5-хлор-4-(4-хлор-1-метил-1h-пиразол-5-ил)-2-тиофенкарбоксамида
BRPI1014865B1 (pt) 2009-04-01 2020-03-17 Bial - Portela & C.A., S.A. Composição que compreende grânulos compreendendo 2,5- dicloro- 3- (5- (3,4- dihidróxi- 5- nitrofenil)- 1,2,4- oxadiazol- 3- il)- 4,6- dimetilpiridina 1- óxido e formulação farmacêutica
US8673920B2 (en) 2009-05-06 2014-03-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
CA2761859A1 (en) 2009-05-15 2010-11-18 Novartis Ag Aryl pyridine as aldosterone synthase inhibitors
MY156727A (en) 2009-05-22 2016-03-15 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
PT2432472T (pt) 2009-05-22 2019-12-09 Incyte Holdings Corp 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octano- ou heptano-nitrilo como inibidores de jak
CN102548986A (zh) 2009-06-05 2012-07-04 链接医药公司 氨基吡咯烷酮衍生物及其用途
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
US8389536B2 (en) 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
US8586581B2 (en) 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
CA2784830C (en) 2009-12-18 2018-03-27 Sunovion Pharmaceuticals Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
CN102762572A (zh) 2010-02-01 2012-10-31 诺瓦提斯公司 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
US8835444B2 (en) 2010-02-02 2014-09-16 Novartis Ag Cyclohexyl amide derivatives as CRF receptor antagonists
MX354212B (es) 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
AR081760A1 (es) 2010-04-07 2012-10-17 Vertex Pharma Una composicion farmaceutica para administracion oral que comprende acido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoico, un metodo para producir la misma, una tableta y una forma unitaria de dosificacion oral que la comprende y el uso de la misma para la fabricacion de un medicamento
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
US20110288107A1 (en) 2010-05-21 2011-11-24 Bhavnish Parikh Topical formulation for a jak inhibitor
JP5813101B2 (ja) 2010-06-04 2015-11-17 アルバニー モレキュラー リサーチ, インコーポレイテッド グリシントランスポーター−1阻害剤、その作製方法および使用方法
US9079880B2 (en) 2010-07-07 2015-07-14 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
US8697911B2 (en) 2010-07-07 2014-04-15 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
JP5769326B2 (ja) 2010-10-19 2015-08-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Rhoキナーゼ阻害薬
WO2012058116A1 (en) 2010-10-27 2012-05-03 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2632464B1 (en) 2010-10-29 2015-04-29 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CA2820262A1 (en) 2010-12-08 2012-06-14 Vanderbilt University Bicyclic pyrazole compounds as allosteric modulators of mglur5 receptors
AU2011343477A1 (en) * 2010-12-17 2013-07-04 Vanderbilt University Bicyclic triazole and pyrazole lactams as allosteric modulators of mGluR5 receptors
WO2012093101A1 (en) 2011-01-04 2012-07-12 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
US20140045900A1 (en) 2011-02-11 2014-02-13 Bial-Portela & Ca, S.A. Administration regime for nitrocatechols
US9993480B2 (en) 2011-02-18 2018-06-12 Novartis Pharma Ag mTOR/JAK inhibitor combination therapy
US8865725B2 (en) 2011-03-15 2014-10-21 Vanderbilt University Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors
US8772300B2 (en) 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
MY165141A (en) 2011-04-26 2018-02-28 Hoffmann La Roche Pyrazolidin-3-one derivatives
SG194120A1 (en) 2011-04-26 2013-11-29 Hoffmann La Roche Ethynyl derivatives as positive allosteric modulators of the mglur5
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
HK1198579A1 (en) 2011-08-10 2015-04-30 Novartis Pharma Ag Jak p13k/mtor combination therapy
WO2013025733A1 (en) 2011-08-15 2013-02-21 Intermune, Inc. Lysophosphatidic acid receptor antagonists
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
AU2012299227A1 (en) 2011-08-19 2014-02-20 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
EP2755656B1 (en) 2011-09-16 2016-09-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US20130123254A1 (en) 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110995C2 (uk) 2011-10-07 2016-03-10 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як модулятори метаботропного глутаматного рецептора
UA110862C2 (uk) 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
US8999991B2 (en) 2011-10-25 2015-04-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2771005B1 (en) 2011-10-25 2016-05-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9139585B2 (en) 2011-10-31 2015-09-22 Merck Sharp & Dohme Corp. Inhibitors of the Renal Outer Medullary Potassium channel
EP2773206B1 (en) 2011-10-31 2018-02-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013066718A2 (en) 2011-10-31 2013-05-10 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
RS59666B1 (sr) 2011-12-13 2020-01-31 BIAL PORTELA & Cª S A Hemijsko jedinjenje korisno kao intermedijer za pripremu inhibitora katehol-o-metiltransferaze
EP2790511B1 (en) 2011-12-16 2016-09-14 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2013192350A1 (en) * 2012-06-20 2013-12-27 Vanderbilt University Substituted bicyclic aralkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors
WO2013192347A1 (en) * 2012-06-20 2013-12-27 Vanderbilt University Substituted bicyclic cycloalkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors
ES2712190T3 (es) 2012-06-28 2019-05-09 Novartis Ag Moduladores de la vía del complemento y sus usos
CN104379579B (zh) 2012-06-28 2017-03-08 诺华股份有限公司 吡咯烷衍生物及其作为补体途径调节剂的用途
US9388199B2 (en) 2012-06-28 2016-07-12 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
US9468661B2 (en) 2012-06-28 2016-10-18 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
WO2014002051A2 (en) 2012-06-28 2014-01-03 Novartis Ag Complement pathway modulators and uses thereof
EA201590200A1 (ru) 2012-07-12 2015-08-31 Новартис Аг Модуляторы пути активации комплемента и их применение
PE20150184A1 (es) 2012-07-17 2015-02-13 Hoffmann La Roche Derivados de ariletinilo
AR092031A1 (es) 2012-07-26 2015-03-18 Merck Sharp & Dohme Inhibidores del canal de potasio medular externo renal
UA113223C2 (xx) 2012-08-13 2016-12-26 Арилетинілпіримідини
AU2013329739B2 (en) 2012-09-27 2017-04-20 F. Hoffmann-La Roche Ag Arylethynyl derivatives
ES2880814T3 (es) 2012-11-15 2021-11-25 Incyte Holdings Corp Formas de dosificación de liberación sostenida de ruxolitinib
US9777002B2 (en) 2012-11-29 2017-10-03 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2934533B1 (en) 2012-12-19 2017-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9604998B2 (en) 2013-02-18 2017-03-28 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
UA116648C2 (uk) 2013-03-14 2018-04-25 Алкермес Фарма Айерленд Лімітед Фумарати як проліки та їх застосування при лікуванні різних захворювань
US8669281B1 (en) 2013-03-14 2014-03-11 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
EP2968288B1 (en) 2013-03-15 2018-07-04 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP3027625B1 (en) 2013-07-31 2018-05-30 Merck Sharp & Dohme Corp. Spiro-fused derivatives of piperidine useful for the treatment of inter alia hypertension and acute or chronic heart failure
TWI789516B (zh) 2013-08-07 2023-01-11 美商英塞特公司 Jak1抑制劑之持續釋放劑型
WO2015057655A1 (en) 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
MY192489A (en) 2013-10-14 2022-08-23 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds
RU2016122882A (ru) 2013-11-12 2017-12-19 Вертекс Фармасьютикалз Инкорпорейтед Способ получения фармацевтических композиций для лечения опосредованных cftr заболеваний
WO2015127450A1 (en) 2014-02-24 2015-08-27 Alkermes Pharma Ireland Limited Sulfonamide and sulfinamide prodrugs of fumarates and their use in treating various diseases
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
WO2016065586A1 (en) * 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Pyrazole, triazole and tetrazole orexin receptor antagonists
WO2016065584A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Piperidine oxadiazole and thiadiazole orexin receptor antagonists
MX381732B (es) 2014-11-18 2025-03-13 Vertex Pharma Proceso para efectuar la prueba de alto rendimiento de la cromatografia liquida de alta resolucion.
WO2016083863A1 (en) 2014-11-28 2016-06-02 Bial - Portela & Ca, S.A. Medicaments for slowing parkinson's disease
WO2016127358A1 (en) 2015-02-12 2016-08-18 Merck Sharp & Dohme Corp. Inhibitors of renal outer medullary potassium channel
RS60199B1 (sr) 2015-06-03 2020-06-30 Hoffmann La Roche Derivati etinila
AU2016295693B2 (en) 2015-07-17 2020-05-21 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
TWI691486B (zh) 2016-01-29 2020-04-21 日商東麗股份有限公司 環狀胺衍生物及其醫藥用途
WO2017201468A1 (en) 2016-05-20 2017-11-23 Xenon Pharmaceuticals Inc. Benzenesulfonamide compounds and their use as therapeutic agents
CN110325531B (zh) 2016-12-09 2022-05-27 泽农医药公司 苯磺酰胺及其作为治疗剂的用途
KR101862765B1 (ko) 2017-04-21 2018-05-30 한국화학연구원 N-아릴사이클릭아민 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 유로텐신-ⅱ 수용체 활성 관련 질환의 예방 또는 치료용 약학적 조성물
KR102717600B1 (ko) 2017-10-06 2024-10-15 포르마 세라퓨틱스 인크. 유비퀴틴 특이적 펩티다제 30의 억제
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
HRP20220510T1 (hr) 2018-01-30 2022-05-27 Incyte Corporation Postupci za pripravu (1-(3-fluoro-2-(trifluorometil)izonikotinil) piperidin-4-ona)
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
CA3098628A1 (en) 2018-05-17 2019-11-21 Forma Therapeutics, Inc. Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors
MX2020013317A (es) 2018-06-13 2021-04-13 Xenon Pharmaceuticals Inc Compuestos de bencenosulfonamida y su uso como agentes terapeuticos.
MX2021001380A (es) 2018-08-31 2021-05-27 Xenon Pharmaceuticals Inc Compuestos de sulfonamida sustituidos con heteroarilo y su uso como agentes terapeuticos.
WO2020047312A1 (en) 2018-08-31 2020-03-05 Xenon Pharmaceuticals Inc. Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors
WO2020061101A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors
PT3860989T (pt) 2018-10-05 2023-06-30 Forma Therapeutics Inc Pirrolinas fundidas que atuam como inibidores da protease 30 específica da ubiquitina (usp30)
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
WO2021127643A1 (en) 2019-12-20 2021-06-24 Tenaya Therapeutics, Inc. Fluoroalkyl-oxadiazoles and uses thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CA3213079A1 (en) 2021-04-13 2022-10-20 Kristin Lynne ANDREWS Amino-substituted heterocycles for treating cancers with egfr mutations
KR20240016950A (ko) 2021-05-04 2024-02-06 테나야 테라퓨틱스, 인코포레이티드 대사 질환 및 hfpef의 치료에 사용하기 위한 2-플루오로알킬-1,3,4-옥사디아졸-5-일-티아졸, hdac6 억제제
CN116903587B (zh) * 2023-06-01 2024-03-22 三峡大学 一种角鲨烯环氧酶抑制剂及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014370A2 (en) * 2002-08-09 2004-02-19 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
WO2004014881A2 (en) * 2002-08-09 2004-02-19 Astra Zeneca Ab '1,2,4'oxadiazoles as modulators of metabotropic glutamate receptor-5

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MC598A1 (fr) 1966-02-16 1967-03-21 Mauvernay Roland Yves Nouveaux composés chimiques et procédé pour leur préparation
MC641A1 (fr) 1967-03-08 1967-12-05 Mauvernay Roland Yves Nouveaux composés chimiques et procédé pour leur préparation
US3509153A (en) 1967-03-24 1970-04-28 Miles Lab 5-phenyl (or 5-phenylalkyl)-2-(omega-(4-phenyl-1-piperazinyl)alkyl)tetrazoles
GB9603755D0 (en) * 1996-02-22 1996-04-24 Pfizer Ltd Therapeutic agents
US7217714B1 (en) * 1998-12-23 2007-05-15 Agouron Pharmaceuticals, Inc. CCR5 modulators
WO2001054506A1 (en) 2000-01-28 2001-08-02 Akkadix Corporation Methods for killing nematodes and nematode eggs using bis-amino-1,2,4-thiadiazoles
MY131890A (en) 2001-03-13 2007-09-28 Schering Corp Piperidine compounds
FR2834406A1 (fr) 2001-12-28 2003-07-04 Thomson Licensing Sa Procede de mise a jour d'une liste de revocation de cles, d'appareils ou de modules non-conformes dans un systeme de diffusion securise de contenu
MXPA05001590A (es) * 2002-08-09 2005-05-23 Astrazeneca Ab Compuestos que tienen actividad en los receptores metabotropicos de glutamato.
JP2006521358A (ja) 2003-03-26 2006-09-21 メルク エンド カムパニー インコーポレーテッド 代謝調節型グルタミン酸受容体のベンズアミドモジュレータ
EP1613615A2 (en) * 2003-04-03 2006-01-11 Merck & Co., Inc. 4-ring imidazole derivatives as modulators of metabotropic glutamate receptor-5
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
BRPI0507481A (pt) * 2004-02-18 2007-07-17 Astrazeneca Ab composto, composição farmacêutica, uso do composto, e, métodos para tratar distúrbios mediados por mglur 5 e para inibir ativação de receptores de mglur 5
GB0510143D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds A1
GB0510141D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
GB0510140D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B2
MX2007014444A (es) * 2005-05-18 2008-04-21 Addex Pharmaceuticals Sa Derivados de oxadiazol sustituido como moduladores aloestericos positivos de los receptores de glutamato metabotropicos.
GB0622202D0 (en) * 2006-11-07 2006-12-20 Addex Pharmaceuticals Sa Novel compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014370A2 (en) * 2002-08-09 2004-02-19 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
WO2004014881A2 (en) * 2002-08-09 2004-02-19 Astra Zeneca Ab '1,2,4'oxadiazoles as modulators of metabotropic glutamate receptor-5

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012524798A (ja) * 2009-04-23 2012-10-18 メルク・シャープ・エンド・ドーム・コーポレイション 2−アルキルピペリジンmglur5受容体モジュレーター
JP2011236157A (ja) * 2010-05-11 2011-11-24 Toray Fine Chemicals Co Ltd 光学活性ニペコチン酸誘導体の製造方法

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