CU24355B1 - Derivados de 2((( oxadiazol/triazol/tetrazol/isoxazol) metil) fenil)-1-(heterociclil)-ona como inhibidores activos de autotaxina - Google Patents

Derivados de 2((( oxadiazol/triazol/tetrazol/isoxazol) metil) fenil)-1-(heterociclil)-ona como inhibidores activos de autotaxina

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Publication number
CU24355B1
CU24355B1 CUP2016000007A CU20160007A CU24355B1 CU 24355 B1 CU24355 B1 CU 24355B1 CU P2016000007 A CUP2016000007 A CU P2016000007A CU 20160007 A CU20160007 A CU 20160007A CU 24355 B1 CU24355 B1 CU 24355B1
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CU
Cuba
Prior art keywords
isoxazol
oxadiazol
tetrazol
triazol
phenyl
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CUP2016000007A
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English (en)
Other versions
CU20160007A7 (es
Inventor
Urs Baettig
David Beattie
Darren Mark Legrand
Andrew Stuart Lister
Jeffrey Mckenna
David William Pearce
David Andrew Sandham
Oliver Ross Steward
Christopher Thomson
Original Assignee
Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CU20160007A7 publication Critical patent/CU20160007A7/es
Publication of CU24355B1 publication Critical patent/CU24355B1/es

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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

<p>La presente invención se relaciona con nuevos compuestos derivados de 2(((oxadiazol/triazol/tetrazol/isoxazol) metil) fenil)-1-(heterociclil)-ona que tienen la fórmula</p> <p> </p> <p>ESPACIO PARA FORMULA</p> <p> </p> <p>activos como inhibidores de autotaxina, procesos para su preparación, composiciones farmaceúticas y medicamentos que los contienen y a su uso en enfermedades y trastornos mediados por autotaxina tales como cáncer, dolor neuropático y fibrosis.</p>
CUP2016000007A 2013-07-18 2014-07-16 Derivados de 2((( oxadiazol/triazol/tetrazol/isoxazol) metil) fenil)-1-(heterociclil)-ona como inhibidores activos de autotaxina CU24355B1 (es)

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Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI633087B (zh) 2012-06-13 2018-08-21 赫孚孟拉羅股份公司 新穎二氮雜螺環烷及氮雜螺環烷
EP3590940B1 (en) 2012-09-25 2021-06-09 F. Hoffmann-La Roche AG Hexahydropyrrolo[3,4-c]pyrrole derivatives and related compounds as autotaxin (atx) inhibitors and as inhibitors of the lysophosphatidic acid (lpa) production for treating e.g. renal diseases
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
PT3022202T (pt) * 2013-07-18 2019-09-03 Novartis Ag Inibidores da autotaxina compreendendo um núcleo beteroaromático anel-benzilo-amida-ciclo
NO3074400T3 (es) 2013-11-26 2018-04-14
EP3122751B1 (en) 2014-03-26 2019-10-30 F.Hoffmann-La Roche Ag Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
MA39792B1 (fr) 2014-03-26 2019-12-31 Hoffmann La Roche Composés bicycliques en tant qu'inhibiteurs de production d'autotaxine (atx) et d'acide lysophosphatidique (lpa)
CR20160496A (es) 2014-04-04 2017-01-02 X-Rx Inc Inhibidores espirocíclicos sustituidos de la autotaxina
CN107406419B (zh) * 2015-01-20 2020-09-11 诺华股份有限公司 Pet显像剂
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CA2988306A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
MX387736B (es) 2015-09-04 2025-03-18 Hoffmann La Roche Derivados de fenoximetilo.
MX2017015034A (es) 2015-09-24 2018-04-13 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
KR20180054634A (ko) 2015-09-24 2018-05-24 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 신규한 이환형 화합물
CN107635995B (zh) 2015-09-24 2022-08-19 豪夫迈·罗氏有限公司 作为atx抑制剂的二环化合物
PE20180451A1 (es) 2015-09-24 2018-03-05 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores de atx
GB201617758D0 (en) 2016-10-20 2016-12-07 Almac Discovery Limited Pharmaceutical compounds
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
MA49879A (fr) 2017-03-16 2020-06-24 Hoffmann La Roche Composés hétérocycliques utiles en tant qu'inhibiteurs doubles d'atx/ca
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
WO2022006470A1 (en) 2020-07-01 2022-01-06 Vanderbilt University Methods of treatment for a kidney disease
CN116730977A (zh) * 2022-03-04 2023-09-12 华东理工大学 新型芳基杂环类化合物及其制备方法和用途
WO2025125486A1 (en) 2023-12-14 2025-06-19 Syngenta Crop Protection Ag Process for the preparation of piperidinyl 1,2,4-oxadiazole derivatives

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1016489B (it) 1974-03-18 1977-05-30 Isf Spa Inalatore
GB2041363B (en) 1979-01-19 1982-10-06 Pfizer Ltd N-benzyl-imidazoles
US6536427B2 (en) 1990-03-02 2003-03-25 Glaxo Group Limited Inhalation device
US6596260B1 (en) 1993-08-27 2003-07-22 Novartis Corporation Aerosol container and a method for storage and administration of a predetermined amount of a pharmaceutically active aerosol
US6051397A (en) 1993-11-16 2000-04-18 Max Planck Gesellschaft Zur Forderung Der Wissenschaften DNA encoding MCK-10, a novel receptor tyrosine kinase
ES2216418T3 (es) 1995-12-07 2004-10-16 Jago Research Ag Boquilla para un inhalador para la administracion de varias dosis de un polvo seco farmacologico.
NZ324374A (en) 1996-01-03 1999-06-29 Glaxo Group Ltd Inhalation device
CZ298885B6 (cs) 1996-02-21 2008-03-05 Schering Corporation Inhalátor práškových léku
US6207665B1 (en) 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
ZA987385B (en) 1997-08-19 2000-04-18 Lilly Co Eli Growth hormone secretagogues.
ZA987383B (en) 1997-08-19 2000-02-17 Lilly Co Eli Treatment of congestive heart failure with growth hormone secretagogues.
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
SE9902765D0 (sv) 1999-07-21 1999-07-21 Astra Pharma Prod Novel compounds
US7069929B2 (en) 2000-02-01 2006-07-04 Quadrant Technologies Limited Dry powder inhaler
US20050065118A1 (en) 2001-10-16 2005-03-24 Jing Wang Organosulfur inhibitors of tyrosine phosphatases
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
CA2492110A1 (en) * 2002-07-18 2004-01-29 Pfizer Products Inc. Bicyclic piperidine derivatives as antagonists of the ccr1 chemokine receptor
CA2493457A1 (en) * 2002-07-24 2004-01-29 Tularik Inc. Acetylamino benzoic acid compounds and their use for nonsense suppression and the treatment of disease
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤
GB0224917D0 (en) * 2002-10-25 2002-12-04 Novartis Ag Organic compounds
TW200418806A (en) * 2003-01-13 2004-10-01 Fujisawa Pharmaceutical Co HDAC inhibitor
US7169797B2 (en) * 2003-02-14 2007-01-30 Abbott Laboratories Protein-tyrosine phosphatase inhibitors and uses thereof
US20040167188A1 (en) 2003-02-14 2004-08-26 Zhili Xin Protein-tyrosine phosphatase inhibitors and uses thereof
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
WO2004080966A1 (ja) 2003-03-14 2004-09-23 Ono Pharmaceutical Co., Ltd. 含窒素複素環誘導体およびそれらを有効成分とする薬剤
CA2534941A1 (en) 2003-08-22 2005-03-03 Schering Aktiengesellschaft Chemokine inhibiting piperazine derivatives and their use to treat myocarditis
GB2407042B (en) 2003-10-17 2007-10-24 Vectura Ltd Inhaler
CA2554974A1 (en) 2004-02-06 2005-08-25 Schering Aktiengesellschaft Chemokine inhibiting piperazine derivatives and their use to treat multiple myeloma
CN100589849C (zh) 2004-02-24 2010-02-17 微计量技术有限公司 基于合成射流的药物输送方法和装置
EA200601514A1 (ru) 2004-02-24 2007-02-27 Шеринг Акциенгезельшафт Производные пиперазинмочевины для лечения эндометриоза
GB0409236D0 (en) 2004-04-26 2004-05-26 Novartis Ag Organic compounds
GB0410712D0 (en) 2004-05-13 2004-06-16 Novartis Ag Organic compounds
GB0413960D0 (en) 2004-06-22 2004-07-28 Novartis Ag Organic compounds
JP5315611B2 (ja) 2004-06-23 2013-10-16 小野薬品工業株式会社 S1p受容体結合能を有する化合物およびその用途
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
WO2006078941A2 (en) 2005-01-20 2006-07-27 Sirtris Pharmaceuticals, Inc. Novel sirtuin activating compounds and methods of use thereof
US20090264650A1 (en) 2005-03-31 2009-10-22 Nobuo Cho Prophylactic/Therapeutic Agent for Diabetes
WO2007044885A2 (en) 2005-10-11 2007-04-19 Chemocentryx, Inc. Piperidine derivatives and methods of use
CA2667225C (en) 2006-10-25 2015-06-09 Novartis Ag Powder dispersion apparatus, method of making and using the apparatus, and components that can be used on the apparatus and other devices
US8614233B2 (en) 2007-05-29 2013-12-24 Universite De Montreal Cinnamoyl inhibitors of transglutaminase
DE102007047738A1 (de) * 2007-10-05 2009-04-09 Merck Patent Gmbh Imidazolderivate
EP2257326A2 (en) 2008-03-21 2010-12-08 Novartis AG Powder dispersion apparatus
EP2623101B1 (en) 2009-04-02 2021-04-21 Merck Patent GmbH Piperidine and piperazine derivatives as autotaxin inhibitors
JP5767205B2 (ja) 2009-04-02 2015-08-19 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung オートタキシン阻害剤としての複素環式化合物
AR082492A1 (es) 2010-08-20 2012-12-12 Allergan Inc N-alquil-2-(1-(5-sustituido-2-(3-oxo-3-(trifluorometilsulfonamido)propil)bencil)pirrolidin-2-il)oxazol-4-carboxamida y su uso para preparar un medicamento util para tratar enfermedades o afecciones mediadas por receptor dp, fp, ep, ep, tp y/o ep
EP2655334B1 (en) 2010-12-22 2018-10-03 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
CN103619837A (zh) 2011-04-22 2014-03-05 阿勒根公司 用于治疗疼痛的脂肪酸酰胺水解酶抑制剂
EP2736883B1 (en) 2011-07-29 2019-09-04 Karyopharm Therapeutics, Inc. Nuclear transport modulators and uses thereof
EP3022201A1 (en) 2013-07-18 2016-05-25 Novartis AG Autotaxin inhibitors
PT3022202T (pt) * 2013-07-18 2019-09-03 Novartis Ag Inibidores da autotaxina compreendendo um núcleo beteroaromático anel-benzilo-amida-ciclo

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