[go: up one dir, main page]

PE20151605A1 - Nuevos derivados de octahidro-pirrolo[3,4-c]-pirrol y analogos de los mismos como inhibidores de autotaxina - Google Patents

Nuevos derivados de octahidro-pirrolo[3,4-c]-pirrol y analogos de los mismos como inhibidores de autotaxina

Info

Publication number
PE20151605A1
PE20151605A1 PE2015001912A PE2015001912A PE20151605A1 PE 20151605 A1 PE20151605 A1 PE 20151605A1 PE 2015001912 A PE2015001912 A PE 2015001912A PE 2015001912 A PE2015001912 A PE 2015001912A PE 20151605 A1 PE20151605 A1 PE 20151605A1
Authority
PE
Peru
Prior art keywords
pirrol
pirrolo
octahydro
analogs
autotaxin inhibitors
Prior art date
Application number
PE2015001912A
Other languages
English (en)
Inventor
Jerome Hert
Daniel Hunziker
Patrizio Mattei
Harald Mauser
Guozhi Tang
Lisha Wang
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20151605A1 publication Critical patent/PE20151605A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La invencion proporciona compuestos que tienen la formula general I, que son inhibidores de autotaxina (ATX), donde: R1 es cicloalquilo sustituido, entre otros.; R2 es fenilo sustituido, entre otros; Y es -OC(O)-, entre otros; A es -N- o CH-; W es -O-, -S-, entre otros; m, n, p y q es 1 o 2. Compuestos preferidos: (3aR,6aS)-5-(5-hidroxipicolinoil)hexahidropirrolo[3,4-c]pirrol-2(1H)-carboxilato de 3,5-diclorobencilo; trans-2-(4-sulfamoilbenzoil)hexahidro-1H-pirrolo[3,4-c]piridina-5(6H)-carboxilato de 3,5-diclorobencilo.
PE2015001912A 2013-03-12 2014-03-11 Nuevos derivados de octahidro-pirrolo[3,4-c]-pirrol y analogos de los mismos como inhibidores de autotaxina PE20151605A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13158724 2013-03-12

Publications (1)

Publication Number Publication Date
PE20151605A1 true PE20151605A1 (es) 2015-11-04

Family

ID=47843184

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015001912A PE20151605A1 (es) 2013-03-12 2014-03-11 Nuevos derivados de octahidro-pirrolo[3,4-c]-pirrol y analogos de los mismos como inhibidores de autotaxina

Country Status (32)

Country Link
US (2) US20150376194A1 (es)
EP (1) EP2970256B1 (es)
JP (2) JP6483034B2 (es)
KR (1) KR20150126036A (es)
CN (1) CN105073748B (es)
AR (1) AR095079A1 (es)
AU (1) AU2014230943B8 (es)
BR (1) BR112015022804A2 (es)
CA (1) CA2901047A1 (es)
CL (1) CL2015002386A1 (es)
CR (1) CR20150436A (es)
DK (1) DK2970256T3 (es)
EA (1) EA035015B1 (es)
ES (1) ES2763417T3 (es)
HR (1) HRP20192274T1 (es)
HU (1) HUE046776T2 (es)
IL (1) IL240796B (es)
LT (1) LT2970256T (es)
MA (1) MA38432B1 (es)
MX (1) MX373247B (es)
MY (1) MY177574A (es)
PE (1) PE20151605A1 (es)
PH (1) PH12015501934B1 (es)
PL (1) PL2970256T3 (es)
PT (1) PT2970256T (es)
RS (1) RS59682B1 (es)
SG (1) SG11201507396YA (es)
SI (1) SI2970256T1 (es)
TW (1) TWI678368B (es)
UA (1) UA115354C2 (es)
WO (1) WO2014139978A1 (es)
ZA (1) ZA201505944B (es)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
CA2878442A1 (en) 2012-09-25 2014-04-03 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
US9540324B2 (en) 2013-09-26 2017-01-10 Luc Therapeutics, Inc. Selective octahydro-cyclopenta[C] pyrrole negative modulators of NR2B
PE20160845A1 (es) 2013-11-26 2016-09-10 Hoffmann La Roche Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo
HUE046820T2 (hu) * 2014-03-26 2020-03-30 Hoffmann La Roche Biciklusos vegyületek autotaxin (ATX) és lizofoszfatidsav (LPA) termelésgátlókként
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
AP2016009496A0 (en) 2014-04-04 2016-10-31 X-Rx Inc Substituted spirocydic inhibitors of autotaxin
JO3579B1 (ar) 2014-09-26 2020-07-05 Luc Therapeutics Inc مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول
GB201501870D0 (en) 2015-02-04 2015-03-18 Cancer Rec Tech Ltd Autotaxin inhibitors
GB201502020D0 (en) 2015-02-06 2015-03-25 Cancer Rec Tech Ltd Autotaxin inhibitory compounds
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
WO2017012502A1 (en) 2015-07-17 2017-01-26 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
MX377277B (es) 2015-09-04 2025-03-07 Hoffmann La Roche Derivados de fenoximetilo.
BR112018006034A2 (pt) 2015-09-24 2018-10-09 Hoffmann La Roche compostos bicíclicos como inibidores de atx
MA42923A (fr) * 2015-09-24 2021-04-28 Hoffmann La Roche Composés bicycliques comme inhibiteurs mixtes de atx/ca
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
RU2725138C2 (ru) * 2015-09-24 2020-06-30 Ф. Хоффманн-Ля Рош Аг Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca)
WO2017071799A1 (en) * 2015-10-30 2017-05-04 Nitsch, Robert Lpa level reduction for treating central nervous system disorders
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
CN108456208B (zh) * 2017-02-22 2021-04-16 广州市恒诺康医药科技有限公司 氮杂螺环类化合物及其制备方法和应用
KR20190129924A (ko) * 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
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
ES2747768T3 (es) 2017-03-20 2020-03-11 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)
EP3728234B1 (en) 2017-12-21 2025-05-14 F. Hoffmann-La Roche AG Radiolabeled compounds
WO2020061255A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
CN113412113B (zh) * 2018-12-11 2024-07-26 豪夫迈·罗氏有限公司 氨基嗪酰胺
WO2020119896A1 (en) * 2018-12-11 2020-06-18 F. Hoffmann-La Roche Ag Heterocyclic inhibitors of atx
US20220378756A1 (en) 2019-09-19 2022-12-01 Forma Therapeutics, Inc. Activating pyruvate kinase r
CN113549063B (zh) * 2020-04-23 2024-04-05 南京药石科技股份有限公司 一种光学异构的八氢-2H-吡咯并[3,4-c]吡啶-2-羧酸叔丁酯的制备方法
WO2022003557A1 (en) * 2020-06-30 2022-01-06 Cadila Healthcare Limited Novel inhibitors of autotaxin
CN116528855A (zh) 2020-10-16 2023-08-01 米拉洛克斯有限责任公司 用于治疗癌症、阿尔茨海默病、血色沉着病和其它病症的金属酶抑制剂
KR20230128511A (ko) 2021-01-05 2023-09-05 자이두스 라이프사이언시즈 리미티드 신규한 오토택신 억제제
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
TW202317560A (zh) * 2021-06-26 2023-05-01 美商賽迪拉治療股份有限公司 Ｃｄｋ２抑制劑及其使用方法

Family Cites Families (138)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1252898B (de) 1965-06-12 1967-10-26 Bayer Ag Verfahren zur Herstellung von Copolymerisaten des Trioxans
US5240928A (en) 1989-07-03 1993-08-31 Merck & Co., Inc. Substituted quinazolinones as angiotensin II antagonists
DE3930262A1 (de) 1989-09-11 1991-03-21 Thomae Gmbh Dr K Kondensierte diazepinone, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
KR910009330B1 (ko) 1989-10-23 1991-11-11 재단법인 한국화학연구소 항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
CA2037630C (en) 1990-03-07 2001-07-03 Akira Morimoto Nitrogen-containing heterocylic compounds, their production and use
US5470975A (en) 1990-10-16 1995-11-28 E.R. Squibb & Sons, Inc. Dihydropyrimidine derivatives
US5290780A (en) 1991-01-30 1994-03-01 American Cyanamid Co. Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
US5238942A (en) 1991-05-10 1993-08-24 Merck & Co., Inc. Substituted quinazolinones bearing acidic functional groups as angiotensin ii antagonists
DE4121214A1 (de) 1991-06-27 1993-01-14 Bayer Ag 7-azaisoindolinyl-chinolon- und -naphthyridoncarbonsaeure-derivate
US5202322A (en) 1991-09-25 1993-04-13 Merck & Co., Inc. Quinazolinone and pyridopyrimidine a-II antagonists
US5532243A (en) * 1992-02-14 1996-07-02 The Dupont Merck Pharmaceutical Company Antipsychotic nitrogen-containing bicyclic compounds
US5358951A (en) 1993-04-23 1994-10-25 American Cyanamid Company Angiotensin II receptor blocking 2, 3, 6 substituted quinazolinones
DE4407047A1 (de) 1994-03-03 1995-09-07 Merck Patent Gmbh Acetamide
US20010016657A1 (en) 1997-03-18 2001-08-23 Smithkline Beecham P.L.C. Substituted isoquinoline derivatives and their use as anticonvulsants
TR200002241T2 (tr) 1998-02-04 2000-11-21 Banyu Pharmaceutical Co., Ltd. N-Asil siklik amin türevleri
JP2001039950A (ja) 1999-07-30 2001-02-13 Banyu Pharmaceut Co Ltd Ｎ−アシル環状アミン誘導体
CA2389034A1 (en) 1999-10-27 2001-05-03 Cor Therapeutics, Inc. Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
WO2002070523A1 (en) 2001-03-07 2002-09-12 Pfizer Products Inc. Modulators of chemokine receptor activity
US7667053B2 (en) 2002-04-12 2010-02-23 Merck & Co., Inc. Bicyclic amides
GB0303852D0 (en) 2003-02-19 2003-03-26 Pfizer Ltd Triazole compounds useful in therapy
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
SE0302811D0 (sv) 2003-10-23 2003-10-23 Astrazeneca Ab Novel compounds
GB0324790D0 (en) 2003-10-24 2003-11-26 Astrazeneca Ab Amide derivatives
US7226951B2 (en) 2003-12-17 2007-06-05 Allergan, Inc. Compounds having selective cytochrome P450RAI-1 or selective cytochrome P450RAI-2 inhibitory activity and methods of obtaining the same
KR100610731B1 (ko) 2004-02-24 2006-08-09 한국과학기술연구원 Ｔ-형 칼슘 채널 차단제로서 유용한 ３,４-디히드로퀴나졸린유도체 및 그의 제조 방법
WO2005084667A1 (en) 2004-03-03 2005-09-15 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
ES2297727T3 (es) 2004-06-09 2008-05-01 F. Hoffmann-La Roche Ag Derivados de octahidropirrolo(3,4-c)pirrol y su empleo como agentes antiviricos.
CN101035773B (zh) 2004-08-10 2012-06-06 詹森药业有限公司 抑制hiv的1,2,4-三嗪-6-酮衍生物
US7410949B2 (en) 2005-01-18 2008-08-12 Hoffmann-La Roche Inc. Neuropeptide-2 receptor (Y-2R) agonists and uses thereof
GB0504019D0 (en) 2005-02-26 2005-04-06 Astrazeneca Ab Amide derivatives
MX2007013469A (es) 2005-04-28 2008-01-22 Wyeth Corp Forma ii polimorfa de tanaproget.
US7737279B2 (en) 2005-05-10 2010-06-15 Bristol-Myers Squibb Company 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same
TW200800999A (en) 2005-09-06 2008-01-01 Astrazeneca Ab Novel compounds
PT1942108E (pt) 2005-10-28 2013-10-24 Ono Pharmaceutical Co Composto com um grupo básico e a sua utilização
WO2007058322A1 (ja) 2005-11-18 2007-05-24 Ono Pharmaceutical Co., Ltd. 塩基性基を含有する化合物およびその用途
JP2007176809A (ja) 2005-12-27 2007-07-12 Hideaki Natsukari 複素環置換アミド化合物、その製造法および医薬組成物
US20070208001A1 (en) 2006-03-03 2007-09-06 Jincong Zhuo Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
JP2008031064A (ja) * 2006-07-27 2008-02-14 Astellas Pharma Inc ジアシルピペラジン誘導体
WO2008033764A2 (en) 2006-09-11 2008-03-20 N.V. Organon Quinazolinone and isoquinolinone acetamide derivatives
EP2061791A1 (en) 2006-09-15 2009-05-27 Schering Corporation Spiro-condensed azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabilism
US8735411B2 (en) 2006-10-02 2014-05-27 Abbvie Inc. Macrocyclic benzofused pyrimidine derivatives
TWI404532B (zh) 2006-11-02 2013-08-11 Targacept Inc 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺
ATE523497T1 (de) 2006-11-15 2011-09-15 High Point Pharmaceuticals Llc Neue 2-(2-hydroxyphenyl)benzimidazole, die sich für die behandlung von obesitas und diabetes eignen
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
EP1975165A1 (de) 2007-03-27 2008-10-01 Boehringer Ingelheim Pharma GmbH & Co. KG Substituierte Pyrrolidinamide, deren Herstellung und deren Verwendung als Arzneimittel
CN101657433A (zh) 2007-03-29 2010-02-24 弗·哈夫曼-拉罗切有限公司 非核苷逆转录酶抑制剂
CL2008001002A1 (es) 2007-04-11 2008-10-17 Actelion Pharmaceuticals Ltd Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana.
DE502008001903D1 (de) 2007-04-27 2011-01-05 Sanofi Aventis 2 -heteroaryl- pyrrolo ä3, 4-cüpyrrol- derivate und deren verwendung als scd inhibitoren
JP5501230B2 (ja) 2007-08-07 2014-05-21 アボット ゲーエムベーハー ウント カンパニー カーゲー セロトニン５−ｈｔ６受容体の調節に応答する障害の治療に好適なキノリン化合物
DE102007047737A1 (de) 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
ES2830024T3 (es) 2007-10-19 2021-06-02 Novartis Ag Composiciones y métodos para el tratamiento del edema macular
PA8802501A1 (es) 2007-10-31 2009-06-23 Janssen Pharmaceutica Nv Diaminas en puente o fusionadas sustituidas con arilo como moduladores de leucotrieno, hidrolasa
JP2009161449A (ja) 2007-12-28 2009-07-23 Lion Corp Ｐｐａｒ活性促進剤並びに美容用飲食品、皮膚外用剤及び医薬
EP2301936A1 (en) 2008-06-19 2011-03-30 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diarylketoxime derivative
WO2010028761A1 (de) 2008-09-09 2010-03-18 Sanofi-Aventis 2-heteroaryl-pyrrolo[3, 4-c]pyrrol-derivate und ihre verwendung als scd inhibitoren
TW201020247A (en) 2008-11-06 2010-06-01 Gruenenthal Gmbh Substituierte disulfonamide
JP5373104B2 (ja) 2008-11-17 2013-12-18 エフ．ホフマン−ラ ロシュ アーゲー Ｃｒｔｈ２アンタゴニスト又は部分アゴニストとして使用されるナフチル酢酸
DE102008059578A1 (de) * 2008-11-28 2010-06-10 Merck Patent Gmbh Benzo-Naphtyridin Verbindungen
JP5697601B2 (ja) * 2008-12-01 2015-04-08 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 癌に対するオータキシン阻害剤としての２，５−ジアミノ−置換ピリド［４，３−ｄ］ピリミジン
TW201035102A (en) 2009-03-04 2010-10-01 Gruenethal Gmbh Sulfonylated tetrahydroazolopyrazines and their use as medicinal products
AU2010219705A1 (en) 2009-03-05 2011-07-21 Daiichi Sankyo Company, Limited Pyridine derivative
WO2010108268A1 (en) 2009-03-23 2010-09-30 Merck Frosst Canada Ltd. Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
TW201038572A (en) 2009-03-25 2010-11-01 Gruenenthal Gmbh Substituted spiro-amide compounds
CN102369186B (zh) * 2009-04-02 2014-07-09 默克专利有限公司 作为自分泌运动因子抑制剂的哌啶和哌嗪衍生物
AU2010230646B2 (en) 2009-04-02 2015-11-26 Merck Patent Gmbh Heterocyclic compounds as autotaxin inhibitors
ES2547124T3 (es) * 2009-04-02 2015-10-01 Merck Patent Gmbh Inhibidores de autotaxina
FR2945534B1 (fr) 2009-05-12 2012-11-16 Sanofi Aventis DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
JP2012527474A (ja) 2009-05-22 2012-11-08 エクセリクシス， インク． 増殖性疾患に対するベンゾキサゼピンベースのｐｉ３ｋ／ｍｔ０ｒ阻害剤
US20120083476A1 (en) 2009-06-05 2012-04-05 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
DE102009033392A1 (de) 2009-07-16 2011-01-20 Merck Patent Gmbh Heterocyclische Verbindungen als Autotaxin-Inhibitoren II
EP2462128B1 (en) 2009-08-04 2016-09-21 Amira Pharmaceuticals, Inc. Compounds as lysophosphatidic acid receptor antagonists
UA107360C2 (en) 2009-08-05 2014-12-25 Biogen Idec Inc Bicyclic aryl sphingosine 1-phosphate analogs
AR079022A1 (es) 2009-11-02 2011-12-21 Sanofi Aventis Derivados de acido carboxilico ciclico sustituidos con acilamino, su uso como productos farmaceuticos, composicion farmaceutica y metodo de preparacion
BR112012016733A2 (pt) 2010-01-07 2015-09-01 Du Pont "composto, composição fungicida e método"
US8815869B2 (en) 2010-03-18 2014-08-26 Abbvie Inc. Lactam acetamides as calcium channel blockers
ME02330B (me) 2010-03-19 2016-06-20 Pfizer Derivati 2,3-dihidro-1h-inden-1-il-2,7-diazaspir0[3.6]nonana i njihova upotreba kao antagonista ili inverznih agonista grelinskog receptora
JP5827677B2 (ja) 2010-03-26 2015-12-02 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ベンゾナフチリジンアミン
GB201008005D0 (en) 2010-05-13 2010-06-30 Sentinel Oncology Ltd Pharmaceutical compounds
EP2575794A2 (en) 2010-06-04 2013-04-10 B.S.R.C. "Alexander Fleming" Autotaxin pathway modulation and uses thereof
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
ES2646834T3 (es) * 2010-08-20 2017-12-18 Amira Pharmaceuticals, Inc. Inhibidores de autotaxina y usos de los mismos
US8859775B2 (en) 2010-09-02 2014-10-14 Merck Patent Gmbh Pyrazolopyridinone derivatives as LPA receptor antagonists
EP2646428B1 (en) 2010-12-02 2016-06-01 Shanghai De Novo Pharmatech Co Ltd. Heterocyclic derivatives, preparation processes and medical uses thereof
CA2818903C (en) 2010-12-14 2021-03-23 Electrophoretics Limited 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor
US9260416B2 (en) * 2011-05-27 2016-02-16 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
WO2013033059A1 (en) 2011-08-29 2013-03-07 Bristol-Myers Squibb Company Spiro bicyclic diamine derivatives as hiv attachment inhibitors
WO2013054185A1 (en) 2011-10-13 2013-04-18 Pfizer, Inc. Pyrimidine and pyridine derivatives useful in therapy
JPWO2013065712A1 (ja) 2011-10-31 2015-04-02 東レ株式会社 ジアザスピロウレア誘導体及びその医薬用途
US8809552B2 (en) 2011-11-01 2014-08-19 Hoffmann-La Roche Inc. Azetidine compounds, compositions and methods of use
WO2013079223A1 (en) 2011-12-02 2013-06-06 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rorϒ, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
TWI638802B (zh) 2012-05-24 2018-10-21 芬蘭商奧利安公司 兒茶酚ｏ－甲基轉移酶活性抑制化合物
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
WO2014001377A1 (en) 2012-06-27 2014-01-03 F. Hoffmann-La Roche Ag 5-azaindazole compounds and methods of use
EP2877166B1 (en) 2012-07-27 2018-02-28 Biogen MA Inc. 1-[7-(cis-4-methyl-cyclohexyloxy)-8-trifluoromethyl-naphthalen-2-ylmethyl]-piperidine-4-carboxylic acid derivatives as autotaxin (ATX) modulators for treating inflammations and autoimmune disorders
KR102127025B1 (ko) 2012-07-27 2020-06-25 비오겐 엠에이 아이엔씨. S1p 조절제 및/또는 atx 조절제인 화합물들
AR092211A1 (es) 2012-09-24 2015-04-08 Merck Patent Ges Mit Beschränkter Haftung Derivados de hidropirrolopirrol
CA2878442A1 (en) 2012-09-25 2014-04-03 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
EP2900269B1 (en) 2012-09-25 2018-08-01 Bayer Pharma Aktiengesellschaft Combination of regorafenib and acetylsalicylic acid for treating colorectal cancer
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
HRP20230162T1 (hr) 2012-10-25 2023-04-14 Tetra Discovery Partners Llc Heteroarilni inhibitori enzima pde4
DK2938598T3 (en) 2012-12-31 2017-02-13 Cadila Healthcare Ltd Substituted phthalazine-1 (2H) -one derivatives as selective inhibitors of poly (adp-ribose) polymerase-1
WO2014133112A1 (ja) 2013-03-01 2014-09-04 国立大学法人東京大学 オートタキシン阻害活性を有する８－置換イミダゾピリミジノン誘導体
EP2970330B1 (en) 2013-03-12 2019-04-17 AbbVie Inc. Tetracyclic bromodomain inhibitors
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
WO2014164905A1 (en) 2013-03-12 2014-10-09 Acucela Inc. Substituted 3-phenylpropylamine derivatives for the treatment of ophthalmic diseases and disorders
TWI593692B (zh) 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
US20160039825A1 (en) 2013-03-15 2016-02-11 Biogen Ma Inc. S1p and/or atx modulating agents
EA035256B1 (ru) 2013-07-18 2020-05-21 Новартис Аг Ингибиторы аутотаксинов, содержащие гетероарил-бензил-амидное ядро
CA2927392C (en) 2013-10-17 2021-11-09 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
MY182095A (en) 2013-11-22 2021-01-18 Sabre Therapeutics Llc Autotaxin inhibitor compounds
AR098475A1 (es) 2013-11-26 2016-06-01 Bayer Cropscience Ag Compuestos pesticidas y usos
PE20160845A1 (es) 2013-11-26 2016-09-10 Hoffmann La Roche Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo
MX2016012540A (es) 2014-03-26 2017-01-09 Basf Se Compuestos de [1,2,4]triazol e imidazol sustituidos, como fungicidas.
HUE046820T2 (hu) 2014-03-26 2020-03-30 Hoffmann La Roche Biciklusos vegyületek autotaxin (ATX) és lizofoszfatidsav (LPA) termelésgátlókként
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
AP2016009496A0 (en) 2014-04-04 2016-10-31 X-Rx Inc Substituted spirocydic inhibitors of autotaxin
JP6632532B2 (ja) 2014-08-29 2020-01-22 国立大学法人 東京大学 オートタキシン阻害活性を有するピリミジノン誘導体
CN107074852B (zh) 2014-10-14 2019-08-16 生命医药有限责任公司 ROR-γ的二氢吡咯并吡啶抑制剂
EA033497B1 (ru) 2015-02-15 2019-10-31 Hoffmann La Roche 1-(тиофенил или фенил)сульфонил-(пирролидин)-2-карбоксамидные производные и их применение в качестве антагонистов trpa1
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CN104927727B (zh) 2015-07-06 2017-01-11 香山红叶建设有限公司 一种玻璃幕墙用结构密封胶及其制备方法
MX377277B (es) 2015-09-04 2025-03-07 Hoffmann La Roche Derivados de fenoximetilo.
PL415078A1 (pl) 2015-09-04 2017-03-13 Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków
BR112018006034A2 (pt) 2015-09-24 2018-10-09 Hoffmann La Roche compostos bicíclicos como inibidores de atx
MA42923A (fr) 2015-09-24 2021-04-28 Hoffmann La Roche Composés bicycliques comme inhibiteurs mixtes de atx/ca
RU2725138C2 (ru) 2015-09-24 2020-06-30 Ф. Хоффманн-Ля Рош Аг Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca)
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
HK1251624A1 (zh) 2015-09-24 2019-02-01 Ionis Pharmaceuticals, Inc. Kras表达的调节剂
WO2017087858A1 (en) 2015-11-20 2017-05-26 Abide Therapeutics, Inc. Pyrazole compounds and methods of making and using same
US10323038B2 (en) 2015-11-20 2019-06-18 Abide Therapeutics, Inc. Pyrazole compounds and methods of making and using same
SG10201913450PA (en) 2015-11-25 2020-03-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
CN108290858B (zh) 2015-12-01 2021-07-06 日本农药株式会社 3h-吡咯并吡啶化合物或其n-氧化物、或它们的盐类及含有该化合物的农业园艺用杀虫剂及其使用方法
WO2017139978A1 (zh) 2016-02-19 2017-08-24 吴伟东 手机app更新方法及系统
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
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
ES2747768T3 (es) 2017-03-20 2020-03-11 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)

Also Published As

Publication number Publication date
SI2970256T1 (sl) 2020-02-28
JP6483034B2 (ja) 2019-03-13
IL240796A0 (en) 2015-10-29
BR112015022804A2 (pt) 2017-07-18
EA035015B1 (ru) 2020-04-17
DK2970256T3 (da) 2020-01-06
US10913745B2 (en) 2021-02-09
KR20150126036A (ko) 2015-11-10
HK1211935A1 (en) 2016-06-03
HUE046776T2 (hu) 2020-03-30
US20150376194A1 (en) 2015-12-31
WO2014139978A1 (en) 2014-09-18
AU2014230943A1 (en) 2015-08-27
CL2015002386A1 (es) 2016-03-04
US20180258095A1 (en) 2018-09-13
CN105073748A (zh) 2015-11-18
EP2970256A1 (en) 2016-01-20
TW201522333A (zh) 2015-06-16
JP2016510780A (ja) 2016-04-11
EP2970256B1 (en) 2019-10-23
JP2019089828A (ja) 2019-06-13
AU2014230943B8 (en) 2016-12-15
UA115354C2 (uk) 2017-10-25
MA38432B1 (fr) 2017-09-29
RS59682B1 (sr) 2020-01-31
PL2970256T3 (pl) 2020-04-30
ZA201505944B (en) 2020-02-26
IL240796B (en) 2019-07-31
CN105073748B (zh) 2018-06-01
TWI678368B (zh) 2019-12-01
ES2763417T3 (es) 2020-05-28
MA38432A1 (fr) 2017-01-31
MY177574A (en) 2020-09-21
PH12015501934A1 (en) 2016-01-11
HRP20192274T1 (hr) 2020-03-06
MX2015011311A (es) 2015-12-03
SG11201507396YA (en) 2015-10-29
EA201591497A1 (ru) 2015-12-30
AR095079A1 (es) 2015-09-16
LT2970256T (lt) 2020-01-10
CR20150436A (es) 2015-09-16
CA2901047A1 (en) 2014-09-18
MX373247B (es) 2020-05-12
PH12015501934B1 (en) 2016-01-11
NZ711002A (en) 2020-09-25
PT2970256T (pt) 2020-01-06
AU2014230943B2 (en) 2016-12-01

Similar Documents

Publication Publication Date Title
PE20151605A1 (es) Nuevos derivados de octahidro-pirrolo[3,4-c]-pirrol y analogos de los mismos como inhibidores de autotaxina
PE20151448A1 (es) Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
CR20160076A (es) NUEVOS DERIVADOS DE TRIAZOLO[4,5-d]PIRIMIDINA
CO6491116A2 (es) Derivados de 5-fluoropirimidinona
CO2018002063A2 (es) Análogos novedosos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5
CO6592042A2 (es) Derivados de n3-sustituido -n1-sulfonil-5-fluorpirimidinona
CR20150378A (es) Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas
PH12016500643B1 (en) NEW OCTAHYDRO-CYCLOBUTA [1,2-c;3,4-c'] DIPYRROL-2-YL
MX2015003538A (es) Derivados de 3-fenilisoxazolina con accion herbicida.
CR20130671A (es) Antagonistas de trpv4
UA112061C2 (uk) Активуючі ampk гетероциклічні сполуки і способи їх використання
PE20142456A1 (es) COMPUESTOS DE OXAZOLIDIN-2-ONA Y USOS DE LOS MISMOS COMO INHIBIDORES DE LA PI3Ks
UY33337A (es) DERIVADOS SUSTITUIDOS DE 1H-PIRAZOL[ 3,4-d]PIRIMIDINA COMO INHIBIDORES DE LAS FOSFOINOSITIDA 3-QUINASAS
PE20170438A1 (es) Inhibidores espirociclicos de catepsina c
MX354021B (es) Derivados de 5-fluor-4-imino-3- (sustituido) -3,4-dihidropirimidin -2 (1h) ona.
CO6491087A2 (es) Compuestos de urea que contienen heteroarilo 5,6 bicíclicos como inhibidores de quinasa
MX2019013979A (es) Metodos para la preparacion de compuestos heterociclicos de 1,3-benzodioxol.
ECSP12011651A (es) Derivados de 5-fluoro-2-oxopirimidina-1(2h)-carboxilato
ECSP12011652A (es) Derivados de 5-fluoro-2-oxopirimidinona-1 (2h)-carboxamida substituida-n1
CR20160070A (es) Compuestos de triazolopiridina, composiciones y métodos de uso de los mismos
CR20150555A (es) Nuevos derivados de pirrolo[2,3-d]pirimidina
CR20150511A (es) Nuevos derivados de purina
CO2018011231A2 (es) Derivados de [1,2,3]triazolo[4,5-d]pirimidina con afinidad por los receptores canabinoides tipo-2
CR20150080A (es) Derivados y analogos de n-etilquinolonas y n-etilazaquinolonas
ECSP12012047A (es) Derivados de 2-aldoximino-5-fluoropirimidina

Legal Events

Date Code Title Description
FG Grant, registration