JP6845230B2 - デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物 - Google Patents

デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物 Download PDF

Info

Publication number
JP6845230B2
JP6845230B2 JP2018515621A JP2018515621A JP6845230B2 JP 6845230 B2 JP6845230 B2 JP 6845230B2 JP 2018515621 A JP2018515621 A JP 2018515621A JP 2018515621 A JP2018515621 A JP 2018515621A JP 6845230 B2 JP6845230 B2 JP 6845230B2
Authority
JP
Japan
Prior art keywords
substituted
alkyl
alkoxy
pyrrole
trans
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2018515621A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018528244A5 (cg-RX-API-DMAC7.html
JP2018528244A (ja
Inventor
ヘルト，イェロム
フンツィカー，ダニエル
マタイ，パトリツィオ
ルドルフ，マルクス
シュミッツ，ペトラ
ウルマー，クリストフ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2018528244A publication Critical patent/JP2018528244A/ja
Publication of JP2018528244A5 publication Critical patent/JP2018528244A5/ja
Application granted granted Critical
Publication of JP6845230B2 publication Critical patent/JP6845230B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
JP2018515621A 2015-09-24 2016-09-20 デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物 Active JP6845230B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15186642 2015-09-24
EP15186642.3 2015-09-24
PCT/EP2016/072277 WO2017050747A1 (en) 2015-09-24 2016-09-20 New bicyclic compounds as dual atx/ca inhibitors

Publications (3)

Publication Number Publication Date
JP2018528244A JP2018528244A (ja) 2018-09-27
JP2018528244A5 JP2018528244A5 (cg-RX-API-DMAC7.html) 2019-10-24
JP6845230B2 true JP6845230B2 (ja) 2021-03-17

Family

ID=54199040

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018515621A Active JP6845230B2 (ja) 2015-09-24 2016-09-20 デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物

Country Status (19)

Country Link
US (2) US10738053B2 (cg-RX-API-DMAC7.html)
EP (1) EP3353181B1 (cg-RX-API-DMAC7.html)
JP (1) JP6845230B2 (cg-RX-API-DMAC7.html)
KR (1) KR20180053408A (cg-RX-API-DMAC7.html)
CN (1) CN107614505B (cg-RX-API-DMAC7.html)
AR (1) AR106100A1 (cg-RX-API-DMAC7.html)
AU (1) AU2016328365B2 (cg-RX-API-DMAC7.html)
BR (1) BR112017026682A2 (cg-RX-API-DMAC7.html)
CA (1) CA2984585A1 (cg-RX-API-DMAC7.html)
CL (1) CL2018000649A1 (cg-RX-API-DMAC7.html)
CO (1) CO2017011152A2 (cg-RX-API-DMAC7.html)
CR (1) CR20180143A (cg-RX-API-DMAC7.html)
IL (1) IL255511B (cg-RX-API-DMAC7.html)
MX (1) MX2017015034A (cg-RX-API-DMAC7.html)
PE (1) PE20180233A1 (cg-RX-API-DMAC7.html)
PH (1) PH12018500409A1 (cg-RX-API-DMAC7.html)
RU (1) RU2725138C2 (cg-RX-API-DMAC7.html)
TW (1) TW201725206A (cg-RX-API-DMAC7.html)
WO (1) WO2017050747A1 (cg-RX-API-DMAC7.html)

Families Citing this family (16)

* 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
ES2753163T3 (es) 2012-09-25 2020-04-07 Hoffmann La Roche Derivados de hexahidropirrolo[3,4-c]pirrol y compuestos relacionados como inhibidores de la autotaxina (ATX) y como inhibidores de la producción de ácido lisofosfatídico (LPA) para tratar, por ejemplo, enfermedades renales
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
CA2923523A1 (en) 2013-11-26 2015-06-04 F. Hoffmann-La Roche Ag New octahydro-cyclobuta [1,2-c;3,4-c']dipyrrol-2-yl
JP6554481B2 (ja) 2014-03-26 2019-07-31 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ オートタキシン（ａｔｘ）及びリゾホスファチジン酸（ｌｐａ）産生の阻害剤としての縮合［１，４］ジアゼピン化合物
SG11201607839UA (en) 2014-03-26 2016-10-28 Hoffmann La Roche Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
EP3353181B1 (en) 2015-09-24 2021-08-11 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
JP6877413B2 (ja) 2015-09-24 2021-05-26 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 二重ａｔｘ／ｃａ阻害剤としての新規な二環式化合物
CA2983782A1 (en) * 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
WO2017050792A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
DK4003978T3 (da) 2019-07-22 2024-07-22 Boehringer Ingelheim Int N-methyl, n-(6-(methoxy)pyridazin-3-yl) aminderivater som autotaxin (atx) modulatorer til behandlingen af inflammatoriske luftvejs- eller fibrotiske sygdomme
JP2024502337A (ja) 2021-01-05 2024-01-18 ザイダス ライフサイエンシズ リミティド オートタキシンの新規阻害剤

Family Cites Families (140)

* 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
WO1999040070A1 (en) 1998-02-04 1999-08-12 Banyu Pharmaceutical Co., Ltd. N-acyl cyclic amine derivatives
JP2001039950A (ja) 1999-07-30 2001-02-13 Banyu Pharmaceut Co Ltd Ｎ−アシル環状アミン誘導体
WO2001030780A2 (en) 1999-10-27 2001-05-03 Cor Therapeutics, Inc. Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
EP1368354A1 (en) 2001-03-07 2003-12-10 Pfizer Products Inc. Modulators of chemokine receptor activity
CA2481313A1 (en) 2002-04-12 2003-10-23 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
JP4845873B2 (ja) 2004-03-03 2011-12-28 ケモセントリックス インコーポレーティッド 二環式および架橋した窒素複素環
WO2005121145A2 (en) 2004-06-09 2005-12-22 F. Hoffmann-La Roche Ag Octahydro-pyrrolo[3,4-c] derivatives and their use as antiviral compounds
ES2442857T3 (es) 2004-08-10 2014-02-13 Janssen Pharmaceutica Nv Derivados de 1,2,4-triazin-6-ona inhibidores de VIH
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
US8318931B2 (en) 2005-10-28 2012-11-27 Ono Pharmaceutical Co., Ltd. Chemokine receptor antagonists and use thereof
EP1961744B1 (en) 2005-11-18 2013-04-17 Ono Pharmaceutical Co., Ltd. Basic group-containing compound and use thereof
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
WO2007103719A2 (en) 2006-03-03 2007-09-13 Incyte Corporation MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
JP2008001743A (ja) 2006-06-20 2008-01-10 Bridgestone Corp トレッド用ゴム組成物及びそれを用いたタイヤ
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
CN101541795A (zh) 2006-09-15 2009-09-23 先灵公司 用于治疗疼痛、糖尿病和脂类代谢紊乱的螺-稠合氮杂环丁烷衍生物
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
EP2142520A1 (en) 2007-03-29 2010-01-13 F. Hoffmann-Roche AG Non-nucleoside reverse transcriptase inhibitors
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.
JP2010524987A (ja) 2007-04-27 2010-07-22 サノフィ−アベンティス ２−ヘテロアリール−ピロロ［３，４−ｃ］ピロール誘導体及びｓｃｄ阻害剤としてのそれらの使用
UA99626C2 (ru) * 2007-08-07 2012-09-10 Эбботт Гмбх Унд Ко. Кг Соединения хинолина, пригодные для лечения нарушений, реагирующих на модуляцию рецептора 5-нт6 серотонина
DE102007047737A1 (de) 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
MX2010004281A (es) 2007-10-19 2010-09-10 Sarcode Corp Composiciones y metodos para el tratamiento de la retinopatia diabetica.
TW200932236A (en) 2007-10-31 2009-08-01 Janssen Pharmaceutica Nv Aryl-substituted bridged diamines as modulators of leukotriene A4 hydrolase
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
CA2739725A1 (en) 2008-11-17 2010-05-20 F. Hoffmann-La Roche Ag Naphthylacetic acids used as crth2 antagonists or partial agonists
DE102008059578A1 (de) 2008-11-28 2010-06-10 Merck Patent Gmbh Benzo-Naphtyridin Verbindungen
AU2009321867B2 (en) 2008-12-01 2015-12-10 Merck Patent Gmbh 2,5-Diamino-substituted pyrido[4,3-d]pyrimidines as autotaxin inhibitors against cancer
TW201035102A (en) 2009-03-04 2010-10-01 Gruenethal Gmbh Sulfonylated tetrahydroazolopyrazines and their use as medicinal products
ES2617191T3 (es) 2009-03-05 2017-06-15 Daiichi Sankyo Company, Limited Derivado de piridina como inhibidor de PPARY
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
JP5591318B2 (ja) 2009-04-02 2014-09-17 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 オートタキシン阻害剤としてのピペリジンおよびピペラジン誘導体
CN102369195B (zh) 2009-04-02 2014-04-16 默克专利有限公司 自分泌运动因子抑制剂
BRPI1009800A2 (pt) 2009-04-02 2016-03-15 Merck Patent Gmbh compostos heterocíclicos como inibidores 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
KR20120034666A (ko) 2009-05-22 2012-04-12 엑셀리시스, 인코포레이티드 증식성 질환에 대한 벤족사제핀 기반 ｐ１３ｋ／ｍｔ０ｒ의 억제제
WO2010141817A1 (en) 2009-06-05 2010-12-09 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
WO2011017350A2 (en) 2009-08-04 2011-02-10 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
WO2011085170A1 (en) 2010-01-07 2011-07-14 E. I. Du Pont De Nemours And Company Fungicidal heterocyclic compounds
WO2011115813A1 (en) 2010-03-18 2011-09-22 Abbott Laboratories Lactam acetamides as calcium channel blockers
KR101455917B1 (ko) 2010-03-19 2014-11-03 화이자 인코포레이티드 2,3-디히드로-1h-인덴-1-일-2,7-디아자스피로[3.5]노난 유도체 및 그렐린 수용체의 길항제 또는 역 작용제로서의 그 용도
ES2562183T3 (es) 2010-03-26 2016-03-02 Merck Patent Gmbh Benzonaftiridinaminas como inhibidores de la autotaxina
GB201008005D0 (en) 2010-05-13 2010-06-30 Sentinel Oncology Ltd Pharmaceutical compounds
WO2011151461A2 (en) 2010-06-04 2011-12-08 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
US8999985B2 (en) 2010-12-02 2015-04-07 Shanghai De Novo Pharmatech Co Ltd. Substituted phthalazin-1(2H)-ones, preparation processes and medical uses thereof
JP2014503528A (ja) 2010-12-14 2014-02-13 エレクトロプホレトイクス リミテッド カゼインキナーゼ１δ（ＣＫ１δ）阻害剤及びタウオパチーなどの神経変性疾患の治療におけるその使用
US9260416B2 (en) 2011-05-27 2016-02-16 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
ES2609579T3 (es) 2011-08-29 2017-04-21 VIIV Healthcare UK (No.5) Limited Derivados espiro de diamina bicíclica como inhibidores de la unión del VIH
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
CA2856946C (en) 2011-12-02 2016-08-02 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rory, nr1f3) activity and for the treatment of chronic inflammatory and autoimmunediseases
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
EP3495367B1 (en) 2012-06-13 2020-09-30 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
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
RU2665462C2 (ru) 2012-06-27 2018-08-30 Ф. Хоффманн-Ля Рош Аг Соединения 5-азаиндазола и способы их применения
MY171486A (en) 2012-07-27 2019-10-15 Biogen Ma Inc Atx modulating agents
MX362346B (es) 2012-07-27 2019-01-11 Biogen Ma Inc Compuestos que son agentes moduladores de s1p y/o agentes moduladores de autotaxina.
AR092211A1 (es) * 2012-09-24 2015-04-08 Merck Patent Ges Mit Beschränkter Haftung Derivados de hidropirrolopirrol
ES2753163T3 (es) * 2012-09-25 2020-04-07 Hoffmann La Roche Derivados de hexahidropirrolo[3,4-c]pirrol y compuestos relacionados como inhibidores de la autotaxina (ATX) y como inhibidores de la producción de ácido lisofosfatídico (LPA) para tratar, por ejemplo, enfermedades renales
MY183969A (en) 2012-09-25 2021-03-17 Bayer Pharma AG Combination of regorafenib and acetylsalicylic acid for treating cancer
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
AU2013334236B2 (en) 2012-10-25 2018-04-05 Tetra Discovery Partners, Llc. Heteroaryl inhibitors of PDE4
WO2014102817A1 (en) 2012-12-31 2014-07-03 Cadila Healthcare Limited Substituted phthalazin-1 (2h)-one derivatives as selective inhibitors of poly (adp-ribose) polymerase-1
JPWO2014133112A1 (ja) 2013-03-01 2017-02-02 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
CA2903910C (en) 2013-03-12 2023-08-15 Steven D. FIDANZE Triazadibenzo[cd,f]azulene derivatives and pharmaceutical compositions thereof useful as bromodomain inhibitors
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
US9133154B2 (en) 2013-03-12 2015-09-15 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
TW201446768A (zh) 2013-03-15 2014-12-16 Biogen Idec Inc S1p及/或atx調節劑
WO2014179564A1 (en) 2013-05-01 2014-11-06 Vitae Pharmaceuticals, Inc. Thiazalopyrrolidine inhibitors of ror-gamma
AP2016009020A0 (en) 2013-07-18 2016-02-29 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
WO2015058031A1 (en) 2013-10-17 2015-04-23 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
EP3878848A1 (en) 2013-11-22 2021-09-15 Sabre Therapeutics LLC Autotaxin inhibiting indole compounds
AR098475A1 (es) 2013-11-26 2016-06-01 Bayer Cropscience Ag Compuestos pesticidas y usos
CA2923523A1 (en) 2013-11-26 2015-06-04 F. Hoffmann-La Roche Ag New octahydro-cyclobuta [1,2-c;3,4-c']dipyrrol-2-yl
JP6554481B2 (ja) 2014-03-26 2019-07-31 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ オートタキシン（ａｔｘ）及びリゾホスファチジン酸（ｌｐａ）産生の阻害剤としての縮合［１，４］ジアゼピン化合物
CN106132935A (zh) 2014-03-26 2016-11-16 巴斯夫欧洲公司 作为杀真菌剂的取代的[1,2,4]三唑和咪唑化合物
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
SG11201607839UA (en) * 2014-03-26 2016-10-28 Hoffmann La Roche Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
MD20160116A2 (ro) 2014-04-04 2017-04-30 X-Rx Discovery, Inc Inhibitori spirociclici substituiţi ai autotaxinei
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
EA031967B1 (ru) 2014-10-14 2019-03-29 Вайтаи Фармасьютиклз, Инк. ДИГИДРОПИРРОЛОПИРИДИНОВЫЕ ИНГИБИТОРЫ ROR-γ
CR20170367A (es) 2015-02-15 2017-09-12 Hoffmann La Roche Derivados de 1-(het)arilsulfonil-(pirrolidin o piperidin)-2-carboxamida y su uso como antagonistas de 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
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
PL415078A1 (pl) 2015-09-04 2017-03-13 Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków
WO2017050792A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
EP3353181B1 (en) 2015-09-24 2021-08-11 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
RU2018113709A (ru) 2015-09-24 2019-10-30 Айонис Фармасьютикалз, Инк. Модуляторы экспрессии kras
CA2983782A1 (en) * 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
JP6877413B2 (ja) * 2015-09-24 2021-05-26 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 二重ａｔｘ／ｃａ阻害剤としての新規な二環式化合物
US10385057B2 (en) * 2015-11-20 2019-08-20 Lundbeck La Jolla Research Center, 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
BR112018009798A8 (pt) 2015-11-25 2019-02-26 Dana Farber Cancer Inst Inc inibidores de bromodomínio bivalentes e usos dos mesmos
MX2018005222A (es) 2015-12-01 2019-04-29 Nihon Nohyaku Co Ltd Compuesto de 3h-pirrolopiridina, n-óxido o sal del mismo, insecticida agrícola y hortícola que comprende el compuesto y método para usar los mismos.
WO2017139978A1 (zh) 2016-02-19 2017-08-24 吴伟东 手机app更新方法及系统
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
ES2788856T3 (es) 2017-03-20 2020-10-23 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)

Also Published As

Publication number Publication date
WO2017050747A1 (en) 2017-03-30
RU2018114518A (ru) 2019-10-28
EP3353181A1 (en) 2018-08-01
MX2017015034A (es) 2018-04-13
BR112017026682A2 (pt) 2018-08-14
CR20180143A (es) 2018-05-03
AU2016328365B2 (en) 2020-04-23
KR20180053408A (ko) 2018-05-21
US20200291038A1 (en) 2020-09-17
TW201725206A (zh) 2017-07-16
CL2018000649A1 (es) 2018-08-17
US10889588B2 (en) 2021-01-12
JP2018528244A (ja) 2018-09-27
AR106100A1 (es) 2017-12-13
RU2018114518A3 (cg-RX-API-DMAC7.html) 2020-01-09
US20180208601A1 (en) 2018-07-26
CN107614505B (zh) 2021-05-07
AU2016328365A1 (en) 2017-11-09
US10738053B2 (en) 2020-08-11
PH12018500409A1 (en) 2018-08-29
CA2984585A1 (en) 2017-03-30
PE20180233A1 (es) 2018-01-31
IL255511B (en) 2020-01-30
CO2017011152A2 (es) 2018-03-28
CN107614505A (zh) 2018-01-19
HK1246788A1 (zh) 2018-09-14
IL255511A (en) 2018-01-31
RU2725138C2 (ru) 2020-06-30
EP3353181B1 (en) 2021-08-11

Similar Documents

Publication Publication Date Title
JP6845230B2 (ja) デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物
JP6846414B2 (ja) Ａｔｘ阻害剤としての二環式化合物
JP6877413B2 (ja) 二重ａｔｘ／ｃａ阻害剤としての新規な二環式化合物
JP6876685B2 (ja) Ａｔｘ阻害剤としての二環式化合物
JP7090099B2 (ja) Ａｔｘインヒビターとしての新規二環式化合物
JP2017508774A (ja) オートタキシン（ａｔｘ）及びリゾホスファチジン酸（ｌｐａ）生成阻害剤としての二環式化合物
HK40073915A (en) Bicyclic compounds as atx inhibitors
HK1246788B (zh) 作为双重atx/ca抑制剂的新型二环化合物
HK1252995B (zh) 新的作为双重atx/ca抑制剂的二环化合物
HK1246787B (en) Bicyclic compounds as atx inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190913

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190913

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20200722

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20200811

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20201016

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20210202

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20210225

R150 Certificate of patent or registration of utility model

Ref document number: 6845230

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250