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PE20180461A1 - Nuevos compuestos biciclicos como inhibidores de la atx - Google Patents

Nuevos compuestos biciclicos como inhibidores de la atx

Info

Publication number
PE20180461A1
PE20180461A1 PE2017002776A PE2017002776A PE20180461A1 PE 20180461 A1 PE20180461 A1 PE 20180461A1 PE 2017002776 A PE2017002776 A PE 2017002776A PE 2017002776 A PE2017002776 A PE 2017002776A PE 20180461 A1 PE20180461 A1 PE 20180461A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibitors
new bicycle
compounds
trifluoromethoxybenzyl
Prior art date
Application number
PE2017002776A
Other languages
English (en)
Inventor
Giorgio Patrick Di
Jerôme Hert
Daniel Hunziker
Patrizio Mattei
Markus Rudolph
Petra Schmitz
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 PE20180461A1 publication Critical patent/PE20180461A1/es

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se refiere a un compuesto de formula I, en donde: R1 es fenilo sustituido, (fenilo sustituido)-alquilo C1-C6, (fenoxi sustituido)-alquilo C1-C6, entre otros; Y es -OC(O)- o -C(O)-; W es C(O), S(O)2 o CR6R7; R2 es un sistema de anillos; R9 es halogeno, alquilo C1-C6 o alcoxi C1-C6 y m, n, p y q son, con independencia, 1 y 2. Un compuesto preferido es trans-5-(1H-benzotriazol-5-carbonil)-3a-fluor-hexahidro-pirrolo[3,4-c]pirrol-2-carboxilato de 4-trifluormetoxibencilo, trans-5-(1H-benzotriazol-5-carbonil)-3a-metoxi-hexahidro-pirrolo[3,4-c]pirrol-2-carboxilato de 4-trifluormetoxibencilo; entre otros. Estos compuestos son inhibidores de la autotaxina (ATX), por lo que son inhibidores de la produccion de acido lisofosfatidico (LPA) y se emplean en el tratamiento de enfermedades del sistema respiratorio, cardiovascular, cancer, entre otras
PE2017002776A 2015-09-24 2016-09-20 Nuevos compuestos biciclicos como inhibidores de la atx PE20180461A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP15186645 2015-09-24

Publications (1)

Publication Number Publication Date
PE20180461A1 true PE20180461A1 (es) 2018-03-06

Family

ID=54199041

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002776A PE20180461A1 (es) 2015-09-24 2016-09-20 Nuevos compuestos biciclicos como inhibidores de la atx

Country Status (20)

Country Link
US (2) US20180208602A1 (es)
EP (1) EP3353180B1 (es)
JP (1) JP6846414B2 (es)
KR (1) KR20180054830A (es)
CN (2) CN107635995B (es)
AR (1) AR106101A1 (es)
AU (1) AU2016328535A1 (es)
BR (1) BR112018006024A2 (es)
CA (1) CA2983782A1 (es)
CL (1) CL2018000596A1 (es)
CO (1) CO2017011151A2 (es)
HK (1) HK1246787A1 (es)
IL (1) IL255570A (es)
MA (1) MA42918A (es)
MX (1) MX2018002217A (es)
PE (1) PE20180461A1 (es)
PH (1) PH12018500408A1 (es)
RU (1) RU2018114289A (es)
TW (1) TW201720824A (es)
WO (1) WO2017050732A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20150023373A (ko) 2012-06-13 2015-03-05 에프. 호프만-라 로슈 아게 신규한 다이아자스피로사이클로알칸 및 아자스피로사이클로알칸
AU2013322838B2 (en) 2012-09-25 2018-02-01 F. Hoffmann-La Roche Ag New bicyclic derivatives
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
DK3074400T3 (en) 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
MA50635A (fr) 2014-03-26 2020-08-12 Hoffmann La Roche Nouveaux composés bicycliques comme inhibiteurs de la production d'autotaxin (atx) et de l'acide lysophosphatidique
SG11201607845RA (en) 2014-03-26 2016-10-28 Hoffmann La Roche Condensed [1,4]diazepine 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
EP3344619B1 (en) 2015-09-04 2020-10-28 H. Hoffnabb-La Roche Ag Phenoxymethyl derivatives
MA42919A (fr) * 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
AU2016328365B2 (en) 2015-09-24 2020-04-23 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
EP3353180B1 (en) 2015-09-24 2022-03-16 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
CN108290887A (zh) 2015-12-10 2018-07-17 拜耳制药股份公司 用于治疗睡眠相关的呼吸病症的作为task-1和task-2通道阻断剂的2-苯基-3-(哌嗪子基甲基)咪唑并[1,2-a]吡啶衍生物
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ．ホフマン－ラ ロシュ アーゲー Ａｔｘインヒビターとしての新規二環式化合物
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
WO2018227427A1 (en) 2017-06-14 2018-12-20 Bayer Aktiengesellschaft Substituted bridged diazepane derivatives and use thereof
JOP20190284A1 (ar) 2017-06-14 2019-12-11 Bayer Pharma AG مركبات إيميدازوبيريميدين مستبدلة بديازا ثنائي الحلقة واستخدامها للمعالجة من اضطرابات التنفس

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
SK11402000A3 (sk) 1998-02-04 2001-03-12 Banyu Pharmaceutical Co., Ltd Cyklické n-acylaminoderiváty
JP2001039950A (ja) 1999-07-30 2001-02-13 Banyu Pharmaceut Co Ltd Ｎ−アシル環状アミン誘導体
DE60005545D1 (de) 1999-10-27 2003-10-30 Millennium Pharm Inc Pyridyl enthaltende spirocyclische verbindungen als inhibitoren der fibrinogen-abhängigen blutplättchen aggregation
EP1368354A1 (en) 2001-03-07 2003-12-10 Pfizer Products Inc. Modulators of chemokine receptor activity
WO2003086288A2 (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
EP1720545B1 (en) 2004-03-03 2014-10-29 ChemoCentryx, Inc. Bicyclic and bridged nitrogen heterocycles
BRPI0511982A (pt) 2004-06-09 2008-01-22 Hoffmann La Roche compostos antiviróticos heterocìclicos
CA2575002C (en) 2004-08-10 2015-01-20 Janssen Pharmaceutica N.V. Hiv inhibiting 1,2,4-triazin-6-one derivatives
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
BRPI0610433A2 (pt) 2005-04-28 2010-11-23 Wyeth Corp forma polimórfica ii de tanaproget, processos para preparar a mesma, e para preparar forma micronizada de um composto, composição farmacêutica, método de preparação de uma composição farmacêutica, e, uso da forma polimórfica ii de tanaproget ou da forma micronizada
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
EP1942108B1 (en) 2005-10-28 2013-09-04 Ono Pharmaceutical Co., Ltd. Compound containing basic group and use thereof
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
ATE523500T1 (de) 2006-09-11 2011-09-15 Organon Nv Chinazolinon- und isochinolinon-acetamid-derivate
WO2008033456A1 (en) 2006-09-15 2008-03-20 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
TWI405763B (zh) 2006-11-02 2013-08-21 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
BRPI0809617A2 (pt) 2007-03-29 2014-09-16 Hoffmann La Roche Inibidores não-nucleosídicos da transcriptase reversa
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.
WO2008135141A1 (de) 2007-04-27 2008-11-13 Sanofi-Aventis 2 -heteroaryl- pyrrolo [3, 4-c] pyrrol- 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
EP2209371B1 (en) 2007-10-19 2017-01-04 SARcode Bioscience Inc. Compositions and methods for treatment of diabetic retinopathy
US7935725B2 (en) 2007-10-31 2011-05-03 Janssen Pharmaceutica Nv Aryl-substituted bridged or fused 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
US20110071129A1 (en) 2008-06-19 2011-03-24 Makoto Ando Spirodiamine-diaryl ketoxime 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
US8188090B2 (en) 2008-11-17 2012-05-29 Hoffman-La Roche Inc. Naphthylacetic acids
DE102008059578A1 (de) 2008-11-28 2010-06-10 Merck Patent Gmbh Benzo-Naphtyridin Verbindungen
US8530650B2 (en) 2008-12-01 2013-09-10 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
SG172469A1 (en) 2009-03-05 2011-08-29 Daiichi Sankyo Co Ltd 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
AU2010230646B2 (en) 2009-04-02 2015-11-26 Merck Patent Gmbh Heterocyclic compounds as autotaxin inhibitors
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
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
FR2945534B1 (fr) 2009-05-12 2012-11-16 Sanofi Aventis DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
MX2011012345A (es) 2009-05-22 2012-01-31 Exelixis Inc Inhibidores de pi3k/mtor basados en benzoxazepinas contra enfermedades proliferativas.
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
IN2012DN00754A (es) 2009-08-04 2015-06-19 Amira Pharmaceuticals Inc
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
AU2011204323B2 (en) 2010-01-07 2013-12-12 E. I. Du Pont De Nemours And Company Fungicidal heterocyclic compounds
US8815869B2 (en) 2010-03-18 2014-08-26 Abbvie Inc. Lactam acetamides as calcium channel blockers
CN102939290B (zh) 2010-03-19 2015-09-16 辉瑞大药厂 2,3-二氢-1h-茚-1-基-2,7-二氮杂螺[3.5]壬烷衍生物及其作为生长激素释放肽受体的拮抗剂或反向激动剂的用途
US9029387B2 (en) 2010-03-26 2015-05-12 Merck Patent Gmbh Benzonaphthyridinamines as autotaxin inhibitors
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
US9000025B2 (en) 2010-08-20 2015-04-07 Amira Pharmaceuticals, Inc. Autotaxin inhibitors and uses thereof
WO2012028243A1 (en) 2010-09-02 2012-03-08 Merck Patent Gmbh Pyrazolopyridinone derivatives as lpa receptor antagonists
KR101528688B1 (ko) 2010-12-02 2015-06-12 상하이 드 노보 파마테크 컴퍼니 리미티드 헤테로사이클릭 유도체, 이의 제조 방법 및 이의 의학적 용도
DK2835131T3 (en) 2010-12-14 2017-12-04 Electrophoretics Ltd Casein kinase 1 delta inhibitors (CK1 delta)
WO2012166415A1 (en) 2011-05-27 2012-12-06 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
US8664213B2 (en) 2011-08-29 2014-03-04 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
WO2013065712A1 (ja) 2011-10-31 2013-05-10 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
KR20150023373A (ko) 2012-06-13 2015-03-05 에프. 호프만-라 로슈 아게 신규한 다이아자스피로사이클로알칸 및 아자스피로사이클로알칸
DK3176170T3 (en) 2012-06-13 2019-01-28 Incyte Holdings Corp SUBSTITUTED TRICYCLIC RELATIONS AS FGFR INHIBITORS
CA2871388A1 (en) 2012-06-27 2014-01-03 F. Hoffmann-La Roche Ag 5-azaindazole compounds and methods of use
ES2668694T3 (es) 2012-07-27 2018-05-21 Biogen Ma Inc. Derivados de ácido 1-[7-(cis-4-metil-ciclohexiloxi)-8-trifluorometil-naftalen-2-ilmetil]-piperidin-4-carboxílico como moduladores de autotaxina (ATX) para tratar inflamaciones y trastornos autoinmunitarios
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
BR112015006686B1 (pt) 2012-09-25 2022-04-05 Bayer Pharma Aktiengellschaft Combinação de regorafenib e ácido acetilsalicílico para tratamento de câncer coloretal
AU2013322838B2 (en) 2012-09-25 2018-02-01 F. Hoffmann-La Roche Ag New bicyclic derivatives
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
SG11201502050XA (en) 2012-10-25 2015-04-29 Tetra Discovery Partners Llc Heteroaryl inhibitors of pde4
MA38080A1 (fr) 2012-12-31 2018-02-28 Cadila Healthcare Ltd Dérivés substitués de phtalazin-1(2h)-one comme inhibiteurs sélectifs de la poly(adp-ribose) polymérase-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
US20160151369A1 (en) 2013-03-12 2016-06-02 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
KR102224992B1 (ko) 2013-03-12 2021-03-10 애브비 인코포레이티드 테트라사이클릭 브로모도메인 억제제
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
WO2014152725A1 (en) 2013-03-15 2014-09-25 Biogen Idec Ma Inc. S1p and/or atx modulating agents
PL3022202T3 (pl) 2013-07-18 2019-10-31 Novartis Ag Inhibitory autotaksyny zawierające heteroaromatyczny rdzeń pierścienia benzylowego - cyklicznego amidu
RS57306B1 (sr) 2013-10-17 2018-08-31 Vertex Pharma Inhibitori dnk-pk
JP6501367B2 (ja) 2013-11-22 2019-04-17 ファーマケア，インク． オートタキシン阻害剤化合物
AR098475A1 (es) 2013-11-26 2016-06-01 Bayer Cropscience Ag Compuestos pesticidas y usos
DK3074400T3 (en) 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
MA50635A (fr) 2014-03-26 2020-08-12 Hoffmann La Roche Nouveaux composés bicycliques comme inhibiteurs de la production d'autotaxin (atx) et de l'acide lysophosphatidique
SG11201607845RA (en) 2014-03-26 2016-10-28 Hoffmann La Roche Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
PL3122732T3 (pl) 2014-03-26 2018-08-31 Basf Se Podstawione związki [1,2,4]triazolowe i imidazolowe jako fungicydy
AU2015240519B2 (en) 2014-04-04 2019-08-15 X-Rx, Inc. Substituted spirocyclic inhibitors of autotaxin
EP3187492A4 (en) 2014-08-29 2018-05-09 The University of Tokyo Pyrimidinone derivative having autotaxin-inhibitory activity
JP6564029B2 (ja) 2014-10-14 2019-08-21 ヴァイティー ファーマシューティカルズ，エルエルシー Ｒｏｒ−ガンマのジヒドロピロロピリジン阻害剤
CA2975196A1 (en) 2015-02-15 2016-08-18 F. Hoffmann-La Roche Ag 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists
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
PL415078A1 (pl) 2015-09-04 2017-03-13 Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków
EP3344619B1 (en) 2015-09-04 2020-10-28 H. Hoffnabb-La Roche Ag Phenoxymethyl derivatives
EP3353180B1 (en) 2015-09-24 2022-03-16 F. Hoffmann-La Roche AG Bicyclic compounds as atx inhibitors
AU2016328365B2 (en) 2015-09-24 2020-04-23 F. Hoffmann-La Roche Ag New 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
MA42919A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
BR112018004620A2 (pt) 2015-09-24 2018-09-25 Ionis Pharmaceuticals, Inc. moduladores da expressão de kras
US10323038B2 (en) 2015-11-20 2019-06-18 Abide Therapeutics, Inc. Pyrazole compounds and methods of making and using same
WO2017087858A1 (en) 2015-11-20 2017-05-26 Abide Therapeutics, Inc. Pyrazole compounds and methods of making and using same
EP3380100A4 (en) 2015-11-25 2019-10-02 Dana-Farber Cancer Institute, Inc. BIVALENT BROMODOMAIN INHIBITORS AND USES THEREOF
WO2017094750A1 (ja) 2015-12-01 2017-06-08 日本農薬株式会社 ３ｈ‐ピロロピリジン化合物若しくはそのｎ‐オキサイド、又はそれらの塩類及び該化合物を含有する農園芸用殺虫剤並びにその使用方法
WO2017139978A1 (zh) 2016-02-19 2017-08-24 吴伟东 手机app更新方法及系统
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ．ホフマン－ラ ロシュ アーゲー Ａｔｘインヒビターとしての新規二環式化合物
DK3483164T3 (da) 2017-03-20 2020-03-23 Forma Therapeutics Inc Pyrrolopyrrolsammensætninger som pyruvatkinase (pkr) aktivatorer

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