TWI609018B - 新穎雙環衍生物 - Google Patents

新穎雙環衍生物 Download PDF

Info

Publication number
TWI609018B
TWI609018B TW102134348A TW102134348A TWI609018B TW I609018 B TWI609018 B TW I609018B TW 102134348 A TW102134348 A TW 102134348A TW 102134348 A TW102134348 A TW 102134348A TW I609018 B TWI609018 B TW I609018B
Authority
TW
Taiwan
Prior art keywords
carbonyl
pyrrolo
substituted
hexahydro
pyrrole
Prior art date
Application number
TW102134348A
Other languages
English (en)
Chinese (zh)
Other versions
TW201422618A (zh
Inventor
傑若米 賀特
丹尼爾 杭基克
帕雷茲歐 麥堤
哈洛德 毛瑟
唐國志
王利莎
Original Assignee
赫孚孟拉羅股份公司
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 赫孚孟拉羅股份公司 filed Critical 赫孚孟拉羅股份公司
Publication of TW201422618A publication Critical patent/TW201422618A/zh
Application granted granted Critical
Publication of TWI609018B publication Critical patent/TWI609018B/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW102134348A 2012-09-25 2013-09-24 新穎雙環衍生物 TWI609018B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12185941 2012-09-25

Publications (2)

Publication Number Publication Date
TW201422618A TW201422618A (zh) 2014-06-16
TWI609018B true TWI609018B (zh) 2017-12-21

Family

ID=47073290

Family Applications (1)

Application Number Title Priority Date Filing Date
TW102134348A TWI609018B (zh) 2012-09-25 2013-09-24 新穎雙環衍生物

Country Status (32)

Country Link
US (4) US20150353559A1 (https=)
EP (2) EP3590940B1 (https=)
JP (1) JP6285444B2 (https=)
KR (1) KR102179599B1 (https=)
CN (1) CN104684915B (https=)
AR (1) AR092645A1 (https=)
AU (1) AU2013322838B2 (https=)
BR (1) BR112015004111A2 (https=)
CA (1) CA2878442A1 (https=)
CL (1) CL2015000706A1 (https=)
CR (1) CR20150120A (https=)
DK (1) DK2900669T3 (https=)
EA (1) EA036630B1 (https=)
ES (1) ES2753163T3 (https=)
HR (1) HRP20191937T1 (https=)
HU (1) HUE045797T2 (https=)
IL (1) IL237126A (https=)
IN (1) IN2015DN00960A (https=)
LT (1) LT2900669T (https=)
MA (1) MA37940B1 (https=)
MX (1) MX368615B (https=)
PE (1) PE20150758A1 (https=)
PH (1) PH12015500263B1 (https=)
PL (1) PL2900669T3 (https=)
PT (1) PT2900669T (https=)
RS (1) RS59512B1 (https=)
SG (1) SG11201500572YA (https=)
SI (1) SI2900669T1 (https=)
TW (1) TWI609018B (https=)
UA (1) UA116547C2 (https=)
WO (1) WO2014048865A1 (https=)
ZA (1) ZA201500345B (https=)

Families Citing this family (51)

* 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
MX368615B (es) 2012-09-25 2019-10-09 Hoffmann La Roche Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos.
US9630945B2 (en) 2012-12-19 2017-04-25 Novartis Ag Autotaxin inhibitors
US9409895B2 (en) 2012-12-19 2016-08-09 Novartis Ag Autotaxin inhibitors
AR095079A1 (es) * 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
CA2917050A1 (en) * 2013-07-03 2015-01-08 Todd K. Jones Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof
AR097794A1 (es) 2013-09-26 2016-04-13 Mnemosyne Pharmaceuticals Inc Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b
EP3071561B1 (en) 2013-11-22 2021-03-24 Sabre Therapeutics LLC Autotaxin inhibitor compounds
DK3074400T3 (en) * 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
CA2937616A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
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)
US9051320B1 (en) 2014-08-18 2015-06-09 Pharmakea, Inc. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
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
CA2986759C (en) 2015-05-27 2025-06-17 Sabre Therapeutics Llc AUTOTAXIN INHIBITORS AND THEIR USES
AU2016270373A1 (en) 2015-06-05 2018-01-04 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
BR112017026682A2 (pt) * 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
AU2016328436B2 (en) * 2015-09-24 2020-05-14 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
JP6876685B2 (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 Atx阻害剤としての二環式化合物
CN106986789B (zh) * 2016-01-20 2019-07-16 中国人民解放军军事医学科学院生物医学分析中心 对苯二酚类化合物及其制备方法与在抗肿瘤或免疫调节中的应用
WO2017197192A1 (en) 2016-05-12 2017-11-16 Abide Therapeutics, Inc. Spirocycle compounds and methods of making and using same
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
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
US20200085791A1 (en) 2016-12-19 2020-03-19 Bayer Pharma Aktiengesellschaft [(phenylsulfonyl)octahydro-epiminoisoindol-yl](1h-1,2,3-triazol-5-yl)methanones
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
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
LT3483164T (lt) 2017-03-20 2020-05-11 Forma Therapeutics, Inc. Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai
JP7257387B2 (ja) 2017-08-29 2023-04-13 ハー・ルンドベック・アクチエゼルスカベット スピロ環化合物並びにその作製及び使用方法
CR20200088A (es) 2017-08-29 2020-04-08 Lundbeck La Jolla Research Center Inc Compuestos espirocíclicos y sus métodos de preparación y uso
KR20200074971A (ko) 2017-10-19 2020-06-25 제이에스 이노팜 (상하이) 리미티드 헤테로사이클릭 화합물, 헤테로사이클릭 화합물을 포함하는 조성물 및 그의 사용 방법
TWI780281B (zh) * 2017-12-14 2022-10-11 丹麥商Nmd藥品公司 用於治療神經肌肉病症的化合物
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
EP3853206B1 (en) 2018-09-19 2024-04-10 Novo Nordisk Health Care AG Treating sickle cell disease with a pyruvate kinase r activating compound
CN111620866A (zh) * 2019-02-27 2020-09-04 南京药石科技股份有限公司 一种顺式-7,7-二氟-六氢-1H 吡咯并[3,4-c]吡啶衍生物及其制备方法
HRP20251148T1 (hr) 2019-09-19 2025-11-21 Novo Nordisk Health Care Ag Pripravci koji aktiviraju piruvat-kinazu r (pkr)
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
TW202211918A (zh) * 2020-06-30 2022-04-01 印度商卡地拉保健有限公司 新穎奧特他新(autotaxin)抑制劑
TWI904281B (zh) 2020-11-13 2025-11-11 丹麥商H 朗德貝克公司 Magl抑制劑
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
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
CN113214111A (zh) * 2021-04-30 2021-08-06 上海立科化学科技有限公司 3-(2-氰基苯基)丙酸及4-氰基-1-茚满酮的制备方法
CA3225439A1 (en) * 2021-06-26 2022-12-29 Cedilla Therapeutics, Inc. Cdk2 inhibitors and methods of using the same
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
KR20250005229A (ko) 2022-05-04 2025-01-09 하. 룬드벡 아크티에셀스카브 모노아실글리세롤 리파제 억제제로서 1,1,1,3,3,3-헥사플루오로프로판-2-일 (s)-1-(피리다진-3-일카르바모일)-6 아자스피로[2.5]옥탄-6-카르복실레이트의 결정질 형태
CN116270625B (zh) * 2023-03-16 2025-06-24 宁夏医科大学 银柴胡胺b在制备抗神经炎性药物中的应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011006569A1 (de) * 2009-07-16 2011-01-20 Merck Patent Gmbh Heterocyclische verbindungen als autotaxin-inhibitoren
WO2012024620A2 (en) * 2010-08-20 2012-02-23 Amira Pharmaceuticals, Inc. Autotaxin inhibitors and uses thereof

Family Cites Families (123)

* 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
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
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
HRP20000495B1 (en) 1998-02-04 2005-12-31 Banyu Pharmaceutical Co. 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
ATE250604T1 (de) 1999-10-27 2003-10-15 Millennium Pharm Inc Pyridyl enthaltende spirocyclische verbindungen als inhibitoren der fibrinogen-abhängigen blutplättchen aggregation
CZ20021550A3 (cs) * 1999-11-09 2003-02-12 Societe De Conseils De Recherches Et D'application Produkt zahrnující inhibitor transdukce signálů heterotrimerického G proteinu kombinovaný s jiným protirakovinným činidlem pro terapeutické použití v léčbě rakoviny
EP1368354A1 (en) 2001-03-07 2003-12-10 Pfizer Products Inc. Modulators of chemokine receptor activity
AU2003223510B2 (en) 2002-04-12 2008-05-08 Merck Sharp & Dohme Corp. 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
US7435831B2 (en) * 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
US7435830B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
ATE382623T1 (de) * 2004-06-09 2008-01-15 Hoffmann La Roche Octahydropyrrolo(3,4-c)pyrrolderivate und deren verwendung als antivirale mitteln
US7923554B2 (en) 2004-08-10 2011-04-12 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
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
EP2657235A1 (en) 2005-10-28 2013-10-30 Ono Pharmaceutical Co., Ltd. Compound containing basic group and use thereof
CA2629530C (en) * 2005-11-14 2014-07-08 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services N-substituted indenoisoquinolines and syntheses 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
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
JP2008031064A (ja) 2006-07-27 2008-02-14 Astellas Pharma Inc ジアシルピペラジン誘導体
CN101600698B (zh) 2006-09-11 2012-01-11 欧加农股份有限公司;药典有限责任公司 喹唑啉酮和异喹啉酮乙酰胺衍生物
CA2663500A1 (en) 2006-09-15 2008-03-20 Schering Corporation Spiro-condensed azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism
US8735411B2 (en) 2006-10-02 2014-05-27 Abbvie Inc. Macrocyclic benzofused pyrimidine derivatives
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
WO2008119662A1 (en) 2007-03-29 2008-10-09 F. Hoffmann-La 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.
BRPI0810858A2 (pt) 2007-04-27 2014-10-29 Sanofi Aventis Derivados de 2-heteroaril-pirrolo[3,4-c] pirrol e seus usos como inibidores de scd
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
AR069126A1 (es) * 2007-10-31 2009-12-30 Janssen Pharmaceutica Nv Diaminas en puente o fusionadas sustituidas con arilo como moduladores de leucotrieno a4 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
JPWO2009154132A1 (ja) 2008-06-19 2011-12-01 Msd株式会社 スピロジアミン−ジアリールケトオキシム誘導体
US8673917B2 (en) 2008-09-09 2014-03-18 Sanofi 2-heteroaryl-pyrrolo [3,4-C]pyrrole derivatives, and use thereof as SCD inhibitors
TW201020247A (en) 2008-11-06 2010-06-01 Gruenenthal Gmbh Substituierte disulfonamide
CN102216273A (zh) 2008-11-17 2011-10-12 霍夫曼-拉罗奇有限公司 用作crth2拮抗剂或部分激动剂的萘乙酸
DE102008059578A1 (de) 2008-11-28 2010-06-10 Merck Patent Gmbh Benzo-Naphtyridin Verbindungen
CN102216299B (zh) 2008-12-01 2015-02-11 默克专利有限公司 作为自体毒素抑制剂的2,5-二氨基取代的吡啶并[4,3-d]嘧啶化合物
TW201035102A (en) 2009-03-04 2010-10-01 Gruenethal Gmbh Sulfonylated tetrahydroazolopyrazines and their use as medicinal products
TW201038572A (en) 2009-03-25 2010-11-01 Gruenenthal Gmbh Substituted spiro-amide compounds
EA201101399A1 (ru) 2009-04-02 2012-08-30 Мерк Патент Гмбх Гетероциклические соединения в качестве ингибиторов аутотаксина
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
MX2011010218A (es) * 2009-04-02 2011-10-10 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
BRPI1010974A2 (pt) 2009-05-22 2019-09-24 Exelixis Inc benzoxazepinas baseada em inibidores p13k/ m tor contra doenças proliferativas
US20120083476A1 (en) 2009-06-05 2012-04-05 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
CN102574822A (zh) 2009-08-04 2012-07-11 阿米拉制药公司 作为溶血磷脂酸受体拮抗剂的化合物
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
KR20120112755A (ko) * 2010-01-07 2012-10-11 이 아이 듀폰 디 네모아 앤드 캄파니 살진균제 복소환 화합물
WO2011115813A1 (en) 2010-03-18 2011-09-22 Abbott Laboratories Lactam acetamides as calcium channel blockers
DK2547679T3 (en) 2010-03-19 2016-01-11 Pfizer 2,3 dihydro-1H-inden-1-yl-2,7-diazaspiro [3.6] nonane derivatives and their use as antagonists or inverse agonists of ghrelin receptor
AU2011232058B2 (en) 2010-03-26 2016-09-08 Merck Patent Gmbh Benzonaphthyridinamines as autotaxin inhibitors
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
JP6039559B2 (ja) * 2010-09-02 2016-12-07 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 Lpa受容体アンタゴニストとしてのピラゾロピリジノン誘導体
WO2012080729A2 (en) 2010-12-14 2012-06-21 Electrophoretics Limited CASEIN KINASE 1δ (CK1δ) INHIBITORS
EP2714680B1 (en) 2011-05-27 2015-11-25 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
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
EP2800745B1 (en) 2011-12-02 2020-02-12 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 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
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
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
JP6324380B2 (ja) 2012-07-27 2018-05-16 バイオジェン・エムエイ・インコーポレイテッドBiogen MA Inc. S1p調節剤および/またはatx調節剤である化合物
TWI616430B (zh) 2012-07-27 2018-03-01 百健Ma公司 Atx調節劑
MX368615B (es) 2012-09-25 2019-10-09 Hoffmann La Roche Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos.
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
US20160002247A1 (en) 2013-03-01 2016-01-07 The University Of Tokyo 8-substituted imidazopyrimidinone derivative having autotaxin inhibitory activity
UY35395A (es) 2013-03-12 2014-10-31 Abbvie Inc Inhibidores de bromodominios tetracíclicos
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
CA2903483A1 (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
WO2014152725A1 (en) 2013-03-15 2014-09-25 Biogen Idec Ma Inc. S1p and/or atx modulating agents
AP2016009020A0 (en) 2013-07-18 2016-02-29 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
HRP20180804T1 (hr) 2013-10-17 2018-08-10 Vertex Pharmaceuticals Incorporated Inhibitori dnk-pk
EP3071561B1 (en) 2013-11-22 2021-03-24 Sabre Therapeutics LLC Autotaxin inhibitor compounds
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
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
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)
CA2937616A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
CU24442B1 (es) 2014-04-04 2019-09-04 X Rx Inc Derivados de n-(1-(espirocíclico)oxo) amida sustituidos como inhibidores de autotaxina
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
JP6700291B2 (ja) 2015-02-15 2020-05-27 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 1−(het)アリールスルホニル−(ピロリジン又はピペリジン)−2−カルボキサミド誘導体、及びtrpa1拮抗薬としてのそれらの使用
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
JP6876685B2 (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 Atx阻害剤としての二環式化合物
CN108513588A (zh) 2015-09-24 2018-09-07 Ionis制药公司 Kras表达的调节剂
BR112017026682A2 (pt) 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
AU2016328436B2 (en) 2015-09-24 2020-05-14 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
MX2018006499A (es) 2015-11-25 2018-08-01 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos.
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
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
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
LT3483164T (lt) 2017-03-20 2020-05-11 Forma Therapeutics, Inc. Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011006569A1 (de) * 2009-07-16 2011-01-20 Merck Patent Gmbh Heterocyclische verbindungen als autotaxin-inhibitoren
WO2012024620A2 (en) * 2010-08-20 2012-02-23 Amira Pharmaceuticals, Inc. Autotaxin inhibitors and uses thereof

Also Published As

Publication number Publication date
LT2900669T (lt) 2019-11-11
KR102179599B1 (ko) 2020-11-19
PT2900669T (pt) 2019-10-29
CN104684915B (zh) 2017-10-31
CR20150120A (es) 2015-04-14
HRP20191937T1 (hr) 2020-01-10
ZA201500345B (en) 2015-12-23
PL2900669T3 (pl) 2020-01-31
KR20150060713A (ko) 2015-06-03
US20200339570A1 (en) 2020-10-29
SG11201500572YA (en) 2015-02-27
SI2900669T1 (sl) 2019-12-31
JP2015531360A (ja) 2015-11-02
US10669268B2 (en) 2020-06-02
PH12015500263A1 (en) 2015-03-30
EP3590940A1 (en) 2020-01-08
CN104684915A (zh) 2015-06-03
EA201590534A1 (ru) 2015-07-30
MA37940A2 (fr) 2016-06-30
MX2015002090A (es) 2015-05-11
EP2900669A1 (en) 2015-08-05
DK2900669T3 (da) 2019-11-04
AU2013322838B2 (en) 2018-02-01
HK1206722A1 (en) 2016-01-15
AR092645A1 (es) 2015-04-29
RS59512B1 (sr) 2019-12-31
PH12015500263B1 (en) 2022-06-17
EP2900669B1 (en) 2019-09-04
CA2878442A1 (en) 2014-04-03
UA116547C2 (uk) 2018-04-10
PE20150758A1 (es) 2015-05-15
BR112015004111A2 (pt) 2017-07-04
EP3590940B1 (en) 2021-06-09
TW201422618A (zh) 2014-06-16
WO2014048865A1 (en) 2014-04-03
HUE045797T2 (hu) 2020-01-28
US20150353559A1 (en) 2015-12-10
US20180118741A1 (en) 2018-05-03
IN2015DN00960A (https=) 2015-06-12
AU2013322838A1 (en) 2015-01-29
EA036630B1 (ru) 2020-12-02
JP6285444B2 (ja) 2018-02-28
MX368615B (es) 2019-10-09
ES2753163T3 (es) 2020-04-07
IL237126A (en) 2016-12-29
MA37940B1 (fr) 2018-09-28
CL2015000706A1 (es) 2015-08-07
US20170050960A1 (en) 2017-02-23

Similar Documents

Publication Publication Date Title
TWI609018B (zh) 新穎雙環衍生物
JP7041198B2 (ja) Jak阻害剤である5-クロロ-2-ジフルオロメトキシフェニルピラゾロピリミジン化合物
TWI678368B (zh) 新穎八氫-吡咯并[3,4-c]-吡咯及-吡啶苯基
CN110248939B (zh) 作为rho-激酶抑制剂的酪氨酸酰胺衍生物
TWI708774B (zh) 新穎雙環化合物
CN105814059B (zh) 作为tnf活性调节剂的咪唑并嘧啶衍生物
CN105814055B (zh) 作为tnf活性调节剂的稠合咪唑和吡唑衍生物
CN102573471B (zh) 新的吡咯烷衍生的β3肾上腺素受体激动剂
JP6496730B2 (ja) 新規なオクタヒドロ−シクロブタ[1,2−c;3,4−c’]ジピロール−2−イル
CN105814061B (zh) 作为tnf活性调节剂的咪唑并哒嗪衍生物
TW201718493A (zh) 作為magl抑制劑的胺基甲酸1,1,1-三氟-3-羥基丙烷-2-基酯衍生物及胺基甲酸1,1,1-三氟-4-羥基丁烷-2-基酯衍生物
TWI833819B (zh) 用於治療與apj受體活性相關的病狀的化合物及組成物
TWI899220B (zh) 作為trpv4拮抗劑之嘧啶-4(3h)-酮衍生物
HK1206722B (en) New bicyclic derivatives
HK40078094B (zh) 作为trpv4拮抗剂的嘧啶-4(3h)-酮衍生物
HK40078094A (en) Pyrimidin-4(3h)-one derivatives as trpv4 antagonists
HK40060283B (zh) 氨基嗪醯胺
HK40008746B (zh) 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物
HK1223921B (zh) 新的八氢-环丁二烯并[1,2-c;3,4-c’]二吡咯-2基
HK1211935B (en) New octahydro-pyrrolo[3,4-c]-pyrrole derivatives and analogs thereof as autotaxin inhibitors
HK1227397B (zh) 化为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees