PE20160546A1 - Compuestos derivados de piridilo biciclicos fusionados a anillo como inhibidores de fgfr4 - Google Patents

Compuestos derivados de piridilo biciclicos fusionados a anillo como inhibidores de fgfr4

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Publication number
PE20160546A1
PE20160546A1 PE2016000534A PE2016000534A PE20160546A1 PE 20160546 A1 PE20160546 A1 PE 20160546A1 PE 2016000534 A PE2016000534 A PE 2016000534A PE 2016000534 A PE2016000534 A PE 2016000534A PE 20160546 A1 PE20160546 A1 PE 20160546A1
Authority
PE
Peru
Prior art keywords
fgfr4
bicycle
inhibitors
ring
derived compounds
Prior art date
Application number
PE2016000534A
Other languages
English (en)
Inventor
Xianglin Zhao
Jing Xiong
Lv Liao
Sebastien Ripoche
Pierre Nimsgern
Robert Mah
Catherine Leblanc
Thomas Knopfel
Pascal Furet
Robin Alec Fairhurst
Nicole Buschmann
Can Wang
Bo Han
Original Assignee
Novartis 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 Novartis Ag filed Critical Novartis Ag
Publication of PE20160546A1 publication Critical patent/PE20160546A1/es

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    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)

Abstract

La presente invencion se refiere a un compuesto de la formula (I) que inhiben el FGFR4 para el tratamiento de cancer, particularmente el tratamiento de cancer hepatico. Donde: V es CH2, O, etc.; W es CH2, CH2CH2 o enlace; X es C(Rx) o N; Y es C(Rx) o N; Z es CH o N; Rx es hidrogeno, halogeno, etc.; Ry es hidrogeno, halogeno, etc.; R1 es es hidrogeno, halogeno, etc. Son compuestos preferidos N-(5-cianopiridin-2-il)-7-formil-3,4-dihidro-1,8-naftiridina-1-(2H)-carboxamida; N-(4,5-cloropiridin-2-il)-7-formil-3,4-dihidro-1,8-naftiridina-1-(2H)-carboxamida; entre otros.
PE2016000534A 2013-10-25 2014-10-24 Compuestos derivados de piridilo biciclicos fusionados a anillo como inhibidores de fgfr4 PE20160546A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2013086003 2013-10-25
CN2014088094 2014-10-03

Publications (1)

Publication Number Publication Date
PE20160546A1 true PE20160546A1 (es) 2016-05-26

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Country Status (27)

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US (3) US9266883B2 (es)
EP (1) EP3060563B1 (es)
JP (3) JP6203954B2 (es)
KR (1) KR101862493B1 (es)
CN (1) CN105683188B (es)
AP (1) AP2016009156A0 (es)
AU (1) AU2014338549B2 (es)
BR (1) BR112016008276B1 (es)
CA (1) CA2927252C (es)
CL (1) CL2016000922A1 (es)
CR (1) CR20160191A (es)
DO (1) DOP2016000094A (es)
EA (1) EA028819B1 (es)
ES (1) ES2682493T3 (es)
HK (1) HK1222388A1 (es)
IL (2) IL244819B (es)
MX (2) MX367723B (es)
NI (1) NI201600058A (es)
PE (1) PE20160546A1 (es)
PH (1) PH12016500756A1 (es)
PL (1) PL3060563T3 (es)
PT (1) PT3060563T (es)
SG (1) SG11201602183QA (es)
SV (1) SV2016005186A (es)
TN (1) TN2016000115A1 (es)
TR (1) TR201810944T4 (es)
WO (1) WO2015059668A1 (es)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101578235B1 (ko) 2007-12-10 2015-12-16 노파르티스 아게 유기 화합물
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
MX2014013373A (es) * 2012-05-15 2015-08-14 Novartis Ag Derivados de benzamida para inhibir la actividad de abl1, abl2 y bcr-abl1.
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
SG11201500125QA (en) 2012-07-11 2015-02-27 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
JP6449244B2 (ja) 2013-04-19 2019-01-09 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ抑制剤としての二環式複素環
US9434700B2 (en) 2013-10-25 2016-09-06 Neil Bifulco, JR. Inhibitors of the fibroblast growth factor receptor
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
CN107108672B (zh) 2014-10-03 2019-11-08 Ucb生物制药私人有限公司 稠合的五环咪唑衍生物
JP6585167B2 (ja) 2014-10-03 2019-10-02 ノバルティス アーゲー Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134320A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3273959A1 (en) * 2015-03-25 2018-01-31 Novartis Ag Pharmaceutical combinations
US9802917B2 (en) 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
KR20170114254A (ko) * 2016-03-24 2017-10-13 재단법인 대구경북첨단의료산업진흥재단 신규한 피리딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 fgfr 관련 질환의 예방 또는 치료용 약학적 조성물
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
JP7103952B2 (ja) * 2016-05-20 2022-07-20 江▲蘇▼豪森▲薬▼▲業▼集▲団▼有限公司 Ｆｇｆｒ４阻害剤、その製造方法及び応用
CA3024532C (en) 2016-05-20 2021-02-09 Zhejiang Hisun Pharmaceutical Co., Ltd. Pyrimidine derivative, method for preparing same and use thereof in medicine
CN111689959B (zh) * 2016-05-27 2022-04-01 石药集团中奇制药技术（石家庄）有限公司 作为fgfr4抑制剂的杂环化合物
CN107619388A (zh) 2016-07-13 2018-01-23 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
WO2018028664A1 (zh) * 2016-08-12 2018-02-15 江苏豪森药业集团有限公司 Fgfr4抑制剂及其制备方法和应用
WO2018049233A1 (en) * 2016-09-08 2018-03-15 Nicolas Stransky Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors
CN107840842A (zh) 2016-09-19 2018-03-27 北京天诚医药科技有限公司 炔代杂环化合物、其制备方法及其在医药学上的应用
WO2018055503A1 (en) 2016-09-20 2018-03-29 Novartis Ag Combination comprising a pd-1 antagonist and an fgfr4 inhibitor
EP3534902B1 (en) 2016-11-02 2022-11-23 Novartis AG Combinations of fgfr4 inhibitors and bile acid sequestrants
CN108264510A (zh) * 2017-01-02 2018-07-10 上海喆邺生物科技有限公司 一种选择性抑制激酶化合物及其用途
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3680236A4 (en) 2017-09-05 2021-04-21 Bioardis LLC AROMATIC DERIVATIVE, MANUFACTURING PROCESS FOR IT AND MEDICAL APPLICATION OF IT
WO2019057053A1 (zh) * 2017-09-20 2019-03-28 北京加科思益新药研发有限公司 用作fgfr4抑制剂的稠环衍生物
WO2019085927A1 (zh) * 2017-10-31 2019-05-09 江苏豪森药业集团有限公司 Fgfr4抑制剂的盐、晶体、制备方法及其用途
WO2019085860A1 (zh) * 2017-10-31 2019-05-09 江苏豪森药业集团有限公司 Fgfr4抑制剂晶型及其制备方法
CN109745321B (zh) * 2017-11-08 2022-04-29 上海翰森生物医药科技有限公司 包含fgfr4抑制剂的药物组合物
CN109928968B (zh) * 2017-12-15 2021-11-05 成都华健未来科技有限公司 一类制备抗癌药物的中间体
DK3788047T3 (da) 2018-05-04 2024-09-16 Incyte Corp Faste former af en FGFR-inhibitor og fremgangsmåder til fremstilling deraf
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
CN111285869A (zh) * 2018-07-05 2020-06-16 成都华健未来科技有限公司 脲类化合物的新型晶型产品及制备方法
CN111285871A (zh) * 2018-07-05 2020-06-16 成都华健未来科技有限公司 一种脲类化合物的新型晶型产品及制备方法
TWI723480B (zh) * 2018-07-27 2021-04-01 大陸商北京加科思新藥研發有限公司 用作fgfr4抑制劑的稠環衍生物
WO2020177067A1 (en) 2019-03-05 2020-09-10 Bioardis Llc Aromatic derivatives, preparation methods, and medical uses thereof
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
CN114126972A (zh) * 2019-05-21 2022-03-01 维实洛克包装系统有限公司 灵活间距产品计量系统
CN114144176A (zh) * 2019-06-21 2022-03-04 拓臻制药公司 用于抑制fgfr4的化合物
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MX2022004513A (es) 2019-10-14 2022-07-19 Incyte Corp Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr).
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
CN113072550B (zh) * 2020-01-06 2023-08-08 周龙兴 一种高选择性成纤维细胞生长因子受体抑制剂和应用
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN116406298A (zh) 2020-10-05 2023-07-07 凯奥目生物科学株式会社 癌治疗用药物
CN116528866A (zh) * 2020-11-02 2023-08-01 北京加科思新药研发有限公司 Fgfr4抑制剂的盐的晶型
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN115504965A (zh) 2021-06-23 2022-12-23 浙江海正药业股份有限公司 嘧啶类衍生物的晶型及其制备方法
WO2023082044A1 (zh) * 2021-11-09 2023-05-19 暨南大学 5-醛基杂环酰胺类化合物及其应用
CN116102549A (zh) * 2021-11-09 2023-05-12 暨南大学 5-醛基杂环酰胺类化合物及其应用

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9420999D0 (en) 1994-10-18 1994-12-07 Smithkline Beecham Plc Novel compounds
CA2261633A1 (en) 1996-07-29 1998-02-05 Banyu Pharmaceutical Co., Ltd. Chemokine receptor antagonists
IL136495A0 (en) 1997-12-17 2001-06-14 Merck & Co Inc Integrin receptor antagonists
WO1999041239A1 (en) 1998-02-10 1999-08-19 Novartis Ag B cell inhibitors
EP1218336A2 (en) 1999-09-20 2002-07-03 Takeda Chemical Industries, Ltd. Melanin concentrating hormone antagonist
JP2003513974A (ja) * 1999-11-08 2003-04-15 メルク エンド カムパニー インコーポレーテッド イミダゾリジノン系αｖ−インテグリン拮抗薬の製造方法および製造用中間体
TW200305423A (en) 2002-02-14 2003-11-01 Ono Pharmaceutical Co N-carbamoyl nitrogen-containing condensed ring compound and medicament containing same as active ingredient
US20060004010A1 (en) 2002-07-10 2006-01-05 Hiromu Habashita Ccr4 antagonist and medical use thereof
EP1581529A1 (en) 2002-12-20 2005-10-05 Warner-Lambert Company Benzoxazines and derivatives thereof as inhibitors of pi3ks
US7098332B2 (en) * 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
MXPA05009771A (es) 2003-03-14 2005-10-26 Ono Pharmaceutical Co Derivados heterociclicos que contienen nitrogeno y medicamentos que los contienen como el ingrediente activo.
JP2006522814A (ja) 2003-04-11 2006-10-05 タイゲン・バイオテクノロジー アミノキノリン化合物
SG146624A1 (en) 2003-09-11 2008-10-30 Kemia Inc Cytokine inhibitors
KR101083506B1 (ko) 2005-07-15 2011-11-16 에프. 호프만-라 로슈 아게 신규한 헤테로아릴 융합된 환형 아민
WO2007071752A2 (en) * 2005-12-21 2007-06-28 Novartis Ag Pyrimidinyl aryl urea derivatives being fgf inhibitors
CA2635845A1 (en) 2005-12-29 2007-07-12 Janssen Pharmaceutica N.V. Prokineticin 2 receptor antagonists
EP1989230B1 (en) 2006-02-10 2016-06-01 Genentech, Inc. Anti-fgf19 antibodies and methods using same
BRPI0708731A2 (pt) 2006-03-10 2011-06-07 Ono Pharmaceutical Co derivado heterocìclico nitrogenado, e agente farmacêutico compreendendo o derivado como ingrediente ativo
WO2007146230A2 (en) 2006-06-14 2007-12-21 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
EP1918376A1 (en) 2006-11-03 2008-05-07 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. FGFR4 promotes cancer cell resistance in response to chemotherapeutic drugs
CA2679268A1 (en) 2007-03-09 2008-09-18 Novartis Ag Treatment of melanoma
EP2550972B1 (en) 2007-04-02 2018-02-21 Genentech, Inc. A Klotho-beta agonist antibody for use in the treatment of diabetes mellitus or insulin resistance
CA2709918A1 (en) 2007-12-21 2009-06-25 The Scripps Research Institute Benzopyrans and analogs as rho kinase inhibitors
FR2933702A1 (fr) 2008-07-08 2010-01-15 Sanofi Aventis Antagonistes specifiques du recepteur fgf-r4
US20110212091A1 (en) 2008-09-03 2011-09-01 Licentia Ltd. Materials and methods for inhibiting cancer cell invasion
JPWO2010027002A1 (ja) 2008-09-05 2012-02-02 塩野義製薬株式会社 Ｐｉ３ｋ阻害活性を有する縮環モルホリン誘導体
KR101633532B1 (ko) 2008-12-19 2016-06-24 제넨테크, 인크. 화합물 및 사용 방법
GB0906472D0 (en) * 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
WO2010129467A1 (en) 2009-05-04 2010-11-11 Plexxikon, Inc. Compounds and methods for inhibition of renin, and indications therefor
EP2493888B1 (en) 2009-10-29 2016-04-06 GlaxoSmithKline LLC Bicyclic pyridines and analogs as sirtuin modulators
WO2011051425A1 (en) 2009-10-30 2011-05-05 Novartis Ag N-oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea
KR20120130104A (ko) 2010-02-01 2012-11-28 닛뽕 케미파 가부시키가이샤 Ｇｐｒ119 작동약
WO2011111880A1 (ko) 2010-03-08 2011-09-15 주식회사 메디젠텍 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
KR101764952B1 (ko) 2010-07-29 2017-08-03 리겔 파마슈티칼스, 인크. Ａｍｐｋ-활성화 헤테로시클릭 화합물 및 그의 사용 방법
JP5620417B2 (ja) * 2011-02-07 2014-11-05 中外製薬株式会社 アミノピラゾール誘導体を含む医薬
CA2829466A1 (en) 2011-03-18 2012-09-27 Lupin Limited Benzo [b] [1,4] oxazin derivatives as calcium sensing receptor modulators
CN103596983B (zh) 2011-04-07 2016-10-26 霍夫曼-拉罗奇有限公司 抗fgfr4抗体及使用方法
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
SG11201500125QA (en) 2012-07-11 2015-02-27 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014079709A1 (en) 2012-11-23 2014-05-30 Ab Science Use of small molecule inhibitors/activators in combination with (deoxy)nucleoside or (deoxy)nucleotide analogs for treatment of cancer and hematological malignancies or viral infections
EA036160B1 (ru) 2013-03-15 2020-10-08 Селджен Кар Ллс Гетероарильные соединения и их применение
JP6449244B2 (ja) 2013-04-19 2019-01-09 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ抑制剤としての二環式複素環
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
AU2014287209B2 (en) 2013-07-09 2019-01-24 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
TW201605452A (zh) 2013-08-28 2016-02-16 安斯泰來製藥股份有限公司 以嘧啶化合物作爲有效成分之醫藥組成物
JO3515B1 (ar) 2013-10-18 2020-07-05 Eisai R&D Man Co Ltd مثبطات fgfr4 بيريميدين
US9434700B2 (en) 2013-10-25 2016-09-06 Neil Bifulco, JR. Inhibitors of the fibroblast growth factor receptor

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