KR102046448B1 - 섬유모세포 성장 인자 수용체 저해제로서 퀴놀론 유도체들 - Google Patents

섬유모세포 성장 인자 수용체 저해제로서 퀴놀론 유도체들 Download PDF

Info

Publication number
KR102046448B1
KR102046448B1 KR1020167021267A KR20167021267A KR102046448B1 KR 102046448 B1 KR102046448 B1 KR 102046448B1 KR 1020167021267 A KR1020167021267 A KR 1020167021267A KR 20167021267 A KR20167021267 A KR 20167021267A KR 102046448 B1 KR102046448 B1 KR 102046448B1
Authority
KR
South Korea
Prior art keywords
alkyl
pharmaceutically acceptable
compounds
halo
optionally substituted
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
KR1020167021267A
Other languages
English (en)
Korean (ko)
Other versions
KR20160121520A (ko
Inventor
에릭 베르너
케네스 알버트 브라멜드
Original Assignee
프린시피아 바이오파마, 인코퍼레이티드
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 프린시피아 바이오파마, 인코퍼레이티드 filed Critical 프린시피아 바이오파마, 인코퍼레이티드
Publication of KR20160121520A publication Critical patent/KR20160121520A/ko
Application granted granted Critical
Publication of KR102046448B1 publication Critical patent/KR102046448B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020167021267A 2014-02-07 2015-02-04 섬유모세포 성장 인자 수용체 저해제로서 퀴놀론 유도체들 Active KR102046448B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201461937211P 2014-02-07 2014-02-07
US61/937,211 2014-02-07
US201462007562P 2014-06-04 2014-06-04
US62/007,562 2014-06-04
US201462069932P 2014-10-29 2014-10-29
US62/069,932 2014-10-29
PCT/US2015/014460 WO2015120049A1 (en) 2014-02-07 2015-02-04 Quinolone derivatives as fibroblast growth factor receptor inhibitors

Publications (2)

Publication Number Publication Date
KR20160121520A KR20160121520A (ko) 2016-10-19
KR102046448B1 true KR102046448B1 (ko) 2019-11-19

Family

ID=52589764

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020167021267A Active KR102046448B1 (ko) 2014-02-07 2015-02-04 섬유모세포 성장 인자 수용체 저해제로서 퀴놀론 유도체들

Country Status (19)

Country Link
US (6) US9815834B2 (https=)
EP (1) EP3102577B1 (https=)
JP (1) JP6553629B2 (https=)
KR (1) KR102046448B1 (https=)
CN (1) CN106459034B (https=)
AU (1) AU2015214328B2 (https=)
BR (1) BR112016017137B1 (https=)
CA (1) CA2937746C (https=)
CY (1) CY1121444T1 (https=)
DK (1) DK3102577T3 (https=)
ES (1) ES2689421T3 (https=)
HU (1) HUE041594T2 (https=)
IL (1) IL246933B (https=)
MX (1) MX369369B (https=)
PL (1) PL3102577T3 (https=)
PT (1) PT3102577T (https=)
RU (1) RU2721723C2 (https=)
SI (1) SI3102577T1 (https=)
WO (1) WO2015120049A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3102577T (pt) 2014-02-07 2018-10-23 Principia Biopharma Inc Derivados de quinolona como inibidores do recetor do fator de crescimento de fibroblastos
CN105294682B (zh) 2014-07-26 2017-07-07 广东东阳光药业有限公司 Cdk类小分子抑制剂的化合物及其用途
TWI695831B (zh) 2014-09-13 2020-06-11 香港商南北兄弟藥業投資有限公司 Ｃｒｔｈ２拮抗劑化合物及其用途
AU2016304852B2 (en) * 2015-08-11 2020-12-10 Principia Biopharma, Inc. Processes for preparing an FGFR inhibitor
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
US11365196B2 (en) * 2017-02-27 2022-06-21 Betta Pharmaceuticals Co., Ltd. FGFR inhibitor and application thereof
KR102583737B1 (ko) * 2017-03-03 2023-09-26 오클랜드 유니서비시즈 리미티드 Fgfr 키나제 저해제 및 약학적 용도
WO2019015593A1 (zh) * 2017-07-19 2019-01-24 江苏奥赛康药业股份有限公司 嘧啶并吡啶酮或者吡啶并吡啶酮类化合物及其应用
CN109384790B (zh) * 2017-08-08 2022-05-10 药捷安康(南京)科技股份有限公司 成纤维细胞生长因子受体抑制剂及其用途
CN110016026B (zh) * 2018-01-08 2022-11-25 上海凌济生物科技有限公司 一类具有抗肿瘤活性的嘧啶并吡啶酮类化合物、制备方法和用途
US12351576B2 (en) 2018-09-14 2025-07-08 Abbisko Therapeutics Co., Ltd. FGFR inhibitor, preparation method therefor and application thereof
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
JP2022529930A (ja) * 2019-04-19 2022-06-27 ファイザー・インク Ｐａｈを処置するための抗増殖薬
CN114174272B (zh) * 2019-08-08 2023-05-12 漳州片仔癀药业股份有限公司 吡嗪-2(1h)-酮类化合物的制备方法
US11697648B2 (en) 2019-11-26 2023-07-11 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as JAK inhibitors
EP4499616A4 (en) * 2022-03-31 2025-10-29 Acerand Therapeutics Hong Kong Ltd SPIROBICYLICIOUS COMPOUNDS
CN115368219B (zh) * 2022-10-25 2022-12-27 苏州康纯医药科技有限公司 一种fgfr抑制剂关键中间体的制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014011900A2 (en) 2012-07-11 2014-01-16 Blueprint Medicines Inhibitors of the fibroblast growth factor receptor

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5620981A (en) 1995-05-03 1997-04-15 Warner-Lambert Company Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
WO2004063195A1 (en) * 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
RU2348632C2 (ru) 2003-11-13 2009-03-10 Ф.Хоффманн-Ля Рош Аг Гидроксиалкилзамещенные пиридо-7-пиримидин-7-оны
WO2005105097A2 (en) 2004-04-28 2005-11-10 Gpc Biotech Ag Pyridopyrimidines for treating inflammatory and other diseases
WO2006082492A1 (en) 2005-02-02 2006-08-10 Ranbaxy Laboratories Limited Azabicyclo derivatives as anti-inflammatory agents
WO2008150260A1 (en) 2007-06-06 2008-12-11 Gpc Biotech, Inc. 8-oxy-2-aminopyrido (2, 3-d) pyrimidin-7-one derivatives as kinase inhibitors and anticancer agents
IT1395724B1 (it) 2009-02-25 2012-10-19 Neuroscienze Pharmaness S C A R L Composti farmaceutici
ES2770550T3 (es) 2011-05-17 2020-07-02 Univ California Inhibidores de quinasa
CN102219860B (zh) * 2011-05-20 2012-09-12 烟台荣昌生物工程有限公司 FGFR-Fc融合蛋白及其用途
JP2015501786A (ja) * 2011-11-04 2015-01-19 アフラクシス・ホールディングス・インコーポレイテッドＡｆｒａｘｉｓ Ｈｏｌｄｉｎｇｓ，Ｉｎｃ． 脆弱ｘ症候群を治療するためのｐａｋ阻害剤
WO2014182829A1 (en) 2013-05-09 2014-11-13 Principia Biopharma Inc. Quinolone derivatives as fibroblast growth factor inhibitors
US9851834B2 (en) 2013-09-10 2017-12-26 Alsentis, Llc Time domain differential techniques to characterize various stimuli
PT3102577T (pt) 2014-02-07 2018-10-23 Principia Biopharma Inc Derivados de quinolona como inibidores do recetor do fator de crescimento de fibroblastos
EP3298011B1 (en) 2015-05-22 2021-11-17 Principia Biopharma Inc. Quinolone derivatives as fibroblast growth factor receptor inhibitors
AU2016304852B2 (en) 2015-08-11 2020-12-10 Principia Biopharma, Inc. Processes for preparing an FGFR inhibitor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014011900A2 (en) 2012-07-11 2014-01-16 Blueprint Medicines Inhibitors of the fibroblast growth factor receptor

Also Published As

Publication number Publication date
US12162882B2 (en) 2024-12-10
HUE041594T2 (hu) 2019-05-28
ES2689421T3 (es) 2018-11-14
IL246933B (en) 2021-05-31
MX2016010106A (es) 2016-11-15
RU2721723C2 (ru) 2020-05-21
US10294223B2 (en) 2019-05-21
PL3102577T3 (pl) 2019-03-29
RU2016130932A3 (https=) 2018-06-19
SI3102577T1 (sl) 2019-03-29
US11078199B2 (en) 2021-08-03
JP2017505782A (ja) 2017-02-23
US9567334B2 (en) 2017-02-14
CN106459034A (zh) 2017-02-22
CN106459034B (zh) 2018-01-12
KR20160121520A (ko) 2016-10-19
US9815834B2 (en) 2017-11-14
PT3102577T (pt) 2018-10-23
CA2937746C (en) 2020-09-01
US20180065960A1 (en) 2018-03-08
WO2015120049A1 (en) 2015-08-13
DK3102577T3 (en) 2018-11-12
BR112016017137B1 (pt) 2022-10-11
US20190233418A1 (en) 2019-08-01
AU2015214328A1 (en) 2016-08-04
MX369369B (es) 2019-11-06
IL246933A0 (en) 2016-09-29
US20160229849A1 (en) 2016-08-11
BR112016017137A2 (https=) 2017-08-08
EP3102577B1 (en) 2018-07-18
JP6553629B2 (ja) 2019-07-31
US20210292323A1 (en) 2021-09-23
CY1121444T1 (el) 2020-05-29
EP3102577A1 (en) 2016-12-14
US20160200725A1 (en) 2016-07-14
US20240092777A1 (en) 2024-03-21
CA2937746A1 (en) 2015-08-13
RU2016130932A (ru) 2018-03-13
AU2015214328B2 (en) 2019-04-18

Similar Documents

Publication Publication Date Title
US12162882B2 (en) Quinolone derivatives as fibroblast growth factor receptor inhibitors
US9630963B2 (en) Quinolone derivatives as fibroblast growth factor inhibitors
US10538517B2 (en) Quinolone derivatives as FGFR inhibitors
US20160257686A1 (en) Purinone Derivatives as Tyrosine Kinase Inhibitors
US11254651B2 (en) Histone methyltransferase inhibitors
HK1228384B (en) Quinolone derivatives as fibroblast growth factor receptor inhibitors
HK1228384A1 (en) Quinolone derivatives as fibroblast growth factor receptor inhibitors

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
AMND Amendment
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E601 Decision to refuse application
PE0601 Decision on rejection of patent

St.27 status event code: N-2-6-B10-B15-exm-PE0601

X091 Application refused [patent]
AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PX0901 Re-examination

St.27 status event code: A-2-3-E10-E12-rex-PX0901

PX0701 Decision of registration after re-examination

St.27 status event code: A-3-4-F10-F13-rex-PX0701

X701 Decision to grant (after re-examination)
GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

FPAY Annual fee payment

Payment date: 20220929

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-OTH-PR1001 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 7

R18 Changes to party contact information recorded

Free format text: ST27 STATUS EVENT CODE: A-5-5-R10-R18-OTH-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000