KR102506327B1 - αV 인테그린 길항제로서의 인다졸 유도체 - Google Patents

αV 인테그린 길항제로서의 인다졸 유도체 Download PDF

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KR102506327B1
KR102506327B1 KR1020197016080A KR20197016080A KR102506327B1 KR 102506327 B1 KR102506327 B1 KR 102506327B1 KR 1020197016080 A KR1020197016080 A KR 1020197016080A KR 20197016080 A KR20197016080 A KR 20197016080A KR 102506327 B1 KR102506327 B1 KR 102506327B1
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tetrahydro
propanoic acid
indazol
naphthyridin
ethoxy
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KR20190076033A (ko
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시앙-양 예
크리스티안 엘. 모랄레스
멘디 에이. 히긴스
에릭 멀
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브리스톨-마이어스 스큅 컴퍼니
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P35/00Antineoplastic agents
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    • A61P37/00Drugs for immunological or allergic disorders
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    • 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
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020197016080A 2016-11-08 2017-11-07 αV 인테그린 길항제로서의 인다졸 유도체 Active KR102506327B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662418842P 2016-11-08 2016-11-08
US62/418,842 2016-11-08
PCT/US2017/060386 WO2018089357A1 (en) 2016-11-08 2017-11-07 INDAZOLE DERIVATIVES AS αV INTEGRIN ANTAGONISTS

Publications (2)

Publication Number Publication Date
KR20190076033A KR20190076033A (ko) 2019-07-01
KR102506327B1 true KR102506327B1 (ko) 2023-03-03

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US (2) US10745384B2 (https=)
EP (1) EP3538519B1 (https=)
JP (1) JP7213804B2 (https=)
KR (1) KR102506327B1 (https=)
CN (1) CN110214137A (https=)
AU (1) AU2017359027A1 (https=)
CA (1) CA3042714A1 (https=)
EA (1) EA201991123A1 (https=)
ES (1) ES2886650T3 (https=)
IL (1) IL266472A (https=)
MA (1) MA46745A (https=)
MX (1) MX378565B (https=)
WO (1) WO2018089357A1 (https=)

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CN109996541A (zh) 2016-09-07 2019-07-09 普利安特治疗公司 N-酰基氨基酸化合物及其使用方法
KR102506327B1 (ko) * 2016-11-08 2023-03-03 브리스톨-마이어스 스큅 컴퍼니 αV 인테그린 길항제로서의 인다졸 유도체
CN110177787A (zh) 2016-12-29 2019-08-27 圣路易斯大学 整合素拮抗剂
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
MA47697A (fr) 2017-02-28 2020-01-08 Morphic Therapeutic Inc Inhibiteurs de l'(alpha-v)(bêta-6) intégrine
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
EP4086254B1 (en) 2018-08-29 2024-12-18 Morphic Therapeutic, Inc. Integrin inhibitors
FI3844162T3 (fi) 2018-08-29 2025-03-27 Morphic Therapeutic Inc Alfa v beeta6 -integriinin estäjiä
AU2019373242B2 (en) 2018-10-30 2023-07-13 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
EP4541422A3 (en) 2018-10-30 2025-06-25 Gilead Sciences, Inc. Quinoline derivatives as alpha4beta7 integrin inhibitors
KR102659859B1 (ko) 2018-10-30 2024-04-25 길리애드 사이언시즈, 인코포레이티드 알파4β7 인테그린의 억제를 위한 화합물
CN112969700B (zh) 2018-10-30 2024-08-20 吉利德科学公司 作为α4β7整合素抑制剂的咪唑并吡啶衍生物
KR102908219B1 (ko) 2019-08-14 2026-01-08 길리애드 사이언시즈, 인코포레이티드 알파 4 베타 7 인테그린의 저해용 화합물
KR102048050B1 (ko) * 2019-08-29 2020-01-22 대한민국 Adb-푸비나카의 대사체 합성 방법
US20230008367A1 (en) 2019-09-26 2023-01-12 Abionyx Pharma Sa Compounds useful for treating liver diseases
WO2022189856A1 (en) 2021-03-08 2022-09-15 Abionyx Pharma Sa Compounds useful for treating liver diseases
WO2022202864A1 (ja) * 2021-03-24 2022-09-29 塩野義製薬株式会社 縮合環を有するglp-1受容体作動薬を含有する医薬組成物

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WO2007141473A1 (en) 2006-06-09 2007-12-13 Astrazeneca Ab N-(benzoyl)-o- [2- (pyridin- 2 -ylamino) ethyl] -l-tyrosine derivatives and related compounds as a5b1 antagonists for the treatment of solid tumors
WO2015091426A1 (de) 2013-12-19 2015-06-25 Bayer Pharma Aktiengesellschaft Neue indazolcarboxamide, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln

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MX2019005243A (es) 2019-08-05
AU2017359027A1 (en) 2019-06-20
EP3538519B1 (en) 2021-07-28
IL266472A (en) 2019-07-31
EP3538519A1 (en) 2019-09-18
EA201991123A1 (ru) 2019-11-29
MA46745A (fr) 2021-03-31
US20190256496A1 (en) 2019-08-22
MX378565B (es) 2025-03-10
KR20190076033A (ko) 2019-07-01
US20200339540A1 (en) 2020-10-29
US11028071B2 (en) 2021-06-08
JP7213804B2 (ja) 2023-01-27
US10745384B2 (en) 2020-08-18
ES2886650T3 (es) 2021-12-20
WO2018089357A1 (en) 2018-05-17
CN110214137A (zh) 2019-09-06
CA3042714A1 (en) 2018-05-17
JP2019536768A (ja) 2019-12-19

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