TWI834321B - αｖβ６整合蛋白之抑制劑 - Google Patents

αｖβ６整合蛋白之抑制劑 Download PDF

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Publication number
TWI834321B
TWI834321B TW111137048A TW111137048A TWI834321B TW I834321 B TWI834321 B TW I834321B TW 111137048 A TW111137048 A TW 111137048A TW 111137048 A TW111137048 A TW 111137048A TW I834321 B TWI834321 B TW I834321B
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mmol
tetrahydro
naphthyridin
compound
esi
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TW111137048A
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Chinese (zh)
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TW202325707A (zh
Inventor
馬克 布爾
馬修 桂格瑞 伯沙維奇
艾力克西 伊格瑞維奇 傑洛西鄔圖
克里斯多夫 奈爾 漢
拜爾斯 艾爾登 哈里森
凱爾 大衛 康梓
林富揚
布雷斯 史考特 莉琶
艾力克斯伊 亞歷三洛維奇 盧格維斯克伊
布魯斯 奈兒森 羅傑斯
麥斯 史維森
唐 馬力 特洛斯特
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美商莫菲克醫療股份有限公司
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D471/08—Bridged systems
    • 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D487/08—Bridged 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
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  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
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  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW111137048A 2017-02-28 2018-02-27 αｖβ６整合蛋白之抑制劑 TWI834321B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762464693P 2017-02-28 2017-02-28
US62/464,693 2017-02-28

Publications (2)

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TW202325707A TW202325707A (zh) 2023-07-01
TWI834321B true TWI834321B (zh) 2024-03-01

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TW107106640A TW201835078A (zh) 2017-02-28 2018-02-27 αvβ6整合蛋白之抑制劑
TW111137048A TWI834321B (zh) 2017-02-28 2018-02-27 αｖβ６整合蛋白之抑制劑

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EP (2) EP3589627A4 (enExample)
JP (2) JP7092784B2 (enExample)
KR (2) KR102891803B1 (enExample)
CN (2) CN116283977A (enExample)
AR (2) AR111009A1 (enExample)
AU (3) AU2018229275B2 (enExample)
BR (1) BR112019017929A2 (enExample)
CA (1) CA3054604A1 (enExample)
IL (3) IL297530B2 (enExample)
MA (1) MA47697A (enExample)
MX (2) MX394210B (enExample)
RU (2) RU2022108080A (enExample)
SG (1) SG11201907820SA (enExample)
TW (2) TW201835078A (enExample)
WO (1) WO2018160521A2 (enExample)

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CA3054604A1 (en) 2017-02-28 2018-09-07 Morphic Therapeutic, Inc. Inhibitors of .alpha.v.beta.6 integrin
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PE20251320A1 (es) 2018-03-07 2025-05-16 Pliant Therapeutics Inc Compuestos de aminoacidos y metodos de uso
TWI841573B (zh) 2018-06-27 2024-05-11 美商普萊恩醫療公司 具有未分支連接子之胺基酸化合物及使用方法
WO2020047207A1 (en) * 2018-08-29 2020-03-05 Morphic Therapeutics, Inc. Inhibitors of (alpha-v)(beta-6) integrin
WO2020047208A1 (en) * 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
SMT202500129T1 (it) * 2018-08-29 2025-05-12 Morphic Therapeutic Inc Inibitori di integrina alfa v beta6
CR20210109A (es) 2018-08-29 2021-06-24 Morphic Therapeutic Inc INHIBICIÓN DE LA INTEGRINA av ß6
TW202028179A (zh) 2018-10-08 2020-08-01 美商普萊恩醫療公司 胺基酸化合物及使用方法
FI3873884T3 (fi) 2018-10-30 2025-02-24 Gilead Sciences Inc 3-(kinolin-8-yyli)-1,4-dihydropyrido[3,4-d]pyrimidiini-2,4-dionijohdannaisia alfa-4-beta-7-integriinin estäjinä tulehdussairauksien hoidossa
EP3873897B1 (en) 2018-10-30 2024-08-14 Gilead Sciences, Inc. N-benzoyl-phenylalanine derivatives as alpha4beta7 integrin inhibitors for treating inflammatory diseases
CA3115830C (en) 2018-10-30 2023-09-12 Gilead Sciences, Inc. Compounds for inhibition of .alpha.4.beta.7 integrin
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
EP3952902A4 (en) 2019-04-08 2022-12-21 Pliant Therapeutics, Inc. DOSAGE FORMS AND THERAPY SCHEMES FOR AMINO ACID COMPOUNDS
EP4013499A1 (en) 2019-08-14 2022-06-22 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
CN115087444B (zh) * 2019-10-16 2024-09-17 莫菲克医疗股份有限公司 抑制人整联蛋白α4β7
CN111718250B (zh) * 2020-06-28 2022-04-22 万华化学集团股份有限公司 一种制备r-香茅醛的方法
PE20240114A1 (es) 2020-11-19 2024-01-22 Pliant Therapeutics Inc Inhibidor de integrina y usos de este
CN121127468A (zh) * 2023-02-14 2025-12-12 莫菲克医疗股份有限公司 抑制αvβ8整合素
CN120957721A (zh) * 2023-02-14 2025-11-14 莫菲克医疗股份有限公司 抑制αvβ8整合素
WO2025106644A1 (en) * 2023-11-15 2025-05-22 Morphic Therapeutic, Inc. Heterocyclic compounds as inhibitors of alpha-v beta-1 integrin

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