CN110650951B - 促生长素抑制素调节剂及其用途 - Google Patents

促生长素抑制素调节剂及其用途 Download PDF

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Publication number
CN110650951B
CN110650951B CN201880033113.8A CN201880033113A CN110650951B CN 110650951 B CN110650951 B CN 110650951B CN 201880033113 A CN201880033113 A CN 201880033113A CN 110650951 B CN110650951 B CN 110650951B
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fluoro
pyridin
methylphenyl
aminopiperidin
benzodiazol
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CN110650951A (zh
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韩相敦
金善姬
朱云飞
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Crinetics Pharmaceuticals Inc
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Crinetics Pharmaceuticals Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201880033113.8A 2017-03-16 2018-03-15 促生长素抑制素调节剂及其用途 Active CN110650951B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762472480P 2017-03-16 2017-03-16
US62/472,480 2017-03-16
PCT/US2018/022665 WO2018170284A1 (en) 2017-03-16 2018-03-15 Somatostatin modulators and uses thereof

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CN110650951A CN110650951A (zh) 2020-01-03
CN110650951B true CN110650951B (zh) 2023-02-24

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US (1) US11072598B2 (https=)
EP (1) EP3596062A4 (https=)
JP (1) JP7106564B2 (https=)
KR (1) KR20190121404A (https=)
CN (1) CN110650951B (https=)
AU (1) AU2018234806A1 (https=)
BR (1) BR112019019168A2 (https=)
CA (1) CA3056131A1 (https=)
EA (1) EA201992083A1 (https=)
IL (1) IL269241B (https=)
MX (1) MX2019010949A (https=)
NZ (1) NZ757081A (https=)
SG (1) SG11201908512YA (https=)
TW (1) TW201840550A (https=)
UA (1) UA127346C2 (https=)
WO (1) WO2018170284A1 (https=)

Families Citing this family (14)

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EP3596062A4 (en) 2017-03-16 2020-08-26 Crinetics Pharmaceuticals, Inc. SOMATOSTATIN MODULATORS AND THEIR USES
MA51840A (fr) 2018-02-12 2021-05-19 Crinetics Pharmaceuticals Inc Modulateurs de somatostatine et leurs utilisations
WO2019240246A1 (ja) * 2018-06-15 2019-12-19 小野薬品工業株式会社 ピペリジノール誘導体の新規な塩および新規結晶形
SMT202500155T1 (it) 2018-09-18 2025-05-12 Crinetics Pharmaceuticals Inc Modulatori della somatostatina e loro usi
TWI841768B (zh) 2019-08-14 2024-05-11 美商克林提克斯醫藥股份有限公司 非肽生長抑制素(somatostatin)5型受體激動劑及其用途
WO2021076448A1 (en) * 2019-10-14 2021-04-22 Crinetics Pharmaceuticals, Inc. Somatostatin modulators for treating pituitary adenomas
US12509444B2 (en) * 2019-12-06 2025-12-30 Plexxikon Inc. Compounds and methods for CD73 modulation and indications therefor
AR121682A1 (es) 2020-03-31 2022-06-29 Takeda Pharmaceuticals Co Derivados de n-(heterociclil y heterociclilalquil)-3-bencilpiridin-2-amina como agonistas de sstr4
CA3191084A1 (en) 2020-09-09 2022-03-17 Gerald Burke Formulations of a somatostatin modulator
JP2024506715A (ja) 2021-02-17 2024-02-14 クリネティックス ファーマシューティカルズ，インク． ソマトスタチンモジュレーターの結晶形態
CN117377495A (zh) * 2021-06-09 2024-01-09 克林提克斯医药股份有限公司 非肽靶向治疗剂及其用途
CN114591326B (zh) * 2022-02-28 2024-02-27 上海筛杰生物医药有限公司 Cct-251921的中间体及其制备方法
IL320483A (en) * 2022-10-28 2025-06-01 Basecamp Bio Inc Somatostatin receptor 2 agonists and uses thereof
TW202440164A (zh) * 2022-12-13 2024-10-16 美商克林提克斯醫藥股份有限公司 生長抑素亞型-2受體（sst2r）靶向治療劑及其用途

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CN110300749A (zh) * 2017-02-08 2019-10-01 小野药品工业株式会社 具有生长抑素受体激动活性的化合物及其医药用途

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CA3056131A1 (en) 2018-09-20
MX2019010949A (es) 2019-10-24
UA127346C2 (uk) 2023-07-26
CN110650951A (zh) 2020-01-03
EP3596062A1 (en) 2020-01-22
JP2020511452A (ja) 2020-04-16
SG11201908512YA (en) 2019-10-30
BR112019019168A2 (pt) 2020-04-14
IL269241B (en) 2022-09-01
TW201840550A (zh) 2018-11-16
US11072598B2 (en) 2021-07-27
EP3596062A4 (en) 2020-08-26
IL269241A (en) 2019-11-28
KR20190121404A (ko) 2019-10-25
AU2018234806A1 (en) 2019-10-03
US20200010453A1 (en) 2020-01-09
NZ757081A (en) 2023-03-31
EA201992083A1 (ru) 2020-03-18
JP7106564B2 (ja) 2022-07-26
WO2018170284A1 (en) 2018-09-20

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