TWI888947B - 用於製備可溶性鳥苷酸環化酶刺激劑之新穎方法及中間物 - Google Patents

用於製備可溶性鳥苷酸環化酶刺激劑之新穎方法及中間物 Download PDF

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Publication number
TWI888947B
TWI888947B TW112138274A TW112138274A TWI888947B TW I888947 B TWI888947 B TW I888947B TW 112138274 A TW112138274 A TW 112138274A TW 112138274 A TW112138274 A TW 112138274A TW I888947 B TWI888947 B TW I888947B
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Taiwan
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formula
compound
base
amount
solvent
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TW112138274A
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Chinese (zh)
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TW202402741A (zh
Inventor
周鳳爾
王雨光
中井崇
菲努 發達 瑞蒂 卡納提
偉恩 C 史查理爾
威廉 基索
松 薛
哈們 哈書
黛博拉 珍 瓦勒斯
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美商賽克瑞恩醫療公司
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Priority claimed from PCT/CN2018/076982 external-priority patent/WO2019161534A1/en
Application filed by 美商賽克瑞恩醫療公司 filed Critical 美商賽克瑞恩醫療公司
Publication of TW202402741A publication Critical patent/TW202402741A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/08Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW112138274A 2018-01-10 2019-01-10 用於製備可溶性鳥苷酸環化酶刺激劑之新穎方法及中間物 TWI888947B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862615678P 2018-01-10 2018-01-10
US62/615,678 2018-01-10
WOPCT/CN2018/076982 2018-02-22
PCT/CN2018/076982 WO2019161534A1 (en) 2018-02-22 2018-02-22 Novel processes and intermediates for preparation of soluble guanylate cyclase stimulators

Publications (2)

Publication Number Publication Date
TW202402741A TW202402741A (zh) 2024-01-16
TWI888947B true TWI888947B (zh) 2025-07-01

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TW112138274A TWI888947B (zh) 2018-01-10 2019-01-10 用於製備可溶性鳥苷酸環化酶刺激劑之新穎方法及中間物
TW108101044A TWI821237B (zh) 2018-01-10 2019-01-10 用於製備可溶性鳥苷酸環化酶刺激劑之新穎方法及中間物

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US (5) US11274096B2 (enExample)
EP (3) EP4570797A3 (enExample)
JP (2) JP7357621B2 (enExample)
KR (3) KR20250002720A (enExample)
CN (3) CN118184645A (enExample)
AU (3) AU2019206560B2 (enExample)
BR (1) BR112020013985A2 (enExample)
CA (1) CA3087943A1 (enExample)
CL (3) CL2020001814A1 (enExample)
ES (1) ES2963447T3 (enExample)
IL (3) IL314714A (enExample)
JO (1) JOP20200165A1 (enExample)
MA (2) MA71753A (enExample)
MX (3) MX2020007364A (enExample)
SG (1) SG11202006311SA (enExample)
TW (2) TWI888947B (enExample)
WO (1) WO2019140095A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109563077B (zh) 2016-07-07 2026-03-10 赛克里翁治疗有限公司 用于制备可溶性鸟苷酸环化酶刺激剂的新方法
US11274096B2 (en) 2018-01-10 2022-03-15 Cyclerion Therapeutics, Inc. Processes and intermediates for the preparation of soluble guanylate cyclase stimulators
CN118221651A (zh) * 2022-12-21 2024-06-21 广东东阳光药业股份有限公司 氟取代的吲唑化合物的晶型及其用途
AU2023412228A1 (en) * 2022-12-21 2025-07-03 Sunshine Lake Pharma Co., Ltd. Crystal form of fluorine-substituted indazole compound and use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012003405A1 (en) * 2010-06-30 2012-01-05 Ironwood Pharmaceuticals, Inc. Sgc stimulators
WO2016044447A1 (en) * 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. Pyrazole derivatives as sgc stimulators
WO2016044441A1 (en) * 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. Sgc stimulators

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA033168B1 (ru) * 2013-03-15 2019-09-30 Сайклерион Терапьютикс, Инк. СТИМУЛЯТОРЫ sGC
EP3094327A1 (en) * 2014-01-13 2016-11-23 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
CA3006746C (en) 2015-11-30 2024-01-30 Ironwood Pharmaceuticals, Inc. Solid dispersions comprising a sgc stimulator
CN109563086B (zh) 2016-07-07 2023-05-23 赛克里翁治疗有限公司 用于制备可溶性鸟苷酸环化酶刺激剂的方法
CN109563077B (zh) 2016-07-07 2026-03-10 赛克里翁治疗有限公司 用于制备可溶性鸟苷酸环化酶刺激剂的新方法
US11274096B2 (en) 2018-01-10 2022-03-15 Cyclerion Therapeutics, Inc. Processes and intermediates for the preparation of soluble guanylate cyclase stimulators

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012003405A1 (en) * 2010-06-30 2012-01-05 Ironwood Pharmaceuticals, Inc. Sgc stimulators
WO2016044447A1 (en) * 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. Pyrazole derivatives as sgc stimulators
WO2016044441A1 (en) * 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. Sgc stimulators

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Publication number Publication date
EP3737679C0 (en) 2023-09-06
US11274096B2 (en) 2022-03-15
SG11202006311SA (en) 2020-07-29
KR20200106920A (ko) 2020-09-15
AU2025202281A9 (en) 2025-05-15
AU2023270260B2 (en) 2026-01-29
AU2019206560B2 (en) 2023-08-24
US11708361B2 (en) 2023-07-25
MX2020007364A (es) 2020-11-18
US20220024909A1 (en) 2022-01-27
US12030874B2 (en) 2024-07-09
WO2019140095A8 (en) 2020-06-18
JP2021511299A (ja) 2021-05-06
IL319883A (en) 2025-05-01
CL2022000907A1 (es) 2022-10-21
JOP20200165A1 (ar) 2022-10-30
ES2963447T3 (es) 2024-03-27
IL314714A (en) 2024-10-01
EP4570797A2 (en) 2025-06-18
IL275748B1 (en) 2024-09-01
KR20250002720A (ko) 2025-01-07
EP4570797A3 (en) 2025-09-03
IL275748A (en) 2020-08-31
KR20250048609A (ko) 2025-04-09
TW201932450A (zh) 2019-08-16
US20210053962A1 (en) 2021-02-25
IL275748B2 (en) 2025-01-01
JP2023182647A (ja) 2023-12-26
AU2025202281A1 (en) 2025-04-17
CA3087943A1 (en) 2019-07-18
MA51565A (fr) 2020-11-18
TW202402741A (zh) 2024-01-16
KR102739727B1 (ko) 2024-12-05
CN111902410B (zh) 2024-04-19
MA71753A (fr) 2025-05-30
US20240391911A1 (en) 2024-11-28
AU2023270260A1 (en) 2023-12-07
US20230339928A1 (en) 2023-10-26
TWI821237B (zh) 2023-11-11
CN111902410A (zh) 2020-11-06
EP4249469A2 (en) 2023-09-27
EP3737679B1 (en) 2023-09-06
MX2023000045A (es) 2023-02-01
JP7357621B2 (ja) 2023-10-06
JP7744955B2 (ja) 2025-09-26
CL2020001814A1 (es) 2020-11-06
EP4249469A3 (en) 2023-12-27
CN118221665A (zh) 2024-06-21
WO2019140095A1 (en) 2019-07-18
AU2019206560A1 (en) 2020-07-30
US12275724B2 (en) 2025-04-15
EP3737679A1 (en) 2020-11-18
US20250361228A1 (en) 2025-11-27
BR112020013985A2 (pt) 2020-12-01
CN118184645A (zh) 2024-06-14
CL2022000904A1 (es) 2022-10-21
MX2023000044A (es) 2023-02-01

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