TWI821237B - 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
TWI821237B
TWI821237B TW108101044A TW108101044A TWI821237B TW I821237 B TWI821237 B TW I821237B TW 108101044 A TW108101044 A TW 108101044A TW 108101044 A TW108101044 A TW 108101044A TW I821237 B TWI821237 B TW I821237B
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TW
Taiwan
Prior art keywords
formula
compound
appropriate amount
base
salt
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TW108101044A
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English (en)
Chinese (zh)
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TW201932450A (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 TW201932450A publication Critical patent/TW201932450A/zh
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    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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
    • C07C237/06—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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
    • C07C237/08—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
TW108101044A 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 TWI821237B (zh)

Applications Claiming Priority (5)

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

Publications (2)

Publication Number Publication Date
TW201932450A TW201932450A (zh) 2019-08-16
TWI821237B true TWI821237B (zh) 2023-11-11

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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
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

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US (5) US11274096B2 (enExample)
EP (3) EP4249469A3 (enExample)
JP (2) JP7357621B2 (enExample)
KR (3) KR102739727B1 (enExample)
CN (3) CN111902410B (enExample)
AU (3) AU2019206560B2 (enExample)
CA (1) CA3087943A1 (enExample)
CL (3) CL2020001814A1 (enExample)
ES (1) ES2963447T3 (enExample)
IL (3) IL275748B2 (enExample)
JO (1) JOP20200165A1 (enExample)
MA (2) MA71753A (enExample)
MX (3) MX2020007364A (enExample)
SG (1) SG11202006311SA (enExample)
TW (2) TWI821237B (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
KR102487872B1 (ko) 2016-07-07 2023-01-12 사이클리온 테라퓨틱스, 인크. 가용성 구아닐레이트 시클라제 자극제의 신규 제조 방법
CN111902410B (zh) 2018-01-10 2024-04-19 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及中间物
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
ES2911276T3 (es) * 2013-03-15 2022-05-18 Cyclerion Therapeutics Inc Estimuladores de sGC
WO2015106268A1 (en) * 2014-01-13 2015-07-16 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
BR112018011154B1 (pt) * 2015-11-30 2023-09-26 Cyclerion Therapeutics, Inc Dispersões sólidas compreendendo um estimulador de sgc
EA201990236A1 (ru) 2016-07-07 2019-08-30 Сайклерион Терапьютикс, Инк. Новые способы получения стимуляторов растворимой гуанилатциклазы
KR102487872B1 (ko) 2016-07-07 2023-01-12 사이클리온 테라퓨틱스, 인크. 가용성 구아닐레이트 시클라제 자극제의 신규 제조 방법
CN111902410B (zh) 2018-01-10 2024-04-19 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及中间物

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

Also Published As

Publication number Publication date
TWI888947B (zh) 2025-07-01
CL2020001814A1 (es) 2020-11-06
US20230339928A1 (en) 2023-10-26
MA71753A (fr) 2025-05-30
US11708361B2 (en) 2023-07-25
US11274096B2 (en) 2022-03-15
ES2963447T3 (es) 2024-03-27
KR20250002720A (ko) 2025-01-07
US20250361228A1 (en) 2025-11-27
KR102739727B1 (ko) 2024-12-05
CA3087943A1 (en) 2019-07-18
CN118184645A (zh) 2024-06-14
MX2020007364A (es) 2020-11-18
IL319883A (en) 2025-05-01
JP7357621B2 (ja) 2023-10-06
JP2023182647A (ja) 2023-12-26
MX2023000044A (es) 2023-02-01
EP3737679A1 (en) 2020-11-18
EP4249469A3 (en) 2023-12-27
MX2023000045A (es) 2023-02-01
US20210053962A1 (en) 2021-02-25
WO2019140095A1 (en) 2019-07-18
KR20200106920A (ko) 2020-09-15
AU2019206560A1 (en) 2020-07-30
EP4249469A2 (en) 2023-09-27
CN111902410A (zh) 2020-11-06
CN111902410B (zh) 2024-04-19
EP3737679B1 (en) 2023-09-06
IL275748A (en) 2020-08-31
EP4570797A2 (en) 2025-06-18
AU2025202281A9 (en) 2025-05-15
IL314714A (en) 2024-10-01
AU2019206560B2 (en) 2023-08-24
JOP20200165A1 (ar) 2022-10-30
US12275724B2 (en) 2025-04-15
CL2022000904A1 (es) 2022-10-21
US20240391911A1 (en) 2024-11-28
BR112020013985A2 (pt) 2020-12-01
AU2023270260B2 (en) 2026-01-29
WO2019140095A8 (en) 2020-06-18
JP2021511299A (ja) 2021-05-06
US12030874B2 (en) 2024-07-09
CN118221665A (zh) 2024-06-21
MA51565A (fr) 2020-11-18
AU2023270260A1 (en) 2023-12-07
SG11202006311SA (en) 2020-07-29
KR20250048609A (ko) 2025-04-09
TW201932450A (zh) 2019-08-16
EP3737679C0 (en) 2023-09-06
JP7744955B2 (ja) 2025-09-26
AU2025202281A1 (en) 2025-04-17
TW202402741A (zh) 2024-01-16
EP4570797A3 (en) 2025-09-03
US20220024909A1 (en) 2022-01-27
CL2022000907A1 (es) 2022-10-21
IL314714B1 (en) 2026-06-01
IL275748B2 (en) 2025-01-01
IL275748B1 (en) 2024-09-01

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