KR102739727B1 - 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체 - Google Patents

가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체 Download PDF

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KR102739727B1
KR102739727B1 KR1020207022640A KR20207022640A KR102739727B1 KR 102739727 B1 KR102739727 B1 KR 102739727B1 KR 1020207022640 A KR1020207022640 A KR 1020207022640A KR 20207022640 A KR20207022640 A KR 20207022640A KR 102739727 B1 KR102739727 B1 KR 102739727B1
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KR20200106920A (ko
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데브라 제인 월러스
펭거 조우
유광 왕
다카시 나카이
비쉬누 바드한 레디 카나티
웨이니 씨. 쉐어러
윌리엄 키슬
송 수에
아마드 하샤쉬
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사이클리온 테라퓨틱스, 인크.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • 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
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/04—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D263/06—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by oxygen atoms, attached to ring carbon atoms
    • 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)
KR1020207022640A 2018-01-10 2019-01-10 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체 Active KR102739727B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020247039985A KR20250002720A (ko) 2018-01-10 2019-01-10 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862615678P 2018-01-10 2018-01-10
US62/615,678 2018-01-10
CNPCT/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
PCT/US2019/013060 WO2019140095A1 (en) 2018-01-10 2019-01-10 Novel processes and intermediates for the preparation of soluble guanylate cyclase stimulators

Related Child Applications (1)

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KR1020247039985A Division KR20250002720A (ko) 2018-01-10 2019-01-10 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체

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KR20200106920A KR20200106920A (ko) 2020-09-15
KR102739727B1 true KR102739727B1 (ko) 2024-12-05

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KR1020207022640A Active KR102739727B1 (ko) 2018-01-10 2019-01-10 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체
KR1020257010603A Pending KR20250048609A (ko) 2018-01-10 2019-01-10 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체
KR1020247039985A Pending KR20250002720A (ko) 2018-01-10 2019-01-10 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체

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KR1020247039985A Pending KR20250002720A (ko) 2018-01-10 2019-01-10 가용성 구아닐레이트 시클라제 자극제의 제조를 위한 신규 방법 및 중간체

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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)
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Families Citing this family (4)

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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)

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Publication number Priority date Publication date Assignee Title
WO2016044447A1 (en) 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. Pyrazole derivatives as sgc stimulators
US20170137439A1 (en) 2013-03-15 2017-05-18 Ironwood Pharmaceuticals, Inc. sGC STIMULATORS
WO2017095697A1 (en) 2015-11-30 2017-06-08 Ironwood Pharmaceuticals, Inc. Solid dispersions comprising a sgc stimulator

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Publication number Priority date Publication date Assignee Title
TWI532737B (zh) * 2010-06-30 2016-05-11 艾諾屋製藥公司 可溶性鳥苷酸環化酶（ｓＧＣ）刺激物
WO2015106268A1 (en) * 2014-01-13 2015-07-16 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
CN107223125B (zh) * 2014-09-17 2019-09-27 赛科理音医疗有限公司 sGC刺激剂
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
US20170137439A1 (en) 2013-03-15 2017-05-18 Ironwood Pharmaceuticals, Inc. sGC STIMULATORS
WO2016044447A1 (en) 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. Pyrazole derivatives as sgc stimulators
WO2017095697A1 (en) 2015-11-30 2017-06-08 Ironwood Pharmaceuticals, Inc. Solid dispersions comprising a sgc stimulator

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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
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
TWI821237B (zh) 2023-11-11
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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