EA201990236A1 - Новые способы получения стимуляторов растворимой гуанилатциклазы - Google Patents
Новые способы получения стимуляторов растворимой гуанилатциклазыInfo
- Publication number
- EA201990236A1 EA201990236A1 EA201990236A EA201990236A EA201990236A1 EA 201990236 A1 EA201990236 A1 EA 201990236A1 EA 201990236 A EA201990236 A EA 201990236A EA 201990236 A EA201990236 A EA 201990236A EA 201990236 A1 EA201990236 A1 EA 201990236A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- stimulants
- new methods
- producing
- soluble
- guanilaticyclase
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/14—Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C235/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same 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
- C07C237/06—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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
-
- 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
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
Abstract
Настоящее изобретение относится к новым способам получения соединений, полезных в качестве стимуляторов растворимой гуанилатциклазы (sGC). Эти способы поддаются крупномасштабному получению и дают стабильные 3-(2-пиримидинил)пиразолы формулы I, включая соединение I, соединение IA и соединение IB, с высокой чистотой и выходами. Настоящее изобретение обладает дополнительным преимуществом простых условий реакции, которые можно масштабировать для крупномасштабного производства. Изобретение также представляет новые промежуточные соединения, полезные при получении указанных соединений.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662359430P | 2016-07-07 | 2016-07-07 | |
PCT/US2017/040817 WO2018009602A2 (en) | 2016-07-07 | 2017-07-06 | Novel processes for preparation of soluble guanylate cyclase stimulators |
Publications (1)
Publication Number | Publication Date |
---|---|
EA201990236A1 true EA201990236A1 (ru) | 2019-08-30 |
Family
ID=59351140
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201990236A EA201990236A1 (ru) | 2016-07-07 | 2017-07-06 | Новые способы получения стимуляторов растворимой гуанилатциклазы |
Country Status (17)
Country | Link |
---|---|
US (1) | US11834444B2 (ru) |
EP (1) | EP3481821B1 (ru) |
JP (1) | JP7054395B2 (ru) |
KR (1) | KR102513357B1 (ru) |
CN (1) | CN109563086B (ru) |
AU (1) | AU2017292811B2 (ru) |
BR (1) | BR112019000292A2 (ru) |
CA (1) | CA3029376A1 (ru) |
CL (1) | CL2019000017A1 (ru) |
EA (1) | EA201990236A1 (ru) |
ES (1) | ES2962829T3 (ru) |
IL (1) | IL263994B (ru) |
JO (1) | JOP20180126A1 (ru) |
MA (1) | MA45593A (ru) |
MX (1) | MX2019000138A (ru) |
SG (2) | SG11201900125PA (ru) |
WO (1) | WO2018009602A2 (ru) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11319308B2 (en) * | 2016-07-07 | 2022-05-03 | Cyclerion Therapeutics, Inc. | Processes for preparation of soluble guanylate cyclase stimulators |
WO2019161534A1 (en) * | 2018-02-22 | 2019-08-29 | Ironwood Pharmaceuticals, Inc. | Novel processes and intermediates for preparation of soluble guanylate cyclase stimulators |
MA51565A (fr) | 2018-01-10 | 2020-11-18 | Cyclerion Therapeutics Inc | Nouveaux procédés et intermédiaires pour la préparation de stimulateurs de la guanylate cyclase soluble |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101955439A (zh) * | 2009-07-14 | 2011-01-26 | 华东理工大学 | 一种α-取代-2-氨基乙酰胺的拆分方法 |
CN107021951B (zh) | 2010-06-30 | 2020-10-20 | 赛克里翁治疗有限公司 | sGC刺激物 |
PL2663561T3 (pl) * | 2011-01-13 | 2016-10-31 | Nowe pochodne heterocykliczne i ich zastosowanie w leczeniu zaburzeń neurologicznych | |
EP2797915B1 (en) | 2011-12-27 | 2016-07-13 | Ironwood Pharmaceuticals, Inc. | 2-benzyl-3-(oxazole/thiazole)-5-(pyrimidin-2-yl)-1(H)-pyrazole derivatives as stimulators of the soluble guanylate cyclase (sGC) for the treatment of e.g. hypertension or heart failure |
HRP20220376T1 (hr) | 2013-03-15 | 2022-07-22 | Cyclerion Therapeutics, Inc. | Sgc stimulatori |
WO2016044447A1 (en) | 2014-09-17 | 2016-03-24 | Ironwood Pharmaceuticals, Inc. | Pyrazole derivatives as sgc stimulators |
CN108883071A (zh) | 2015-11-30 | 2018-11-23 | 铁木医药有限公司 | 包含sGC刺激剂的固体分散体 |
CA3029333A1 (en) | 2016-07-07 | 2018-01-11 | Ironwood Pharmaceuticals, Inc. | Solid forms of an sgc stimulator |
US11319308B2 (en) | 2016-07-07 | 2022-05-03 | Cyclerion Therapeutics, Inc. | Processes for preparation of soluble guanylate cyclase stimulators |
-
2017
- 2017-07-06 EA EA201990236A patent/EA201990236A1/ru unknown
- 2017-07-06 ES ES17740238T patent/ES2962829T3/es active Active
- 2017-07-06 CA CA3029376A patent/CA3029376A1/en active Pending
- 2017-07-06 SG SG11201900125PA patent/SG11201900125PA/en unknown
- 2017-07-06 US US16/315,221 patent/US11834444B2/en active Active
- 2017-07-06 EP EP17740238.5A patent/EP3481821B1/en active Active
- 2017-07-06 KR KR1020197003461A patent/KR102513357B1/ko active IP Right Grant
- 2017-07-06 CN CN201780048199.7A patent/CN109563086B/zh active Active
- 2017-07-06 AU AU2017292811A patent/AU2017292811B2/en active Active
- 2017-07-06 BR BR112019000292-8A patent/BR112019000292A2/pt active Search and Examination
- 2017-07-06 SG SG10202100168XA patent/SG10202100168XA/en unknown
- 2017-07-06 WO PCT/US2017/040817 patent/WO2018009602A2/en unknown
- 2017-07-06 MA MA045593A patent/MA45593A/fr unknown
- 2017-07-06 JP JP2019500469A patent/JP7054395B2/ja active Active
- 2017-07-06 MX MX2019000138A patent/MX2019000138A/es unknown
-
2018
- 2018-12-24 JO JOP/2018/0126A patent/JOP20180126A1/ar unknown
- 2018-12-27 IL IL263994A patent/IL263994B/en unknown
-
2019
- 2019-01-04 CL CL2019000017A patent/CL2019000017A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
JP7054395B2 (ja) | 2022-04-13 |
ES2962829T3 (es) | 2024-03-21 |
WO2018009602A3 (en) | 2018-03-15 |
US20210284632A1 (en) | 2021-09-16 |
US11834444B2 (en) | 2023-12-05 |
CN109563086B (zh) | 2023-05-23 |
JOP20180126A1 (ar) | 2019-01-30 |
SG11201900125PA (en) | 2019-02-27 |
BR112019000292A2 (pt) | 2019-04-16 |
CA3029376A1 (en) | 2018-01-11 |
IL263994B (en) | 2021-10-31 |
EP3481821C0 (en) | 2023-09-06 |
IL263994A (en) | 2019-01-31 |
EP3481821B1 (en) | 2023-09-06 |
AU2017292811B2 (en) | 2021-10-21 |
CL2019000017A1 (es) | 2019-05-03 |
KR20190025987A (ko) | 2019-03-12 |
MA45593A (fr) | 2019-05-15 |
KR102513357B1 (ko) | 2023-03-24 |
AU2017292811A1 (en) | 2019-02-07 |
CN109563086A (zh) | 2019-04-02 |
SG10202100168XA (en) | 2021-02-25 |
WO2018009602A2 (en) | 2018-01-11 |
JP2019524712A (ja) | 2019-09-05 |
MX2019000138A (es) | 2019-06-10 |
EP3481821A2 (en) | 2019-05-15 |
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