JOP20180126A1 - عمليات جديدة من أجل تحضير منشطات محلقة غوانيلات قابلة للذوبان - Google Patents
عمليات جديدة من أجل تحضير منشطات محلقة غوانيلات قابلة للذوبانInfo
- Publication number
- JOP20180126A1 JOP20180126A1 JOP/2018/0126A JOP20180126A JOP20180126A1 JO P20180126 A1 JOP20180126 A1 JO P20180126A1 JO P20180126 A JOP20180126 A JO P20180126A JO P20180126 A1 JOP20180126 A1 JO P20180126A1
- Authority
- JO
- Jordan
- Prior art keywords
- compound
- preparation
- novel processes
- guanylate cyclase
- soluble guanylate
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title abstract 3
- 102000007637 Soluble Guanylyl Cyclase Human genes 0.000 title 1
- 108010007205 Soluble Guanylyl Cyclase Proteins 0.000 title 1
- 239000003119 guanylate cyclase activator Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 229940125890 compound Ia Drugs 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- BWIHJLOBZMKPKS-UHFFFAOYSA-N 2-(1h-pyrazol-5-yl)pyrimidine Chemical class N1C=CC(C=2N=CC=CN=2)=N1 BWIHJLOBZMKPKS-UHFFFAOYSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003054 catalyst Substances 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
يتعلق الكشف الحالي بالعمليات الجديدة لتحضير مركبات مفيدة كمحفزات من إنزيم حلقي جوانيلات قابل للذوبان (sGC). تكون هذه العمليات قابلة للتعديل لعملية تحضير واسعة النطاق وإنتاج مركبات 3-(2-بيريميدينيل) بيرازول مستقرة وفقا للصيغة I، بما في ذلك مركب I، مركب IA ومركب IB، بنقاء ونتائج عالية. يكون للاختراع الحالي الميزة الإضافية لظروف تفاعل سهلة، قابلة للتعديل لزيادة التصنيع واسع النطاق. يقدم الكشف أيضا مركبات وسيطة جديدة مفيدة في تحضير المركبات المفيدة. الصيغة I مركب I مركب IA مركب IB
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 |
|---|---|
| JOP20180126A1 true JOP20180126A1 (ar) | 2019-01-30 |
Family
ID=59351140
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2018/0126A JOP20180126A1 (ar) | 2016-07-07 | 2018-12-24 | عمليات جديدة من أجل تحضير منشطات محلقة غوانيلات قابلة للذوبان |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11834444B2 (ar) |
| EP (1) | EP3481821B1 (ar) |
| JP (1) | JP7054395B2 (ar) |
| KR (1) | KR102513357B1 (ar) |
| CN (1) | CN109563086B (ar) |
| AU (1) | AU2017292811B2 (ar) |
| BR (1) | BR112019000292A2 (ar) |
| CA (2) | CA3247345A1 (ar) |
| CL (1) | CL2019000017A1 (ar) |
| EA (1) | EA201990236A1 (ar) |
| ES (1) | ES2962829T3 (ar) |
| IL (1) | IL263994B (ar) |
| JO (1) | JOP20180126A1 (ar) |
| MA (1) | MA45593A (ar) |
| MX (1) | MX382762B (ar) |
| SG (2) | SG11201900125PA (ar) |
| WO (1) | WO2018009602A2 (ar) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2019161534A1 (en) * | 2018-02-22 | 2019-08-29 | Ironwood Pharmaceuticals, Inc. | Novel processes and intermediates for preparation of soluble guanylate cyclase stimulators |
Family Cites Families (10)
| 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 |
| EP2588465B1 (en) | 2010-06-30 | 2017-01-25 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| MY162413A (en) | 2011-01-13 | 2017-06-15 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
| CN106117194A (zh) * | 2011-12-27 | 2016-11-16 | 铁木医药有限公司 | 可用作sgc刺激剂的2‑苄基、3‑(嘧啶‑2‑基)取代的吡唑类 |
| EA033168B1 (ru) | 2013-03-15 | 2019-09-30 | Сайклерион Терапьютикс, Инк. | СТИМУЛЯТОРЫ sGC |
| EP3194382B1 (en) * | 2014-09-17 | 2021-09-08 | Cyclerion Therapeutics, Inc. | Pyrazole derivatives as sgc stimulators |
| 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 |
| CN109563087A (zh) | 2016-07-07 | 2019-04-02 | 铁木医药有限公司 | sGC刺激剂的固体形式 |
| 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 |
-
2017
- 2017-07-06 CN CN201780048199.7A patent/CN109563086B/zh active Active
- 2017-07-06 BR BR112019000292-8A patent/BR112019000292A2/pt not_active Application Discontinuation
- 2017-07-06 US US16/315,221 patent/US11834444B2/en active Active
- 2017-07-06 AU AU2017292811A patent/AU2017292811B2/en not_active Ceased
- 2017-07-06 ES ES17740238T patent/ES2962829T3/es active Active
- 2017-07-06 JP JP2019500469A patent/JP7054395B2/ja active Active
- 2017-07-06 SG SG11201900125PA patent/SG11201900125PA/en unknown
- 2017-07-06 MX MX2019000138A patent/MX382762B/es unknown
- 2017-07-06 EA EA201990236A patent/EA201990236A1/ru unknown
- 2017-07-06 KR KR1020197003461A patent/KR102513357B1/ko active Active
- 2017-07-06 MA MA045593A patent/MA45593A/fr unknown
- 2017-07-06 WO PCT/US2017/040817 patent/WO2018009602A2/en not_active Ceased
- 2017-07-06 CA CA3247345A patent/CA3247345A1/en active Pending
- 2017-07-06 SG SG10202100168XA patent/SG10202100168XA/en unknown
- 2017-07-06 EP EP17740238.5A patent/EP3481821B1/en active Active
- 2017-07-06 CA CA3029376A patent/CA3029376C/en active Active
-
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
-
2023
- 2023-10-30 US US18/385,025 patent/US12247025B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| MX2019000138A (es) | 2019-06-10 |
| BR112019000292A2 (pt) | 2019-04-16 |
| CN109563086A (zh) | 2019-04-02 |
| MA45593A (fr) | 2019-05-15 |
| KR102513357B1 (ko) | 2023-03-24 |
| EA201990236A1 (ru) | 2019-08-30 |
| WO2018009602A3 (en) | 2018-03-15 |
| IL263994B (en) | 2021-10-31 |
| US12247025B2 (en) | 2025-03-11 |
| EP3481821A2 (en) | 2019-05-15 |
| CN109563086B (zh) | 2023-05-23 |
| US20240199595A1 (en) | 2024-06-20 |
| SG11201900125PA (en) | 2019-02-27 |
| ES2962829T3 (es) | 2024-03-21 |
| CL2019000017A1 (es) | 2019-05-03 |
| MX382762B (es) | 2025-03-13 |
| US20210284632A1 (en) | 2021-09-16 |
| CA3247345A1 (en) | 2025-11-29 |
| JP7054395B2 (ja) | 2022-04-13 |
| CA3029376A1 (en) | 2018-01-11 |
| EP3481821B1 (en) | 2023-09-06 |
| AU2017292811B2 (en) | 2021-10-21 |
| AU2017292811A1 (en) | 2019-02-07 |
| CA3029376C (en) | 2025-11-18 |
| WO2018009602A2 (en) | 2018-01-11 |
| EP3481821C0 (en) | 2023-09-06 |
| US11834444B2 (en) | 2023-12-05 |
| SG10202100168XA (en) | 2021-02-25 |
| JP2019524712A (ja) | 2019-09-05 |
| KR20190025987A (ko) | 2019-03-12 |
| IL263994A (en) | 2019-01-31 |
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