IL287102B2 - Novel synthetic options towards the manufacture of (6r,10s)-10- {4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6h)-one - Google Patents
Novel synthetic options towards the manufacture of (6r,10s)-10- {4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6h)-oneInfo
- Publication number
- IL287102B2 IL287102B2 IL287102A IL28710221A IL287102B2 IL 287102 B2 IL287102 B2 IL 287102B2 IL 287102 A IL287102 A IL 287102A IL 28710221 A IL28710221 A IL 28710221A IL 287102 B2 IL287102 B2 IL 287102B2
- Authority
- IL
- Israel
- Prior art keywords
- compound
- alkyl
- formula
- acid
- yield
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/18—Bridged systems
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- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/61—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/10—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 linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962832614P | 2019-04-11 | 2019-04-11 | |
| PCT/US2020/027655 WO2020210613A1 (en) | 2019-04-11 | 2020-04-10 | Novel synthetic options towards the manufacture of (6r,10s)-10- {4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6h)-one |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| IL287102A IL287102A (en) | 2021-12-01 |
| IL287102B1 IL287102B1 (en) | 2025-08-01 |
| IL287102B2 true IL287102B2 (en) | 2025-12-01 |
Family
ID=70457148
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL287102A IL287102B2 (en) | 2019-04-11 | 2020-04-10 | Novel synthetic options towards the manufacture of (6r,10s)-10- {4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6h)-one |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US12378246B2 (https=) |
| EP (2) | EP4234555A3 (https=) |
| JP (2) | JP7631218B2 (https=) |
| KR (2) | KR20260047658A (https=) |
| CN (2) | CN114375290B (https=) |
| AR (1) | AR118649A1 (https=) |
| AU (2) | AU2020272973B2 (https=) |
| BR (1) | BR112021020368A2 (https=) |
| CA (1) | CA3132365A1 (https=) |
| EA (1) | EA202192807A1 (https=) |
| ES (1) | ES2969253T3 (https=) |
| IL (1) | IL287102B2 (https=) |
| MX (2) | MX2021012286A (https=) |
| SG (1) | SG11202111132WA (https=) |
| TW (1) | TWI880924B (https=) |
| WO (1) | WO2020210613A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4133064A4 (en) | 2020-04-10 | 2024-07-24 | Codexis, Inc. | Engineered transaminase polypeptides |
| TW202229280A (zh) * | 2020-10-12 | 2022-08-01 | 美商必治妥美雅史谷比公司 | （６ｒ，１０ｓ）－１０－｛４－［５－氯－２－（４－氯－１ｈ－１，２，３－三唑－１－基）苯基］－６－側氧基－１（６ｈ）－嘧啶基｝－１－（二氟甲基）－６－甲基－１，４，７，８，９，１０－六氫－１１，１５－（亞甲橋基）吡唑并［４，３－ｂ］［１，７］二氮雜環十四炔－５（６ｈ）－酮之製備方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012125797A1 (en) | 2011-03-15 | 2012-09-20 | Abbott Laboratories | Nuclear hormone receptor modulators |
| SG10201908467RA (en) | 2014-01-31 | 2019-10-30 | Bristol Myers Squibb Co | Macrocycles with hetrocyclic p2' groups as factor xia inhibitors |
| NO2721243T3 (https=) | 2014-10-01 | 2018-10-20 | ||
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| CN105294496A (zh) * | 2015-09-28 | 2016-02-03 | 中山大学 | 一种西酞普兰中间体的制备方法 |
| CN110062757B (zh) | 2017-01-18 | 2022-03-04 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
| WO2020211781A1 (zh) * | 2019-04-16 | 2020-10-22 | 南京明德新药研发有限公司 | 作为XIa因子抑制剂的大环衍生物 |
| CN114008047B (zh) * | 2019-07-23 | 2023-03-21 | 南京明德新药研发有限公司 | 作为XIa因子抑制剂的大环衍生物 |
| JP7747337B2 (ja) * | 2020-04-10 | 2025-10-01 | コデクシス， インコーポレイテッド | 速度論的光学分割のためのカルボキシエステラーゼポリペプチド |
-
2020
- 2020-04-10 BR BR112021020368A patent/BR112021020368A2/pt unknown
- 2020-04-10 EP EP23169596.6A patent/EP4234555A3/en active Pending
- 2020-04-10 EP EP20721374.5A patent/EP3953334B1/en active Active
- 2020-04-10 MX MX2021012286A patent/MX2021012286A/es unknown
- 2020-04-10 CN CN202080041935.8A patent/CN114375290B/zh active Active
- 2020-04-10 AU AU2020272973A patent/AU2020272973B2/en active Active
- 2020-04-10 JP JP2021559890A patent/JP7631218B2/ja active Active
- 2020-04-10 IL IL287102A patent/IL287102B2/en unknown
- 2020-04-10 KR KR1020267004972A patent/KR20260047658A/ko active Pending
- 2020-04-10 KR KR1020217036807A patent/KR102929951B1/ko active Active
- 2020-04-10 SG SG11202111132WA patent/SG11202111132WA/en unknown
- 2020-04-10 WO PCT/US2020/027655 patent/WO2020210613A1/en not_active Ceased
- 2020-04-10 TW TW109112263A patent/TWI880924B/zh active
- 2020-04-10 CN CN202411615118.5A patent/CN119775276A/zh active Pending
- 2020-04-10 MX MX2025014306A patent/MX2025014306A/es unknown
- 2020-04-10 EA EA202192807A patent/EA202192807A1/ru unknown
- 2020-04-10 CA CA3132365A patent/CA3132365A1/en active Pending
- 2020-04-10 US US17/602,059 patent/US12378246B2/en active Active
- 2020-04-10 ES ES20721374T patent/ES2969253T3/es active Active
- 2020-04-13 AR ARP200101024A patent/AR118649A1/es unknown
-
2025
- 2025-02-05 JP JP2025017468A patent/JP2025084766A/ja active Pending
- 2025-06-18 US US19/242,506 patent/US20260092066A1/en active Pending
-
2026
- 2026-02-25 AU AU2026201396A patent/AU2026201396A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP3953334A1 (en) | 2022-02-16 |
| TWI880924B (zh) | 2025-04-21 |
| US20220144836A1 (en) | 2022-05-12 |
| IL287102A (en) | 2021-12-01 |
| AR118649A1 (es) | 2021-10-20 |
| KR20220045105A (ko) | 2022-04-12 |
| BR112021020368A2 (pt) | 2021-12-07 |
| EP4234555A2 (en) | 2023-08-30 |
| JP2022526659A (ja) | 2022-05-25 |
| TW202104188A (zh) | 2021-02-01 |
| ES2969253T3 (es) | 2024-05-17 |
| IL287102B1 (en) | 2025-08-01 |
| EP3953334B1 (en) | 2023-11-22 |
| CN119775276A (zh) | 2025-04-08 |
| CA3132365A1 (en) | 2020-10-15 |
| WO2020210613A1 (en) | 2020-10-15 |
| AU2020272973B2 (en) | 2025-11-27 |
| EP4234555A3 (en) | 2024-01-03 |
| KR102929951B1 (ko) | 2026-02-24 |
| SG11202111132WA (en) | 2021-11-29 |
| JP7631218B2 (ja) | 2025-02-18 |
| EA202192807A1 (ru) | 2022-02-24 |
| MX2021012286A (es) | 2022-04-06 |
| MX2025014306A (es) | 2026-01-07 |
| JP2025084766A (ja) | 2025-06-03 |
| AU2020272973A1 (en) | 2021-12-02 |
| CN114375290A (zh) | 2022-04-19 |
| KR20260047658A (ko) | 2026-04-08 |
| US12378246B2 (en) | 2025-08-05 |
| CN114375290B (zh) | 2024-11-29 |
| AU2026201396A1 (en) | 2026-03-19 |
| US20260092066A1 (en) | 2026-04-02 |
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