CN109563077A - 用于制备可溶性鸟苷酸环化酶刺激剂的新方法 - Google Patents
用于制备可溶性鸟苷酸环化酶刺激剂的新方法 Download PDFInfo
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- 238000000034 method Methods 0.000 title claims abstract description 130
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- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 5
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- 238000001556 precipitation Methods 0.000 description 1
- UORVCLMRJXCDCP-UHFFFAOYSA-N propynoic acid Chemical compound OC(=O)C#C UORVCLMRJXCDCP-UHFFFAOYSA-N 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
- 238000005086 pumping Methods 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 150000003217 pyrazoles Chemical class 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 150000003230 pyrimidines Chemical class 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 238000005956 quaternization reaction Methods 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000004064 recycling Methods 0.000 description 1
- 230000004648 relaxation of smooth muscle Effects 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
- 230000008439 repair process Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 229940125526 sGC activator Drugs 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- WRIKHQLVHPKCJU-UHFFFAOYSA-N sodium bis(trimethylsilyl)amide Chemical compound C[Si](C)(C)N([Na])[Si](C)(C)C WRIKHQLVHPKCJU-UHFFFAOYSA-N 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 230000005062 synaptic transmission Effects 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- DZLFLBLQUQXARW-UHFFFAOYSA-N tetrabutylammonium Chemical compound CCCC[N+](CCCC)(CCCC)CCCC DZLFLBLQUQXARW-UHFFFAOYSA-N 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000003325 tomography Methods 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
Classifications
-
- 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
- C07D413/14—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
- 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)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662359453P | 2016-07-07 | 2016-07-07 | |
| US62/359,453 | 2016-07-07 | ||
| PCT/US2017/040810 WO2018009597A1 (en) | 2016-07-07 | 2017-07-06 | Novel processes for preparation of soluble guanylate cyclase stimulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109563077A true CN109563077A (zh) | 2019-04-02 |
Family
ID=59416789
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780047020.6A Pending CN109563077A (zh) | 2016-07-07 | 2017-07-06 | 用于制备可溶性鸟苷酸环化酶刺激剂的新方法 |
Country Status (16)
| Country | Link |
|---|---|
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| EP (2) | EP3481818B1 (enExample) |
| JP (1) | JP7112384B2 (enExample) |
| KR (1) | KR102487872B1 (enExample) |
| CN (1) | CN109563077A (enExample) |
| AU (1) | AU2017291827B2 (enExample) |
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| CA (1) | CA3029375A1 (enExample) |
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| SG (1) | SG11201900096QA (enExample) |
| WO (1) | WO2018009597A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3481818B1 (en) | 2016-07-07 | 2023-09-06 | Cyclerion Therapeutics, Inc. | Novel processes for preparation of soluble guanylate cyclase stimulators |
| BR112019000292A2 (pt) | 2016-07-07 | 2019-04-16 | Ironwood Pharmaceuticals, Inc. | processos inovadores para a preparação de estimuladores de guanilato ciclase solúvel |
| WO2019161534A1 (en) * | 2018-02-22 | 2019-08-29 | Ironwood Pharmaceuticals, Inc. | Novel processes and intermediates for preparation of soluble guanylate cyclase stimulators |
| JOP20200165A1 (ar) | 2018-01-10 | 2022-10-30 | Cyclerion Therapeutics Inc | عمليات ووسائط جديدة لتحضير محفزات إنزيم حلقي جوانيلات قابلة للذوبان |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103038229A (zh) * | 2010-05-26 | 2013-04-10 | 桑诺维恩药品公司 | 杂芳基化合物及其使用方法 |
| CN104066731A (zh) * | 2011-12-27 | 2014-09-24 | 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 |
| WO2015089182A1 (en) * | 2013-12-11 | 2015-06-18 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| CN105408328A (zh) * | 2013-03-15 | 2016-03-16 | 铁木医药有限公司 | sGC刺激剂 |
| WO2016044447A1 (en) * | 2014-09-17 | 2016-03-24 | Ironwood Pharmaceuticals, Inc. | Pyrazole derivatives as sgc stimulators |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY33476A (es) | 2010-06-30 | 2012-02-29 | Ironwood Pharmaceuticals Inc | Estimuladores de sgc |
| CA2885645A1 (en) * | 2012-09-19 | 2014-03-27 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| WO2016044446A2 (en) * | 2014-09-17 | 2016-03-24 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| US20170298055A1 (en) * | 2014-09-17 | 2017-10-19 | Ironwood Pharmaceuticals, Inc. | sGC STIMULATORS |
| MX2017003517A (es) * | 2014-09-17 | 2017-07-28 | Ironwood Pharmaceuticals Inc | Estimuladores de guanilato ciclasa soluble (sgc). |
| MX389961B (es) * | 2015-11-30 | 2025-03-20 | Cyclerion Therapeutics Inc | Dispersiones sólidas que comprenden estimulador de heme guanilato ciclasa soluble (sgc). |
| EP3481818B1 (en) | 2016-07-07 | 2023-09-06 | Cyclerion Therapeutics, Inc. | Novel processes for preparation of soluble guanylate cyclase stimulators |
| BR112019000293A2 (pt) * | 2016-07-07 | 2019-04-16 | Ironwood Pharmaceuticals, Inc. | formas sólidas de um estimulador de sgc |
| BR112019000292A2 (pt) * | 2016-07-07 | 2019-04-16 | Ironwood Pharmaceuticals, Inc. | processos inovadores para a preparação de estimuladores de guanilato ciclase solúvel |
| US11897887B2 (en) * | 2017-12-19 | 2024-02-13 | Tisento Therapeutics Inc. | sGC stimulators |
| JOP20200165A1 (ar) * | 2018-01-10 | 2022-10-30 | Cyclerion Therapeutics Inc | عمليات ووسائط جديدة لتحضير محفزات إنزيم حلقي جوانيلات قابلة للذوبان |
-
2017
- 2017-07-06 EP EP17745553.2A patent/EP3481818B1/en active Active
- 2017-07-06 ES ES17745553T patent/ES2963563T3/es active Active
- 2017-07-06 WO PCT/US2017/040810 patent/WO2018009597A1/en not_active Ceased
- 2017-07-06 SG SG11201900096QA patent/SG11201900096QA/en unknown
- 2017-07-06 CA CA3029375A patent/CA3029375A1/en active Pending
- 2017-07-06 MX MX2019000105A patent/MX389920B/es unknown
- 2017-07-06 EP EP23185002.5A patent/EP4249488A3/en active Pending
- 2017-07-06 MA MA045603A patent/MA45603A/fr unknown
- 2017-07-06 AU AU2017291827A patent/AU2017291827B2/en active Active
- 2017-07-06 JP JP2019500355A patent/JP7112384B2/ja active Active
- 2017-07-06 BR BR112019000291A patent/BR112019000291A2/pt not_active Application Discontinuation
- 2017-07-06 US US16/315,218 patent/US11319308B2/en active Active
- 2017-07-06 CN CN201780047020.6A patent/CN109563077A/zh active Pending
- 2017-07-06 EA EA201990237A patent/EA201990237A1/ru unknown
- 2017-07-06 KR KR1020197003459A patent/KR102487872B1/ko active Active
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2018
- 2018-12-27 IL IL263995A patent/IL263995B/en active IP Right Grant
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2019
- 2019-01-04 CL CL2019000016A patent/CL2019000016A1/es unknown
- 2019-01-07 MX MX2022001495A patent/MX2022001495A/es unknown
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2022
- 2022-03-30 US US17/708,296 patent/US11773089B2/en active Active
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2023
- 2023-01-24 CL CL2023000228A patent/CL2023000228A1/es unknown
- 2023-08-24 US US18/237,435 patent/US20240059684A1/en not_active Abandoned
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103038229A (zh) * | 2010-05-26 | 2013-04-10 | 桑诺维恩药品公司 | 杂芳基化合物及其使用方法 |
| CN104066731A (zh) * | 2011-12-27 | 2014-09-24 | 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 |
| CN105408328A (zh) * | 2013-03-15 | 2016-03-16 | 铁木医药有限公司 | sGC刺激剂 |
| WO2015089182A1 (en) * | 2013-12-11 | 2015-06-18 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| WO2016044447A1 (en) * | 2014-09-17 | 2016-03-24 | Ironwood Pharmaceuticals, Inc. | Pyrazole derivatives as sgc stimulators |
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| Title |
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| ALI RAOOF等: "Toxoflavins and Deazaflavins as the First Reported Selective Small Molecule Inhibitors of Tyrosyl-DNA Phosphodiesterase II", 《JOURNAL OF MEDICINAL CHEMISTRY》 * |
| B.BAASNER等: "A new route to the synthesis of 5-fluorouracil", 《JOURNAL OF FLUORINE CHEMISTRY》 * |
| TAKASHI NAKAI等: "Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans", 《ACS MEDICINAL CHEMISTRY LETTERS》 * |
| 卞克勤 等: "《工业化学反应及应用》", 28 February 1999 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CL2019000016A1 (es) | 2019-05-03 |
| US11773089B2 (en) | 2023-10-03 |
| KR20190025986A (ko) | 2019-03-12 |
| AU2017291827B2 (en) | 2021-10-21 |
| WO2018009597A1 (en) | 2018-01-11 |
| MX389920B (es) | 2025-03-20 |
| CL2023000228A1 (es) | 2023-09-29 |
| EP3481818C0 (en) | 2023-09-06 |
| EP4249488A2 (en) | 2023-09-27 |
| JP2019525913A (ja) | 2019-09-12 |
| US11319308B2 (en) | 2022-05-03 |
| EP3481818A1 (en) | 2019-05-15 |
| AU2017291827A1 (en) | 2019-02-07 |
| IL263995B (en) | 2021-02-28 |
| ES2963563T3 (es) | 2024-03-27 |
| EA201990237A1 (ru) | 2019-08-30 |
| US20210323951A1 (en) | 2021-10-21 |
| MX2019000105A (es) | 2019-04-22 |
| SG11201900096QA (en) | 2019-02-27 |
| NZ750123A (en) | 2025-02-28 |
| US20240059684A1 (en) | 2024-02-22 |
| MA45603A (fr) | 2019-05-15 |
| EP3481818B1 (en) | 2023-09-06 |
| JP7112384B2 (ja) | 2022-08-03 |
| CA3029375A1 (en) | 2018-01-11 |
| BR112019000291A2 (pt) | 2019-04-16 |
| KR102487872B1 (ko) | 2023-01-12 |
| IL263995A (en) | 2019-02-28 |
| EP4249488A3 (en) | 2023-12-20 |
| MX2022001495A (es) | 2022-03-11 |
| US20220227748A1 (en) | 2022-07-21 |
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