AR116880A1 - Compuestos de pirimidinodiona bicíclicos sustituidos con tetrahidropirano, forma polimórfica del mismo y el uso de los mismos para el tratamiento del hcm - Google Patents
Compuestos de pirimidinodiona bicíclicos sustituidos con tetrahidropirano, forma polimórfica del mismo y el uso de los mismos para el tratamiento del hcmInfo
- Publication number
- AR116880A1 AR116880A1 ARP190103118A ARP190103118A AR116880A1 AR 116880 A1 AR116880 A1 AR 116880A1 AR P190103118 A ARP190103118 A AR P190103118A AR P190103118 A ARP190103118 A AR P190103118A AR 116880 A1 AR116880 A1 AR 116880A1
- Authority
- AR
- Argentina
- Prior art keywords
- same
- fluoro
- optionally substituted
- hcm
- treatment
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical group C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 title 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 3
- NPPSFOUMKWFJKX-HOTGVXAUSA-N (6S,7S)-6-fluoro-7-(2-fluoro-5-methylphenyl)-3-(oxan-4-yl)-5,6,7,8-tetrahydro-1H-pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound F[C@H]1CC2=C(NC(N(C2=O)C2CCOCC2)=O)N[C@H]1C1=C(C=CC(=C1)C)F NPPSFOUMKWFJKX-HOTGVXAUSA-N 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- JADVOEZJVRXVIF-UHFFFAOYSA-N 5,6,7,8-tetrahydro-1h-pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound N1CCCC2=C1NC(=O)NC2=O JADVOEZJVRXVIF-UHFFFAOYSA-N 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 239000013078 crystal Substances 0.000 abstract 1
- 238000001938 differential scanning calorimetry curve Methods 0.000 abstract 1
- 208000019622 heart disease Diseases 0.000 abstract 1
- 230000001969 hypertrophic effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Steroid Compounds (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hospice & Palliative Care (AREA)
Abstract
Compuestos derivados de 5,6,7,8-tetrahidropirido[2,3-d]pirimidina-2,4(1H,3H)-diona, polimorfo del mismo y composiciones farmacéuticas que los comprenden. Estos compuestos se utilizan en el tratamiento de la cardiopatía hipertrófica (HCM). Reivindicación 1: Un compuesto que tiene la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde el subíndice n es 1 ó 2; cada R¹ es un miembro seleccionado del grupo que consiste de fluoro, cloro, alquilo C₁₋₄ opcionalmente sustituido, haloalquilo C₁₋₄ opcionalmente sustituido, alcoxi C₁₋₄ opcionalmente sustituido, haloalcoxi C₁₋₄ opcionalmente sustituido y alquinilo C₂₋₄ opcionalmente sustituido; en donde al menos un R¹ es fluoro; y uno de R²ᵃ y R²ᵇ es fluoro y el otro de R²ᵃ y R²ᵇ es H. Reivindicación 31: Polimorfo de forma 1 de (6S,7S)-6-fluoro-7-(2-fluoro-5-metilfenil)-3-(tetrahidro-2H-piran-4-il)-5,6,7,8-tetrahidropirido[2,3-d]pirimidina-2,4(1H,3H)-diona caracterizada por al menos uno de: a) un patrón de difracción de rayos X en polvo que tiene dos o más picos expresados en grados 2-q ± 0.2º y seleccionados de 11.3, 12.4, 13.3, 16.5, 17.3, 19.3, 20.4, 21.2, 22.5, 23.2, 25.5, 26.4, 28.2, 29.5, 31.5, 32.9, 34.3, 35.5 y 38.8 grados; b) un termograma DSC que muestra endotermas a aproximadamente 226.05ºC, a aproximadamente 302.47ºC y a aproximadamente 310.13ºC; o c) una estructura cristalina de rayos X sustancialmente igual a la de la figura mostrada a continuación.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862752278P | 2018-10-29 | 2018-10-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR116880A1 true AR116880A1 (es) | 2021-06-23 |
Family
ID=68841171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190103118A AR116880A1 (es) | 2018-10-29 | 2019-10-28 | Compuestos de pirimidinodiona bicíclicos sustituidos con tetrahidropirano, forma polimórfica del mismo y el uso de los mismos para el tratamiento del hcm |
Country Status (29)
| Country | Link |
|---|---|
| US (5) | US11034693B2 (es) |
| EP (2) | EP3873904B1 (es) |
| JP (3) | JP7447110B2 (es) |
| KR (2) | KR102797129B1 (es) |
| CN (3) | CN113056465B (es) |
| AR (1) | AR116880A1 (es) |
| AU (2) | AU2019373206B2 (es) |
| BR (1) | BR112021008077A2 (es) |
| CA (1) | CA3118293A1 (es) |
| CL (1) | CL2021001083A1 (es) |
| CO (1) | CO2021005540A2 (es) |
| DK (1) | DK3873904T3 (es) |
| EA (1) | EA202191152A1 (es) |
| ES (1) | ES2986923T3 (es) |
| FI (1) | FI3873904T3 (es) |
| HR (1) | HRP20241065T1 (es) |
| HU (1) | HUE068265T2 (es) |
| IL (1) | IL282740B1 (es) |
| LT (1) | LT3873904T (es) |
| MX (2) | MX2021004955A (es) |
| PE (1) | PE20211780A1 (es) |
| PL (1) | PL3873904T3 (es) |
| PT (1) | PT3873904T (es) |
| RS (1) | RS65963B1 (es) |
| SG (1) | SG11202104218SA (es) |
| SI (1) | SI3873904T1 (es) |
| SM (1) | SMT202400358T1 (es) |
| TW (3) | TWI837202B (es) |
| WO (1) | WO2020092208A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11649238B2 (en) | 2018-01-17 | 2023-05-16 | Glaxosmithkline Intellectual Property Development Limited | Substituted pyrazolo[1,5-a]pyrimidines as PI4K inhibitors |
| KR102797129B1 (ko) * | 2018-10-29 | 2025-04-18 | 미요카디아, 인크. | 테트라히드로피란 (thp)-치환된 비시클릭-피리미딘디온 화합물 |
| IL300775A (en) | 2020-08-28 | 2023-04-01 | Myokardia Inc | Treatment methods with myosin modulator |
| CN114149423B (zh) * | 2020-09-08 | 2023-12-12 | 江苏恒瑞医药股份有限公司 | 四氢吡啶并嘧啶二酮类衍生物、其制备方法及其在医药上的应用 |
| CN114456163B (zh) * | 2020-11-09 | 2023-08-11 | 江苏恒瑞医药股份有限公司 | 四氢吡啶并嘧啶二酮类衍生物、其制备方法及其在医药上的应用 |
| AU2021381664A1 (en) | 2020-11-20 | 2023-06-15 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Triazine dione derivative, preparation method therefor and application thereof in medicine |
| CA3209557A1 (en) | 2021-03-04 | 2022-09-09 | Bradley P. Morgan | Cardiac sarcomere inhibitors |
| AU2023270440A1 (en) | 2022-05-20 | 2024-12-19 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Crystal forms of triazine dione derivative and preparation method therefor |
| CA3262711A1 (en) | 2022-07-29 | 2024-02-01 | MyoKardia, Inc. | CRYSTALLINE FORMS OF (6S,7S)-6-FLUORO-7-(2-FLUORO-5-METHYLPHENYL)-3-(TETRAHYDRO-2H-PYRAN-4-YL)-5,6,7,8-TETRAHYDROPYRIDO[2,3-D]PYRIMIDINE-2,4(1H,3H)-DIONE |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1142793C (zh) | 1995-06-07 | 2004-03-24 | G·D·瑟尔公司 | 环氧-甾族化合物醛甾酮拮抗剂和血管紧张肽ⅱ拮抗剂联合治疗用于治疗充血性心衰 |
| GB9715892D0 (en) | 1997-07-29 | 1997-10-01 | Zeneca Ltd | Heterocyclic compounds |
| SMT202000071T1 (it) * | 2013-06-21 | 2020-03-13 | Myokardia Inc | Composti di pirimidinadione contro le condizioni cardiache |
| US9663516B2 (en) * | 2014-12-18 | 2017-05-30 | MyoKardia, Inc. | Bicyclic-pyrimidinedione compounds |
| KR102797129B1 (ko) | 2018-10-29 | 2025-04-18 | 미요카디아, 인크. | 테트라히드로피란 (thp)-치환된 비시클릭-피리미딘디온 화합물 |
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2019
- 2019-10-28 KR KR1020217016041A patent/KR102797129B1/ko active Active
- 2019-10-28 JP JP2021523927A patent/JP7447110B2/ja active Active
- 2019-10-28 HU HUE19817827A patent/HUE068265T2/hu unknown
- 2019-10-28 EP EP19817827.9A patent/EP3873904B1/en active Active
- 2019-10-28 FI FIEP19817827.9T patent/FI3873904T3/fi active
- 2019-10-28 US US16/665,897 patent/US11034693B2/en active Active
- 2019-10-28 CN CN201980071171.4A patent/CN113056465B/zh active Active
- 2019-10-28 RS RS20241031A patent/RS65963B1/sr unknown
- 2019-10-28 TW TW108138912A patent/TWI837202B/zh active
- 2019-10-28 PL PL19817827.9T patent/PL3873904T3/pl unknown
- 2019-10-28 DK DK19817827.9T patent/DK3873904T3/da active
- 2019-10-28 PT PT198178279T patent/PT3873904T/pt unknown
- 2019-10-28 CA CA3118293A patent/CA3118293A1/en active Pending
- 2019-10-28 ES ES19817827T patent/ES2986923T3/es active Active
- 2019-10-28 HR HRP20241065TT patent/HRP20241065T1/hr unknown
- 2019-10-28 WO PCT/US2019/058297 patent/WO2020092208A1/en not_active Ceased
- 2019-10-28 BR BR112021008077-5A patent/BR112021008077A2/pt unknown
- 2019-10-28 CN CN202510034967.XA patent/CN119977962A/zh active Pending
- 2019-10-28 EP EP24186221.8A patent/EP4464321B1/en active Active
- 2019-10-28 AR ARP190103118A patent/AR116880A1/es unknown
- 2019-10-28 MX MX2021004955A patent/MX2021004955A/es unknown
- 2019-10-28 SI SI201930816T patent/SI3873904T1/sl unknown
- 2019-10-28 LT LTEPPCT/US2019/058297T patent/LT3873904T/lt unknown
- 2019-10-28 SG SG11202104218SA patent/SG11202104218SA/en unknown
- 2019-10-28 KR KR1020257012076A patent/KR20250053228A/ko active Pending
- 2019-10-28 EA EA202191152A patent/EA202191152A1/ru unknown
- 2019-10-28 PE PE2021000596A patent/PE20211780A1/es unknown
- 2019-10-28 SM SM20240358T patent/SMT202400358T1/it unknown
- 2019-10-28 TW TW113107743A patent/TWI876902B/zh active
- 2019-10-28 TW TW114104487A patent/TW202521537A/zh unknown
- 2019-10-28 CN CN202510034970.1A patent/CN119977963A/zh active Pending
- 2019-10-28 AU AU2019373206A patent/AU2019373206B2/en active Active
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2021
- 2021-04-27 CL CL2021001083A patent/CL2021001083A1/es unknown
- 2021-04-28 IL IL282740A patent/IL282740B1/en unknown
- 2021-04-28 CO CONC2021/0005540A patent/CO2021005540A2/es unknown
- 2021-04-29 MX MX2024004892A patent/MX2024004892A/es unknown
- 2021-12-17 US US17/554,353 patent/US20220106314A1/en not_active Abandoned
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2022
- 2022-06-30 US US17/854,398 patent/US20220340569A1/en not_active Abandoned
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2023
- 2023-08-01 US US18/228,911 patent/US12344607B2/en active Active
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2024
- 2024-02-28 JP JP2024028058A patent/JP7703716B2/ja active Active
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2025
- 2025-02-13 AU AU2025200975A patent/AU2025200975A1/en active Pending
- 2025-05-27 US US19/219,406 patent/US20250282779A1/en active Pending
- 2025-06-25 JP JP2025106973A patent/JP2025138748A/ja active Pending
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