ES2980885T3 - Polimorfos de (R)-N-(5-(5-etil-1,2,4-oxadiazol-3-il)-2,3-dihidro-1H-inden-1-il)-1-metil-1H-pirazol-4-carboxamida - Google Patents
Polimorfos de (R)-N-(5-(5-etil-1,2,4-oxadiazol-3-il)-2,3-dihidro-1H-inden-1-il)-1-metil-1H-pirazol-4-carboxamida Download PDFInfo
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- ES2980885T3 ES2980885T3 ES20753562T ES20753562T ES2980885T3 ES 2980885 T3 ES2980885 T3 ES 2980885T3 ES 20753562 T ES20753562 T ES 20753562T ES 20753562 T ES20753562 T ES 20753562T ES 2980885 T3 ES2980885 T3 ES 2980885T3
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- inden
- ethyl
- pyrazole
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- 238000007634 remodeling Methods 0.000 description 1
- 239000002461 renin inhibitor Substances 0.000 description 1
- 229940086526 renin-inhibitors Drugs 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 230000004043 responsiveness Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 238000010955 robust manufacturing process Methods 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical class O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
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- 210000002966 serum Anatomy 0.000 description 1
- 208000013220 shortness of breath Diseases 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- 201000002859 sleep apnea Diseases 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000012265 solid product Substances 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 229940035044 sorbitan monolaurate Drugs 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 238000011272 standard treatment Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- IFOWJFMJQQROCQ-GFCCVEGCSA-N tert-butyl N-[(1R)-5-[(Z)-N'-hydroxycarbamimidoyl]-2,3-dihydro-1H-inden-1-yl]carbamate Chemical compound ONC(=N)C=1C=C2CC[C@H](C2=CC=1)NC(OC(C)(C)C)=O IFOWJFMJQQROCQ-GFCCVEGCSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
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- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 229940117013 triethanolamine oleate Drugs 0.000 description 1
- UPCXAARSWVHVLY-UHFFFAOYSA-N tris(2-hydroxyethyl)azanium;acetate Chemical compound CC(O)=O.OCCN(CCO)CCO UPCXAARSWVHVLY-UHFFFAOYSA-N 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
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- 206010047302 ventricular tachycardia Diseases 0.000 description 1
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Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- C07D413/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962875350P | 2019-07-17 | 2019-07-17 | |
| PCT/US2020/042387 WO2021011807A1 (en) | 2019-07-17 | 2020-07-16 | Polymorphs of (r)-n-(5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1h-inden-1-yl)-1-methyl-1h-pyrazole-4-carboxamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2980885T3 true ES2980885T3 (es) | 2024-10-03 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES20753562T Active ES2980885T3 (es) | 2019-07-17 | 2020-07-16 | Polimorfos de (R)-N-(5-(5-etil-1,2,4-oxadiazol-3-il)-2,3-dihidro-1H-inden-1-il)-1-metil-1H-pirazol-4-carboxamida |
Country Status (25)
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|---|---|
| US (1) | US20220315571A1 (https=) |
| EP (2) | EP3999180B1 (https=) |
| JP (2) | JP7624431B2 (https=) |
| KR (1) | KR20220084008A (https=) |
| CN (3) | CN114555590B (https=) |
| AU (1) | AU2020313965A1 (https=) |
| BR (1) | BR112022000494A2 (https=) |
| CA (1) | CA3144975A1 (https=) |
| CL (1) | CL2022000054A1 (https=) |
| DK (1) | DK3999180T3 (https=) |
| ES (1) | ES2980885T3 (https=) |
| FI (1) | FI3999180T3 (https=) |
| HR (1) | HRP20240713T1 (https=) |
| HU (1) | HUE066891T2 (https=) |
| IL (1) | IL289875A (https=) |
| LT (1) | LT3999180T (https=) |
| MX (1) | MX2022000504A (https=) |
| PH (1) | PH12022550123A1 (https=) |
| PL (1) | PL3999180T3 (https=) |
| PT (1) | PT3999180T (https=) |
| RS (1) | RS65611B1 (https=) |
| SI (1) | SI3999180T1 (https=) |
| SM (1) | SMT202400224T1 (https=) |
| TW (1) | TWI865562B (https=) |
| WO (1) | WO2021011807A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019144041A1 (en) | 2018-01-19 | 2019-07-25 | Cytokinetics, Inc. | Dihydrobenzofuran and inden analogs as cardiac sarcomere inhibitors |
| JP7610985B2 (ja) | 2018-06-26 | 2025-01-09 | サイトキネティックス， インコーポレイテッド | 心臓サルコメア阻害剤 |
| JP7438148B2 (ja) | 2018-06-26 | 2024-02-26 | サイトキネティックス， インコーポレイテッド | 心臓サルコメア阻害剤 |
| MA53491A (fr) | 2018-08-31 | 2021-09-15 | Cytokinetics Inc | Inhibiteurs de sarcomes cardiaques |
| CN117083275A (zh) | 2021-03-04 | 2023-11-17 | 赛特凯恩蒂克公司 | 心脏肌节抑制剂 |
| PT4370116T (pt) | 2021-07-16 | 2025-03-14 | Cytokinetics Inc | Regimes de administração de aficamten para o tratamento da cardiomiopatia hipertrófica obstrutiva |
| MX2024001294A (es) | 2021-08-03 | 2024-02-13 | Cytokinetics Inc | Proceso para la preparacion de aficamten. |
| WO2024020468A1 (en) | 2022-07-20 | 2024-01-25 | Cytokinetics, Incorporated | Methods for treating non-obstructive hypertrophic cardiomyopathy |
| EP4565230A1 (en) | 2022-08-04 | 2025-06-11 | Cytokinetics, Inc. | Methods for treating obstructive hypertrophic cardiomyopathy |
| WO2024134498A1 (en) | 2022-12-22 | 2024-06-27 | Assia Chemical Industries Ltd. | Solid state forms of aficamten and process for preparation thereof |
| WO2024179422A1 (zh) * | 2023-03-02 | 2024-09-06 | 苏州科睿思制药有限公司 | Aficamten的共晶及其制备方法和用途 |
| US20250295639A1 (en) | 2024-03-20 | 2025-09-25 | Cytokinetics, Incorporated | Methods for treating heart diseases |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019144041A1 (en) | 2018-01-19 | 2019-07-25 | Cytokinetics, Inc. | Dihydrobenzofuran and inden analogs as cardiac sarcomere inhibitors |
| MX2024001294A (es) * | 2021-08-03 | 2024-02-13 | Cytokinetics Inc | Proceso para la preparacion de aficamten. |
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2020
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- 2020-07-16 CN CN202080059660.0A patent/CN114555590B/zh active Active
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- 2020-07-16 CN CN202411172321.XA patent/CN119119018A/zh active Pending
- 2020-07-16 ES ES20753562T patent/ES2980885T3/es active Active
- 2020-07-16 PT PT207535626T patent/PT3999180T/pt unknown
- 2020-07-16 RS RS20240598A patent/RS65611B1/sr unknown
- 2020-07-16 MX MX2022000504A patent/MX2022000504A/es unknown
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- 2020-07-16 PL PL20753562.6T patent/PL3999180T3/pl unknown
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- 2020-07-16 SI SI202030443T patent/SI3999180T1/sl unknown
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- 2020-07-16 WO PCT/US2020/042387 patent/WO2021011807A1/en not_active Ceased
- 2020-07-16 CA CA3144975A patent/CA3144975A1/en active Pending
- 2020-07-16 HR HRP20240713TT patent/HRP20240713T1/hr unknown
- 2020-07-16 US US17/627,599 patent/US20220315571A1/en active Pending
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- 2020-07-16 AU AU2020313965A patent/AU2020313965A1/en active Pending
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2022
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- 2022-01-16 IL IL289875A patent/IL289875A/en unknown
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2025
- 2025-01-20 JP JP2025007662A patent/JP7755090B2/ja active Active
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