TWI865562B - (r)-n-(5-(5-乙基-1,2,4-二唑-3-基)-2,3-二氫-1h-茚-1-基)-1-甲基-1h-吡唑-4-羧醯胺之多晶型物 - Google Patents
(r)-n-(5-(5-乙基-1,2,4-二唑-3-基)-2,3-二氫-1h-茚-1-基)-1-甲基-1h-吡唑-4-羧醯胺之多晶型物 Download PDFInfo
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- TWI865562B TWI865562B TW109124093A TW109124093A TWI865562B TW I865562 B TWI865562 B TW I865562B TW 109124093 A TW109124093 A TW 109124093A TW 109124093 A TW109124093 A TW 109124093A TW I865562 B TWI865562 B TW I865562B
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- 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
- 229920006395 saturated elastomer Polymers 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
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- 235000017281 sodium acetate Nutrition 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
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- 208000011580 syndromic disease Diseases 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
- 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
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
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- UPCXAARSWVHVLY-UHFFFAOYSA-N tris(2-hydroxyethyl)azanium;acetate Chemical compound CC(O)=O.OCCN(CCO)CCO UPCXAARSWVHVLY-UHFFFAOYSA-N 0.000 description 1
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Classifications
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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
- A61K31/41—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 | |
| US62/875,350 | 2019-07-17 |
Publications (2)
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|---|---|
| TW202116763A TW202116763A (zh) | 2021-05-01 |
| TWI865562B true TWI865562B (zh) | 2024-12-11 |
Family
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| TW109124093A TWI865562B (zh) | 2019-07-17 | 2020-07-16 | (r)-n-(5-(5-乙基-1,2,4-二唑-3-基)-2,3-二氫-1h-茚-1-基)-1-甲基-1h-吡唑-4-羧醯胺之多晶型物 |
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| EP (2) | EP3999180B1 (https=) |
| JP (2) | JP7624431B2 (https=) |
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| 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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2022
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2025
- 2025-01-20 JP JP2025007662A patent/JP7755090B2/ja active Active
Non-Patent Citations (1)
| Title |
|---|
| 期刊 Taub PR, et.al., Perturbations in skeletal muscle sarcomere structure in patients with heart failure and type 2 diabetes: restorative effects of (-)-epicatechin-rich cocoa, Clin Sci (Lond), 125(8), 20131001, page 383-389. |
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