KR20230118142A - 심부전 치료용 rxfp1 조절제로서의 4-(2-플루오로-4-메톡시-5-3-(((1-메틸시클로부틸)메틸)카바모일)바이시클로[2.2.1]헵탄-2-일)카바모일)페녹시)-1-메틸시클로헥산-1-카복실산유도체 및 유사 화합물 - Google Patents
심부전 치료용 rxfp1 조절제로서의 4-(2-플루오로-4-메톡시-5-3-(((1-메틸시클로부틸)메틸)카바모일)바이시클로[2.2.1]헵탄-2-일)카바모일)페녹시)-1-메틸시클로헥산-1-카복실산유도체 및 유사 화합물 Download PDFInfo
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- KR20230118142A KR20230118142A KR1020237022785A KR20237022785A KR20230118142A KR 20230118142 A KR20230118142 A KR 20230118142A KR 1020237022785 A KR1020237022785 A KR 1020237022785A KR 20237022785 A KR20237022785 A KR 20237022785A KR 20230118142 A KR20230118142 A KR 20230118142A
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- Prior art keywords
- carbamoyl
- fluoro
- carboxylic acid
- bicyclo
- methoxy
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07C233/00—Carboxylic acid amides
- C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
- C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
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- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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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
- A61K31/275—Nitriles; Isonitriles
- A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/57—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
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- 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
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- 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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- 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
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
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- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
- C07D237/20—Nitrogen atoms
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
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- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- C07C2602/42—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing seven carbon atoms
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- Cardiology (AREA)
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- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyridine Compounds (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063122690P | 2020-12-08 | 2020-12-08 | |
| US63/122,690 | 2020-12-08 | ||
| PCT/EP2021/084673 WO2022122773A1 (en) | 2020-12-08 | 2021-12-07 | 4-(2-fluoro-4-methoxy-5-3-(((1-methylcyclobutyl)methyl)carbamoyl)bicyclo[2.2.1]heptan-2-yl)carbamoyl)phenoxy)-1-methylcyclohexane-1-carboxylic acid derivatives and similar compounds as rxfp1 modulators for the treatment of heart failure |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20230118142A true KR20230118142A (ko) | 2023-08-10 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020237022785A Pending KR20230118142A (ko) | 2020-12-08 | 2021-12-07 | 심부전 치료용 rxfp1 조절제로서의 4-(2-플루오로-4-메톡시-5-3-(((1-메틸시클로부틸)메틸)카바모일)바이시클로[2.2.1]헵탄-2-일)카바모일)페녹시)-1-메틸시클로헥산-1-카복실산유도체 및 유사 화합물 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US11667602B2 (https=) |
| EP (1) | EP4259605A1 (https=) |
| JP (1) | JP2023552793A (https=) |
| KR (1) | KR20230118142A (https=) |
| CN (1) | CN116547270A (https=) |
| AR (1) | AR124193A1 (https=) |
| AU (1) | AU2021395353B2 (https=) |
| CA (1) | CA3203024A1 (https=) |
| CL (1) | CL2023001572A1 (https=) |
| CO (1) | CO2023008303A2 (https=) |
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| US20250221966A1 (en) * | 2021-10-29 | 2025-07-10 | Bristol-Myers Squibb Company | Rxfp1 agonists |
| US20250268903A1 (en) * | 2021-10-29 | 2025-08-28 | Bristol-Myers Squibb Company | Rxfp1 agonists |
| KR20240095290A (ko) * | 2021-10-29 | 2024-06-25 | 브리스톨-마이어스 스큅 컴퍼니 | 심부전의 치료를 위한 rxfp1 조정제 |
| ES3062200T3 (en) * | 2021-10-29 | 2026-04-09 | Bristol Myers Squibb Co | Rxfp1 agonists |
| US20260069558A1 (en) * | 2022-06-07 | 2026-03-12 | Astrazeneca Ab | Rxfp1 modulators for treating resistant hypertension or heart failure with pulmonary hypertension |
| CN119630638A (zh) * | 2022-06-07 | 2025-03-14 | 阿斯利康(瑞典)有限公司 | Rxfp1调节剂的固体形式 |
| US20260069559A1 (en) * | 2022-06-07 | 2026-03-12 | Astrazeneca Ab | Combinations of rxfp1 modulators and sglt2 inhibitors |
| CN121605099A (zh) * | 2023-08-10 | 2026-03-03 | 深圳信立泰药业股份有限公司 | 一种rxfp1受体调节剂及其制备方法和医药用途 |
| CN121729228A (zh) | 2023-08-15 | 2026-03-24 | 阿斯利康(瑞典)有限公司 | 在治疗心力衰竭中使用的化合物azd5462 |
| TW202530177A (zh) * | 2023-10-13 | 2025-08-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 醯胺取代的環烷基類化合物、其製備方法及其在醫藥上的應用 |
| WO2025106780A1 (en) | 2023-11-17 | 2025-05-22 | Eli Lilly And Company | Rxfp1 receptor agonists |
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| US5223534A (en) * | 1989-12-04 | 1993-06-29 | G. D. Searle & Co. | Benzofuuranyl/benofuranylaklyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino acid derivatives |
| WO2004041795A1 (en) * | 2002-10-30 | 2004-05-21 | Guilford Pharmaceuticals Inc. | Novel inhibitors of dipeptidyl peptidase iv |
| US9452973B2 (en) * | 2012-05-04 | 2016-09-27 | The United States Of America, As Represented By The Secretary Department Of Health And Human Services | Modulators of the relaxin receptor 1 |
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| US20230078576A1 (en) | 2023-03-16 |
| ECSP23050133A (es) | 2023-08-31 |
| EP4259605A1 (en) | 2023-10-18 |
| WO2022122773A1 (en) | 2022-06-16 |
| TW202237559A (zh) | 2022-10-01 |
| PE20240655A1 (es) | 2024-04-04 |
| JP2023552793A (ja) | 2023-12-19 |
| AU2021395353A1 (en) | 2023-07-13 |
| CO2023008303A2 (es) | 2023-09-18 |
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| MX2023006178A (es) | 2023-06-08 |
| US20230348363A1 (en) | 2023-11-02 |
| CA3203024A1 (en) | 2022-06-16 |
| DOP2023000111A (es) | 2023-07-09 |
| UY39559A (es) | 2022-06-30 |
| CN116547270A (zh) | 2023-08-04 |
| IL303220A (en) | 2023-07-01 |
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