TW202346256A - 結晶edg-2受體拮抗劑之製造方法 - Google Patents
結晶edg-2受體拮抗劑之製造方法 Download PDFInfo
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- TW202346256A TW202346256A TW112107594A TW112107594A TW202346256A TW 202346256 A TW202346256 A TW 202346256A TW 112107594 A TW112107594 A TW 112107594A TW 112107594 A TW112107594 A TW 112107594A TW 202346256 A TW202346256 A TW 202346256A
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- compound
- citric acid
- crystalline form
- formula
- methanol
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- 238000000034 method Methods 0.000 title claims abstract description 130
- 230000008569 process Effects 0.000 title claims description 38
- 239000002464 receptor antagonist Substances 0.000 title description 6
- 229940044551 receptor antagonist Drugs 0.000 title description 6
- 102000004137 Lysophosphatidic Acid Receptors Human genes 0.000 title 1
- 108090000642 Lysophosphatidic Acid Receptors Proteins 0.000 title 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 387
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Classifications
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- C07C231/00—Preparation of carboxylic acid amides
- C07C231/22—Separation; Purification; Stabilisation; Use of additives
- C07C231/24—Separation; Purification
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/54—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
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| US6969529B2 (en) | 2000-09-21 | 2005-11-29 | Elan Pharma International Ltd. | Nanoparticulate compositions comprising copolymers of vinyl pyrrolidone and vinyl acetate as surface stabilizers |
| AU5300000A (en) | 1999-06-01 | 2000-12-18 | Elan Pharma International Limited | Small-scale mill and method thereof |
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| CA2415900A1 (en) | 2000-07-14 | 2002-01-31 | The Uab Research Foundation | Uses for nad synthetase inhibitors |
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| WO2003006628A2 (en) | 2001-07-13 | 2003-01-23 | Virtual Drug Development, Inc. | Nad synthetase inhibitors and uses thereof |
| US20040157919A1 (en) | 2002-01-25 | 2004-08-12 | Yong-Qian Wu | Trisubstituted carbocyclic cyclophilin binding compounds and their use |
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| WO2004099127A1 (en) | 2003-05-07 | 2004-11-18 | Novo Nordisk A/S | Novel compounds as kinase inhibitors |
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| JPWO2005012221A1 (ja) | 2003-08-04 | 2006-09-14 | 小野薬品工業株式会社 | ジフェニルエーテル化合物、その製造方法および用途 |
| US7208601B2 (en) | 2003-08-08 | 2007-04-24 | Mjalli Adnan M M | Aryl and heteroaryl compounds, compositions, and methods of use |
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| US7501538B2 (en) | 2003-08-08 | 2009-03-10 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions and methods of use |
| EP1836182A2 (en) | 2004-11-18 | 2007-09-26 | The Institutes for Pharmaceutical Discovery, LLC | Heterocyclylbiphenyl derivates as protein tyrosine phosphatase inhibitors |
| US20090124654A1 (en) | 2005-03-01 | 2009-05-14 | Mjalli Adnan M M | Aryl and Heteroaryl Compounds, Compositions, Methods of Use |
| PL2003132T3 (pl) | 2006-04-03 | 2014-10-31 | Astellas Pharma Inc | Pochodne oksadiazolu jako agoniści S1P1 |
| US8969386B2 (en) | 2007-05-09 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| PT2303270T (pt) | 2008-05-05 | 2017-08-25 | Sanofi Sa | Derivados fundidos do ácido ciclopentanocarboxílico substituídos por acilamino e sua utilização como produtos farmacêuticos |
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| WO2012016133A2 (en) | 2010-07-29 | 2012-02-02 | President And Fellows Of Harvard College | Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers |
| CN112184094B (zh) | 2019-07-03 | 2024-08-20 | 北京京东振世信息技术有限公司 | 一种地址信息采集方法和装置 |
| KR20220161476A (ko) | 2020-04-02 | 2022-12-06 | 호라이즌 테라퓨틱스 아일랜드 디에이씨 | 전신 경화증의 치료 방법 |
| TW202227390A (zh) | 2020-08-31 | 2022-07-16 | 法商賽諾菲公司 | 結晶型edg-2受體拮抗劑及製造方法 |
| US12391640B2 (en) | 2022-03-02 | 2025-08-19 | Horizon Therapeutics Ireland Dac | Process of making a crystalline EDG-2 receptor antagonist |
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- 2023-03-01 JP JP2024551569A patent/JP2025507801A/ja active Pending
- 2023-03-01 WO PCT/IB2023/000120 patent/WO2023166346A1/en not_active Ceased
- 2023-03-01 EP EP23718334.8A patent/EP4486719A1/en active Pending
- 2023-03-01 CA CA3251849A patent/CA3251849A1/en active Pending
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- 2023-03-01 AU AU2023228095A patent/AU2023228095A1/en active Pending
- 2023-03-02 TW TW112107594A patent/TW202346256A/zh unknown
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| JP2025507801A (ja) | 2025-03-21 |
| CA3251849A1 (en) | 2023-09-07 |
| WO2023166346A1 (en) | 2023-09-07 |
| EP4486719A1 (en) | 2025-01-08 |
| MX2024010565A (es) | 2024-09-06 |
| US12391640B2 (en) | 2025-08-19 |
| US20230295073A1 (en) | 2023-09-21 |
| AU2023228095A1 (en) | 2024-08-15 |
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