BR112021000467A2 - Sal de xinafoato de um composto inibidor de jak - Google Patents
Sal de xinafoato de um composto inibidor de jak Download PDFInfo
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- BR112021000467A2 BR112021000467A2 BR112021000467-0A BR112021000467A BR112021000467A2 BR 112021000467 A2 BR112021000467 A2 BR 112021000467A2 BR 112021000467 A BR112021000467 A BR 112021000467A BR 112021000467 A2 BR112021000467 A2 BR 112021000467A2
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- formula
- subject
- amino
- xinafoate salt
- carboxy
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 53
- 229950000339 xinafoate Drugs 0.000 title claims abstract description 49
- 229940122245 Janus kinase inhibitor Drugs 0.000 title abstract description 4
- 239000000203 mixture Substances 0.000 claims abstract description 54
- 238000000034 method Methods 0.000 claims abstract description 30
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 42
- 238000011282 treatment Methods 0.000 claims description 31
- -1 5-methyl-2 - ((3,4,5-trimethylphenyl) -amino) pyrimidin-4-yl Chemical group 0.000 claims description 30
- 208000006673 asthma Diseases 0.000 claims description 28
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 28
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 5
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- 239000001358 L(+)-tartaric acid Substances 0.000 claims description 3
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/255—Tartaric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
- C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
- C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- 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)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pulmonology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
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| US201862699955P | 2018-07-18 | 2018-07-18 | |
| US62/699,955 | 2018-07-18 | ||
| US201962866013P | 2019-06-25 | 2019-06-25 | |
| US62/866,013 | 2019-06-25 | ||
| PCT/EP2019/069252 WO2020016302A1 (en) | 2018-07-18 | 2019-07-17 | A xinafoate salt of a jak inhibiting compound |
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| BR112021000467A2 true BR112021000467A2 (pt) | 2021-04-06 |
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| BR112021000467-0A BR112021000467A2 (pt) | 2018-07-18 | 2019-07-17 | Sal de xinafoato de um composto inibidor de jak |
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|---|---|
| US (1) | US11149029B2 (https=) |
| EP (1) | EP3823964A1 (https=) |
| JP (2) | JP7422732B2 (https=) |
| KR (1) | KR102849420B1 (https=) |
| CN (2) | CN118580223A (https=) |
| AU (1) | AU2019304014B2 (https=) |
| BR (1) | BR112021000467A2 (https=) |
| CA (1) | CA3105585A1 (https=) |
| IL (1) | IL280025B2 (https=) |
| MA (1) | MA53162A (https=) |
| MX (1) | MX2021000611A (https=) |
| MY (1) | MY209356A (https=) |
| SG (1) | SG11202100240RA (https=) |
| WO (1) | WO2020016302A1 (https=) |
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| CN115260128B (zh) * | 2022-09-21 | 2022-12-09 | 苏州凯瑞医药科技有限公司 | 一种新型jak抑制剂关键中间体的制备方法 |
| GB202316063D0 (en) | 2023-10-20 | 2023-12-06 | Astrazeneca Ab | Dosing regime |
| GB202403369D0 (en) | 2024-03-08 | 2024-04-24 | Astrazeneca Ab | Process and intermediates for the production of a jak1 inhibitor |
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| BRPI0816278A2 (pt) | 2007-09-05 | 2015-09-22 | Pfizer Ltd | forma sal |
| TW201217387A (en) * | 2010-09-15 | 2012-05-01 | Hoffmann La Roche | Azabenzothiazole compounds, compositions and methods of use |
| AP2016009099A0 (en) * | 2013-11-01 | 2016-03-31 | Novartis Ag | Aminoheteroaryl benzamides as kinase inhibitors |
| EP3189045B1 (en) | 2014-08-11 | 2022-02-09 | Sun Pharmaceutical Industries Limited | Novel salts of nilotinib and polymorphs thereof |
| JP6767491B2 (ja) * | 2015-09-25 | 2020-10-14 | ディザル（ジァンスー）ファーマシューティカル・カンパニー・リミテッド | Ｊａｋを阻害するための化合物及び方法 |
| ES2938648T3 (es) | 2017-01-17 | 2023-04-13 | Astrazeneca Ab | Inhibidores selectivos de JAK1 |
| CN106831538B (zh) * | 2017-01-22 | 2019-06-25 | 苏州楚凯药业有限公司 | 托法替尼中间体的制备方法 |
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- 2019-07-17 MY MYPI2021000231A patent/MY209356A/en unknown
- 2019-07-17 US US16/513,781 patent/US11149029B2/en active Active
- 2019-07-17 CN CN201980047093.4A patent/CN112424187B/zh active Active
- 2019-07-17 CA CA3105585A patent/CA3105585A1/en active Pending
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- 2019-07-17 JP JP2021502626A patent/JP7422732B2/ja active Active
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2023
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|---|---|
| JP2024001109A (ja) | 2024-01-09 |
| US11149029B2 (en) | 2021-10-19 |
| CN112424187A (zh) | 2021-02-26 |
| CN112424187B (zh) | 2024-06-21 |
| CA3105585A1 (en) | 2020-01-23 |
| KR20210033474A (ko) | 2021-03-26 |
| JP7644190B2 (ja) | 2025-03-11 |
| MA53162A (fr) | 2021-05-26 |
| KR102849420B1 (ko) | 2025-08-25 |
| AU2019304014A1 (en) | 2021-03-04 |
| US20200062737A1 (en) | 2020-02-27 |
| WO2020016302A1 (en) | 2020-01-23 |
| CN118580223A (zh) | 2024-09-03 |
| IL280025A (en) | 2021-03-01 |
| IL280025B2 (en) | 2025-02-01 |
| IL280025B1 (en) | 2024-10-01 |
| JP2021530526A (ja) | 2021-11-11 |
| WO2020016302A8 (en) | 2020-11-12 |
| SG11202100240RA (en) | 2021-02-25 |
| MY209356A (en) | 2025-07-03 |
| AU2019304014B2 (en) | 2022-08-18 |
| JP7422732B2 (ja) | 2024-01-26 |
| MX2021000611A (es) | 2021-04-13 |
| EP3823964A1 (en) | 2021-05-26 |
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