RU2020110358A - Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор- пиридин-3-ил]-пиразоло[1,5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы - Google Patents
Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор- пиридин-3-ил]-пиразоло[1,5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы Download PDFInfo
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- RU2020110358A RU2020110358A RU2020110358A RU2020110358A RU2020110358A RU 2020110358 A RU2020110358 A RU 2020110358A RU 2020110358 A RU2020110358 A RU 2020110358A RU 2020110358 A RU2020110358 A RU 2020110358A RU 2020110358 A RU2020110358 A RU 2020110358A
- Authority
- RU
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- Prior art keywords
- fluoro
- inositol
- solid form
- compound
- laborated
- Prior art date
Links
- 239000007787 solid Substances 0.000 title claims 11
- LPCQBTAOTIZGAE-UHFFFAOYSA-N 2h-pyrimidine-1-carboxamide Chemical compound NC(=O)N1CN=CC=C1 LPCQBTAOTIZGAE-UHFFFAOYSA-N 0.000 title 1
- GLKBURZOEQPSNS-UHFFFAOYSA-N C1C=CN(N1N)C2=CC(=C(N=C2)F)F Chemical compound C1C=CN(N1N)C2=CC(=C(N=C2)F)F GLKBURZOEQPSNS-UHFFFAOYSA-N 0.000 title 1
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 title 1
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 title 1
- 229960000367 inositol Drugs 0.000 title 1
- 150000004001 inositols Chemical class 0.000 title 1
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 10
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 4
- 235000002906 tartaric acid Nutrition 0.000 claims 4
- 239000011975 tartaric acid Substances 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 230000005855 radiation Effects 0.000 claims 2
- 239000012458 free base Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (12)
1. Твердая форма соединения формулы I-1:
где эту форму выбирают из группы, состоящей из соединения I-1 в виде безводного свободного основания, соединения I-1 в виде гидрата или соединения I-1 в виде аддукта с винной кислотой.
2. Твердая форма по п. 1, где эта форма представляет собой кристаллическое соединение I-1 в виде гидрата.
3. Твердая форма по п. 2, где кристаллическое соединение I-1 в виде гидрата имеет соотношение соединения I-1 к воде, составляющее 1:3.
4. Твердая форма по п. 2, характеризующаяся потерей массы от примерно 12,6% в диапазоне температуры от примерно 40°С до примерно 100°С.
5. Твердая форма по п. 2, характеризующаяся одним или более пиками, выраженными значениями 2-тета ± 0,2, равными примерно 27,5, 20,6 и 9,7 градусов, на порошковой рентгеновской дифрактограмме, полученной с использованием излучения Cu-K-альфа.
6. Твердая форма по п. 2, характеризующаяся порошковой рентгеновской дифрактограммой, по существу такой же, как приведена на Фиг.1b.
7. Твердая форма по п. 1, где форма представляет собой кристаллическое соединение I-1 в виде аддукта с винной кислотой.
8. Твердая форма по п. 7, где кристаллическое соединение I-1в виде аддукта с винной кислотой имеет соотношение соединения I-1 к винной кислоте, составляющее 1:1.
9. Твердая форма по п. 7, характеризующаяся одним или более пиками, выраженными значениями 2-тета ± 0,2, равными примерно 7,1, 18,3 и 13,2 градусов, на порошковой рентгенограмме, полученной с использованием излучения Cu-K-альфа.
10. Твердая форма по п. 7, характеризующаяся порошковой рентгенограммой, по существу такой же, как представлена на Фиг. 1с.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462008277P | 2014-06-05 | 2014-06-05 | |
| US62/008,277 | 2014-06-05 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016151208A Division RU2719583C2 (ru) | 2014-06-05 | 2015-05-28 | Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор-пиридин-3-ил]-пиразоло[1, 5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы |
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| Publication Number | Publication Date |
|---|---|
| RU2020110358A true RU2020110358A (ru) | 2020-04-30 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016151208A RU2719583C2 (ru) | 2014-06-05 | 2015-05-28 | Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор-пиридин-3-ил]-пиразоло[1, 5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы |
| RU2020110358A RU2020110358A (ru) | 2014-06-05 | 2015-05-28 | Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор- пиридин-3-ил]-пиразоло[1,5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2016151208A RU2719583C2 (ru) | 2014-06-05 | 2015-05-28 | Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор-пиридин-3-ил]-пиразоло[1, 5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US9670215B2 (ru) |
| EP (1) | EP3152212B9 (ru) |
| JP (2) | JP6568111B2 (ru) |
| KR (1) | KR102575125B1 (ru) |
| CN (2) | CN110590787A (ru) |
| AU (2) | AU2015271030B2 (ru) |
| BR (1) | BR112016028273B1 (ru) |
| CA (1) | CA2950587C (ru) |
| DK (1) | DK3152212T3 (ru) |
| ES (1) | ES2777608T3 (ru) |
| HR (1) | HRP20200186T1 (ru) |
| IL (1) | IL249361B (ru) |
| LT (1) | LT3152212T (ru) |
| MX (2) | MX373102B (ru) |
| PL (1) | PL3152212T3 (ru) |
| PT (1) | PT3152212T (ru) |
| RS (1) | RS60013B1 (ru) |
| RU (2) | RU2719583C2 (ru) |
| SG (2) | SG11201610197XA (ru) |
| SI (1) | SI3152212T1 (ru) |
| WO (1) | WO2015187451A1 (ru) |
| ZA (1) | ZA201700035B (ru) |
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| EP3878851A1 (en) | 2011-09-30 | 2021-09-15 | Vertex Pharmaceuticals Incorporated | Process for making compounds useful as inhibitors of atr kinase |
| CN103957917A (zh) | 2011-09-30 | 2014-07-30 | 沃泰克斯药物股份有限公司 | 用atr抑制剂治疗胰腺癌和非小细胞肺癌 |
| HK1205028A1 (en) | 2012-04-05 | 2015-12-11 | 沃泰克斯药物股份有限公司 | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
| HRP20180859T1 (hr) | 2012-12-07 | 2018-07-13 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-(5-fluoro-4-(4-(4-(oksetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamid kao inhibitor atr kinaze |
| EP2970286A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| HRP20192183T1 (hr) * | 2013-12-06 | 2020-02-21 | Vertex Pharmaceuticals Inc. | Spoj 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-karboksamida koristan kao inhibitor atr kinase, njegova priprava, različiti kruti oblici te njegovi radioaktivno označeni derivati |
| EP3152212B9 (en) | 2014-06-05 | 2020-05-27 | Vertex Pharmaceuticals Inc. | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
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| EP3630116B1 (en) | 2017-05-26 | 2024-05-01 | The Board Of Regents Of The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
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