NZ734993B2 - Salts of pi3k inhibitor and processes for their preparation - Google Patents
Salts of pi3k inhibitor and processes for their preparation Download PDFInfo
- Publication number
- NZ734993B2 NZ734993B2 NZ734993A NZ73499316A NZ734993B2 NZ 734993 B2 NZ734993 B2 NZ 734993B2 NZ 734993 A NZ734993 A NZ 734993A NZ 73499316 A NZ73499316 A NZ 73499316A NZ 734993 B2 NZ734993 B2 NZ 734993B2
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- New Zealand
- Prior art keywords
- salt
- processes
- salts
- preparation
- pi3k inhibitor
- Prior art date
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- 150000003839 salts Chemical class 0.000 title claims abstract 6
- 239000012828 PI3K inhibitor Substances 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- -1 4-aminomethyl-1H-pyrazolo[3,4-d]pyrimidin- 1-yl Chemical group 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 1
- ZQPDJCIXJHUERQ-QWRGUYRKSA-N (4r)-4-[3-[(1s)-1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl]pyrrolidin-2-one Chemical compound CCOC1=C([C@H](C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(F)=C1[C@@H]1CNC(=O)C1 ZQPDJCIXJHUERQ-QWRGUYRKSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 150000003906 phosphoinositides Chemical class 0.000 abstract 1
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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
- A61K31/495—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
-
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- C—CHEMISTRY; METALLURGY
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- 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
- 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
Abstract
The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kd), as well as a salt form and intermediates related thereto.
Claims (4)
1. A salt which is (R)(3-((S)(4-aminomethyl-1H-pyrazolo[3,4-d]pyrimidin- 1-yl)ethyl)chloroethoxyfluorophenyl)pyrrolidinone hydrochloric acid salt that is crystalline.
2. The salt of claim 1 that is a 1:1 stoichiometric ratio of (R)(3-((S)(4-amino- 3-methyl-1H-pyrazolo[3,4-d]pyrimidinyl)ethyl)chloroethoxy fluorophenyl)pyrrolidinone to hydrochloric acid.
3. The salt of claim 1 or 2, characterized by a DSC thermogram having an endothermic peak at about 207 °C.
4. The salt of any one of claims 1 to 3, having a DSC thermogram substantially as shown in
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NZ773226A NZ773226B2 (en) | 2016-02-26 | Salts of pi3k inhibitor and processes for their preparation |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562121697P | 2015-02-27 | 2015-02-27 | |
| PCT/US2016/019741 WO2016138363A1 (en) | 2015-02-27 | 2016-02-26 | Salts of pi3k inhibitor and processes for their preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NZ734993A NZ734993A (en) | 2024-03-22 |
| NZ734993B2 true NZ734993B2 (en) | 2024-06-25 |
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