AR102569A1 - SYNTHESIS OF PI3K INHIBITOR, CRYSTAL AND SALES FORMS OF THE SAME AND A PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS - Google Patents
SYNTHESIS OF PI3K INHIBITOR, CRYSTAL AND SALES FORMS OF THE SAME AND A PHARMACEUTICAL COMPOSITION THAT UNDERSTANDSInfo
- Publication number
- AR102569A1 AR102569A1 ARP150103618A ARP150103618A AR102569A1 AR 102569 A1 AR102569 A1 AR 102569A1 AR P150103618 A ARP150103618 A AR P150103618A AR P150103618 A ARP150103618 A AR P150103618A AR 102569 A1 AR102569 A1 AR 102569A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- understands
- synthesis
- crystal
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000012828 PI3K inhibitor Substances 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 10
- 150000003839 salts Chemical class 0.000 abstract 4
- 238000000034 method Methods 0.000 abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 2
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Método para preparar un compuesto de fórmula (1) o una sal del mismo, con compuestos intermediarios, con el uso de estos en la preparación de dicho compuesto de fórmula (1) o una sal del mismo. También se relaciona con formas cristalinas, la forma A, de un compuesto de fórmula (1), composiciones farmacéuticas y usos de las mismas. Reivindicación 27: El método de acuerdo con cualquiera de las reivindicaciones 1 a 26, donde el compuesto de fórmula (1) se prepara por medio de los pasos, infra del Esquema [1]. Reivindicación 28: Un compuesto caracterizado porque se selecciona entre un compuesto de fórmula (10), o una sal del mismo, un compuesto de fórmula (9), o una sal del mismo, un compuesto de fórmula (9a), un compuesto de fórmula (8), o un compuesto de fórmula (5). Reivindicación 33: La forma A de acuerdo con la reivindicación 32 caracterizada porque tiene un patrón XRPD con picos a 5,6, 7,5, 10,2, 11,1, 12,2, 15,5, 22,2 º2q ± 0,2 º2q. Reivindicación 34: La forma A de acuerdo con la reivindicación 33 caracterizada porque tiene un patrón XRPD con picos adicionales a 5,8, 9,8, 13,2, 15,1, 16,3, 17,5, 18,9, 20,2, 20,7, 21,3, 21,6, 22,6, 23,1, 23,4, 23,9, 24,4, 24,9, 25,1, 25,4, 25,8, 26,6, 27,2, 27,6, 28,1, 28,6, 28,9, 29,2, 29,9, 30,4, 30,8, 32,0, 32,7, 33,9, 36,3, 37,4 º2q ± 0,2 º2q.Method for preparing a compound of formula (1) or a salt thereof, with intermediates, with the use of these in the preparation of said compound of formula (1) or a salt thereof. It also relates to crystalline forms, form A, of a compound of formula (1), pharmaceutical compositions and uses thereof. Claim 27: The method according to any one of claims 1 to 26, wherein the compound of formula (1) is prepared by means of the steps, infra of Scheme [1]. Claim 28: A compound characterized in that it is selected from a compound of formula (10), or a salt thereof, a compound of formula (9), or a salt thereof, a compound of formula (9a), a compound of formula (8), or a compound of formula (5). Claim 33: Form A according to claim 32 characterized in that it has an XRPD pattern with peaks at 5.6, 7.5, 10.2, 11.1, 12.2, 15.5, 22.2 º2q ± 0.2 º2q. Claim 34: Form A according to claim 33 characterized in that it has an XRPD pattern with additional peaks at 5.8, 9.8, 13.2, 15.1, 16.3, 17.5, 18.9, 20.2, 20.7, 21.3, 21.6, 22.6, 23.1, 23.4, 23.9, 24.4, 24.9, 25.1, 25.4, 25, 8, 26.6, 27.2, 27.6, 28.1, 28.6, 28.9, 29.2, 29.9, 30.4, 30.8, 32.0, 32.7, 33.9, 36.3, 37.4 º2q ± 0.2 º2q.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14192207 | 2014-11-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR102569A1 true AR102569A1 (en) | 2017-03-08 |
Family
ID=51866062
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150103618A AR102569A1 (en) | 2014-11-07 | 2015-11-06 | SYNTHESIS OF PI3K INHIBITOR, CRYSTAL AND SALES FORMS OF THE SAME AND A PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS |
Country Status (4)
| Country | Link |
|---|---|
| AR (1) | AR102569A1 (en) |
| TW (1) | TW201625632A (en) |
| UY (1) | UY36393A (en) |
| WO (1) | WO2016071382A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018215282A1 (en) | 2017-05-26 | 2018-11-29 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and pi3k inhibitors |
| CN112824387B (en) * | 2019-11-21 | 2023-03-21 | 济南尚博生物科技有限公司 | 2-methyl nicotinate and preparation method and application thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA113280C2 (en) * | 2010-11-11 | 2017-01-10 | AMINOSPIRT-SUBSTITUTED Derivatives of 2,3-Dihydroimimidase $ 1,2-c] QINAZOLINE, SUITABLE FOR THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS, DISEASES AND DISEASES |
-
2015
- 2015-11-04 WO PCT/EP2015/075670 patent/WO2016071382A1/en not_active Ceased
- 2015-11-05 UY UY0001036393A patent/UY36393A/en not_active Application Discontinuation
- 2015-11-06 TW TW104136724A patent/TW201625632A/en unknown
- 2015-11-06 AR ARP150103618A patent/AR102569A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW201625632A (en) | 2016-07-16 |
| WO2016071382A1 (en) | 2016-05-12 |
| UY36393A (en) | 2016-06-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |