SI2909188T1 - Nov postopek za izdelavo spojin za uporabo pri zdravljenju raka - Google Patents
Nov postopek za izdelavo spojin za uporabo pri zdravljenju raka Download PDFInfo
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- SI2909188T1 SI2909188T1 SI201331045T SI201331045T SI2909188T1 SI 2909188 T1 SI2909188 T1 SI 2909188T1 SI 201331045 T SI201331045 T SI 201331045T SI 201331045 T SI201331045 T SI 201331045T SI 2909188 T1 SI2909188 T1 SI 2909188T1
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Classifications
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- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- 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
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
Claims (22)
- NOV POSTOPEK ZA IZDELAVO SPOJIN ZA UPORABO PRI ZDRAVUENJU RAKA Patentni zahtevki1. Postopek za izdelavo spojine s formulo I:pri čemer: je A arilen ali heteroarilen,opcijsko substituiran z eno, dvema, tremi ali štirimi skupinami, izbranimi med R6, R7, R8 in R9, vsaka izmed teh je neodvisno izbrana med vodikom, halom, (Ci-C8)alkilom, halo(Ci-C8)alkilom, hidroksijem, (Ci-C6)alkoksijem in halo(Ci-Cejalkoksijem; je X alkil, halo, halo(Ci-C8)alkil ali halo(Ci-C8)alkoksi; so R1, R2, R3 in R4 vsak neodvisno vodik, (Ci-C8)alkil ali halo(Ci-C8)alkil; je R5 vodik, halo ali (Ci-C8)alkil; obsegajoč: stikanje spojine s formulo IIa-l, pri čemer sta X in R5, kot sta definirana zgoraj, s spojino s formulo II-l, pri čemer je R10 F, Br, Cl, I ali -OSO2-CF3 in R11 je H ali zaščitna skupina, da dobimo spojino s formulo I:
- 2. Postopek po zahtevku 1, pri čemer omenjeni postopek je postopek za pripravo spojine s formulo Γ, ki obsega stikanje spojine s formulo IIa s spojino s formulo II:
- 3. Postopek po zahtevku 2, ki nadalje obsega močno osnovo, pri čemer je močna osnova izbrana iz skupine, ki sestoji iz butillitija, t-butillitija, litijevih, natrijevih ali kalijevih soli mono ali bis substituiranega alkila ali aromatskih aminov in sililalkila ali sililaromatskih aminov.
- 4. Postopek po zahtevku 2, pri čemer je omenjena spojina s formulo II pripravljena s hidrogenizacijo spojine s formulo III, da dobimo spojino s formulo II:
- 5. Spojina po zahtevku 4, pri čemer je omenjena spojina III pripravljena z reagiranjem spojine s formulo IV s spojino s formulo IVa, da dobimo spojino s formulo III:
- 6. Postopek po zahtevku 5, pri čemer se omenjeno spojino s formulo IV pripravi z odstranitvijo zaščite azetidinilnega obroča spojine s formulo V, pri čemer je PG aminozaščitna skupina, da dobimo spojino s formulo IV:
- 7. Postopek po zahtevku 6, pri čemer je omenjena spojina s formulo V pripravljena z reduciranjem spojine s formulo VI z reducirnim sredstvom, izbranim iz skupine, ki sestoji iz borohidridov, da dobimo spojino s formulo V:
- 8. Postopek za pripravo spojine s formulo II, ki obsega odstranitev zaščite spojine s formulo III:
- 9. Postopek za pripravo spojine s formulo III, ki obsega stikanje spojine s formulo IVa s spojino s formulo IV:
- 10. Postopek za pripravo spojine s formulo IV, ki obsega odstranitev zaščite spojine s formulo V:pri čemer je PG amino zaščitna skupina.
- 11. Postopek za pripravo spojine s formulo V, pri čemer je PG amino zaščitna skupina, ki obsega reduciranje spojine s formulo VI:
- 12. Postopek za pripravo spojine, ki obsega (i) reagiranje spojine s formulo VII s spojino s formulo VIIa:kjer je PG amino zaščitna skupina.
- 13. Postopek po zahtevku 12, ki dalje obsega: (ii) reduciranje spojine s formulo VI z reducirnim sredstvom, izbranim iz skupine, ki sestoji iz borohidridov, da dobimo spojino s formulo V:
- 14. Postopek po zahtevku 13, ki dalje obsega: (iii) odstranitev zaščite azetidinilnega obroča s spojino s formulo V, da dobimo spojino s formulo IV:
- 15. Postopek po zahtevku 14, ki dalje obsega: (iv) reagiranje spojine s formulo IV s spojino s formulo IVa, da dobimo spojino s formulo III:
- 16. Postopek po zahtevku 15, ki dalje obsega: (v) hidrogenizacijo spojine s formulo III, da dobimo spojino s formulo II:
- 17. Postopek po zahtevku 16, ki dalje obsega: (vi) reagiranje spojine s formulo II s spojino s formulo IIa, da dobimo spojino s formulo I’:
- 18. Spojina, ki je:pri čemer je PG Ci-Cealkoksikarbonil, Cs-Cecikloalkiloksikarbonil, feniloksikarbonil ali toluensulfonil skupina.
- 19. Spojina, ki je:in pri čemer je PG izbran iz skupine, ki sestoji iz tert-butoksikarbonila (Boc), benziloksikarbonila (Cbz), p-Toluensulfonila (Ts) in fluorenilmetiloksikarbonila (Fmoc).
- 20. Spojina po zahtevku 18, pri čemer je omenjena spojina:
- 21. Spojina po zahtevku 18, pri čemer je omenjena spojina:
- 22. Spojina po zahtevku 18, pri čemer je omenjena spojina:
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261713104P | 2012-10-12 | 2012-10-12 | |
| EP13780303.7A EP2909188B1 (en) | 2012-10-12 | 2013-10-14 | Novel process for making compounds for use in the treatment of cancer |
| PCT/US2013/064866 WO2014059422A1 (en) | 2012-10-12 | 2013-10-14 | Novel process for making compounds for use in the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SI2909188T1 true SI2909188T1 (sl) | 2018-07-31 |
Family
ID=49474740
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI201331045T SI2909188T1 (sl) | 2012-10-12 | 2013-10-14 | Nov postopek za izdelavo spojin za uporabo pri zdravljenju raka |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US9771347B2 (sl) |
| EP (1) | EP2909188B1 (sl) |
| JP (2) | JP6300042B2 (sl) |
| KR (1) | KR102204520B1 (sl) |
| CN (2) | CN104837826B (sl) |
| AU (1) | AU2013328929B2 (sl) |
| BR (1) | BR112015008113B1 (sl) |
| CA (1) | CA2889466C (sl) |
| CL (1) | CL2015000926A1 (sl) |
| CR (2) | CR20200237A (sl) |
| EA (1) | EA030613B1 (sl) |
| ES (1) | ES2671502T3 (sl) |
| GE (1) | GEP201706690B (sl) |
| HK (1) | HK1213567A1 (sl) |
| HR (1) | HRP20180670T1 (sl) |
| IL (1) | IL238116B (sl) |
| IN (1) | IN2015DN03928A (sl) |
| MA (1) | MA38085B1 (sl) |
| MX (2) | MX372708B (sl) |
| MY (1) | MY186549A (sl) |
| NZ (1) | NZ706723A (sl) |
| PE (3) | PE20191818A1 (sl) |
| PH (1) | PH12015500785A1 (sl) |
| PL (1) | PL2909188T3 (sl) |
| SA (1) | SA515360271B1 (sl) |
| SG (1) | SG11201502795VA (sl) |
| SI (1) | SI2909188T1 (sl) |
| TR (1) | TR201807861T4 (sl) |
| UA (1) | UA115455C2 (sl) |
| WO (1) | WO2014059422A1 (sl) |
| ZA (1) | ZA201502349B (sl) |
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| EP3316867B1 (en) | 2015-06-30 | 2021-03-10 | Genentech, Inc. | Immediate-release tablets containing a drug and processes for forming the tablets |
| AR105483A1 (es) | 2015-06-30 | 2017-10-11 | Exelixis Inc | Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona |
| CN105330643B (zh) | 2015-12-09 | 2017-12-05 | 苏州明锐医药科技有限公司 | 卡比替尼的制备方法 |
| CN106045969B (zh) * | 2016-05-27 | 2019-04-12 | 湖南欧亚药业有限公司 | 一种卡比替尼的合成方法 |
| MX2019001635A (es) | 2016-08-12 | 2019-06-10 | Genentech Inc | Terapia de combinacion con un inhibidor de mek, un inhibidor del eje de pd-1, y un inhibidor de vegf. |
| TW201815419A (zh) | 2016-09-29 | 2018-05-01 | 美商建南德克公司 | Mek抑制劑、 pd-1軸抑制劑及紫杉烷之組合療法 |
| WO2020187674A1 (en) | 2019-03-15 | 2020-09-24 | Sandoz Ag | Crystalline (s)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl][3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl]methanone hemisuccinate |
| JP2024509269A (ja) | 2021-03-09 | 2024-02-29 | ジェネンテック， インコーポレイテッド | 脳がんの治療における使用のためのベルバラフェニブ |
| KR20230165795A (ko) | 2021-04-06 | 2023-12-05 | 제넨테크, 인크. | 벨바라페닙 및 코비메티닙 또는 벨바라페닙, 코비메티닙 및 아테졸리주맙을 이용한 병용 요법 |
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| TR201807861T4 (tr) | 2012-10-12 | 2018-06-21 | Exelixis Inc | Kanser tedavisinde kullanım için bileşikler yapmak için yeni işlem. |
| DK3103789T3 (en) | 2014-02-07 | 2019-01-28 | Sumitomo Chemical Co | METHOD FOR PREPARING (R) -1,1,3-TRIMETHYL-4-AMINOINDAN |
| AR105483A1 (es) | 2015-06-30 | 2017-10-11 | Exelixis Inc | Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona |
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