DK2822939T3 - Kondenseret bicyklisk 2,4-diaminopyrimidinderivat som dual alk- og fak-inhibitorer - Google Patents
Kondenseret bicyklisk 2,4-diaminopyrimidinderivat som dual alk- og fak-inhibitorer Download PDFInfo
- Publication number
- DK2822939T3 DK2822939T3 DK13710258.8T DK13710258T DK2822939T3 DK 2822939 T3 DK2822939 T3 DK 2822939T3 DK 13710258 T DK13710258 T DK 13710258T DK 2822939 T3 DK2822939 T3 DK 2822939T3
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- Prior art keywords
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- compound
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Classifications
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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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (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)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
Claims (14)
1. Forbindelse med formel (I)
(i) eller et salt deraf
2. Forbindelsen med formel I ifølge krav 1.
3. Salt af forbindelsen med formel (I) ifølge krav 1, hvor saltet er et syreadditionssalt.
4. Salt af forbindelsen med formel (I) ifølge krav 1, hvor saltet er et tribenzensulfonatsalt.
5. Tribenzensulfonatsalt af forbindelsen med formel (I) ifølge krav 4 med: (a) et XRPD-mønster omfattende én eller flere toppe valgt fra 7,62 ± 0,2 grader 2Θ, 13,11 ± 0,2 grader 20, 13,76 ± 0,2 grader 20, og 14,05 ± 0,2 grader 20; eller (b) et XRPD-mønster omfattende én eller flere toppe valgt fra 6,85 ± 0,2 grader 2Θ, 7,62 ± 0,2 grader 2Θ, 8,01 ± 0,2 grader 2Θ, 13,11 ± 0,2 grader 2Θ, 13,76 ± 0,2 grader 20, 14,05 ± 0,2 grader 20, og 14,60 ± 0,2 grader 20; eller (c) et XRPD-mønster omfattende én eller flere toppe valgt fra 7,62 ± 0,2 grader 2Θ, 13,11± 0,2 grader 20, 13,76 ± 0,2 grader 20, 14,05 ± 0,2 grader 20, 17,10 ± 0,2 grader 20, 17,86 ± 0,2 grader 20, og 18,10 ± 0,2 grader 2Θ.
6. Salt af forbindelsen med formel (I) ifølge krav 1, hvor saltet er et trihydrochlorid-dihyd ratsa It.
7. Trihydrochlorid-dihydratsalt af forbindelsen med formel (I) ifølge krav 6 med: (a) et XRPD-mønster omfattende én eller flere toppe valgt fra 5,42 ± 0,2 grader 20, 8,86 ± 0,2 grader 20, 14,06 ± 0,2 grader 20, 17,52 ± 0,2 grader 2Θ og 18,51 ± 0,2 grader 20; eller (b) et XRPD-mønster omfattende én eller flere toppe valgt fra 5.42 ± 0,2 grader 2Θ, 5,91 ± 0,2 grader 2Θ, 8,86 ± 0,2 grader 2Θ, 10,80 ± 0,2 grader 2Θ, 11,79 ± 0,2 grader 20, 14,06 ± 0,2 grader 20, 14,72 ± 0,2 grader 20, 17,02 ± 0,2 grader 20, 17,52 ± 0,2 grader 2Θ og 18,51 ± 0,2 grader 2Θ.
8. Farmaceutisk sammensætning omfattende en forbindelse eller salt ifølge et hvilket som helst af kravene 1-7 og en farmaceutisk acceptabel excipiens.
9. Farmaceutisk sammensætning ifølge krav 8, hvor sammensætningen er i form af en tablet eller kapsel.
10. Forbindelse eller salt ifølge et hvilket som helst af kravene 1-7 til anvendelse i behandling af en ALK- eller FAK-medieret tilstand eller lidelse valgt fra anaplastisk storcellet lymfom (ALCL), ikke-småcellet lungecancer (NSCLC), neuroblastom, glioblastom, prostatacancer, skvamøs cellecarcinom (SCC), og brystcancer.
11. Forbindelsen til anvendelse ifølge krav 10, hvor den ALK- eller FAK-medierede tilstand eller lidelse er valgt fra: (a) ALK-positiv ALCL, EML4-ALK-positiv NSCLC, neuroblastom, glioblastom, androgen-afhængige prostatacancere, brystcancere, og hoved- og hals-skvamøse cellecarcinomer (HNSCC'er); eller (b) ALK-positiv ALCL, EML4-ALK-positiv NSCLC, neuroblastom, androgen-afhængige prostatacancere, brystcancere, og HNSCC'er; eller (c) ALK-positiv ALCL, EML4-ALK-positiv NSCLC, neuroblastom, og glioblastom; eller (d) ALK-positiv ALCL, EML4-ALK-positiv NSCLC, og neuroblastom; eller (e) ALK-positiv ALCL og EML4-ALK-positiv NSCLC.
12. Forbindelsen til anvendelse ifølge krav 10, hvor den ALK- eller FAK-medierede tilstand eller lidelse er valgt fra androgen-afhængige prostatacancere, brystcancere, og HNSCC'er.
13. Forbindelsen til anvendelse ifølge krav 10, hvor den ALK- eller FAK-medierede tilstand eller lidelse er en ALK-medieret tilstand eller lidelse.
14. Forbindelsen til anvendelse ifølge krav 10, hvor den ALK- eller FAK-medierede tilstand eller lidelse er en FAK-medieret tilstand eller lidelse.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261607305P | 2012-03-06 | 2012-03-06 | |
| PCT/US2013/029304 WO2013134353A1 (en) | 2012-03-06 | 2013-03-06 | Fused bicyclic 2,4-diaminopyrimidine derivative as a dual alk and fak inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2822939T3 true DK2822939T3 (da) | 2016-03-14 |
Family
ID=47892060
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK13710258.8T DK2822939T3 (da) | 2012-03-06 | 2013-03-06 | Kondenseret bicyklisk 2,4-diaminopyrimidinderivat som dual alk- og fak-inhibitorer |
Country Status (29)
| Country | Link |
|---|---|
| US (5) | US9132128B2 (da) |
| EP (2) | EP3056494B1 (da) |
| JP (2) | JP6016953B2 (da) |
| KR (1) | KR102068374B1 (da) |
| CN (2) | CN106166155B (da) |
| AU (1) | AU2013229995B2 (da) |
| CA (1) | CA2865420C (da) |
| CL (1) | CL2014002353A1 (da) |
| CY (1) | CY1117565T1 (da) |
| DK (1) | DK2822939T3 (da) |
| EA (2) | EA025859B1 (da) |
| ES (2) | ES2681487T3 (da) |
| HK (2) | HK1205119A1 (da) |
| HR (1) | HRP20160387T1 (da) |
| HU (1) | HUE027976T2 (da) |
| IL (2) | IL234239A (da) |
| ME (1) | ME02460B (da) |
| MX (1) | MX347772B (da) |
| MY (1) | MY177290A (da) |
| NZ (1) | NZ630251A (da) |
| PH (1) | PH12014501979B1 (da) |
| PL (1) | PL2822939T3 (da) |
| RS (1) | RS54689B1 (da) |
| SG (2) | SG11201405371PA (da) |
| SI (1) | SI2822939T1 (da) |
| SM (1) | SMT201600134B (da) |
| UA (1) | UA115052C2 (da) |
| WO (1) | WO2013134353A1 (da) |
| ZA (1) | ZA201406147B (da) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013229995B2 (en) * | 2012-03-06 | 2017-04-13 | Cephalon, Inc. | Fused bicyclic 2,4-diaminopyrimidine derivative as a dual ALK and FAK inhibitor |
| AU2015240465B2 (en) | 2014-04-04 | 2020-02-27 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| EP3237408B1 (en) | 2014-12-23 | 2018-10-31 | Cephalon, Inc. | Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives |
| US20200046690A1 (en) | 2018-08-07 | 2020-02-13 | In3Bio Ltd. | Methods and compositions for inhibition of egf/egfr pathway in combination with anaplastic lymphoma kinase inhibitors |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005009389A2 (en) | 2003-07-23 | 2005-02-03 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| KR100904570B1 (ko) | 2003-08-15 | 2009-06-25 | 노파르티스 아게 | 종양성 질환, 염증성 및 면역계 장애의 치료에 유용한2,4-피리미딘디아민 |
| JP4989233B2 (ja) * | 2004-02-14 | 2012-08-01 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| EP1730128A1 (en) | 2004-03-31 | 2006-12-13 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| CA2642229C (en) * | 2006-02-24 | 2015-05-12 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| AR063527A1 (es) | 2006-10-23 | 2009-01-28 | Cephalon Inc | Derivados biciclicos fusionados de 2,4-diaminopirimidina como inhibidores de alk y c-met |
| EP2311807B1 (en) * | 2006-12-08 | 2015-11-11 | Novartis AG | Compounds and composition as protein kinase inhibitors |
| BRPI0810411B8 (pt) * | 2007-04-18 | 2021-05-25 | Pfizer Prod Inc | derivados de sulfonil amida para o tratamento de crescimento celular anormal, seu sos, bem como composição farmacêutica |
| CA2764653C (en) * | 2009-06-10 | 2018-01-02 | Chugai Seiyaku Kabushiki Kaisha | Tetracyclic compounds |
| AU2013229995B2 (en) * | 2012-03-06 | 2017-04-13 | Cephalon, Inc. | Fused bicyclic 2,4-diaminopyrimidine derivative as a dual ALK and FAK inhibitor |
| KR101446742B1 (ko) * | 2012-08-10 | 2014-10-01 | 한국화학연구원 | Ｎ2,ｎ4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| EP3237408B1 (en) * | 2014-12-23 | 2018-10-31 | Cephalon, Inc. | Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives |
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2013
- 2013-03-06 AU AU2013229995A patent/AU2013229995B2/en active Active
- 2013-03-06 CA CA2865420A patent/CA2865420C/en active Active
- 2013-03-06 CN CN201610591742.5A patent/CN106166155B/zh active Active
- 2013-03-06 SG SG11201405371PA patent/SG11201405371PA/en unknown
- 2013-03-06 NZ NZ630251A patent/NZ630251A/en unknown
- 2013-03-06 UA UAA201410832A patent/UA115052C2/uk unknown
- 2013-03-06 CN CN201380012764.6A patent/CN104159894B/zh active Active
- 2013-03-06 ES ES15202516.9T patent/ES2681487T3/es active Active
- 2013-03-06 KR KR1020147027590A patent/KR102068374B1/ko active IP Right Grant
- 2013-03-06 ME MEP-2016-68A patent/ME02460B/me unknown
- 2013-03-06 SG SG10201507865QA patent/SG10201507865QA/en unknown
- 2013-03-06 MX MX2014010613A patent/MX347772B/es active IP Right Grant
- 2013-03-06 ES ES13710258T patent/ES2570976T3/es active Active
- 2013-03-06 WO PCT/US2013/029304 patent/WO2013134353A1/en active Application Filing
- 2013-03-06 EA EA201491641A patent/EA025859B1/ru not_active IP Right Cessation
- 2013-03-06 DK DK13710258.8T patent/DK2822939T3/da active
- 2013-03-06 MY MYPI2014002428A patent/MY177290A/en unknown
- 2013-03-06 HU HUE13710258A patent/HUE027976T2/en unknown
- 2013-03-06 EP EP15202516.9A patent/EP3056494B1/en active Active
- 2013-03-06 RS RS20160238A patent/RS54689B1/en unknown
- 2013-03-06 SI SI201330151T patent/SI2822939T1/sl unknown
- 2013-03-06 PL PL13710258T patent/PL2822939T3/pl unknown
- 2013-03-06 JP JP2014561069A patent/JP6016953B2/ja active Active
- 2013-03-06 EA EA201691574A patent/EA033124B1/ru not_active IP Right Cessation
- 2013-03-06 EP EP13710258.8A patent/EP2822939B1/en active Active
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2014
- 2014-08-21 IL IL234239A patent/IL234239A/en active IP Right Grant
- 2014-08-21 ZA ZA2014/06147A patent/ZA201406147B/en unknown
- 2014-09-02 US US14/474,928 patent/US9132128B2/en active Active
- 2014-09-05 CL CL2014002353A patent/CL2014002353A1/es unknown
- 2014-09-05 PH PH12014501979A patent/PH12014501979B1/en unknown
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2015
- 2015-06-19 HK HK15105852.9A patent/HK1205119A1/zh unknown
- 2015-08-12 US US14/824,750 patent/US9339502B2/en active Active
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2016
- 2016-04-14 HR HRP20160387TT patent/HRP20160387T1/hr unknown
- 2016-05-04 US US15/146,164 patent/US9623026B2/en active Active
- 2016-05-10 CY CY20161100390T patent/CY1117565T1/el unknown
- 2016-05-10 SM SM201600134T patent/SMT201600134B/it unknown
- 2016-09-27 JP JP2016188585A patent/JP2017039741A/ja active Pending
- 2016-12-22 HK HK16114598A patent/HK1226300A1/zh unknown
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- 2017-03-07 US US15/451,960 patent/US10111872B2/en active Active
- 2017-05-18 IL IL252364A patent/IL252364B/en active IP Right Grant
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2018
- 2018-10-26 US US16/172,368 patent/US10632119B2/en active Active
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