ME02460B - Spojeni biciklični 2,4-diaminopirimidin derivat kao dualni alk i fak inhibitor - Google Patents
Spojeni biciklični 2,4-diaminopirimidin derivat kao dualni alk i fak inhibitorInfo
- Publication number
- ME02460B ME02460B MEP-2016-68A MEP201668A ME02460B ME 02460 B ME02460 B ME 02460B ME P201668 A MEP201668 A ME P201668A ME 02460 B ME02460 B ME 02460B
- Authority
- ME
- Montenegro
- Prior art keywords
- degrees
- alk
- compound
- salt
- degrees20
- Prior art date
Links
- YAAWASYJIRZXSZ-UHFFFAOYSA-N pyrimidine-2,4-diamine Chemical class NC1=CC=NC(N)=N1 YAAWASYJIRZXSZ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 10
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 7
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 230000001404 mediated effect Effects 0.000 claims 7
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 7
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 7
- 102100033793 ALK tyrosine kinase receptor Human genes 0.000 claims 6
- 102100037813 Focal adhesion kinase 1 Human genes 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 206010029260 Neuroblastoma Diseases 0.000 claims 5
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 4
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 239000003098 androgen Substances 0.000 claims 3
- 102000004895 Lipoproteins Human genes 0.000 claims 2
- 108090001030 Lipoproteins Proteins 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 201000008275 breast carcinoma Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 201000001514 prostate carcinoma Diseases 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- -1 dihydrate salt Chemical class 0.000 claims 1
- IZCQDRVQVRENLX-UHFFFAOYSA-N dihydrate;trihydrochloride Chemical group O.O.Cl.Cl.Cl IZCQDRVQVRENLX-UHFFFAOYSA-N 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Classifications
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (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. Jedinjenje formule (I) (I)ili njegova so
2. Jedinjenje formule l prema patentnom zahtevu 1.
3. So jedinjenja formule (l) prema patentnom zahtevu 1 pri čemu je so adiciona so kiseline.
4.So jedinjenja formule (l) prema patentnom zahtevu 1 pričemu so jeste tribenzensulfonat so.
5.Tribenzensulfonat so jedinjenja formule (l) prema patentnom zahtevu 4 imajući: (a) XRPD šablon koji sadrži jedan iliviše vrhova izabranih od 7,62 :1:0,2 stepeni 26, 13.11 :1:0,2 stepeni 20, 13.76 :1:0.2 stepeni 20,i14.05 :1:0.2 stepeni20; ili (b) XRPD šablon koji sadrži jedan ili više vrhova izabranih od 6.85 :1: 0,2 stepeni 26, 7.62 :1: 0,2 stepeni26, 8.01 :1: 0,2 stepeni26, 13.11 :1: 0,2 stepeni 26, 13.76 :1: 0,2 stepeni 20, 14,05 :1: 0,2 stepeni 20, i 14.60 :1: 0,2 stepeni 20; ili (e) XRPD šablon koji sadrži jedan ili više vrhova izabranih od 7,62 :1: 0,2 stepeni 26, 13,11:1: 0,2 stepeni 20, 13.76 :1:0,2 stepeni 20, 14,05:1:0,2 stepeni 20, 17.10 :1:0,2 stepeni 20, 17.86 :1:0,2 stepeni20, i18.10 :1: 0.2 stepeni 26.
6.So jedinjenja formule (l) prema patentnom zahtevu 1 pri čemu je so trihidrohlorid dihidrat so.
7. Trihldrohlorid dihidrat so jedinjenja formule (l) prema patentnom zahtevu 6 imajući: (a) XRPD šablon koji sadrži jedan ili više vrhova izabranih od 5.42 :1: 0,2 stepeni 20, 8.86 :1: 0,2 stepeni 20, 14.06:1:0,2 stepeni 20, 17.52:1:0,2 stepeni26 i 18.51 :1:0,2 stepenl20;ili (a) XRPD šablon kojisadrži jedan iliviše vrhova izabranih od 5.42 ± 0,2 stepeni20, 8.86 ± 0,2 stepeni20, 14.06 ± 0,2 stepeni20,17.52 ± 0,2 stepeni29 i18.51 ± 0,2 stepeni20;ili (b) XRPD šablon kojisadrži jedan ili više vrhova izabranih od 5.42 ± 0,2 stepeni29, 5.91 ± 0,2 stepeni29, 8.86 ± 0,2 stepeni29,10.80 ± 0,2 stepeni29,11.79 ± 0,2 stepeni20,14.06 ± 0,2 stepeni20,14.n ± 0,2 stepeni20,17.02 ± 0,2 stepeni20, 17.52 ± 0,2 stepeni29 l18.51 ± 0.2 stepeni29.
8.Farmaceutska kompozicija koja sadržijedinjenje iliso prema bilo kojem od patentnih zahteva od 1 do 7 i farmaceutskiprihvatljiv ekscipijent.
9.Farmaceutska kompozicija patentnog zahteva 8,pri čemu je pomenuta kompozicija u obliku tablete ili kapsule.
10. Jedinjenje iliso bilo kog od patentnih zahteva od 1 do 7 za upotrebu u lečenju ALK-iliFAK- posredovanog stanja ili poremećaja izabrano od anaplastičkog limfoma velikih ćelija (ALCL), nemalog ćelijskog karcinoma pluća (NSCLC),neuroblastoma,glioblastoma,karcinoma prostate, karcinoma skvamoznih ćelija (SCC),ikarcinoma dojke.
11.Jedinjenje za upotrebu iz patentnog zahteva 10, pri čemu je ALK- ili FAK- posredovano stanje ili poremećaj izabrano od: (a) ALK-pozitivnog ALCL, EML4-ALK-pozitivnog NSCLC, neuroblastoma, glloblastoma, androgeno nezavisnih karcinoma prostate,karcinoma dojki,ikarcinoma skvamoznih ćelija glave lvrata (HNSCCs);lli (b) ALK-pozitivnog ALCL,EML4-ALK-pozitivnog NSCLC, neuroblastoma, androgeno nezavisnih karcinoma prostate,karcinoma dojki,i HNSCCs; ili (e) ALK-pozitivnog ALCL, EML4-ALK-pozitivnog NSCLC, neuroblastoma, iglloblastoma;ili (d) ALK-pozitivnog ALCL, EML4-ALK-pozltlvnog NSCLC, l neuroblastoma; ili (e) ALK-pozitivnog ALCL,lEML4-ALK-pozitivnog NSCLC.
12. Jedlnjenje za upotrebu iz patentnog zahteva 10, pri čemu ALK-Ili FAK- posredovano stanje lli poremećaj je izabrano od androgeno nezavisnih karcinoma prostate,karcinoma dojki,iHNSCCs.
13. Jedinjenje za upotrebu iz patentnog zahteva 10,pri čemu ALK-iliFAK- posredovano stanje iliporemećaj je ALK- posredovano stanje iliporemećaj.
14.Jedinjenje za upotrebu iz patentnog zahteva 10, pri čemu ALK-iliFAK- posredovano stanje iliporemećaj je FAK-posredovano stanje ili poremećaj. 2
Applications Claiming Priority (3)
| 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 |
| EP13710258.8A EP2822939B1 (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 |
|---|---|
| ME02460B true ME02460B (me) | 2017-02-20 |
Family
ID=47892060
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-68A ME02460B (me) | 2012-03-06 | 2013-03-06 | Spojeni biciklični 2,4-diaminopirimidin derivat kao dualni alk i fak inhibitor |
Country Status (28)
| Country | Link |
|---|---|
| US (5) | US9132128B2 (me) |
| EP (2) | EP3056494B1 (me) |
| JP (2) | JP6016953B2 (me) |
| KR (1) | KR102068374B1 (me) |
| CN (2) | CN104159894B (me) |
| AU (1) | AU2013229995B2 (me) |
| CA (1) | CA2865420C (me) |
| CL (1) | CL2014002353A1 (me) |
| CY (1) | CY1117565T1 (me) |
| DK (1) | DK2822939T3 (me) |
| EA (2) | EA025859B1 (me) |
| ES (2) | ES2570976T3 (me) |
| HR (1) | HRP20160387T1 (me) |
| HU (1) | HUE027976T2 (me) |
| IL (2) | IL234239A (me) |
| ME (1) | ME02460B (me) |
| MX (2) | MX347772B (me) |
| MY (1) | MY177290A (me) |
| NZ (1) | NZ630251A (me) |
| PH (1) | PH12014501979A1 (me) |
| PL (1) | PL2822939T3 (me) |
| RS (1) | RS54689B1 (me) |
| SG (2) | SG10201507865QA (me) |
| SI (1) | SI2822939T1 (me) |
| SM (1) | SMT201600134B (me) |
| UA (1) | UA115052C2 (me) |
| WO (1) | WO2013134353A1 (me) |
| ZA (1) | ZA201406147B (me) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA115052C2 (uk) * | 2012-03-06 | 2017-09-11 | Сефалон, Інк. | Конденсоване біциклічне 2,4-діамінопіримідинове похідне як подвійний alk- i fak-інгібітор |
| WO2015154064A2 (en) | 2014-04-04 | 2015-10-08 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| WO2016105529A1 (en) | 2014-12-23 | 2016-06-30 | Cephalon, Inc. | Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives |
| MX2021001398A (es) | 2018-08-07 | 2021-08-16 | In3Bio Ltd | Métodos y composiciones para la inhibición de la vía egf/egfr en combinación con inhibidores de la cinasa del linfoma anaplásico. |
| WO2024178339A2 (en) * | 2023-02-23 | 2024-08-29 | The Regents Of The University Of Michigan | Methods for treating neuroblastoma with a dual anaplastic lymphoma kinase and focal adhesion kinase inhibitor |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7872014B2 (en) | 2003-07-23 | 2011-01-18 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| JP4607879B2 (ja) | 2003-08-15 | 2011-01-05 | ノバルティス アーゲー | 新生物疾患、炎症および免疫障害の処置に有用な２，４−ピリミジンジアミン |
| PL1713806T3 (pl) * | 2004-02-14 | 2013-09-30 | Irm Llc | Związki i kompozycje jako inhibitory kinaz białkowych |
| AU2005230847B2 (en) | 2004-03-31 | 2012-11-08 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| US8962643B2 (en) * | 2006-02-24 | 2015-02-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| JP5512274B2 (ja) * | 2006-10-23 | 2014-06-04 | セファロン、インク． | ＡＬＫ阻害剤およびｃ−ＭＥＴ阻害剤としての２，４−ジアミノピリミジンの縮合二環式誘導体 |
| RS53588B1 (sr) * | 2006-12-08 | 2015-02-27 | Irm Llc | Jedinjenja i kompozicije kao inhibitori protein kinaza |
| JP4782239B2 (ja) * | 2007-04-18 | 2011-09-28 | ファイザー・プロダクツ・インク | 異常細胞増殖治療のためのスルホニルアミド誘導体 |
| HUE046402T2 (hu) * | 2009-06-10 | 2020-03-30 | Chugai Pharmaceutical Co Ltd | Tetraciklusos vegyületek |
| UA115052C2 (uk) * | 2012-03-06 | 2017-09-11 | Сефалон, Інк. | Конденсоване біциклічне 2,4-діамінопіримідинове похідне як подвійний alk- i fak-інгібітор |
| 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 |
| WO2016105529A1 (en) * | 2014-12-23 | 2016-06-30 | Cephalon, Inc. | Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives |
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2013
- 2013-03-06 UA UAA201410832A patent/UA115052C2/uk unknown
- 2013-03-06 AU AU2013229995A patent/AU2013229995B2/en active Active
- 2013-03-06 KR KR1020147027590A patent/KR102068374B1/ko active Active
- 2013-03-06 WO PCT/US2013/029304 patent/WO2013134353A1/en not_active Ceased
- 2013-03-06 JP JP2014561069A patent/JP6016953B2/ja not_active Expired - Fee Related
- 2013-03-06 EP EP15202516.9A patent/EP3056494B1/en active Active
- 2013-03-06 HU HUE13710258A patent/HUE027976T2/en unknown
- 2013-03-06 CA CA2865420A patent/CA2865420C/en active Active
- 2013-03-06 ME MEP-2016-68A patent/ME02460B/me unknown
- 2013-03-06 HR HRP20160387TT patent/HRP20160387T1/hr unknown
- 2013-03-06 PL PL13710258T patent/PL2822939T3/pl unknown
- 2013-03-06 EA EA201491641A patent/EA025859B1/ru not_active IP Right Cessation
- 2013-03-06 EP EP13710258.8A patent/EP2822939B1/en active Active
- 2013-03-06 EA EA201691574A patent/EA033124B1/ru not_active IP Right Cessation
- 2013-03-06 ES ES13710258T patent/ES2570976T3/es active Active
- 2013-03-06 SG SG10201507865QA patent/SG10201507865QA/en unknown
- 2013-03-06 NZ NZ630251A patent/NZ630251A/en unknown
- 2013-03-06 MX MX2014010613A patent/MX347772B/es active IP Right Grant
- 2013-03-06 SI SI201330151T patent/SI2822939T1/sl unknown
- 2013-03-06 RS RS20160238A patent/RS54689B1/sr unknown
- 2013-03-06 MX MX2017006206A patent/MX372740B/es unknown
- 2013-03-06 DK DK13710258.8T patent/DK2822939T3/en active
- 2013-03-06 ES ES15202516.9T patent/ES2681487T3/es active Active
- 2013-03-06 CN CN201380012764.6A patent/CN104159894B/zh 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 MY MYPI2014002428A patent/MY177290A/en unknown
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2014
- 2014-08-21 ZA ZA2014/06147A patent/ZA201406147B/en unknown
- 2014-08-21 IL IL234239A patent/IL234239A/en active IP Right Grant
- 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/PH12014501979A1/en unknown
-
2015
- 2015-08-12 US US14/824,750 patent/US9339502B2/en active Active
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2016
- 2016-05-04 US US15/146,164 patent/US9623026B2/en not_active Expired - Fee Related
- 2016-05-10 SM SM201600134T patent/SMT201600134B/it unknown
- 2016-05-10 CY CY20161100390T patent/CY1117565T1/el unknown
- 2016-09-27 JP JP2016188585A patent/JP2017039741A/ja active Pending
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2017
- 2017-03-07 US US15/451,960 patent/US10111872B2/en active Active
- 2017-05-18 IL IL252364A patent/IL252364B/en active IP Right Grant
-
2018
- 2018-10-26 US US16/172,368 patent/US10632119B2/en active Active
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