HRP20191653T1 - N-((4,6-dimetil-2-okso-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2h-piran-4-il)amino)-4-metil-4' (morfolinometil)-[l,1'-bifenil]-3-karboksamid hidrobromid za uporabu u liječenju proliferativnih poremećaja stanica hematološkog sustava - Google Patents
N-((4,6-dimetil-2-okso-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2h-piran-4-il)amino)-4-metil-4' (morfolinometil)-[l,1'-bifenil]-3-karboksamid hidrobromid za uporabu u liječenju proliferativnih poremećaja stanica hematološkog sustava Download PDFInfo
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- 210000005096 hematological system Anatomy 0.000 title claims 4
- 230000002062 proliferating effect Effects 0.000 title claims 4
- 239000004305 biphenyl Substances 0.000 title 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 7
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000002489 hematologic effect Effects 0.000 claims 3
- UQRICAQPWZSJNF-UHFFFAOYSA-N n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide;hydrobromide Chemical compound Br.C=1C(C=2C=CC(CN3CCOCC3)=CC=2)=CC(C(=O)NCC=2C(NC(C)=CC=2C)=O)=C(C)C=1N(CC)C1CCOCC1 UQRICAQPWZSJNF-UHFFFAOYSA-N 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 238000001757 thermogravimetry curve Methods 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000035865 Chronic mast cell leukemia Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 201000002797 childhood leukemia Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 239000012535 impurity Substances 0.000 claims 1
- 230000000527 lymphocytic effect Effects 0.000 claims 1
- 201000006512 mast cell neoplasm Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 201000009612 pediatric lymphoma Diseases 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- 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
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Pyridine Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Claims (23)
1. N-((4,6-dimetil-2-okso-1,2-dihidropiridin-3-il)metil)-5-(etil (tetrahidro-2H-piran-4-il)amino)-4-metil-4’-(morfolinometil)-[1,1’-bifenil]-3-karboksamid hidrobromid za uporabu u liječenju proliferativnog poremećaja stanica hematološkog sustava.
2. Spoj za uporabu prema patentnom zahtjevu 1, koji je monohidrobromid.
3. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1 do 2, naznačen time što je navedeni spoj kristalan.
4. Spoj za uporabu prema bilo kojem od prethodno navedenih patentnih zahtjeva, naznačen time što je navedeni spoj bez nečistoća.
5. Spoj za uporabu prema bilo kojem od prethodno navedenih patentnih zahtjeva, naznačen time što je navedeni spoj kristalna kruta tvar koja je suštinski bez amorfnog N-((4,6-dimetil-2-okso-1,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H-piran-4-il)amino)-4-metil-4’-(morfolinometil)-[1,1’-bifenil]-3-karboksamid hidrobromida.
6. Polimorf A N-((4,6-dimetil-2-okso-1,2-dihidropiridin-3-il)metil)-5-(etil (tetrahidro-2H-piran-4-il)amino)-4-metil-4’-(morfolinometil)-[1,1’-bifenil]-3-karboksamid hidrobromida za uporabu u liječenju proliferativnog poremećaja stanica hematološkog sustava; naznačen time što polimorf A prikazuje rendgenski difraktogram praha koji ima jedan ili više karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja i 22.0 +/- 0.3 stupnja 2-teta.
7. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima karakteristične vrhove izražene u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja i 22.0 +/- 0.3 stupnja 2-teta.
8. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima jedan ili više karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja, i oko 23.6 +/- 0.3 stupnja 2-teta.
9. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima najmanje 5 karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 10.1 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 20.6 +/- 0.3 stupnja, 20.9 +/- 0.3 stupnja, 21.8 +/- 0.3 stupnja, 22.0 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja i 23.6 +/- 0.3 stupnja 2-teta.
10. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima najmanje 6 karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 10.1 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 20.6 +/- 0.3 stupnja, 20.9 +/- 0.3 stupnja, 21.8 +/- 0.3 stupnja, 22.0 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja i 23.6 +/- 0.3 stupnja 2-teta.
11. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima najmanje 7 karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 10.1 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 20.6 +/- 0.3 stupnja, 20.9 +/- 0.3 stupnja, 21.8 +/- 0.3 stupnja, 22.0 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja i 23.6 +/- 0.3 stupnja 2-teta.
12. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima najmanje 8 karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 10.1 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 20.6 +/- 0.3 stupnja, 20.9 +/- 0.3 stupnja, 21.8 +/- 0.3 stupnja, 22.0 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja i 23.6 +/- 0.3 stupnja 2-teta.
13. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima najmanje 9 karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 10.1 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 20.6 +/- 0.3 stupnja, 20.9 +/- 0.3 stupnja, 21.8 +/- 0.3 stupnja, 22.0 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja i 23.6 +/- 0.3 stupnja 2-teta.
14. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima najmanje 10 karakterističnih vrhova izraženih u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 10.1 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 20.6 +/- 0.3 stupnja, 20.9 +/- 0.3 stupnja, 21.8 +/- 0.3 stupnja, 22.0 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja i 23.6 +/- 0.3 stupnja 2-teta.
15. Polimorf za uporabu prema patentnom zahtjevu 7; naznačen time što polimorf prikazuje rendgenski difraktogram praha koji ima karakteristične vrhove izražene u stupnjevima 2-teta na 3.9 +/- 0.3 stupnja, 10.1 +/- 0.3 stupnja, 14.3 +/- 0.3 stupnja, 17.5 +/- 0.3 stupnja, 18.7 +/- 0.3 stupnja, 20.6 +/- 0.3 stupnja, 20.9 +/- 0.3 stupnja, 21.8 +/- 0.3 stupnja, 22.0 +/- 0.3 stupnja, 23.3 +/- 0.3 stupnja i 23.6 +/- 0.3 stupnja 2-teta.
16. Polimorf za uporabu prema bilo kojem od patentnih zahtjeva 6 do 15, naznačen time što polimorf prikazuje rendgenski difraktogram praha koji je suštinski u skladu sa slikom 1 i/ili polimorf prikazuje rendgenski difraktogram praha koji je suštinski u skladu s tablicom 1:
Tablica 1
17. Polimorf za uporabu prema bilo kojem od patentnih zahtjeva 6 do 16, naznačen time što polimorf prikazuje termogram diferencijalne skenirajuće kalorimetrije koji ima karakterističan vrh izražen u jedinicama °C, na temperaturi od 255 +/- 5°C.
18. Polimorf za uporabu prema bilo kojem od patentnih zahtjeva 6 do 17, naznačen time što polimorf prikazuje termogram diferencijalne skenirajuće kalorimetrije koji je suštinski u skladu sa slikom 3.
19. Polimorf za uporabu prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time što je proliferativni poremećaj stanica hematološkog sustava hematološki karcinom.
20. Polimorf za uporabu prema patentnom zahtjevu 19, naznačen time što je hematološki karcinom odabran od multiplog mijeloma, limfoma, leukemije, mijeloidnih neoplazmi i neoplazmi mastocita.
21. Polimorf za uporabu prema patentnom zahtjevu 20, naznačen time što je limfom odabran od Hodgkinovog limfoma, limfoma dječjeg uzrasta i limfoma limfocitnog i kožnog porijekla.
22. Polimorf za uporabu prema patentnom zahtjevu 20, naznačen time što je leukemija odabrana od leukemije dečjeg uzrasta, leukemije vlasastih stanica, akutne limfocitne leukemije, akutne mijelocitne leukemije, kronične limfocitne leukemije, kronične mijelocitne leukemije, kronične mijeloične leukemije i leukemije mastocita.
23. Polimorf za uporabu prema patentnom zahtjevu 20, naznačen time što je hematološki karcinom multipli mijelom.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261624215P | 2012-04-13 | 2012-04-13 | |
EP16191716.6A EP3184523B1 (en) | 2012-04-13 | 2013-04-11 | N-((4,6-dimethyl-2-oxo-l,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[l,1'-biphenyl]-3-carboxamide hydrobromide for use in the treatment of a cell proliferative disorder of the hematologic system |
Publications (1)
Publication Number | Publication Date |
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HRP20191653T1 true HRP20191653T1 (hr) | 2020-02-21 |
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HRP20170295TT HRP20170295T1 (hr) | 2012-04-13 | 2017-02-22 | Oblik soli inhibitora ljudske histonske metiltransferaze ezh2 |
HRP20191653TT HRP20191653T1 (hr) | 2012-04-13 | 2019-09-13 | N-((4,6-dimetil-2-okso-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2h-piran-4-il)amino)-4-metil-4' (morfolinometil)-[l,1'-bifenil]-3-karboksamid hidrobromid za uporabu u liječenju proliferativnih poremećaja stanica hematološkog sustava |
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HRP20170295TT HRP20170295T1 (hr) | 2012-04-13 | 2017-02-22 | Oblik soli inhibitora ljudske histonske metiltransferaze ezh2 |
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US (6) | US9394283B2 (hr) |
EP (4) | EP2836491B1 (hr) |
JP (3) | JP6255382B2 (hr) |
KR (3) | KR102120883B1 (hr) |
CN (2) | CN104603130B (hr) |
AU (2) | AU2013245878B2 (hr) |
BR (1) | BR112014025508B1 (hr) |
CA (1) | CA2870005C (hr) |
CY (2) | CY1119383T1 (hr) |
DK (3) | DK3628670T3 (hr) |
ES (3) | ES2745016T3 (hr) |
HR (2) | HRP20170295T1 (hr) |
HU (3) | HUE060881T2 (hr) |
IL (4) | IL296199A (hr) |
IN (1) | IN2014DN09068A (hr) |
LT (2) | LT2836491T (hr) |
MX (1) | MX362339B (hr) |
NZ (1) | NZ700761A (hr) |
PL (3) | PL2836491T3 (hr) |
PT (3) | PT2836491T (hr) |
RS (2) | RS59392B1 (hr) |
RU (1) | RU2658911C2 (hr) |
SG (3) | SG10201608577RA (hr) |
SI (2) | SI2836491T1 (hr) |
WO (1) | WO2013155317A1 (hr) |
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KR20160003115A (ko) | 2013-04-30 | 2016-01-08 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 제스트 인핸서 상동체 2 억제제 |
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