HRP20201492T1 - Hidrokloridne soli n-(cijanometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida - Google Patents
Hidrokloridne soli n-(cijanometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida Download PDFInfo
- Publication number
- HRP20201492T1 HRP20201492T1 HRP20201492TT HRP20201492T HRP20201492T1 HR P20201492 T1 HRP20201492 T1 HR P20201492T1 HR P20201492T T HRP20201492T T HR P20201492TT HR P20201492 T HRP20201492 T HR P20201492T HR P20201492 T1 HRP20201492 T1 HR P20201492T1
- Authority
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- Croatia
- Prior art keywords
- pharmaceutical preparation
- morpholinophenylamino
- cyanomethyl
- pyrimidin
- disease
- Prior art date
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- NGOUSYFDVUVHDA-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide;hydrochloride Chemical class Cl.C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 NGOUSYFDVUVHDA-UHFFFAOYSA-N 0.000 title 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 239000010949 copper Substances 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 102000015617 Janus Kinases Human genes 0.000 claims 2
- 108010024121 Janus Kinases Proteins 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- RQKCPSIFARJBOR-UHFFFAOYSA-N N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide hydrate dihydrochloride Chemical compound O.Cl.Cl.O=C(NCC#N)c1ccc(cc1)-c1ccnc(Nc2ccc(cc2)N2CCOCC2)n1 RQKCPSIFARJBOR-UHFFFAOYSA-N 0.000 claims 2
- 208000033755 Neutrophilic Chronic Leukemia Diseases 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 201000010903 chronic neutrophilic leukemia Diseases 0.000 claims 2
- 229910052802 copper Inorganic materials 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 206010028537 myelofibrosis Diseases 0.000 claims 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- 208000003476 primary myelofibrosis Diseases 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 208000005485 Thrombocytosis Diseases 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- ZVHNDZWQTBEVRY-UHFFFAOYSA-N momelotinib Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 ZVHNDZWQTBEVRY-UHFFFAOYSA-N 0.000 claims 1
Classifications
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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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (8)
1. Spoj koji je
Oblik II N-(cijanometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamid-dihidroklorida monohidrata, naznačen time što ima:
(A) kristale s parametrima jedinične ćelije na T=100°K od: a =10,2837(6) Å, b = 10,4981(6) Å, c = 11,5143(7) Å, α = 83,297(2)°, β = 87,649(2)°, γ = 67,445(2)°, te triklinsku prostornu skupinu P-1, ili
(B) uzorak difrakcije rendgenskih zraka na prahu (XRPD) s maksimumima na 7,7°, 19,3°, 24,0°, 25,7°, te 29,6° 2θ ± 0,2° gdje je 2θ određen uz pomoć zračenja na bakru (Cu Kα, λ = 1,5418 Å).
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima kristale s parametrima jedinične ćelije na T=100 °K od: a =10,2837(6) Å, b = 10,4981(6) Å, c = 11,5143(7) Å, α = 83,297(2)°, β = 87,649(2)°, γ = 67,445(2)°, te triklinsku prostornu skupinu P-1.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (XRPD) s maksimumima na 7,7°, 19,3°, 24,0°, 25,7°, te 29,6° 2θ ± 0,2° gdje je 2θ određen uz pomoć zračenja na bakru (Cu Kα, λ = 1,5418 Å).
4. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-3.
5. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je Oblik II N-(cijanometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamid-dihidroklorida monohidrata prisutan u količini ekvivalentnoj 50 mg, 100 mg, 150 mg ili 200 slobodne baze N-(cijanometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida.
6. Farmaceutski pripravak u skladu s patentnim zahtjevima 4 ili 5, naznačen time što je u obliku tablete.
7. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen upotrebi u postupku liječenja bolesti povezane s Janus kinazom (JAK), gdje je bolest mijeloproliferativna bolest, koju se bira iz skupine koju čine policitemija vera (PV), mijelofibroza, trombocitemija, esencijalna trombocitemija (ET), idiopatska mijelofibroza, kronična mijelogena leukemija, sistemna mastocitoza (SM), kronična neutrofilna leukemija (CNL), mijelodisplastični sindrom (MDS) i sistemna mastocitna bolest (SMCD).
8. Farmaceutski pripravak u skladu s bilo kojim od patentnih zahtjeva 4 do 6, naznačen time što je namijenjen upotrebi u postupku liječenja primarne mijelofibroze.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462011315P | 2014-06-12 | 2014-06-12 | |
EP15739042.8A EP3154950B1 (en) | 2014-06-12 | 2015-06-11 | N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide hydrochloride salts |
PCT/US2015/035316 WO2015191846A1 (en) | 2014-06-12 | 2015-06-11 | N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide hydrochloride salts |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20201492T1 true HRP20201492T1 (hr) | 2021-01-08 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20201492TT HRP20201492T1 (hr) | 2014-06-12 | 2020-09-18 | Hidrokloridne soli n-(cijanometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida |
Country Status (35)
Country | Link |
---|---|
US (4) | US9469613B2 (hr) |
EP (3) | EP3907219A1 (hr) |
JP (5) | JP6600649B2 (hr) |
KR (1) | KR101928225B1 (hr) |
CN (2) | CN106458929A (hr) |
AP (1) | AP2016009551A0 (hr) |
AR (1) | AR100818A1 (hr) |
AU (1) | AU2015274554B9 (hr) |
BR (1) | BR112016028749A2 (hr) |
CA (1) | CA2951883C (hr) |
CR (1) | CR20160575A (hr) |
CU (1) | CU20160183A7 (hr) |
CY (1) | CY1123604T1 (hr) |
DK (1) | DK3154950T3 (hr) |
EA (1) | EA032639B1 (hr) |
EC (1) | ECSP16093323A (hr) |
ES (1) | ES2822773T3 (hr) |
FI (1) | FIC20240025I1 (hr) |
FR (1) | FR24C1030I1 (hr) |
HR (1) | HRP20201492T1 (hr) |
HU (2) | HUE051360T2 (hr) |
IL (3) | IL249038B (hr) |
LT (1) | LT3154950T (hr) |
MA (1) | MA40067A (hr) |
MX (3) | MX2016016294A (hr) |
NZ (1) | NZ725966A (hr) |
PH (1) | PH12016502461A1 (hr) |
PL (1) | PL3154950T3 (hr) |
PT (1) | PT3154950T (hr) |
RS (1) | RS61065B1 (hr) |
SG (2) | SG11201610079VA (hr) |
SI (1) | SI3154950T1 (hr) |
TW (3) | TWI729644B (hr) |
UY (1) | UY36166A (hr) |
WO (1) | WO2015191846A1 (hr) |
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TWI729644B (zh) * | 2014-06-12 | 2021-06-01 | 美商西爾拉癌症醫學公司 | N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺 |
CN106316963B (zh) * | 2015-06-26 | 2021-06-08 | 苏州泽璟生物制药股份有限公司 | 吗啡啉苯基氨基嘧啶化合物或其盐的多晶型物 |
CN106316964B (zh) * | 2015-06-26 | 2019-06-25 | 苏州泽璟生物制药股份有限公司 | 苯基氨基嘧啶化合物或其盐的多晶型物 |
TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Hdac抑制劑與pd-l1抑制劑之組合治療 |
TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
US10245268B2 (en) | 2016-08-10 | 2019-04-02 | Sierra Oncology, Inc. | Treatment of ACVR1-mediated diseases |
CN115844894B (zh) * | 2018-05-15 | 2024-08-06 | 江苏豪森药业集团有限公司 | 包含第三代小分子egfr抑制剂的药物组合物及其制备方法 |
CN113015527A (zh) | 2018-08-21 | 2021-06-22 | 西拉肿瘤学公司 | 治疗骨髓纤维化的血小板计数诊断方法 |
EP3923948A4 (en) * | 2019-02-12 | 2022-11-16 | Impact Biomedicines, Inc. | CRYSTALLINE SHAPES OF A JAK2 INHIBITOR |
EP4376849A1 (en) | 2021-07-30 | 2024-06-05 | GlaxoSmithKline LLC | Biomarker and patient selection in treatment for myelofibrosis |
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TWI729644B (zh) * | 2014-06-12 | 2021-06-01 | 美商西爾拉癌症醫學公司 | N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺 |
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