HRP20210681T1 - Kristalne soli (s)-6-((1-acetilpiperidin-4-il)amino)-n-(3-(3,4-dihidroizokinolin-2(1h)-il)-2-hidroksipropil)pirimidin-4-karboksamida - Google Patents
Kristalne soli (s)-6-((1-acetilpiperidin-4-il)amino)-n-(3-(3,4-dihidroizokinolin-2(1h)-il)-2-hidroksipropil)pirimidin-4-karboksamida Download PDFInfo
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- HRP20210681T1 HRP20210681T1 HRP20210681TT HRP20210681T HRP20210681T1 HR P20210681 T1 HRP20210681 T1 HR P20210681T1 HR P20210681T T HRP20210681T T HR P20210681TT HR P20210681 T HRP20210681 T HR P20210681T HR P20210681 T1 HRP20210681 T1 HR P20210681T1
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- JLCCNYVTIWRPIZ-NRFANRHFSA-N 6-[(1-acetylpiperidin-4-yl)amino]-n-[(2s)-3-(3,4-dihydro-1h-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide Chemical class C1CN(C(=O)C)CCC1NC1=CC(C(=O)NC[C@H](O)CN2CC3=CC=CC=C3CC2)=NC=N1 JLCCNYVTIWRPIZ-NRFANRHFSA-N 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 12
- 230000005855 radiation Effects 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- GXLSVNOMQNNGQM-BOXHHOBZSA-N 6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide butanedioic acid Chemical compound OC(=O)CCC(O)=O.CC(=O)N1CCC(CC1)Nc1cc(ncn1)C(=O)NC[C@H](O)CN1CCc2ccccc2C1 GXLSVNOMQNNGQM-BOXHHOBZSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- -1 benzoate salt (S)-6-((1-acetylpiperidin-4-yl)amino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)pyrimidine -4-carboxamide Chemical compound 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
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
- C07D401/14—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 three or more hetero rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
-
- 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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (12)
1. Kristalni oblik sukcinatne soli (S)-6-((1-acetilpiperidin-4-il)amino)-N-(3-(3,4-dihidroizokinolin-2(1H)-il)-2-hidroksipropil)pirimidin-4-karboksamida, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (XRPD) koji sadrži najmanje tri kuta difrakcije, prilikom mjerenja uz pomoć zračenja Cu Kα, koje se bira iz skupine koju čine:
(i) otprilike 4,5, 8,2, 9,0, 10,4, 13,5, 15,8, 16,4, 17,3, 17,7, 18,1, 18,8, 19,6, 20,8, 21,9, 22,7, 23,3, 24,0, 24,7, 26,4, 28,2, te 29,6 stupnjeva 2θ;
(ii) otprilike 4,5, 8,2, 10,4, 13,5, 15,8, 16,4, 17,3, 17,7, 18,1, 18,8, 19,6, 20,8, 21,9, 23,3, te 24,0 stupnjeva 2θ; ili
(iii) otprilike 4,5, 8,2, 10,4, 13,5, 15,8, 16,4, 17,7, 18,1, 18,8, 20,8, 21,9, 23,3, te 24,0 stupnjeva 2θ.
2. Kristalni oblik u skladu s patentnim zahtjevom 1, gdje je kristalni oblik naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (XRPD) koji sadrži kutove difrakcije, prilikom mjerenja uz pomoć zračenja Cu Kα, od otprilike 4,5, 10,4, 17,7, 18,1, 20,8, te 24,0 stupnjeva 2θ.
3. Kristalni oblik u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, gdje je kristalni oblik naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (XRPD) koji uglavnom odgovara slici 1.
4. Kristalni oblik benzoatne soli (S)-6-((1-acetilpiperidin-4-il)amino)-N-(3-(3,4-dihidroizokinolin-2(1H)-il)-2-hidroksipropil)pirimidin-4-karboksamida, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (XRPD) koji sadrži najmanje tri kuta difrakcije, prilikom mjerenja uz pomoć zračenja Cu Kα, koje se bira iz skupine koju čine:
(i) otprilike 4,3, 7,7, 9,2, 10,9, 12,8, 14,2, 15,6, 16,6, 16,9, 18,1, 18,6, 21,5, 22,1, 23,4, 24,0, 24,2, 25,1, 25,9, 27,1, 28,8, te 30,7 stupnjeva 2θ;
(ii) otprilike 4,3, 7,7, 9,2, 10,9, 12,8, 14,2, 15,6, 16,6, 16,9, 18,1, 18,6, 22,1, 24,0, 24,2, 25,9, 27,1, te 28,8 stupnjeva 2θ; ili
(iii) otprilike 4,3, 7,7, 15,6, 16,6, 16,9, 18,1, 18,6, 22,1, 24,0, 27,1, te 28,8 stupnjeva 2θ.
5. Kristalni oblik u skladu s patentnim zahtjevom 4, gdje je kristalni oblik naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (XRPD) koji sadrži kutove difrakcije, prilikom mjerenja uz pomoć zračenja Cu Kα, od otprilike 4,3, 7,7, 18,1, 18,6, 22,1, te 24,0 stupnjeva 2θ.
6. Kristalni oblik u skladu s patentnim zahtjevom 4 ili patentnim zahtjevom 5, gdje je kristalni oblik naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (XRPD) koji uglavnom odgovara slici 2.
7. Farmaceutski pripravak, naznačen time što sadrži kristalni oblik u skladu s bilo kojim od patentnih zahtjeva 1-6, kao i farmaceutski prihvatljivi nosač.
8. Pripravak u skladu s patentnim zahtjevom 7, naznačen time što je pripravak prilagođen za oralnu primjenu.
9. Pripravak u skladu s patentnim zahtjevom 8, naznačen time što je pripravak u obliku tablete ili kapsule.
10. Kristalni oblik u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time što je namijenjen upotrebi u terapiji.
11. Kristalni oblik u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time što je namijenjen upotrebi u liječenju raka.
12. Kristalni oblik u skladu s patentnim zahtjevom 11, naznačen time što se rak bira iz skupine koju čine hematopoetski rak, rak pluća, rak prostate, melanom, te rak gušterače.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462016819P | 2014-06-25 | 2014-06-25 | |
PCT/IB2015/054712 WO2015198229A1 (en) | 2014-06-25 | 2015-06-23 | Crystalline salts of (s)-6-((1-acetylpiperidin-4-yl)amino)-n-(3-(3,4-dihydroisoquinolin-2(1h)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide |
EP15733921.9A EP3160958B1 (en) | 2014-06-25 | 2015-06-23 | Crystalline salts of (s)-6-((1-acetylpiperidin-4-yl)amino)-n-(3-(3,4-dihydroisoquinolin-2(1h)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20210681T1 true HRP20210681T1 (hr) | 2021-06-11 |
Family
ID=53510948
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20210681TT HRP20210681T1 (hr) | 2014-06-25 | 2021-04-29 | Kristalne soli (s)-6-((1-acetilpiperidin-4-il)amino)-n-(3-(3,4-dihidroizokinolin-2(1h)-il)-2-hidroksipropil)pirimidin-4-karboksamida |
Country Status (29)
Country | Link |
---|---|
US (2) | US9884846B2 (hr) |
EP (1) | EP3160958B1 (hr) |
JP (1) | JP6559719B2 (hr) |
KR (1) | KR102493854B1 (hr) |
CN (1) | CN106536511B (hr) |
AU (1) | AU2015278728B2 (hr) |
BR (1) | BR112016030586B1 (hr) |
CA (1) | CA2952567A1 (hr) |
CL (1) | CL2016003278A1 (hr) |
CR (1) | CR20160598A (hr) |
CY (1) | CY1124085T1 (hr) |
DK (1) | DK3160958T3 (hr) |
DO (1) | DOP2016000333A (hr) |
EA (1) | EA032017B1 (hr) |
ES (1) | ES2869374T3 (hr) |
HR (1) | HRP20210681T1 (hr) |
HU (1) | HUE054454T2 (hr) |
IL (1) | IL249491A0 (hr) |
LT (1) | LT3160958T (hr) |
MA (1) | MA40219B1 (hr) |
MX (1) | MX2017000134A (hr) |
PE (1) | PE20170146A1 (hr) |
PH (1) | PH12016502523A1 (hr) |
PL (1) | PL3160958T3 (hr) |
PT (1) | PT3160958T (hr) |
RS (1) | RS61731B1 (hr) |
SG (1) | SG11201610709UA (hr) |
SI (1) | SI3160958T1 (hr) |
WO (1) | WO2015198229A1 (hr) |
Families Citing this family (16)
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DK2935222T3 (en) | 2012-12-21 | 2019-01-07 | Epizyme Inc | PRMT5 INHIBITORS AND APPLICATIONS THEREOF |
WO2016022605A1 (en) * | 2014-08-04 | 2016-02-11 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
GB201604029D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604030D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604020D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604022D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604027D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604031D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
US11098059B2 (en) | 2017-11-08 | 2021-08-24 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
CN111712498B (zh) | 2017-12-13 | 2023-09-29 | 鲁平有限公司 | 作为prmt5抑制剂的取代的二环杂环化合物 |
WO2020250123A1 (en) | 2019-06-10 | 2020-12-17 | Lupin Limited | Prmt5 inhibitors |
CR20220175A (es) | 2019-10-22 | 2022-06-21 | Lupin Ltd | Combinación farmacéutica de inhibidores de PRMT5 |
US20230066014A1 (en) | 2019-12-03 | 2023-03-02 | Lupin Limited | Substituted nucleoside analogs as prmt5 inhibitors |
CN112206218B (zh) * | 2020-10-24 | 2022-08-23 | 迪沙药业集团有限公司 | 一种甲硝唑维生素b6组合物 |
WO2024038004A1 (en) | 2022-08-15 | 2024-02-22 | Astrazeneca Ab | Mta-cooperative prmt5 inhibitors for use in the treatment of cancer |
KR20240024419A (ko) * | 2022-08-16 | 2024-02-26 | 제이투에이치바이오텍 (주) | 피리미딘-4-카복사마이드 화합물의 결정형 및 이를 포함하는 경구용 약학 제제 |
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2015
- 2015-06-23 HU HUE15733921A patent/HUE054454T2/hu unknown
- 2015-06-23 ES ES15733921T patent/ES2869374T3/es active Active
- 2015-06-23 PL PL15733921T patent/PL3160958T3/pl unknown
- 2015-06-23 KR KR1020177001796A patent/KR102493854B1/ko active IP Right Grant
- 2015-06-23 EP EP15733921.9A patent/EP3160958B1/en active Active
- 2015-06-23 LT LTEP15733921.9T patent/LT3160958T/lt unknown
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2021
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