HRP20201582T1 - Polimorf sik inhibitora - Google Patents
Polimorf sik inhibitora Download PDFInfo
- Publication number
- HRP20201582T1 HRP20201582T1 HRP20201582TT HRP20201582T HRP20201582T1 HR P20201582 T1 HRP20201582 T1 HR P20201582T1 HR P20201582T T HRP20201582T T HR P20201582TT HR P20201582 T HRP20201582 T HR P20201582T HR P20201582 T1 HRP20201582 T1 HR P20201582T1
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- Prior art keywords
- polymorph
- mixture
- lymphoma
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- polymorph according
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- 239000003112 inhibitor Substances 0.000 title 1
- 238000000034 method Methods 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 8
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 6
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 5
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 3
- 238000002441 X-ray diffraction Methods 0.000 claims 3
- 201000003444 follicular lymphoma Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 2
- 238000001816 cooling Methods 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 2
- 201000007924 marginal zone B-cell lymphoma Diseases 0.000 claims 2
- 208000021937 marginal zone lymphoma Diseases 0.000 claims 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000011874 heated mixture Substances 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- QLYCZINKZANMRY-UHFFFAOYSA-N methanesulfonic acid;hydrate Chemical compound O.CS(O)(=O)=O.CS(O)(=O)=O QLYCZINKZANMRY-UHFFFAOYSA-N 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 239000012258 stirred mixture Substances 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Steroid Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (15)
1. Polimorf monohidratne bis-mezilatne soli spoja formule I:
[image]
naznačen rendgenskim uzorkom difrakcije koji sadrži 2θ-refleksije, plus ili minus 0.2 stupnja 2θ, odabranu iz skupine koja se sastoji od A: 13.8, 16.9, 22.9, i 26.1; B: 7.7, 12.9, 17.7, i 18,1; i C: 7.7, 12.9, 13.8, 16.9, 17.7, 18.1, 22.9, i 26.1.
2. Polimorf prema zahtjevu 1, naznačen rendgenskim uzorkom difrakcije prikazan na Sl. 1A ili 1B.
3. Postupak za proizvodnju polimorfa prema zahtjevu 1 ili 2, sadrži:
dodavanje količine sjemenki polimorfa prema zahtjevu 1 ili 2 i otapala polimorfnom obliku 7 hidratne, bis-mezilatne soli spoja formule I da se dobije mješavina;
i
proizvodeći polimorf prema zahtjevu 1 ili 2 u mješavini,
pri čemu polimorfni oblik 7 ima rendgenski uzorak difrakcije koji sadrži 2θ-refleksije, plus ili minus 0.2 stupnja 2θ, odabranu iz skupine koja se sastoji od A: 4.9, 9.8 i 26.7; B: 15.0 i 18.0; i C: 4.9, 9.8, 15.0, 18.0 i 26.7.
4. Postupak prema zahtjevu 3, nadalje sadrži izoliranje polimorfa prema zahtjevu 1 ili 2.
5. Postupak prema zahtjevu 4, naznačen time što otapalo sadrži aceton.
6. Postupak prema zahtjevu 5, naznačen time što otapalo nadalje sadrži vodu.
7. Postupak prema zahtjevu 6, naznačen time što je omjer vode i acetona 1:15 do 1:40, ili gdje je omjer vode i acetona 1:18 do 1:22.
8. Postupak prema bilo kojem od zahtjeva 3 do 7, koji nadalje sadrži:
miješanje mješavine;
zagrijavanje uzburkane mješavine; i
hlađenje zagrijane mješavine.
9. Postupak za proizvodnju polimorfa prema zahtjevu 1 ili 2, sadrži:
a) dodavanje otapala spoju formule I da se dobije mješavina;
b) dodavanje količine metansulfonske kiseline u mješavinu iz koraka (a);
c) zagrijavanje mješavine iz koraka (b);
d) dodavanje količine sjemena polimorfa prema zahtjevu 1 ili 2 mješavini iz koraka (c); i
e) hlađenje mješavine iz koraka (d) da bi se dobio polimorf prema zahtjevu 1 ili 2.
10. Postupak prema zahtjevu 9, nadalje sadrži izoliranje polimorfa prema zahtjevu 1 ili 2.
11. Postupak prema zahtjevu 9, naznačen time što je količina dodane metansulfonske kiseline između 2.0 i 2.4 molarnih ekvivalenata u odnosu na 1 molarni ekvivalent spoja formule I.
12. Polimorf prema zahtjevu 1 ili 2 pripremljen postupkom prema bilo kojem zahtjevu 3 do 11.
13. Farmaceutski pripravak koji sadrži:
polimorf prema bilo kojem od zahtjeva 1, 2 i 12; i
farmaceutski nosač, ekscipijent, pomoćno sredstvo, ili nosač.
14. Predmet proizvodnje koji sadrži polimorf prema bilo kojem od zahtjeva 1, 2 i 12 ili farmaceutski pripravak prema zahtjevu 13.
15. Polimorf prema bilo kojem od zahtjeva 1, 2 i 12; ili farmaceutski pripravak prema zahtjevu 13, se koristi u postupku liječenja stanja kod čovjeka kojem je to potrebno, pri čemu je to stanje odabrano iz skupine koju čine rak i autoimuna bolest,
izborno pri čemu
(a) stanje je odabrano iz skupine koja se sastoji od akutne limfocitne leukemije (ALL), akutne mijeloične leukemije (AML), kronične limfocitne leukemije (CLL), malog limfocitnog limfoma (SLL), mijelodisplastičnog sindroma (MDS), mijeloproliferativne bolesti (MPD) ), kronične mijeloične leukemije (CML), multiplog mijeloma (MM), ne-Hodgkinovog limfoma (NHL), limfoma plaštenih stanica (MCL), folikularnog limfoma (FL), Waldenströmove makroglobulinemije (WM), limfoma T-stanice, limfoma B-stanice, difuznog limfoma velike B-stanice (DLBCL), limfoplazmacitnog limfoma (LPL) i limfoma rubne zone (MZL), poželjno je stanje ne-Hodgkinov limfom (NHL), još poželjnije indolentni ne-Hodgkinov limfom (iNHL), najpoželjnije vatrostalni iNHL ili ne-FL iNHL; ili
(b) pri čemu je stanje odabrano iz skupine koja se sastoji od astme, reumatoidnog artritisa, multiple skleroze, i lupusa.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361860197P | 2013-07-30 | 2013-07-30 | |
| PCT/US2014/048733 WO2015017460A1 (en) | 2013-07-30 | 2014-07-29 | Polymorph of syk inhibitors |
| EP14750289.2A EP3027618B1 (en) | 2013-07-30 | 2014-07-29 | Polymorph of syk inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20201582T1 true HRP20201582T1 (hr) | 2021-02-19 |
Family
ID=51301367
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20201582TT HRP20201582T1 (hr) | 2013-07-30 | 2020-10-05 | Polimorf sik inhibitora |
Country Status (32)
| Country | Link |
|---|---|
| US (4) | US20160168155A1 (hr) |
| EP (1) | EP3027618B1 (hr) |
| JP (1) | JP6230709B2 (hr) |
| KR (1) | KR101810798B1 (hr) |
| CN (1) | CN105452252A (hr) |
| AP (1) | AP2016009008A0 (hr) |
| AR (1) | AR097158A1 (hr) |
| AU (2) | AU2014296308C1 (hr) |
| CA (1) | CA2919661C (hr) |
| CL (1) | CL2016000238A1 (hr) |
| CR (1) | CR20160098A (hr) |
| DK (1) | DK3027618T3 (hr) |
| EA (2) | EA201791873A1 (hr) |
| ES (1) | ES2822285T3 (hr) |
| HK (1) | HK1222390A1 (hr) |
| HR (1) | HRP20201582T1 (hr) |
| HU (1) | HUE052090T2 (hr) |
| IL (1) | IL243579A0 (hr) |
| MD (1) | MD4659B1 (hr) |
| MX (1) | MX2016001304A (hr) |
| MY (1) | MY176803A (hr) |
| NZ (1) | NZ715776A (hr) |
| PE (1) | PE20160862A1 (hr) |
| PH (1) | PH12016500169A1 (hr) |
| PL (1) | PL3027618T3 (hr) |
| PT (1) | PT3027618T (hr) |
| SG (1) | SG11201600385TA (hr) |
| SI (1) | SI3027618T1 (hr) |
| SV (1) | SV2016005149A (hr) |
| TW (1) | TW201602108A (hr) |
| UY (1) | UY35683A (hr) |
| WO (1) | WO2015017460A1 (hr) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104059073B (zh) | 2008-12-08 | 2017-04-12 | 吉利德康涅狄格公司 | 咪唑并哌嗪syk抑制剂 |
| KR101717809B1 (ko) | 2010-03-11 | 2017-03-17 | 질레드 코네티컷 인코포레이티드 | 이미다조피리딘 ｓｙｋ 억제제 |
| ES2822285T3 (es) | 2013-07-30 | 2021-04-30 | Kronos Bio Inc | Polimorfo de inhibidores de SYK |
| SI3027171T1 (sl) * | 2013-07-30 | 2020-08-31 | Gilead Connecticut, Inc. | Formulacija inhibitorjev SYK |
| KR20180002888A (ko) | 2013-12-04 | 2018-01-08 | 길리애드 사이언시즈, 인코포레이티드 | 암을 치료하는 방법 |
| US9290505B2 (en) | 2013-12-23 | 2016-03-22 | Gilead Sciences, Inc. | Substituted imidazo[1,2-a]pyrazines as Syk inhibitors |
| UY35898A (es) | 2013-12-23 | 2015-07-31 | Gilead Sciences Inc | ?compuestos inhibidores de syk y composiciones que los comprenden?. |
| BR112016028641A2 (pt) * | 2014-07-14 | 2017-08-22 | Gilead Sciences Inc | ?método para tratar câncer? |
| TW201639573A (zh) | 2015-02-03 | 2016-11-16 | 吉李德科學股份有限公司 | 有關治療癌症之合併治療 |
| KR20170137200A (ko) | 2015-04-21 | 2017-12-12 | 길리애드 사이언시즈, 인코포레이티드 | Syk 억제제를 사용한 만성 이식편 대 숙주 질환의 치료 |
| WO2017106564A1 (en) | 2015-12-17 | 2017-06-22 | Gilead Sciences, Inc. | Combination of a jak inhibitor and a syk inhibitor for treating cancers and inflammatory disorders |
| CN109071547A (zh) * | 2016-02-26 | 2018-12-21 | 苏州晶云药物科技股份有限公司 | (6-(1H-吲唑-6-基)-N-[4-(4-吗啉基)苯基]咪唑并[1,2-a]吡嗪-8-胺)甲磺酸盐的新晶型 |
| TW201822764A (zh) | 2016-09-14 | 2018-07-01 | 美商基利科學股份有限公司 | Syk抑制劑 |
| US10111882B2 (en) | 2016-09-14 | 2018-10-30 | Gilead Sciences, Inc. | SYK inhibitors |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| WO2018195471A1 (en) | 2017-04-21 | 2018-10-25 | Gilead Sciences, Inc. | Syk inhibitors in combination with hypomethylating agents |
| CA3073871A1 (en) * | 2017-08-25 | 2019-02-28 | Gilead Sciences, Inc. | Polymorphs of syk inhibitors |
| TWI796596B (zh) | 2018-02-13 | 2023-03-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| JP7242702B2 (ja) | 2018-04-19 | 2023-03-20 | ギリアード サイエンシーズ， インコーポレイテッド | Ｐｄ－１／ｐｄ－ｌ１阻害剤 |
| CA3099152C (en) | 2018-05-14 | 2023-10-24 | Gilead Sciences, Inc. | Mcl-1 inhibitors |
| EP4234030A3 (en) | 2018-07-13 | 2023-10-18 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| CN112955435A (zh) | 2018-10-24 | 2021-06-11 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| CN113950479A (zh) | 2019-02-22 | 2022-01-18 | 克洛诺斯生物股份有限公司 | 作为syk抑制剂的缩合吡嗪的固体形式 |
| CN113402506B (zh) * | 2021-06-17 | 2023-06-16 | 四川大学 | 中间体和制备方法及其在合成长春布宁上的应用 |
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