HRP20180067T1 - Inhibitori histon demetilaze - Google Patents
Inhibitori histon demetilaze Download PDFInfo
- Publication number
- HRP20180067T1 HRP20180067T1 HRP20180067TT HRP20180067T HRP20180067T1 HR P20180067 T1 HRP20180067 T1 HR P20180067T1 HR P20180067T T HRP20180067T T HR P20180067TT HR P20180067 T HRP20180067 T HR P20180067T HR P20180067 T1 HRP20180067 T1 HR P20180067T1
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- Prior art keywords
- pharmaceutically acceptable
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- acceptable salt
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- 102000008157 Histone Demethylases Human genes 0.000 title 1
- 108010074870 Histone Demethylases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000004452 carbocyclyl group Chemical group 0.000 claims 5
- 125000005884 carbocyclylalkyl group Chemical group 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- JAMULYFATHSZJM-UHFFFAOYSA-N 8-(4-dibenzothiophenyl)-2-(4-morpholinyl)-1-benzopyran-4-one Chemical compound O1C2=C(C=3C=4SC5=CC=CC=C5C=4C=CC=3)C=CC=C2C(=O)C=C1N1CCOCC1 JAMULYFATHSZJM-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
-
- 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
-
- 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
Claims (16)
1. Spoj formule (IIIb), ili njegova farmaceutski prihvatljiva sol,
[image]
gdje, Q je -CO2R1; X je O ili NR5;
R1 je vodik ili alkil; svaki R3 se neovisno bira od hidroksi, halogen, cijano, NH2, NHR4, N(R4)2, NHC(O)R4, NHC(O)OR4, NHC(O)NHR4, NHC(O)N(R4)2, NHS(O)2R4, NR4C(O)R4, NR4C(O)OR4, NR4C(O)NHR4, NR4C(O)N(R4)2, NR4S(O)2R4, alkil, alkenil, alkinil, alkoksi, aril, ariloksi, aralkil, karbociklil, heterociklil, heteroaril, karbociklilalkil, heterociklilalkil ili heteroarilalkil;
svaki R4 se neovisno bira od alkil, aril, aralkil, karbociklil, heterociklil, heteroaril, karbociklilalkil, heterociklilalkil ili heteroarilalkil;
R5 je alkil, alkenil, alkinil, aril, aralkil, karbociklil, heterociklil, heteroaril, karbociklilalkil, heterociklilalkil ili heteroarilalkil; i
n je cijeli broj obabran od 0 ili 1.
2. Spoj ili farmaceutski prihvatljiva sol sukladno patentnom zahtjevu 1, naznačeno time što X je O.
3. Spoj ili farmaceutski prihvatljiva sol sukladno patentnom zahtjevu 1, naznačeno time što X je NR5.
4. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1-3, naznačeno time što R1 je vodik.
5. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1-3, naznačeno time što R1 je alkil.
6. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1, 3 ili 4, naznačeno time što R5 je alkil, i alkil skupina je izborno supstituirana s hidroksi, halo, cijano, alkenil, alkinil, alkoksi, ariloksi, (alkoksi)alkoksi, aminoalkoksi, hidroksalkoksi, NH2, NHR4, N(R4)2, NHC(O)R4, NHC(O)OR4, NHC(O)NHR4, NHC(O)N(R4)2, NHS(O)2R4, NR4C(O)R4, NR4C(O)OR4, NR4C(O)NHR4, NR4C(O)N(R4)2, NR4S(O)2R4, C(O)NHR4, C(O)N(R4)2, C(O)R4, C(O)OR4, S(O)2R4, S(O)2NHR4, S(O)2N(R4)2; i svaki R4 se neovisno bira od alkil, aril, aralkil, karbociklil, heterociklil, heteroaril, karbociklilalkil, heterociklilalkil ili heteroarilalkil.
7. Spoj ili farmacetska prihvatljiva sol sukladno patentnom zahtjevu 1, naznačeno time što R5 je karbociklilalkil, aralkil, heterociklilalkil ili heteroarilalkil.
8. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 ili 3-5, naznačeno time što R5 je karbociklil.
9. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 ili 3-5, naznačeno time što R5 je heterociklil.
10. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1-9, naznačeno time što n je 0.
11. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1-9, naznačeno time što n je 1.
12. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1-11, naznačeno time što R3 je halogen, alkil ili alkoksi.
13. Spoj ili farmaceutski prihvatljiva sol sukladno patentnom zahtjevu 1, izabrano od:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili
[image]
14. Spoj ili farmaceutski prihvatljiva sol odabrano iz:
[image]
[image]
ili
[image]
15. Farmaceutski pripravak koji sadrži spoj ili farmaceutski prihvatljivu sol sukladno bilo kojem od patentnih zahtjeva 1 do 14, i farmaceutski prihvatljiv nosač.
16. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 do 14 za liječenje karcinoma.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261739521P | 2012-12-19 | 2012-12-19 | |
| US201361792930P | 2013-03-15 | 2013-03-15 | |
| EP13866465.1A EP2934145B1 (en) | 2012-12-19 | 2013-12-19 | Histone demethylase inhibitors |
| PCT/US2013/076666 WO2014100463A1 (en) | 2012-12-19 | 2013-12-19 | Histone demethylase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20180067T1 true HRP20180067T1 (hr) | 2018-02-23 |
Family
ID=50931614
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20180067TT HRP20180067T1 (hr) | 2012-12-19 | 2018-01-15 | Inhibitori histon demetilaze |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US9617242B2 (hr) |
| EP (1) | EP2934145B1 (hr) |
| JP (1) | JP6256772B2 (hr) |
| AU (1) | AU2013361255B2 (hr) |
| CA (1) | CA2895355A1 (hr) |
| CY (1) | CY1119901T1 (hr) |
| DK (1) | DK2934145T3 (hr) |
| ES (1) | ES2658597T3 (hr) |
| HR (1) | HRP20180067T1 (hr) |
| HU (1) | HUE037312T2 (hr) |
| LT (1) | LT2934145T (hr) |
| PL (1) | PL2934145T3 (hr) |
| PT (1) | PT2934145T (hr) |
| RS (1) | RS56821B1 (hr) |
| SI (1) | SI2934145T1 (hr) |
| WO (1) | WO2014100463A1 (hr) |
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| CA3139033A1 (en) | 2012-08-22 | 2014-02-27 | Cornell University | Methods for inhibiting fascin |
| AP2015008389A0 (en) | 2012-10-02 | 2015-04-30 | Epitherapeutics Aps | Inhibitors of histone demethylases |
| ES2658597T3 (es) | 2012-12-19 | 2018-03-12 | Celgene Quanticel Research, Inc. | Inhibidores de histona desmetilasa |
| AU2013363957B2 (en) | 2012-12-21 | 2018-03-22 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| AP2015008676A0 (en) | 2013-02-27 | 2015-08-31 | Epitherapeutics Aps | Inhibitors of histone demethylases |
| US9738637B2 (en) | 2013-03-12 | 2017-08-22 | Celgene Quantical Research, Inc. | Histone demethylase inhibitors |
| BR112015022545A2 (pt) | 2013-03-13 | 2017-07-18 | Constellation Pharmaceuticals Inc | compostos de pirazolo e os usos disso |
| CN111349087B (zh) | 2014-02-20 | 2023-07-14 | 康奈尔大学 | 用于抑制肌成束蛋白的化合物和方法 |
| JP6521535B2 (ja) | 2014-06-25 | 2019-05-29 | セルジーン クオンティセル リサーチ，インク． | ヒストンデメチラーゼ阻害剤 |
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| KR20240006683A (ko) | 2021-05-13 | 2024-01-15 | 길리애드 사이언시즈, 인코포레이티드 | TLR8 조절 화합물과 항-HBV siRNA 치료제의 조합물 |
| EP4359389A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| CA3222595A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| US11976072B2 (en) | 2021-06-23 | 2024-05-07 | Gilead Sciences, Inc. | Diacylglycerol kinase modulating compounds |
| CA3222439A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6593349B2 (en) | 2001-03-19 | 2003-07-15 | Icagen, Inc. | Bisarylamines as potassium channel openers |
| WO2004022544A1 (fr) * | 2002-09-05 | 2004-03-18 | Aventis Pharma S.A. | Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant |
| US7442698B2 (en) * | 2003-07-24 | 2008-10-28 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| FR2882361A1 (fr) | 2005-02-22 | 2006-08-25 | Aventis Pharma Sa | Nouveaux derives de 3-aryl-1,2-benzisoxazole, compositions les contenant et leur utilisation |
| EP2069020B1 (en) * | 2006-07-20 | 2010-01-27 | Amgen Inc. | Benzo[d]isoxazole derivatives as c-kit tyrosine kinase inhibitors for the treatment of disorders associated with the over production of histamine |
| JP5506674B2 (ja) | 2007-07-20 | 2014-05-28 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤として活性な置換インダゾール誘導体 |
| EA021367B1 (ru) * | 2008-11-28 | 2015-06-30 | Кова Компани, Лтд. | Производное пиридин-3-карбоксамида |
| US8846935B2 (en) | 2010-05-07 | 2014-09-30 | Glaxosmithkline Llc | Indazoles |
| JP2014511389A (ja) | 2011-02-28 | 2014-05-15 | エピザイム インコーポレイテッド | 置換６，５−縮合二環式ヘテロアリール化合物 |
| ES2658597T3 (es) | 2012-12-19 | 2018-03-12 | Celgene Quanticel Research, Inc. | Inhibidores de histona desmetilasa |
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| ES2658597T3 (es) | 2018-03-12 |
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| AU2013361255B2 (en) | 2017-01-05 |
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| AU2013361255A1 (en) | 2015-07-09 |
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| PL2934145T3 (pl) | 2018-04-30 |
| JP6256772B2 (ja) | 2018-01-10 |
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