KR20160003115A - 제스트 인핸서 상동체 2 억제제 - Google Patents
제스트 인핸서 상동체 2 억제제 Download PDFInfo
- Publication number
- KR20160003115A KR20160003115A KR1020157033651A KR20157033651A KR20160003115A KR 20160003115 A KR20160003115 A KR 20160003115A KR 1020157033651 A KR1020157033651 A KR 1020157033651A KR 20157033651 A KR20157033651 A KR 20157033651A KR 20160003115 A KR20160003115 A KR 20160003115A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- methyl
- carboxamide
- cycloalkyl
- heterocycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
- 0 CCN(C1CCOCC1)c1c[s]c(C(NCC2=C(C)C=C(C)NC2=O)=*)c1C Chemical compound CCN(C1CCOCC1)c1c[s]c(C(NCC2=C(C)C=C(C)NC2=O)=*)c1C 0.000 description 8
- AIIOKHOKGAEZOV-HFCKKAISSA-N CC(C)(C)OC(N[C@H](CC1)CC[C@@H]1/C(/c1c(C)c(C(OC)=O)c[s]1)=C\C)=O Chemical compound CC(C)(C)OC(N[C@H](CC1)CC[C@@H]1/C(/c1c(C)c(C(OC)=O)c[s]1)=C\C)=O AIIOKHOKGAEZOV-HFCKKAISSA-N 0.000 description 2
- PCJPGNCABBDNJU-UHFFFAOYSA-N CC(C=C(C)N1)=C(CN)C1=O Chemical compound CC(C=C(C)N1)=C(CN)C1=O PCJPGNCABBDNJU-UHFFFAOYSA-N 0.000 description 2
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- SAPSRQJMZHFDOW-UHFFFAOYSA-N CC(NC1=O)=CC(Cl)=C1C#N Chemical compound CC(NC1=O)=CC(Cl)=C1C#N SAPSRQJMZHFDOW-UHFFFAOYSA-N 0.000 description 1
- WMPRWVSFHGPPNE-UHFFFAOYSA-N CC(NC1=O)=CC(O)=C1C#N Chemical compound CC(NC1=O)=CC(O)=C1C#N WMPRWVSFHGPPNE-UHFFFAOYSA-N 0.000 description 1
- ZDIWSICUBDWNBI-UHFFFAOYSA-N CC(c1c(C)c(C(OC)=O)c[s]1)=O Chemical compound CC(c1c(C)c(C(OC)=O)c[s]1)=O ZDIWSICUBDWNBI-UHFFFAOYSA-N 0.000 description 1
- CHYKQJNGGRRADW-UHFFFAOYSA-N CC(c1c(C)c(C(OC)=O)c[s]1)O Chemical compound CC(c1c(C)c(C(OC)=O)c[s]1)O CHYKQJNGGRRADW-UHFFFAOYSA-N 0.000 description 1
- XCCDOHKTQIGIQF-UHFFFAOYSA-N CC1(C)OB(c2c(C)c(C(OC)=O)c[s]2)OC1(C)C Chemical compound CC1(C)OB(c2c(C)c(C(OC)=O)c[s]2)OC1(C)C XCCDOHKTQIGIQF-UHFFFAOYSA-N 0.000 description 1
- HXOSRBBMCNHVHF-UHFFFAOYSA-N CCC(C)C(C(CCN(C1)C(OC(C)(C)C)=O)C1F)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 Chemical compound CCC(C)C(C(CCN(C1)C(OC(C)(C)C)=O)C1F)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 HXOSRBBMCNHVHF-UHFFFAOYSA-N 0.000 description 1
- QWQOUCCBLMVBJR-YGQOYYDZSA-N CCC([C@H](CC1)CC[C@@H]1NC(OC(C)(C)C)=O)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 Chemical compound CCC([C@H](CC1)CC[C@@H]1NC(OC(C)(C)C)=O)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 QWQOUCCBLMVBJR-YGQOYYDZSA-N 0.000 description 1
- OBWHFTGGXGNDQX-UHFFFAOYSA-N CCC(c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1)=C1CCNCC1 Chemical compound CCC(c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1)=C1CCNCC1 OBWHFTGGXGNDQX-UHFFFAOYSA-N 0.000 description 1
- LVGCTQDARMZPSW-UHFFFAOYSA-N CCC(c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1)N(CC1)CCC1N(C)C Chemical compound CCC(c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1)N(CC1)CCC1N(C)C LVGCTQDARMZPSW-UHFFFAOYSA-N 0.000 description 1
- ZJLVOCSRTYKWRM-WDZFZDKYSA-N CCCC/C(/c1c(C)c(C(OC)=O)c[s]1)=C/C Chemical compound CCCC/C(/c1c(C)c(C(OC)=O)c[s]1)=C/C ZJLVOCSRTYKWRM-WDZFZDKYSA-N 0.000 description 1
- CSCSQDXFHIMCOA-UHFFFAOYSA-N CCN(C(CCN(C1)C(OC(C)(C)C)=O)C1F)c1c(C)c(C(O)=O)c[s]1 Chemical compound CCN(C(CCN(C1)C(OC(C)(C)C)=O)C1F)c1c(C)c(C(O)=O)c[s]1 CSCSQDXFHIMCOA-UHFFFAOYSA-N 0.000 description 1
- FZYCWJYPPHUYEK-UHFFFAOYSA-N CCN(C(CCNC1)C1F)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 Chemical compound CCN(C(CCNC1)C1F)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 FZYCWJYPPHUYEK-UHFFFAOYSA-N 0.000 description 1
- SBXDDBKIMZNNKE-SHTZXODSSA-N CCN(C)[C@H](CC1)CC[C@@H]1N(CC)c1c(C)c(C(CO)=O)c[s]1 Chemical compound CCN(C)[C@H](CC1)CC[C@@H]1N(CC)c1c(C)c(C(CO)=O)c[s]1 SBXDDBKIMZNNKE-SHTZXODSSA-N 0.000 description 1
- CJIZFOICFTVTGK-UHFFFAOYSA-N CCN(C1CCCCC1)c1c(C)c(C(OC)=[U])c(C#N)[s]1 Chemical compound CCN(C1CCCCC1)c1c(C)c(C(OC)=[U])c(C#N)[s]1 CJIZFOICFTVTGK-UHFFFAOYSA-N 0.000 description 1
- DLGUGHVRKSRQGE-UHFFFAOYSA-N CCN(C1CCOCC1)c([s]1)c(C)c(C(O)=O)c1Cl Chemical compound CCN(C1CCOCC1)c([s]1)c(C)c(C(O)=O)c1Cl DLGUGHVRKSRQGE-UHFFFAOYSA-N 0.000 description 1
- IESJTEZXBWQDBI-UHFFFAOYSA-N CCN(C1CCOCC1)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)n[n]1C Chemical compound CCN(C1CCOCC1)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)n[n]1C IESJTEZXBWQDBI-UHFFFAOYSA-N 0.000 description 1
- ZOVDMQIGZGEXDX-UHFFFAOYSA-N CCN(C1CCOCC1)c1c(C)c(C(O)=O)c(C)[s]1 Chemical compound CCN(C1CCOCC1)c1c(C)c(C(O)=O)c(C)[s]1 ZOVDMQIGZGEXDX-UHFFFAOYSA-N 0.000 description 1
- WAUYOOANGDXOEM-UHFFFAOYSA-N CCN(C1CCOCC1)c1c(C)c(C(OC)=O)c(C)[s]1 Chemical compound CCN(C1CCOCC1)c1c(C)c(C(OC)=O)c(C)[s]1 WAUYOOANGDXOEM-UHFFFAOYSA-N 0.000 description 1
- QHNQZPFKGBKHQM-UHFFFAOYSA-N CCN(CC)c1c(C)c(C(OC)=O)c[s]1 Chemical compound CCN(CC)c1c(C)c(C(OC)=O)c[s]1 QHNQZPFKGBKHQM-UHFFFAOYSA-N 0.000 description 1
- ZSCQVKGNHJVDAL-DNLFPKPLSA-N CCN([C@H](CC1)CC[C@@H]1C(C)CC(OC(C)(C)C)=O)c1c(C)c(C(OC)=O)c[s]1 Chemical compound CCN([C@H](CC1)CC[C@@H]1C(C)CC(OC(C)(C)C)=O)c1c(C)c(C(OC)=O)c[s]1 ZSCQVKGNHJVDAL-DNLFPKPLSA-N 0.000 description 1
- NEGOYFGGWMLPMB-UHFFFAOYSA-N Cc([n](CC1CCOCC1)nc1)c1C(NCC1=C(C)C=C(C)NC1=O)=O Chemical compound Cc([n](CC1CCOCC1)nc1)c1C(NCC1=C(C)C=C(C)NC1=O)=O NEGOYFGGWMLPMB-UHFFFAOYSA-N 0.000 description 1
- MBNIQASQLNRJAV-UHFFFAOYSA-N Cc(c(C(OC)=O)c[s]1)c1I Chemical compound Cc(c(C(OC)=O)c[s]1)c1I MBNIQASQLNRJAV-UHFFFAOYSA-N 0.000 description 1
- IDHWXXAKXBPVRT-UHFFFAOYSA-N Cc1c(C(CCN)=O)[nH]cc1C(OC)=O Chemical compound Cc1c(C(CCN)=O)[nH]cc1C(OC)=O IDHWXXAKXBPVRT-UHFFFAOYSA-N 0.000 description 1
- QDPUOXFZEKRPQG-UHFFFAOYSA-N Cc1c(C)[s]c(Br)c1C(OC)=O Chemical compound Cc1c(C)[s]c(Br)c1C(OC)=O QDPUOXFZEKRPQG-UHFFFAOYSA-N 0.000 description 1
- FCKSGPKSSPUXOP-UHFFFAOYSA-N Cc1c[s]cc1C(OC)=O Chemical compound Cc1c[s]cc1C(OC)=O FCKSGPKSSPUXOP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- 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
- 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
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
Landscapes
- 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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361817436P | 2013-04-30 | 2013-04-30 | |
| US61/817,436 | 2013-04-30 | ||
| US201361842038P | 2013-07-02 | 2013-07-02 | |
| US61/842,038 | 2013-07-02 | ||
| US201361907024P | 2013-11-21 | 2013-11-21 | |
| US61/907,024 | 2013-11-21 | ||
| US201461936460P | 2014-02-06 | 2014-02-06 | |
| US61/936,460 | 2014-02-06 | ||
| PCT/IB2014/061012 WO2014177982A1 (en) | 2013-04-30 | 2014-04-25 | Enhancer of zeste homolog 2 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20160003115A true KR20160003115A (ko) | 2016-01-08 |
Family
ID=50877537
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020157033651A Ceased KR20160003115A (ko) | 2013-04-30 | 2014-04-25 | 제스트 인핸서 상동체 2 억제제 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US9505745B2 (enExample) |
| EP (1) | EP2991980B1 (enExample) |
| JP (1) | JP6373973B2 (enExample) |
| KR (1) | KR20160003115A (enExample) |
| CN (1) | CN105308038B (enExample) |
| AU (1) | AU2014261075B2 (enExample) |
| BR (1) | BR112015027527A2 (enExample) |
| CA (1) | CA2910873A1 (enExample) |
| CL (1) | CL2015003200A1 (enExample) |
| DO (1) | DOP2015000270A (enExample) |
| EA (1) | EA030196B1 (enExample) |
| ES (1) | ES2717680T3 (enExample) |
| HK (1) | HK1214815A1 (enExample) |
| MX (1) | MX2015015144A (enExample) |
| NZ (1) | NZ630205A (enExample) |
| PE (1) | PE20151981A1 (enExample) |
| PH (1) | PH12015502414A1 (enExample) |
| SG (1) | SG11201508203TA (enExample) |
| WO (1) | WO2014177982A1 (enExample) |
| ZA (1) | ZA201507398B (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2862289C (en) * | 2012-02-10 | 2019-11-26 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| KR102021642B1 (ko) | 2012-10-15 | 2019-09-16 | 에피자임, 인코포레이티드 | 암을 치료하는 방법 |
| US9505745B2 (en) * | 2013-04-30 | 2016-11-29 | Glaxosmithkline Intellectual Property (No. 2) Limited | Enhancer of zeste homolog 2 inhibitors |
| EP3019494B1 (en) | 2013-07-10 | 2017-06-21 | Glaxosmithkline Intellectual Property (No. 2) Limited | Enhancer of zeste homolog 2 inhibitors |
| EP3102568B1 (en) | 2014-02-06 | 2018-06-27 | Heptares Therapeutics Limited | Bicyclic aza compounds as muscarinic m1 receptor agonists. |
| CN107148419A (zh) * | 2014-10-28 | 2017-09-08 | 葛兰素史密斯克莱知识产权（第2 号）有限公司 | Zeste增强子同源物2抑制剂 |
| TW201636344A (zh) | 2014-12-05 | 2016-10-16 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| UY36758A (es) * | 2015-06-30 | 2016-12-30 | Glaxosmithkline Ip No 2 Ltd | Inhibidores del potenciador del homólogo zeste 2 |
| CN108025191A (zh) | 2015-08-24 | 2018-05-11 | Epizyme股份有限公司 | 治疗癌症的方法 |
| TW201718598A (zh) * | 2015-08-27 | 2017-06-01 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| US20190070188A1 (en) * | 2015-11-06 | 2019-03-07 | Epizyme, Inc. | Pediatric dosing for treatment of cancer with an ezh2 inhibitor |
| WO2017084494A1 (zh) | 2015-11-19 | 2017-05-26 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| MX2018013519A (es) * | 2016-05-05 | 2019-03-14 | Glaxosmithkline Ip No 2 Ltd | Inhibidores del potenciador del homologo zeste 2. |
| US20170337814A1 (en) * | 2016-05-20 | 2017-11-23 | Donald Edward Morgan | Safety alerting drivers device and system |
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| CA2910873A1 (en) | 2014-11-06 |
| US9790212B2 (en) | 2017-10-17 |
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| ES2717680T3 (es) | 2019-06-24 |
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