JP2018538244A5 - - Google Patents
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- Publication number
- JP2018538244A5 JP2018538244A5 JP2018520428A JP2018520428A JP2018538244A5 JP 2018538244 A5 JP2018538244 A5 JP 2018538244A5 JP 2018520428 A JP2018520428 A JP 2018520428A JP 2018520428 A JP2018520428 A JP 2018520428A JP 2018538244 A5 JP2018538244 A5 JP 2018538244A5
- Authority
- JP
- Japan
- Prior art keywords
- ring
- nitrogen
- oxygen
- sulfur
- membered
- 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.)
- Granted
Links
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 118
- 229910052757 nitrogen Inorganic materials 0.000 claims description 72
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 64
- 229910052760 oxygen Inorganic materials 0.000 claims description 64
- 239000001301 oxygen Chemical group 0.000 claims description 64
- 125000005842 heteroatom Chemical group 0.000 claims description 62
- 229910052717 sulfur Chemical group 0.000 claims description 62
- 239000011593 sulfur Chemical group 0.000 claims description 60
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 56
- 229920006395 saturated elastomer Polymers 0.000 claims description 44
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 21
- 239000000203 mixture Substances 0.000 claims description 17
- 125000000623 heterocyclic group Chemical group 0.000 claims description 14
- 125000002950 monocyclic group Chemical group 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 125000004429 atom Chemical group 0.000 claims description 12
- 125000002619 bicyclic group Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 125000001931 aliphatic group Chemical group 0.000 claims description 6
- 125000002947 alkylene group Chemical group 0.000 claims description 6
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 6
- 125000002837 carbocyclic group Chemical group 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 125000001475 halogen functional group Chemical group 0.000 claims description 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 4
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims description 4
- 238000002648 combination therapy Methods 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 238000009472 formulation Methods 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 201000005787 hematologic cancer Diseases 0.000 claims description 4
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 4
- 125000005549 heteroarylene group Chemical group 0.000 claims description 4
- 230000003993 interaction Effects 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims description 4
- 239000000758 substrate Substances 0.000 claims description 4
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 208000017604 Hodgkin disease Diseases 0.000 claims description 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 2
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 208000000389 T-cell leukemia Diseases 0.000 claims description 2
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims description 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims description 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 claims description 2
- 125000004450 alkenylene group Chemical group 0.000 claims description 2
- 125000004419 alkynylene group Chemical group 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 210000001185 bone marrow Anatomy 0.000 claims description 2
- 230000005907 cancer growth Effects 0.000 claims description 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 230000001419 dependent effect Effects 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 208000031223 plasma cell leukemia Diseases 0.000 claims description 2
- 230000035755 proliferation Effects 0.000 claims description 2
- 201000006845 reticulosarcoma Diseases 0.000 claims description 2
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 230000004083 survival effect Effects 0.000 claims description 2
- 238000000034 method Methods 0.000 description 10
- 0 C[C@@](C(CC1F)=CCC1F)NC(C1=*=CC(*)CN=C1NI**C1CCCCCCC1)=O Chemical compound C[C@@](C(CC1F)=CCC1F)NC(C1=*=CC(*)CN=C1NI**C1CCCCCCC1)=O 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562245606P | 2015-10-23 | 2015-10-23 | |
| US62/245,606 | 2015-10-23 | ||
| PCT/US2016/058255 WO2017070565A1 (en) | 2015-10-23 | 2016-10-21 | Heterocyclic pdk1 inhibitors for use to treat cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018538244A JP2018538244A (ja) | 2018-12-27 |
| JP2018538244A5 true JP2018538244A5 (enExample) | 2019-11-28 |
| JP7094879B2 JP7094879B2 (ja) | 2022-07-04 |
Family
ID=57209945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018520428A Active JP7094879B2 (ja) | 2015-10-23 | 2016-10-21 | がんを処置する使用のための複素環式ｐｄｋ１インヒビター |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US20190015410A1 (enExample) |
| EP (2) | EP3364971B1 (enExample) |
| JP (1) | JP7094879B2 (enExample) |
| KR (1) | KR20180101329A (enExample) |
| CN (1) | CN108697699A (enExample) |
| AU (2) | AU2016342352B2 (enExample) |
| BR (1) | BR112018008025A2 (enExample) |
| CA (1) | CA3002907A1 (enExample) |
| DK (1) | DK3364971T3 (enExample) |
| ES (1) | ES2820770T3 (enExample) |
| MX (1) | MX381727B (enExample) |
| PL (1) | PL3364971T3 (enExample) |
| RU (1) | RU2018118786A (enExample) |
| WO (1) | WO2017070565A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114763326A (zh) * | 2021-01-13 | 2022-07-19 | 南京宁丹新药技术有限公司 | 一类氨基酸酯衍生物及其用途 |
| WO2022221227A1 (en) | 2021-04-13 | 2022-10-20 | Nuvalent, Inc. | Amino-substituted heterocycles for treating cancers with egfr mutations |
| WO2024040241A1 (en) | 2022-08-19 | 2024-02-22 | Viracta Therapeutics, Inc. | Pharmaceutical formulations, processes for preparation, and methods of use |
| WO2024040242A1 (en) * | 2022-08-19 | 2024-02-22 | Viracta Therapeutics, Inc. | Combinations of pdk1 inhibitors and kinase inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| DE69212850T2 (de) | 1991-01-15 | 1997-03-06 | Alcon Lab Inc | Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| DE102005061655A1 (de) * | 2005-12-22 | 2007-06-28 | Merck Patent Gmbh | Diazepinone |
| DK3070077T3 (en) * | 2009-10-06 | 2019-04-01 | Millennium Pharm Inc | HETEROCYCLIC COMPOUNDS USING PDK1 INHIBITORS |
| WO2011067145A1 (en) * | 2009-12-04 | 2011-06-09 | Nerviano Medical Sciences S.R.L. | Tricyclopyrazole derivatives |
| WO2019094779A1 (en) * | 2017-11-09 | 2019-05-16 | Sunesis Pharmaceuticals, Inc. | Pharmaceutical formulations, processes for preparation, and methods of use |
-
2016
- 2016-10-21 US US15/770,369 patent/US20190015410A1/en not_active Abandoned
- 2016-10-21 JP JP2018520428A patent/JP7094879B2/ja active Active
- 2016-10-21 CN CN201680072623.7A patent/CN108697699A/zh active Pending
- 2016-10-21 CA CA3002907A patent/CA3002907A1/en active Pending
- 2016-10-21 RU RU2018118786A patent/RU2018118786A/ru unknown
- 2016-10-21 PL PL16788389T patent/PL3364971T3/pl unknown
- 2016-10-21 EP EP16788389.1A patent/EP3364971B1/en active Active
- 2016-10-21 KR KR1020187014416A patent/KR20180101329A/ko not_active Ceased
- 2016-10-21 MX MX2018004977A patent/MX381727B/es unknown
- 2016-10-21 ES ES16788389T patent/ES2820770T3/es active Active
- 2016-10-21 DK DK16788389.1T patent/DK3364971T3/da active
- 2016-10-21 BR BR112018008025-0A patent/BR112018008025A2/pt not_active Application Discontinuation
- 2016-10-21 EP EP20180303.8A patent/EP3763368A1/en not_active Withdrawn
- 2016-10-21 AU AU2016342352A patent/AU2016342352B2/en not_active Ceased
- 2016-10-21 WO PCT/US2016/058255 patent/WO2017070565A1/en not_active Ceased
-
2022
- 2022-05-12 AU AU2022203204A patent/AU2022203204A1/en not_active Abandoned
- 2022-06-02 US US17/831,041 patent/US20230099829A1/en not_active Abandoned
-
2024
- 2024-03-11 US US18/600,974 patent/US20240207258A1/en not_active Abandoned
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