JP7030827B2 - Ssao阻害剤として有用なアミノピリミジン化合物 - Google Patents
Ssao阻害剤として有用なアミノピリミジン化合物 Download PDFInfo
- Publication number
- JP7030827B2 JP7030827B2 JP2019543810A JP2019543810A JP7030827B2 JP 7030827 B2 JP7030827 B2 JP 7030827B2 JP 2019543810 A JP2019543810 A JP 2019543810A JP 2019543810 A JP2019543810 A JP 2019543810A JP 7030827 B2 JP7030827 B2 JP 7030827B2
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- Japan
- Prior art keywords
- mmol
- mixture
- tert
- give
- methyl
- 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.)
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- 0 *c(nc1)ncc1OCC(CN)=CF Chemical compound *c(nc1)ncc1OCC(CN)=CF 0.000 description 6
- MSRUASHLBGHFBF-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1(CCBr)C(OC)=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1(CCBr)C(OC)=O)=O MSRUASHLBGHFBF-UHFFFAOYSA-N 0.000 description 1
- ZIXCCEUQDJBJIZ-XNTDXEJSSA-N CC(C)(C)OC(NC/C(/COc1cnc(N(CC2)CCC2C(N(C)C)=O)nc1)=C\F)=O Chemical compound CC(C)(C)OC(NC/C(/COc1cnc(N(CC2)CCC2C(N(C)C)=O)nc1)=C\F)=O ZIXCCEUQDJBJIZ-XNTDXEJSSA-N 0.000 description 1
- IRLLLHYGMMQKFU-UHFFFAOYSA-N CC(C)(CN1)NC1=O Chemical compound CC(C)(CN1)NC1=O IRLLLHYGMMQKFU-UHFFFAOYSA-N 0.000 description 1
- XZZAOUXSAPIJCE-RIYZIHGNSA-N CC(CC1(CC2)CCN2C2N=CC(OC/C(/CN)=C/F)=CN2)N(C)C1=O Chemical compound CC(CC1(CC2)CCN2C2N=CC(OC/C(/CN)=C/F)=CN2)N(C)C1=O XZZAOUXSAPIJCE-RIYZIHGNSA-N 0.000 description 1
- AMFRKQGBWOZZCA-UHFFFAOYSA-N CN(CCC1OC2CCNCC2)C1=O Chemical compound CN(CCC1OC2CCNCC2)C1=O AMFRKQGBWOZZCA-UHFFFAOYSA-N 0.000 description 1
- ZCKOCBUOHZFIMC-RUDMXATFSA-N CN(CCN1c(nc2)ncc2OC/C(/CN)=C/F)C1=O Chemical compound CN(CCN1c(nc2)ncc2OC/C(/CN)=C/F)C1=O ZCKOCBUOHZFIMC-RUDMXATFSA-N 0.000 description 1
- QAWUUSAAEXRQOF-BJMVGYQFSA-N NC/C(/COc(cc1)cnc1N(CCN1)CC1=O)=C\F Chemical compound NC/C(/COc(cc1)cnc1N(CCN1)CC1=O)=C\F QAWUUSAAEXRQOF-BJMVGYQFSA-N 0.000 description 1
- DGYUSABUTWNBOU-UHFFFAOYSA-N O=C1NCCC1(CC1)CCN1c(nc1)ncc1OCc1ccccc1 Chemical compound O=C1NCCC1(CC1)CCN1c(nc1)ncc1OCc1ccccc1 DGYUSABUTWNBOU-UHFFFAOYSA-N 0.000 description 1
- HDACDDSPBQTVCH-UHFFFAOYSA-N OC(CC1)CN1C=O Chemical compound OC(CC1)CN1C=O HDACDDSPBQTVCH-UHFFFAOYSA-N 0.000 description 1
- VCPPNRNBMQRKGE-UHFFFAOYSA-N Oc1cnc(N(CC2)CCC2(CCCN2)C2=O)nc1 Chemical compound Oc1cnc(N(CC2)CCC2(CCCN2)C2=O)nc1 VCPPNRNBMQRKGE-UHFFFAOYSA-N 0.000 description 1
- COXYYNSHUGDIRL-UHFFFAOYSA-N Oc1cnc(N(CC2)CCC2(CCN2C3CC3)C2=O)nc1 Chemical compound Oc1cnc(N(CC2)CCC2(CCN2C3CC3)C2=O)nc1 COXYYNSHUGDIRL-UHFFFAOYSA-N 0.000 description 1
- WTDRWDUTUWDVBC-UHFFFAOYSA-N Oc1cnc(N(CC2)CCC2(CCN2CC3CC3)C2=O)nc1 Chemical compound Oc1cnc(N(CC2)CCC2(CCN2CC3CC3)C2=O)nc1 WTDRWDUTUWDVBC-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- General Chemical & Material Sciences (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2022025774A JP7247389B2 (ja) | 2017-02-14 | 2022-02-22 | Ssao阻害剤として有用なアミノピリミジン化合物 |
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNPCT/CN2017/000157 | 2017-02-14 | ||
PCT/CN2017/000157 WO2018148856A1 (en) | 2017-02-14 | 2017-02-14 | Diazaspirodecanyl-pyrimidine compounds useful as ssao inhibitors |
CNPCT/CN2017/117791 | 2017-12-21 | ||
PCT/CN2017/117791 WO2018149226A1 (en) | 2017-02-14 | 2017-12-21 | Amino pyrimidine compounds useful as ssao inhibitors |
PCT/US2018/017152 WO2018151985A1 (en) | 2017-02-14 | 2018-02-07 | Amino pyrimidine compounds useful as ssao inhibitors |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2022025774A Division JP7247389B2 (ja) | 2017-02-14 | 2022-02-22 | Ssao阻害剤として有用なアミノピリミジン化合物 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2020507589A JP2020507589A (ja) | 2020-03-12 |
JP2020507589A5 JP2020507589A5 (US20070167479A1-20070719-C00034.png) | 2021-03-11 |
JP7030827B2 true JP7030827B2 (ja) | 2022-03-07 |
Family
ID=63169081
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2019543810A Active JP7030827B2 (ja) | 2017-02-14 | 2018-02-07 | Ssao阻害剤として有用なアミノピリミジン化合物 |
JP2022025774A Active JP7247389B2 (ja) | 2017-02-14 | 2022-02-22 | Ssao阻害剤として有用なアミノピリミジン化合物 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2022025774A Active JP7247389B2 (ja) | 2017-02-14 | 2022-02-22 | Ssao阻害剤として有用なアミノピリミジン化合物 |
Country Status (13)
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2018027892A1 (en) | 2016-08-12 | 2018-02-15 | Eli Lilly And Company | Amino pyrimidine ssao inhibitors |
WO2018148856A1 (en) | 2017-02-14 | 2018-08-23 | Eli Lilly And Company | Diazaspirodecanyl-pyrimidine compounds useful as ssao inhibitors |
CN109251166B (zh) * | 2017-07-13 | 2021-11-05 | 广东东阳光药业有限公司 | 抑制ssao/vap-1的胺类化合物及其在医药上的应用 |
CN109810041B (zh) * | 2017-11-21 | 2023-08-15 | 药捷安康(南京)科技股份有限公司 | 卤代烯丙基胺类ssao/vap-1抑制剂及其应用 |
CN109988106B (zh) * | 2017-12-29 | 2023-03-31 | 广东东阳光药业有限公司 | 抑制ssao/vap-1的胺类化合物及其在医药上的应用 |
WO2020006177A1 (en) * | 2018-06-29 | 2020-01-02 | Blade Therapeutics, Inc. | Vascular adhesion protein-1 (vap-1) modulators and therapeutic uses thereof |
CN110938059A (zh) * | 2018-09-25 | 2020-03-31 | 上海轶诺药业有限公司 | 胺基脲敏感性胺氧化酶抑制剂制备及其应用 |
WO2020063854A1 (zh) * | 2018-09-27 | 2020-04-02 | 南京明德新药研发有限公司 | 作为vap-1抑制剂的喹啉类衍生物 |
DK3873600T5 (da) | 2018-10-29 | 2024-03-18 | Boehringer Ingelheim Int | Pyridinylsulfonamidderivater, farmaceutiske sammensætninger og anvendelser deraf |
JP7425793B2 (ja) * | 2018-10-29 | 2024-01-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ピリジニルスルホンアミド誘導体、医薬組成物およびそれらの使用 |
JP2022517085A (ja) * | 2019-01-11 | 2022-03-04 | 南京薬捷安康生物科技有限公司 | ハロゲン化アリルアミン系化合物及びその適用 |
CN111471037B (zh) * | 2019-01-23 | 2023-02-10 | 药捷安康(南京)科技股份有限公司 | 烯丙基胺类化合物及其应用 |
MX2022005199A (es) | 2019-10-29 | 2022-08-04 | Eccogene Shanghai Co Ltd | Inhibidores de ssao y uso de los mismos. |
CN113149957A (zh) * | 2020-01-23 | 2021-07-23 | 轶诺(浙江)药业有限公司 | 胺基脲敏感性胺氧化酶抑制剂制备及其应用 |
MX2023002308A (es) | 2020-08-25 | 2023-07-11 | Lilly Co Eli | Polimorfos de un inhibidor de ssao. |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2011504485A (ja) | 2007-11-21 | 2011-02-10 | ファーマクシス リミテッド | Ssao/vap−1のハロアリルアミン阻害剤およびその用途 |
JP2011034078A (ja) | 2009-07-15 | 2011-02-17 | Toshiba Corp | 現像剤、及びその製造方法 |
JP2015521167A (ja) | 2012-05-02 | 2015-07-27 | ファームアクシス・リミテッドPharmaxis Ltd | Ssaoの置換3−ハロアリルアミン阻害剤およびその使用 |
JP2019527717A (ja) | 2016-08-12 | 2019-10-03 | イーライ リリー アンド カンパニー | アミノピリミジンssao阻害剤 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2008123469A1 (ja) | 2007-03-30 | 2008-10-16 | Japan Tobacco Inc. | 6員環アミド化合物およびその用途 |
AU2008280784A1 (en) | 2007-07-20 | 2009-01-29 | Merck Frosst Canada Ltd | Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
TW201116276A (en) * | 2009-09-16 | 2011-05-16 | Astellas Pharma Inc | Glycine compounds |
JP2011136942A (ja) | 2009-12-28 | 2011-07-14 | Kowa Co | 新規な置換ピリミジン誘導体およびこれを含有する医薬 |
HUE028394T2 (en) * | 2011-03-15 | 2016-12-28 | Astellas Pharma Inc | Guanidin Compound |
ES2606197T3 (es) | 2012-11-16 | 2017-03-23 | Bristol-Myers Squibb Company | Moduladores pirrolidina de GPR40 |
US8962641B2 (en) * | 2013-04-17 | 2015-02-24 | Boehringer Ingelheim International Gmbh | Pyrimidine-substituted pyrrolidine derivatives, pharmaceutical compositions and uses thereof |
EP2997024B1 (en) | 2013-05-17 | 2018-03-28 | Boehringer Ingelheim International GmbH | Pyrrolidine derivatives, pharmaceutical compositions and uses thereof |
GB201416444D0 (en) * | 2014-09-17 | 2014-10-29 | Proximagen Ltd | New compounds |
WO2018148856A1 (en) | 2017-02-14 | 2018-08-23 | Eli Lilly And Company | Diazaspirodecanyl-pyrimidine compounds useful as ssao inhibitors |
-
2017
- 2017-02-14 WO PCT/CN2017/000157 patent/WO2018148856A1/en active Application Filing
- 2017-12-21 WO PCT/CN2017/117791 patent/WO2018149226A1/en active Application Filing
-
2018
- 2018-02-07 SG SG11201907032RA patent/SG11201907032RA/en unknown
- 2018-02-07 SG SG10201913492YA patent/SG10201913492YA/en unknown
- 2018-02-07 MX MX2019009501A patent/MX2019009501A/es unknown
- 2018-02-07 JP JP2019543810A patent/JP7030827B2/ja active Active
- 2018-02-07 ES ES18706109T patent/ES2897666T3/es active Active
- 2018-02-07 EP EP18706109.8A patent/EP3582780B1/en active Active
- 2018-02-07 CA CA3052044A patent/CA3052044A1/en active Pending
- 2018-02-07 CN CN202210027271.0A patent/CN114369095A/zh active Pending
- 2018-02-07 DK DK18706109.8T patent/DK3582780T3/da active
- 2018-02-07 WO PCT/US2018/017152 patent/WO2018151985A1/en unknown
- 2018-02-07 KR KR1020197026490A patent/KR20190117007A/ko not_active Application Discontinuation
- 2018-02-07 CN CN201880000825.XA patent/CN108778278B/zh active Active
- 2018-02-07 AU AU2018221322A patent/AU2018221322B2/en active Active
- 2018-06-19 US US16/012,140 patent/US10278970B2/en active Active
-
2019
- 2019-03-18 US US16/356,895 patent/US10471060B2/en active Active
- 2019-08-11 IL IL26862519A patent/IL268625A/en unknown
-
2022
- 2022-02-22 JP JP2022025774A patent/JP7247389B2/ja active Active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2011504485A (ja) | 2007-11-21 | 2011-02-10 | ファーマクシス リミテッド | Ssao/vap−1のハロアリルアミン阻害剤およびその用途 |
JP2011034078A (ja) | 2009-07-15 | 2011-02-17 | Toshiba Corp | 現像剤、及びその製造方法 |
JP2015521167A (ja) | 2012-05-02 | 2015-07-27 | ファームアクシス・リミテッドPharmaxis Ltd | Ssaoの置換3−ハロアリルアミン阻害剤およびその使用 |
JP2019527717A (ja) | 2016-08-12 | 2019-10-03 | イーライ リリー アンド カンパニー | アミノピリミジンssao阻害剤 |
Also Published As
Publication number | Publication date |
---|---|
SG10201913492YA (en) | 2020-03-30 |
KR20190117007A (ko) | 2019-10-15 |
IL268625A (en) | 2019-10-31 |
WO2018149226A1 (en) | 2018-08-23 |
MX2019009501A (es) | 2019-11-05 |
AU2018221322B2 (en) | 2022-04-14 |
SG11201907032RA (en) | 2019-08-27 |
US20190275041A1 (en) | 2019-09-12 |
ES2897666T3 (es) | 2022-03-02 |
EP3582780A1 (en) | 2019-12-25 |
CN108778278A (zh) | 2018-11-09 |
CN108778278B (zh) | 2022-01-28 |
JP7247389B2 (ja) | 2023-03-28 |
US10278970B2 (en) | 2019-05-07 |
JP2020507589A (ja) | 2020-03-12 |
AU2018221322A1 (en) | 2019-08-15 |
WO2018148856A1 (en) | 2018-08-23 |
WO2018151985A1 (en) | 2018-08-23 |
JP2022068325A (ja) | 2022-05-09 |
US20180296560A1 (en) | 2018-10-18 |
CA3052044A1 (en) | 2018-08-23 |
CN114369095A (zh) | 2022-04-19 |
DK3582780T3 (da) | 2021-11-01 |
US10471060B2 (en) | 2019-11-12 |
EP3582780B1 (en) | 2021-10-13 |
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