KR20130142137A - 모노아실글리세롤 리파아제 억제제로서의 피페리딘-4-일-아제티딘 다이아미드 - Google Patents
모노아실글리세롤 리파아제 억제제로서의 피페리딘-4-일-아제티딘 다이아미드 Download PDFInfo
- Publication number
- KR20130142137A KR20130142137A KR1020137012911A KR20137012911A KR20130142137A KR 20130142137 A KR20130142137 A KR 20130142137A KR 1020137012911 A KR1020137012911 A KR 1020137012911A KR 20137012911 A KR20137012911 A KR 20137012911A KR 20130142137 A KR20130142137 A KR 20130142137A
- Authority
- KR
- South Korea
- Prior art keywords
- phenyl
- thiazol
- group
- trifluoromethyl
- unsubstituted
- Prior art date
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- BOCVQFNQLOJDLV-UHFFFAOYSA-N CCCNC(c1ncc[s]1)=O Chemical compound CCCNC(c1ncc[s]1)=O BOCVQFNQLOJDLV-UHFFFAOYSA-N 0.000 description 2
- 0 C*(C)c1cccc(C(F)(F)F)c1 Chemical compound C*(C)c1cccc(C(F)(F)F)c1 0.000 description 1
- PJKWQSLEIWSWPK-LHHJGKSTSA-N CC(C)C/C(/Nc(cc1)ccc1F)=C\C=C Chemical compound CC(C)C/C(/Nc(cc1)ccc1F)=C\C=C PJKWQSLEIWSWPK-LHHJGKSTSA-N 0.000 description 1
- QOVJYSPFWNEOTD-UHFFFAOYSA-N COC(CC1)(CCN1C(c1ccccc1)=O)C(C1)CN1C(c1cc(cc(C(F)(F)F)cc2)c2[s]1)=O Chemical compound COC(CC1)(CCN1C(c1ccccc1)=O)C(C1)CN1C(c1cc(cc(C(F)(F)F)cc2)c2[s]1)=O QOVJYSPFWNEOTD-UHFFFAOYSA-N 0.000 description 1
- ZCHJKNUFQIPLCL-UHFFFAOYSA-N COC(c(cc1)cc(cc2)c1[n]2-c(cc1)ccc1F)=O Chemical compound COC(c(cc1)cc(cc2)c1[n]2-c(cc1)ccc1F)=O ZCHJKNUFQIPLCL-UHFFFAOYSA-N 0.000 description 1
- DRYBMFJLYYEOBZ-UHFFFAOYSA-N COC(c(cc1)cc2c1[nH]cc2)=O Chemical compound COC(c(cc1)cc2c1[nH]cc2)=O DRYBMFJLYYEOBZ-UHFFFAOYSA-N 0.000 description 1
- AITNMTXHTIIIBB-UHFFFAOYSA-N Fc(cc1)ccc1Br Chemical compound Fc(cc1)ccc1Br AITNMTXHTIIIBB-UHFFFAOYSA-N 0.000 description 1
- IBCVAYQWXMWFLD-UHFFFAOYSA-N IC(C1)CN1C(c1ccccc1)c1ccccc1 Chemical compound IC(C1)CN1C(c1ccccc1)c1ccccc1 IBCVAYQWXMWFLD-UHFFFAOYSA-N 0.000 description 1
- NZAXGZYPZGEVBD-UHFFFAOYSA-N O=C(c1ccccc1)N(CC1)CCC1=O Chemical compound O=C(c1ccccc1)N(CC1)CCC1=O NZAXGZYPZGEVBD-UHFFFAOYSA-N 0.000 description 1
- NGPMQRXGAGKLNA-UHFFFAOYSA-N O=C(c1ncc[s]1)N(CC1)CCC1C(C1)CN1C(c(cc1)ccc1-c1cccc(C(F)(F)F)c1)=O Chemical compound O=C(c1ncc[s]1)N(CC1)CCC1C(C1)CN1C(c(cc1)ccc1-c1cccc(C(F)(F)F)c1)=O NGPMQRXGAGKLNA-UHFFFAOYSA-N 0.000 description 1
- PPDMNMAECIVDQS-UHFFFAOYSA-N O=C(c1ncc[s]1)N(CC1)CCC1C1CNC1 Chemical compound O=C(c1ncc[s]1)N(CC1)CCC1C1CNC1 PPDMNMAECIVDQS-UHFFFAOYSA-N 0.000 description 1
- OOFNWBRCNZBLOJ-UHFFFAOYSA-N OC(CC1)(CCN1C(c1ccccc1)=O)C(C1)CN1C(c1ccccc1)c1ccccc1 Chemical compound OC(CC1)(CCN1C(c1ccccc1)=O)C(C1)CN1C(c1ccccc1)c1ccccc1 OOFNWBRCNZBLOJ-UHFFFAOYSA-N 0.000 description 1
- CYVZLFMJYDLKEM-UHFFFAOYSA-N OC(CC1)(CCN1C(c1ccccc1)=O)C1CNC1 Chemical compound OC(CC1)(CCN1C(c1ccccc1)=O)C1CNC1 CYVZLFMJYDLKEM-UHFFFAOYSA-N 0.000 description 1
- OHQPVSORYCUZRN-UHFFFAOYSA-N OC(c(cc1)cc(cc2)c1[n]2-c(cc1)ccc1F)=O Chemical compound OC(c(cc1)cc(cc2)c1[n]2-c(cc1)ccc1F)=O OHQPVSORYCUZRN-UHFFFAOYSA-N 0.000 description 1
- LFMPHDUPXVEMAB-UHFFFAOYSA-N OC(c(cc1)ccc1-c1cccc(C(F)(F)F)c1)=O Chemical compound OC(c(cc1)ccc1-c1cccc(C(F)(F)F)c1)=O LFMPHDUPXVEMAB-UHFFFAOYSA-N 0.000 description 1
- ROIKYRUNAMGSHG-UHFFFAOYSA-N OC(c1cc2cc(C(F)(F)F)ccc2[s]1)=O Chemical compound OC(c1cc2cc(C(F)(F)F)ccc2[s]1)=O ROIKYRUNAMGSHG-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
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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
- C07D401/04—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
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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
- C07D401/14—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
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- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
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- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
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- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40587610P | 2010-10-22 | 2010-10-22 | |
| US61/405,876 | 2010-10-22 | ||
| PCT/US2011/057085 WO2012054716A1 (en) | 2010-10-22 | 2011-10-20 | Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20130142137A true KR20130142137A (ko) | 2013-12-27 |
Family
ID=44993878
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020137012911A KR20130142137A (ko) | 2010-10-22 | 2011-10-20 | 모노아실글리세롤 리파아제 억제제로서의 피페리딘-4-일-아제티딘 다이아미드 |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP2629851A1 (he) |
| JP (1) | JP2013540159A (he) |
| KR (1) | KR20130142137A (he) |
| CN (1) | CN103260703A (he) |
| AR (1) | AR083542A1 (he) |
| AU (1) | AU2011316970A1 (he) |
| BR (1) | BR112013009858A2 (he) |
| CA (1) | CA2815350A1 (he) |
| IL (1) | IL225769A0 (he) |
| RU (1) | RU2013123275A (he) |
| TW (1) | TW201305136A (he) |
| WO (1) | WO2012054716A1 (he) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20180129849A (ko) * | 2016-03-31 | 2018-12-05 | 다케다 야쿠힌 고교 가부시키가이샤 | 헤테로시클릭 화합물 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| MX364438B (es) * | 2013-03-15 | 2019-04-26 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| WO2015099196A1 (en) | 2013-12-26 | 2015-07-02 | Takeda Pharmaceutical Company Limited | 4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (magl) inhibitors |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| WO2016049524A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10106556B2 (en) | 2015-03-30 | 2018-10-23 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| BR112017021869A2 (pt) | 2015-04-10 | 2018-12-11 | Araxes Pharma Llc | compostos quinazolina substituídos e métodos de uso dos mesmos |
| EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10882847B2 (en) | 2015-09-28 | 2021-01-05 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| JP2018533939A (ja) | 2015-10-19 | 2018-11-22 | アラクセス ファーマ エルエルシー | Ｒａｓの阻害剤をスクリーニングするための方法 |
| CN108779097A (zh) | 2015-11-16 | 2018-11-09 | 亚瑞克西斯制药公司 | 包含取代的杂环基的2-取代的喹唑啉化合物及其使用方法 |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017143283A1 (en) | 2016-02-19 | 2017-08-24 | Abide Therapeutics, Inc. | Radiolabeled monoacylglycerol lipase occupancy probe |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| WO2017170830A1 (ja) | 2016-03-31 | 2017-10-05 | 武田薬品工業株式会社 | 複素環化合物 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
| JP2019534260A (ja) | 2016-10-07 | 2019-11-28 | アラクセス ファーマ エルエルシー | Ｒａｓの阻害剤としての複素環式化合物およびその使用方法 |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| EP3573967A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused hetero-hetero bicyclic compounds and methods of use thereof |
| EP3630746A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Compounds and methods of use thereof for treatment of cancer |
| EP3630745A2 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Covalent inhibitors of kras |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| WO2019065791A1 (ja) | 2017-09-29 | 2019-04-04 | 武田薬品工業株式会社 | 複素環化合物 |
| EP3717477B1 (en) * | 2017-11-28 | 2022-07-20 | F. Hoffmann-La Roche AG | New heterocyclic compounds |
| AU2019349962A1 (en) * | 2018-09-28 | 2021-03-18 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| CN109879797A (zh) * | 2019-01-10 | 2019-06-14 | 安徽昊帆生物有限公司 | N-苄基-四氢吡啶类化合物及其制备方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9812037D0 (en) * | 1998-06-04 | 1998-07-29 | Pfizer Ltd | Piperidones |
| US8106208B2 (en) * | 2006-05-18 | 2012-01-31 | Albireo Ab | Benzamide compounds that act as NK receptor antagonists |
| FR2915198B1 (fr) * | 2007-04-18 | 2009-12-18 | Sanofi Aventis | Derives de triazolopyridine-carboxamides et triazolopyridine -carboxamides, leur preparation et leur application en therapeutique. |
| AU2009240460B2 (en) * | 2008-04-25 | 2016-03-17 | Janssen Pharmaceutica Nv | Crystal structure of monoacylglycerol lipase (MGLL) |
| KR20120027177A (ko) * | 2009-04-02 | 2012-03-21 | 메르크 파텐트 게엠베하 | 오토탁신 저해제로서의 피페리딘 및 피라진 유도체 |
| RU2549547C2 (ru) * | 2009-04-22 | 2015-04-27 | Янссен Фармацевтика Нв | Азетидинилдиамиды в качестве ингибиторов моноацилглицерин-липазы |
-
2011
- 2011-10-20 JP JP2013535086A patent/JP2013540159A/ja active Pending
- 2011-10-20 CN CN201180061809XA patent/CN103260703A/zh active Pending
- 2011-10-20 WO PCT/US2011/057085 patent/WO2012054716A1/en active Application Filing
- 2011-10-20 KR KR1020137012911A patent/KR20130142137A/ko not_active Application Discontinuation
- 2011-10-20 RU RU2013123275/04A patent/RU2013123275A/ru not_active Application Discontinuation
- 2011-10-20 CA CA2815350A patent/CA2815350A1/en not_active Abandoned
- 2011-10-20 AU AU2011316970A patent/AU2011316970A1/en not_active Abandoned
- 2011-10-20 BR BR112013009858A patent/BR112013009858A2/pt not_active IP Right Cessation
- 2011-10-20 EP EP11784828.3A patent/EP2629851A1/en not_active Withdrawn
- 2011-10-21 TW TW100138198A patent/TW201305136A/zh unknown
- 2011-10-24 AR ARP110103927A patent/AR083542A1/es not_active Application Discontinuation
-
2013
- 2013-04-15 IL IL225769A patent/IL225769A0/he unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20180129849A (ko) * | 2016-03-31 | 2018-12-05 | 다케다 야쿠힌 고교 가부시키가이샤 | 헤테로시클릭 화합물 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103260703A (zh) | 2013-08-21 |
| CA2815350A1 (en) | 2012-04-26 |
| EP2629851A1 (en) | 2013-08-28 |
| TW201305136A (zh) | 2013-02-01 |
| RU2013123275A (ru) | 2014-11-27 |
| IL225769A0 (he) | 2013-06-27 |
| JP2013540159A (ja) | 2013-10-31 |
| AU2011316970A1 (en) | 2013-05-09 |
| BR112013009858A2 (pt) | 2016-07-26 |
| AR083542A1 (es) | 2013-03-06 |
| WO2012054716A1 (en) | 2012-04-26 |
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| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |