KR20110050654A - Ｊａｋ3 억제제로서의 피페리딘 유도체 - Google Patents
Ｊａｋ3 억제제로서의 피페리딘 유도체 Download PDFInfo
- Publication number
- KR20110050654A KR20110050654A KR1020117004724A KR20117004724A KR20110050654A KR 20110050654 A KR20110050654 A KR 20110050654A KR 1020117004724 A KR1020117004724 A KR 1020117004724A KR 20117004724 A KR20117004724 A KR 20117004724A KR 20110050654 A KR20110050654 A KR 20110050654A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- formula
- aryl
- heteroaryl
- mmol
- Prior art date
Links
- 0 *c1ccnc2ncc[n]12 Chemical compound *c1ccnc2ncc[n]12 0.000 description 6
- VHJPXPSPHYSBRL-UHFFFAOYSA-N CC(C)c1ncn[n]2ncnc12 Chemical compound CC(C)c1ncn[n]2ncnc12 VHJPXPSPHYSBRL-UHFFFAOYSA-N 0.000 description 1
- BCKTYXNWSVGFKH-UHFFFAOYSA-N CC1NN2C(NC)=CC=NC2=C1 Chemical compound CC1NN2C(NC)=CC=NC2=C1 BCKTYXNWSVGFKH-UHFFFAOYSA-N 0.000 description 1
- XAVAFPFKHDXGGB-UHFFFAOYSA-N CCCc1ncn[n]2c1cnc2 Chemical compound CCCc1ncn[n]2c1cnc2 XAVAFPFKHDXGGB-UHFFFAOYSA-N 0.000 description 1
- LJNNSXVKBWARPK-UHFFFAOYSA-N CNc1nccc2c1cc[nH]2 Chemical compound CNc1nccc2c1cc[nH]2 LJNNSXVKBWARPK-UHFFFAOYSA-N 0.000 description 1
- KKKYYKCAPCBIMZ-MNOVXSKESA-N C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1c2nc[s]c2ncn1 Chemical compound C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1c2nc[s]c2ncn1 KKKYYKCAPCBIMZ-MNOVXSKESA-N 0.000 description 1
- UWKXZBALEGSYLM-YPMHNXCESA-N C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1nc(F)n[n]2c1ccc2 Chemical compound C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1nc(F)n[n]2c1ccc2 UWKXZBALEGSYLM-YPMHNXCESA-N 0.000 description 1
- KJJBHKBCZFOUGL-YPMHNXCESA-N C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1nc(N)n[n]2c1ccc2 Chemical compound C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1nc(N)n[n]2c1ccc2 KJJBHKBCZFOUGL-YPMHNXCESA-N 0.000 description 1
- RAARAKJOALZEMB-YPMHNXCESA-N C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1ncn[n]2c(N)ccc12 Chemical compound C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1ncn[n]2c(N)ccc12 RAARAKJOALZEMB-YPMHNXCESA-N 0.000 description 1
- FTVOOCZJFWWPOB-OCCSQVGLSA-N C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1ncn[n]2c1ccc2 Chemical compound C[C@H](CCN(C1)C(CC#N)=O)[C@H]1N(C)c1ncn[n]2c1ccc2 FTVOOCZJFWWPOB-OCCSQVGLSA-N 0.000 description 1
- IBGRZUYDNYNYGR-ZBFHGGJFSA-N C[C@H](CCN(C1)C2(CC#N)COC2)[C@H]1N(C)c1ncn[n]2c1ccc2 Chemical compound C[C@H](CCN(C1)C2(CC#N)COC2)[C@H]1N(C)c1ncn[n]2c1ccc2 IBGRZUYDNYNYGR-ZBFHGGJFSA-N 0.000 description 1
- ANEJYCBZWKDEAO-UHFFFAOYSA-N Cc1ncnc2c1[nH]cc2 Chemical compound Cc1ncnc2c1[nH]cc2 ANEJYCBZWKDEAO-UHFFFAOYSA-N 0.000 description 1
- NKNFAJHOXKRJJK-UHFFFAOYSA-N Ic1ccnc2ccn[n]12 Chemical compound Ic1ccnc2ccn[n]12 NKNFAJHOXKRJJK-UHFFFAOYSA-N 0.000 description 1
- QGXVGAKMSFELHC-UHFFFAOYSA-N Ic1nccc2c1cc[nH]2 Chemical compound Ic1nccc2c1cc[nH]2 QGXVGAKMSFELHC-UHFFFAOYSA-N 0.000 description 1
- RINRRWDHGQAUGT-UHFFFAOYSA-N Ic1ncn[n]2c1ccc2 Chemical compound Ic1ncn[n]2c1ccc2 RINRRWDHGQAUGT-UHFFFAOYSA-N 0.000 description 1
- SDMUYXVMHJAEFH-UHFFFAOYSA-N Ic1ncnc2c1[nH]cc2 Chemical compound Ic1ncnc2c1[nH]cc2 SDMUYXVMHJAEFH-UHFFFAOYSA-N 0.000 description 1
- QWZFYLPTEFARKF-UHFFFAOYSA-N Ic1ncnc2c1[o]cc2 Chemical compound Ic1ncnc2c1[o]cc2 QWZFYLPTEFARKF-UHFFFAOYSA-N 0.000 description 1
- GJJOKTGMQVRISZ-UHFFFAOYSA-O Nc1c(C=[NH2+])ncnc1I Chemical compound Nc1c(C=[NH2+])ncnc1I GJJOKTGMQVRISZ-UHFFFAOYSA-O 0.000 description 1
- VASAZSNMKDILTC-UHFFFAOYSA-N Nc1ccn[n]2nccc12 Chemical compound Nc1ccn[n]2nccc12 VASAZSNMKDILTC-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8570508P | 2008-08-01 | 2008-08-01 | |
| US61/085,705 | 2008-08-01 | ||
| US9856208P | 2008-09-19 | 2008-09-19 | |
| US61/098,562 | 2008-09-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20110050654A true KR20110050654A (ko) | 2011-05-16 |
Family
ID=41170025
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020117004724A KR20110050654A (ko) | 2008-08-01 | 2009-07-31 | Ｊａｋ3 억제제로서의 피페리딘 유도체 |
Country Status (13)
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2010278730A1 (en) | 2009-07-31 | 2012-03-01 | Biocryst Pharmaceuticals, Inc. | Pyrrolo [1, 2-b] pyridazine derivatives as janus kinase inhibitors |
| AR081428A1 (es) * | 2010-05-28 | 2012-08-29 | Biocryst Pharm Inc | Derivados heterociclicos condensados nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos para suprimir una respuesta inmune o tratar cancer. |
| MX2013013331A (es) * | 2011-05-17 | 2014-10-17 | Principia Biopharma Inc | Derivados de azaindol como inhibidores de tirosina-cinasas. |
| EP2825533B1 (en) | 2012-03-13 | 2016-10-19 | Basf Se | Fungicidal pyrimidine compounds |
| MX361815B (es) | 2012-09-10 | 2018-12-17 | Principia Biopharma Inc | Compuestos pirazolopirimidinicos como inhibidores de cinasas. |
| CN104780924B (zh) * | 2012-11-20 | 2016-09-14 | 葛兰素史克有限责任公司 | 干扰素诱导剂化合物 |
| WO2014097150A1 (en) * | 2012-12-17 | 2014-06-26 | Ranbaxy Laboratories Limited | Process for the preparation of tofacitinib and intermediates thereof |
| WO2014102826A1 (en) * | 2012-12-28 | 2014-07-03 | Glenmark Pharmaceuticals Limited; | The present invention relates to process for the preparation of tofacitinib and intermediates thereof. |
| WO2015036058A1 (en) | 2013-09-16 | 2015-03-19 | Basf Se | Fungicidal pyrimidine compounds |
| WO2015036059A1 (en) | 2013-09-16 | 2015-03-19 | Basf Se | Fungicidal pyrimidine compounds |
| CA2925211A1 (en) * | 2013-09-27 | 2015-04-02 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| ES2865058T3 (es) * | 2013-12-09 | 2021-10-14 | Unichem Lab Ltd | Un proceso mejorado para la preparación de (3R,4R)-(1-bencil-4-metilpiperidin-3-il)-metilamina |
| KR20220027271A (ko) | 2014-02-21 | 2022-03-07 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| CN104860950A (zh) * | 2014-02-24 | 2015-08-26 | 重庆医药工业研究院有限责任公司 | 一种制备4-氯吡咯[2,3-d]并嘧啶的方法 |
| CN104059016A (zh) * | 2014-06-20 | 2014-09-24 | 湖南天地恒一制药有限公司 | 制备托法替布的中间体及所述中间体的制备方法 |
| KR101710127B1 (ko) * | 2014-08-29 | 2017-02-27 | 한화제약주식회사 | 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민 |
| WO2016100914A1 (en) | 2014-12-18 | 2016-06-23 | Gourlay Steven | Treatment of pemphigus |
| CN105732637B (zh) * | 2014-12-30 | 2020-04-21 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| EP3078665A1 (en) * | 2015-04-10 | 2016-10-12 | OLON S.p.A. | Efficient method for the preparation of tofacitinib citrate |
| SG11201710604SA (en) * | 2015-06-22 | 2018-01-30 | Ono Pharmaceutical Co | Brk inhibitory compound |
| TW201718572A (zh) | 2015-06-24 | 2017-06-01 | 普林斯匹亞生物製藥公司 | 酪胺酸激酶抑制劑 |
| WO2017004134A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN105622616A (zh) * | 2016-02-25 | 2016-06-01 | 上海雅本化学有限公司 | 一种4-氯吡咯并嘧啶的制备方法 |
| IL293621B2 (en) | 2016-06-29 | 2023-09-01 | Principia Biopharma Inc | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[4,3-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4 -Methyl-4-[4-(oxane-3-yl)piperazine-1-yl)penta-2-ananitrile |
| GB201617758D0 (en) | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| US11459334B2 (en) | 2018-04-16 | 2022-10-04 | Shenzhen Targetrx, Inc. | Substituted pyrrolo[2,1-f][1,2,4]triazines as KIT and/or PDGFR-α inhibitors |
| CN117164519A (zh) * | 2023-08-18 | 2023-12-05 | 杭州小蓓医药科技有限公司 | 一种l-肌肽的合成方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS50087B (sr) * | 1998-06-19 | 2009-01-22 | Pfizer Products Inc., | Pirolo (2,3-d) pirimidin jedinjenja |
| EA006227B1 (ru) * | 1999-12-10 | 2005-10-27 | Пфайзер Продактс Инк. | СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА |
| CA2412560C (en) * | 2000-06-26 | 2008-12-30 | Pfizer Products Inc. | Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents |
| US7301023B2 (en) * | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| PL378246A1 (pl) * | 2002-11-26 | 2006-03-20 | Pfizer Products Inc. | Sposób leczenia odrzucania przeszczepu |
| OA13050A (en) * | 2003-04-29 | 2006-11-10 | Pfizer Ltd | 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension. |
| EP1689407A1 (en) * | 2003-11-25 | 2006-08-16 | Pfizer Products Inc. | Method of treatment of atherosclerosis |
| AR054416A1 (es) * | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
| US8163767B2 (en) * | 2005-07-14 | 2012-04-24 | Astellas Pharma Inc. | Heterocyclic Janus Kinase 3 inhibitors |
| NL2000291C2 (nl) * | 2005-11-10 | 2009-02-17 | Pfizer Prod Inc | 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H- pyrazool(4,3-d)pyrimidine-5-yl)piperidine-4-carbonzuur en zouten daarvan. |
| TW201111385A (en) * | 2009-08-27 | 2011-04-01 | Biocryst Pharm Inc | Heterocyclic compounds as janus kinase inhibitors |
| SG189837A1 (en) * | 2010-10-08 | 2013-06-28 | Abbvie Inc | FURO[3,2-d]PYRIMIDINE COMPOUNDS |
-
2009
- 2009-07-31 MX MX2011001259A patent/MX2011001259A/es unknown
- 2009-07-31 EP EP09791064A patent/EP2324020A2/en not_active Withdrawn
- 2009-07-31 BR BRPI0916931A patent/BRPI0916931A2/pt not_active IP Right Cessation
- 2009-07-31 AU AU2009276420A patent/AU2009276420A1/en not_active Abandoned
- 2009-07-31 KR KR1020117004724A patent/KR20110050654A/ko not_active Application Discontinuation
- 2009-07-31 US US13/057,100 patent/US20110165183A1/en not_active Abandoned
- 2009-07-31 WO PCT/US2009/052449 patent/WO2010014930A2/en active Application Filing
- 2009-07-31 JP JP2011521361A patent/JP2011529918A/ja active Pending
- 2009-07-31 RU RU2011105768/04A patent/RU2011105768A/ru not_active Application Discontinuation
- 2009-07-31 CA CA2732628A patent/CA2732628A1/en not_active Abandoned
- 2009-07-31 CN CN2009801396041A patent/CN102171211A/zh active Pending
- 2009-07-31 NZ NZ590922A patent/NZ590922A/xx not_active IP Right Cessation
-
2011
- 2011-02-01 IL IL210990A patent/IL210990A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20110165183A1 (en) | 2011-07-07 |
| BRPI0916931A2 (pt) | 2015-11-24 |
| CA2732628A1 (en) | 2010-02-04 |
| NZ590922A (en) | 2012-09-28 |
| RU2011105768A (ru) | 2012-09-10 |
| AU2009276420A1 (en) | 2010-02-04 |
| WO2010014930A2 (en) | 2010-02-04 |
| IL210990A0 (en) | 2011-04-28 |
| WO2010014930A3 (en) | 2010-07-29 |
| EP2324020A2 (en) | 2011-05-25 |
| CN102171211A (zh) | 2011-08-31 |
| JP2011529918A (ja) | 2011-12-15 |
| MX2011001259A (es) | 2011-03-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |