KR20170032421A - Pde4 억제제로서의 신규한 2,5-치환된 피리미딘 - Google Patents
Pde4 억제제로서의 신규한 2,5-치환된 피리미딘 Download PDFInfo
- Publication number
- KR20170032421A KR20170032421A KR1020177004412A KR20177004412A KR20170032421A KR 20170032421 A KR20170032421 A KR 20170032421A KR 1020177004412 A KR1020177004412 A KR 1020177004412A KR 20177004412 A KR20177004412 A KR 20177004412A KR 20170032421 A KR20170032421 A KR 20170032421A
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- South Korea
- Prior art keywords
- alkyl
- alkylene
- mmol
- compound
- alkoxy
- 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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- FQOYSLAHADTEEB-UHFFFAOYSA-N CSc(c(c1c2)ccc2C(O)=O)n[n]1-c(nc1)ncc1-c(cccc1)c1F Chemical compound CSc(c(c1c2)ccc2C(O)=O)n[n]1-c(nc1)ncc1-c(cccc1)c1F FQOYSLAHADTEEB-UHFFFAOYSA-N 0.000 description 2
- AJRJUAZESCXGHV-UHFFFAOYSA-O CC(C)(C)OC(N(CC1)CCN1C(c(cc1)cc([NH2+]c(nc2)ncc2-c(cccc2)c2F)c1C(SC)=N)=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCN1C(c(cc1)cc([NH2+]c(nc2)ncc2-c(cccc2)c2F)c1C(SC)=N)=O)=O AJRJUAZESCXGHV-UHFFFAOYSA-O 0.000 description 1
- MAOVVPKVYMTXCL-UHFFFAOYSA-N CS(c(c(c1c2)ccc2C(N2CCOCC2)=O)n[n]1-c(nc1)ncc1-c(cc(C1CC1)cc1)c1F)=O Chemical compound CS(c(c(c1c2)ccc2C(N2CCOCC2)=O)n[n]1-c(nc1)ncc1-c(cc(C1CC1)cc1)c1F)=O MAOVVPKVYMTXCL-UHFFFAOYSA-N 0.000 description 1
- SUFYBFUMHHPQBM-UHFFFAOYSA-O CSC(c(ccc(C(N1CCOCC1)=O)c1)c1[NH2+]c(nc1)ncc1-c(cccc1)c1F)=N Chemical compound CSC(c(ccc(C(N1CCOCC1)=O)c1)c1[NH2+]c(nc1)ncc1-c(cccc1)c1F)=N SUFYBFUMHHPQBM-UHFFFAOYSA-O 0.000 description 1
- JWXKHKGCEVXFEJ-UHFFFAOYSA-N Cc(c(c1c2)ccc2C(OC)=O)n[n]1-c(nc1)ncc1-c1ccccc1F Chemical compound Cc(c(c1c2)ccc2C(OC)=O)n[n]1-c(nc1)ncc1-c1ccccc1F JWXKHKGCEVXFEJ-UHFFFAOYSA-N 0.000 description 1
- 0 Cc(c(c1c2)ccc2O*)n[n]1-c(nc1)ncc1-c(cccc1)c1F Chemical compound Cc(c(c1c2)ccc2O*)n[n]1-c(nc1)ncc1-c(cccc1)c1F 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- 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
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- 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
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- Y10S514/825—
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- General Health & Medical Sciences (AREA)
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- Engineering & Computer Science (AREA)
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- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
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- Diabetes (AREA)
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- Urology & Nephrology (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
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- Pain & Pain Management (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14002450 | 2014-07-16 | ||
| EP14002450.6 | 2014-07-16 | ||
| PCT/EP2015/001473 WO2016008590A1 (en) | 2014-07-16 | 2015-07-16 | Novel 2,5-substituted pyrimidines as pde4 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20170032421A true KR20170032421A (ko) | 2017-03-22 |
Family
ID=51210959
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020177004412A Withdrawn KR20170032421A (ko) | 2014-07-16 | 2015-07-16 | Pde4 억제제로서의 신규한 2,5-치환된 피리미딘 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US9546158B2 (enExample) |
| EP (2) | EP3169679A1 (enExample) |
| JP (1) | JP6723217B2 (enExample) |
| KR (1) | KR20170032421A (enExample) |
| CN (1) | CN106660996B (enExample) |
| AR (1) | AR101198A1 (enExample) |
| AU (1) | AU2015291475B2 (enExample) |
| BR (1) | BR112017000830A2 (enExample) |
| CA (1) | CA2955053A1 (enExample) |
| CL (1) | CL2017000106A1 (enExample) |
| CO (1) | CO2017001506A2 (enExample) |
| EA (1) | EA201790206A1 (enExample) |
| EC (1) | ECSP17010481A (enExample) |
| IL (1) | IL250026A0 (enExample) |
| MX (1) | MX366839B (enExample) |
| PE (1) | PE20170251A1 (enExample) |
| TW (1) | TW201613896A (enExample) |
| WO (1) | WO2016008590A1 (enExample) |
| ZA (1) | ZA201701131B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR101196A1 (es) | 2014-07-16 | 2016-11-30 | Gruenenthal Gmbh | Compuestos de pirimidina sustituidos |
| AR101198A1 (es) | 2014-07-16 | 2016-11-30 | Gruenenthal Gmbh | Pirimidinas 2,5-sustituidas como inhibidores de pde4b |
| WO2018065849A1 (en) | 2016-10-03 | 2018-04-12 | Koninklijke Philips N.V. | Radiopaque arrangement of electronic components in intra-cardiac echocardiography (ice) catheter |
| CN108570052A (zh) * | 2017-03-13 | 2018-09-25 | 中国科学院上海药物研究所 | 五元杂环并吡嗪化合物、制备方法、中间体、组合和应用 |
| WO2018234354A1 (en) | 2017-06-20 | 2018-12-27 | Grünenthal GmbH | Novel substituted 3-indole and 3-indazole compounds as phosphodiesterase inhibitors |
| WO2018234353A1 (en) | 2017-06-20 | 2018-12-27 | Grünenthal GmbH | Novel substituted indole and indazole compounds as phosphodiesterase inhibitors |
| BR112021007435A2 (pt) * | 2018-10-25 | 2021-08-03 | Merck Patent Gmbh | derivados de 5-azaindazol como antagonistas de receptor de adenosina |
| CN110156785B (zh) * | 2019-04-15 | 2020-08-28 | 浙江大学 | 吲唑类化合物及其制备方法和应用 |
| US20240066027A1 (en) * | 2020-12-03 | 2024-02-29 | Domain Therapeutics | Novel par-2 inhibitors |
| CN115108992B (zh) * | 2022-06-29 | 2024-05-31 | 浙江手心制药有限公司 | 6-氯-2-甲基-2h-吲唑-5-胺的制备方法 |
| CN116836162B (zh) * | 2023-05-24 | 2025-09-05 | 南方医科大学 | 吡唑[4,3-c]吡啶类化合物或其药学上可接受的盐及其应用 |
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| DE3818830A1 (de) | 1988-06-03 | 1989-12-14 | Boehringer Mannheim Gmbh | Bicyclische carboxamide, verfahren zu ihrer herstellung, deren vorstufen, und diese verbindungen enthaltende arzneimittel |
| KR100331255B1 (ko) | 1993-07-02 | 2002-10-25 | 빅굴덴 롬베르그 케미쉐 화부리크 게엠베하 | 플루오로알콕시-치환된벤즈아미드및시클릭뉴클레오티드포스포디에스테라아제억제제로서의그의용도 |
| JP2000198734A (ja) | 1998-12-30 | 2000-07-18 | Pfizer Inc | 胃運動性減弱および関連疾患の治療のための運動性増強薬 |
| PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| US7087597B1 (en) * | 1999-10-12 | 2006-08-08 | Takeda Pharmaceutical Company Limited | Pyrimidine 5-carboxamide compounds, process for producing the same and use thereof |
| JP2001233875A (ja) * | 1999-10-12 | 2001-08-28 | Takeda Chem Ind Ltd | ピリミジン−5−カルボキサミド化合物、その製造法およびその用途 |
| US6436965B1 (en) | 2000-03-02 | 2002-08-20 | Merck Frosst Canada & Co. | PDE IV inhibiting amides, compositions and methods of treatment |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| DE10163991A1 (de) | 2001-12-24 | 2003-07-03 | Merck Patent Gmbh | Pyrrolo-pyrimidine |
| US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
| PL2489659T3 (pl) | 2004-06-24 | 2018-06-29 | Vertex Pharma | Modulatory transporterów posiadających kasetę wiążącą atp |
| US20060293343A1 (en) | 2005-05-18 | 2006-12-28 | Asahi Kasei Pharma Corporation | Pyrimidine derivatives |
| NZ567133A (en) | 2005-09-30 | 2011-07-29 | Vertex Pharma | Deazapurines useful as inhibitors of janus kinases |
| EP1973884B1 (en) * | 2006-01-19 | 2016-08-03 | Orchid Pharma Limited | Novel heterocycles |
| US7863446B2 (en) | 2006-01-19 | 2011-01-04 | Orchid Research Laboratories Limited | Heterocycles |
| US20080207659A1 (en) | 2007-02-15 | 2008-08-28 | Asit Kumar Chakraborti | Inhibitors of phosphodiesterase type 4 |
| TW201512189A (zh) | 2013-04-16 | 2015-04-01 | Gruenenthal Chemie | 新型被取代之嘧啶縮合化合物 |
| AR101197A1 (es) * | 2014-07-16 | 2016-11-30 | Gruenenthal Gmbh | Pirimidinas 2,5-sustituidas |
| AR101198A1 (es) | 2014-07-16 | 2016-11-30 | Gruenenthal Gmbh | Pirimidinas 2,5-sustituidas como inhibidores de pde4b |
| AR101196A1 (es) * | 2014-07-16 | 2016-11-30 | Gruenenthal Gmbh | Compuestos de pirimidina sustituidos |
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- 2015-07-15 US US14/800,252 patent/US9546158B2/en not_active Expired - Fee Related
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- 2015-07-16 PE PE2017000066A patent/PE20170251A1/es not_active Application Discontinuation
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| EP3415510A1 (en) | 2018-12-19 |
| AR101198A1 (es) | 2016-11-30 |
| AU2015291475A1 (en) | 2017-03-09 |
| MX366839B (es) | 2019-07-26 |
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| CO2017001506A2 (es) | 2017-05-10 |
| WO2016008590A1 (en) | 2016-01-21 |
| IL250026A0 (en) | 2017-03-30 |
| PE20170251A1 (es) | 2017-04-21 |
| CL2017000106A1 (es) | 2017-08-04 |
| JP2017520598A (ja) | 2017-07-27 |
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| CN106660996A (zh) | 2017-05-10 |
| MX2017000521A (es) | 2017-05-01 |
| EP3169679A1 (en) | 2017-05-24 |
| US9546158B2 (en) | 2017-01-17 |
| AU2015291475B2 (en) | 2019-02-07 |
| US10391099B2 (en) | 2019-08-27 |
| BR112017000830A2 (pt) | 2017-12-05 |
| JP6723217B2 (ja) | 2020-07-15 |
| ECSP17010481A (es) | 2017-03-31 |
| CN106660996B (zh) | 2020-10-16 |
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