KR20110041536A - 5-알키닐-피리미딘 - Google Patents
5-알키닐-피리미딘 Download PDFInfo
- Publication number
- KR20110041536A KR20110041536A KR1020117003951A KR20117003951A KR20110041536A KR 20110041536 A KR20110041536 A KR 20110041536A KR 1020117003951 A KR1020117003951 A KR 1020117003951A KR 20117003951 A KR20117003951 A KR 20117003951A KR 20110041536 A KR20110041536 A KR 20110041536A
- Authority
- KR
- South Korea
- Prior art keywords
- mmol
- membered
- amino
- pyrimidin
- methyl
- Prior art date
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- 125000004404 heteroalkyl group Chemical group 0.000 claims description 14
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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-
- A—HUMAN NECESSITIES
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
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- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- 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
- C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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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- Rheumatology (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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| EP08161369.7 | 2008-07-29 |
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| KR20110041536A true KR20110041536A (ko) | 2011-04-21 |
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| JP5651110B2 (ja) | 2008-07-29 | 2015-01-07 | 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 | 新規化合物 |
| MX2011000729A (es) | 2008-07-29 | 2011-03-15 | Boehringer Ingelheim Int | 5-alquinil-pirimidinas. |
| AR076332A1 (es) * | 2009-04-21 | 2011-06-01 | Boehringer Ingelheim Int | Derivados heterociclicos de 5-alquinil-piridinas, composiciones farmaceuticas que los comprenden y uso de los mismos para el tratamiento y/o prevencion del cancer, procesos inflamatorios, autoinmunes, y/o infecciones. |
| US8633183B2 (en) * | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| UY33198A (es) * | 2010-01-26 | 2011-08-31 | Boehringer Ingelheim Int | 5-alquinil-pirimidinas. |
| TW201245176A (en) * | 2011-01-26 | 2012-11-16 | Boehringer Ingelheim Int | New 5-alkynyl-pyridines |
| US8466162B2 (en) * | 2011-01-26 | 2013-06-18 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyridines |
| JP6016915B2 (ja) * | 2011-07-28 | 2016-10-26 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール |
| UA110995C2 (uk) * | 2011-10-07 | 2016-03-10 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як модулятори метаботропного глутаматного рецептора |
| WO2015089192A1 (en) * | 2013-12-11 | 2015-06-18 | Quanticel Pharmaceuticals, Inc. | Inhibitors of lysine specific demethylase-1 |
| SG11201609033TA (en) | 2014-05-01 | 2016-11-29 | Celgene Quanticel Res Inc | Inhibitors of lysine specific demethylase-1 |
| CN107074787B (zh) * | 2014-09-05 | 2020-10-27 | 赛尔基因昆蒂赛尔研究公司 | 赖氨酸特异性脱甲基酶-1的抑制剂 |
| CN104803921A (zh) * | 2015-03-14 | 2015-07-29 | 长沙深橙生物科技有限公司 | 一种苯取代嘧啶衍生物的制备方法 |
| CN104744376A (zh) * | 2015-03-14 | 2015-07-01 | 长沙深橙生物科技有限公司 | 一种2-异丙基嘧啶衍生物的制备方法 |
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| DE3832570A1 (de) * | 1988-09-24 | 1990-03-29 | Hoechst Ag | 7-substituierte derivate der 3,5-dihydroxyhept-6-insaeure, verfahren zur ihrer herstellung, ihre verwendung als arzneimittel, sowie zwischenprodukte |
| JPH08504798A (ja) | 1992-12-18 | 1996-05-21 | ザ ウエルカム ファウンデーション リミテッド | 酵素阻害薬としての,ピリミジン,ピリジン,プテリジノンおよびインダゾール誘導体 |
| US5622954A (en) | 1994-05-11 | 1997-04-22 | Fmc Corporation | 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides |
| RU2277911C2 (ru) * | 2000-02-25 | 2006-06-20 | Ф.Хоффманн-Ля Рош Аг | Модуляторы аденозиновых рецепторов |
| DK1303495T3 (da) * | 2000-07-24 | 2010-09-20 | Krenitsky Pharmaceuticals Inc | Substituerede 5-alkylnylpyrimidiner med neurotrofisk aktivitet |
| EP1648463A2 (en) * | 2003-06-13 | 2006-04-26 | Zentaris GmbH | Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof |
| ES2309591T3 (es) | 2003-12-24 | 2008-12-16 | Astrazeneca Ab | Pirimidinas con actividad tie2(tek). |
| ES2607804T3 (es) * | 2004-05-13 | 2017-04-04 | Icos Corporation | Quinazolinones como inhibidores de la fosfatidilinositol humana 3-quinasa delta |
| US7776869B2 (en) * | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| US20080146599A1 (en) | 2005-02-01 | 2008-06-19 | Astrazeneca Ab | Pyrimidine Compounds Having Tie-2 (Tek) Inhibitory Activity |
| US20100048543A1 (en) | 2005-02-01 | 2010-02-25 | Astrazeneca Ab | Pyrimidine compounds having ties (tek) inhibitory activity |
| US20070135437A1 (en) | 2005-03-04 | 2007-06-14 | Alsgen, Inc. | Modulation of neurodegenerative diseases |
| WO2006106721A1 (ja) | 2005-03-30 | 2006-10-12 | Shionogi & Co., Ltd. | チロシンキナーゼ阻害作用を有するピリミジン誘導体 |
| US20080194552A1 (en) | 2005-03-31 | 2008-08-14 | Astrazeneca Ab | Aminopyrimidine Derivatives With Tie2 Inhibiting Activity |
| RS53627B1 (sr) * | 2005-10-07 | 2015-04-30 | Exelixis Inc. | Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova upotreba kao inhibitora fosfatidilinozitol3-kinaze |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| EP2057129A1 (en) | 2006-08-24 | 2009-05-13 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| JP5283633B2 (ja) | 2006-12-29 | 2013-09-04 | テイボテク・フアーマシユーチカルズ | Hiv阻害性5,6−置換ピリミジン |
| EP2022785A1 (en) | 2007-06-20 | 2009-02-11 | Bayer Schering Pharma Aktiengesellschaft | Alkynylpyrimidines as Tie2 kinase inhibitors |
| MX2011000729A (es) | 2008-07-29 | 2011-03-15 | Boehringer Ingelheim Int | 5-alquinil-pirimidinas. |
| US8633183B2 (en) | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
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Also Published As
| Publication number | Publication date |
|---|---|
| EA201100255A1 (ru) | 2011-08-30 |
| EP2323992B1 (en) | 2016-07-20 |
| TW201010984A (en) | 2010-03-16 |
| JP5599791B2 (ja) | 2014-10-01 |
| HUE029837T2 (en) | 2017-04-28 |
| MX2011000729A (es) | 2011-03-15 |
| BRPI0916679A2 (pt) | 2015-11-17 |
| AR072845A1 (es) | 2010-09-22 |
| US8916548B2 (en) | 2014-12-23 |
| JP2011529468A (ja) | 2011-12-08 |
| IL210343A0 (en) | 2011-03-31 |
| UY32009A (es) | 2010-02-26 |
| MA32505B1 (fr) | 2011-07-03 |
| CN102112450A (zh) | 2011-06-29 |
| CL2011000195A1 (es) | 2011-07-08 |
| NZ590558A (en) | 2012-12-21 |
| ECSP11010786A (es) | 2011-02-28 |
| US20110281838A1 (en) | 2011-11-17 |
| AU2009275957A1 (en) | 2010-02-04 |
| CO6341617A2 (es) | 2011-11-21 |
| WO2010012740A1 (en) | 2010-02-04 |
| PE20110196A1 (es) | 2011-04-03 |
| EP2323992A1 (en) | 2011-05-25 |
| PL2323992T3 (pl) | 2017-01-31 |
| CA2731909A1 (en) | 2010-02-04 |
| ES2597903T3 (es) | 2017-01-24 |
| DK2323992T3 (en) | 2016-10-31 |
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