CN102971306A - 作为激酶lrrk2的抑制剂的吡唑并吡啶 - Google Patents
作为激酶lrrk2的抑制剂的吡唑并吡啶 Download PDFInfo
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- CN102971306A CN102971306A CN201180033483XA CN201180033483A CN102971306A CN 102971306 A CN102971306 A CN 102971306A CN 201180033483X A CN201180033483X A CN 201180033483XA CN 201180033483 A CN201180033483 A CN 201180033483A CN 102971306 A CN102971306 A CN 102971306A
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- alkyl
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- 0 CC=CCCCC(N(*)*)=O Chemical compound CC=CCCCC(N(*)*)=O 0.000 description 6
- WSCIDZXOMOMUHW-CMDGGOBGSA-N CC1(C)OB(/C(/CC=C)=C/NN)OC1(C)C Chemical compound CC1(C)OB(/C(/CC=C)=C/NN)OC1(C)C WSCIDZXOMOMUHW-CMDGGOBGSA-N 0.000 description 1
- ZBONCJDUPOADKZ-AZZJQTQESA-O CC1C=CC=CC1C(c1ccccc1)(c1ccccc1)N/C(/C=C(/C)\N)=C(/C(OC1CCOCC1)=C)\C(c1c[nH]nc1)=[NH2+] Chemical compound CC1C=CC=CC1C(c1ccccc1)(c1ccccc1)N/C(/C=C(/C)\N)=C(/C(OC1CCOCC1)=C)\C(c1c[nH]nc1)=[NH2+] ZBONCJDUPOADKZ-AZZJQTQESA-O 0.000 description 1
- XCDZWNHCHWCZSW-UHFFFAOYSA-N Cc1cc([n](C(c2ccccc2)(c2ccccc2)c2ccccc2)nc2I)c2c(Cl)n1 Chemical compound Cc1cc([n](C(c2ccccc2)(c2ccccc2)c2ccccc2)nc2I)c2c(Cl)n1 XCDZWNHCHWCZSW-UHFFFAOYSA-N 0.000 description 1
- RULPWVJAZIXJSQ-UHFFFAOYSA-N Cc1n[nH]c2c1c(NC1CCCCC1)cnc2 Chemical compound Cc1n[nH]c2c1c(NC1CCCCC1)cnc2 RULPWVJAZIXJSQ-UHFFFAOYSA-N 0.000 description 1
- HCSRSWLHKKJDJM-UHFFFAOYSA-N Cc1n[nH]c2cncc(-c3ccc[o]3)c12 Chemical compound Cc1n[nH]c2cncc(-c3ccc[o]3)c12 HCSRSWLHKKJDJM-UHFFFAOYSA-N 0.000 description 1
- YYRIQTLBJWWQMZ-UHFFFAOYSA-N Cc1nc(Cl)c(CO)c(Cl)c1 Chemical compound Cc1nc(Cl)c(CO)c(Cl)c1 YYRIQTLBJWWQMZ-UHFFFAOYSA-N 0.000 description 1
- GJXUNKKKYAYFSQ-UHFFFAOYSA-N Cc1nc(Cl)c2c(I)n[nH]c2c1 Chemical compound Cc1nc(Cl)c2c(I)n[nH]c2c1 GJXUNKKKYAYFSQ-UHFFFAOYSA-N 0.000 description 1
- JYJADUJTBJPHKJ-UHFFFAOYSA-O Cc1nc(OC2CCOCC2)c(C(I)=[NH2+])c(NC(c2ccccc2)(c2ccccc2)c2ccccc2)c1 Chemical compound Cc1nc(OC2CCOCC2)c(C(I)=[NH2+])c(NC(c2ccccc2)(c2ccccc2)c2ccccc2)c1 JYJADUJTBJPHKJ-UHFFFAOYSA-O 0.000 description 1
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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
-
- 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
- A61K31/535—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB1008134.7 | 2010-05-14 | ||
GBGB1008134.7A GB201008134D0 (en) | 2010-05-14 | 2010-05-14 | Compounds |
PCT/GB2011/050937 WO2011141756A1 (en) | 2010-05-14 | 2011-05-16 | Pyrazolopyridines as inhibitors of the kinase lrrk2 |
Publications (1)
Publication Number | Publication Date |
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CN102971306A true CN102971306A (zh) | 2013-03-13 |
Family
ID=42334821
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201180033483XA Pending CN102971306A (zh) | 2010-05-14 | 2011-05-16 | 作为激酶lrrk2的抑制剂的吡唑并吡啶 |
Country Status (8)
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103819396A (zh) * | 2014-02-26 | 2014-05-28 | 四川大学 | 一种手性的1-(3,5-二氯吡啶-4-基)-乙醇的合成方法 |
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WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
WO2012135631A1 (en) | 2011-03-30 | 2012-10-04 | Arrien Pharmaeuticals Llc | Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors |
GB201204985D0 (en) | 2012-03-21 | 2012-05-02 | Genentech Inc | Compounds |
US9187484B2 (en) | 2012-05-02 | 2015-11-17 | Southern Research Institute | Triazolopyridazine compounds, use as inhibitors of the kinase LRRK2, and methods for preparation thereof |
CN102675310B (zh) * | 2012-05-09 | 2014-12-24 | 林辉 | 制备吡唑并芳杂环化合物的方法 |
PT3495367T (pt) | 2012-06-13 | 2020-11-12 | Incyte Holdings Corp | Compostos tricíclicos substituídos como inibidores de fgfr |
CN105732639A (zh) * | 2012-06-29 | 2016-07-06 | 辉瑞大药厂 | 作为LRRK2抑制剂的4-(取代的氨基)-7H-吡咯并〔2,3-d〕嘧啶类 |
WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
BR112015010412A2 (pt) | 2012-11-08 | 2017-07-11 | Pfizer | compostos heteroaromáticos e seu uso como ligantes de dopamina d1 |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
US9440952B2 (en) | 2013-03-04 | 2016-09-13 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
WO2014134772A1 (en) | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
WO2014134774A1 (en) | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
WO2014134776A1 (en) | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
PT2970333T (pt) * | 2013-03-15 | 2017-08-01 | Oncodesign Sa | Inibidores macrocíclicos de lrrk2 quinase |
US20140288043A1 (en) * | 2013-03-19 | 2014-09-25 | Genentech, Inc. | Pyrazolopyridine compounds |
TW201533043A (zh) * | 2013-04-18 | 2015-09-01 | Lundbeck & Co As H | 作爲lrrk2抑制劑的芳基吡咯并吡啶衍生化合物 |
TWI715901B (zh) | 2013-04-19 | 2021-01-11 | 美商英塞特控股公司 | 作為fgfr抑制劑之雙環雜環 |
US9718818B2 (en) | 2013-08-22 | 2017-08-01 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
EP3083618B1 (en) * | 2013-12-17 | 2018-02-21 | Pfizer Inc | Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors |
US9868744B2 (en) | 2014-04-25 | 2018-01-16 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine D1 ligands |
US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
CN113004278B (zh) | 2015-02-20 | 2023-07-21 | 因赛特控股公司 | 作为fgfr抑制剂的双环杂环 |
MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
EP3325449B1 (en) * | 2015-07-23 | 2021-01-13 | GlaxoSmithKline Intellectual Property Development Limited | Heterocyclic compounds, particularly pyrimidinylindazole compounds for treating parkinson's disease |
JP6873980B2 (ja) | 2015-09-14 | 2021-05-19 | ファイザー・インク | LRRK2阻害薬としての新規のイミダゾ[4,5−c]キノリンおよびイミダゾ[4,5−c][1,5]ナフチリジン誘導体 |
WO2017087905A1 (en) | 2015-11-20 | 2017-05-26 | Denali Therapeutics Inc. | Compound, compositions, and methods |
CN108934162A (zh) | 2015-12-16 | 2018-12-04 | 南方研究所 | 吡咯并嘧啶化合物、作为激酶lrrk2抑制剂的用途及其制备方法 |
US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
HUE056678T2 (hu) | 2016-06-16 | 2022-02-28 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1H-pirazolok mint LRRK2 inhibitorok neurodegeneratív rendellenességek kezelésére való alkalmazásra |
WO2018049214A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
WO2018049191A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridone derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
TW201811799A (zh) | 2016-09-09 | 2018-04-01 | 美商英塞特公司 | 吡唑并嘧啶化合物及其用途 |
AU2017322427B2 (en) * | 2016-09-09 | 2021-12-23 | Incyte Corporation | Pyrazolopyridine derivatives as HPK1 modulators and uses thereof for the treatment of cancer |
US10040211B2 (en) | 2016-12-09 | 2018-08-07 | Bettcher Industries, Inc. | Power operated rotary knife |
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WO2019213544A2 (en) | 2018-05-04 | 2019-11-07 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
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US10899755B2 (en) | 2018-08-08 | 2021-01-26 | Incyte Corporation | Benzothiazole compounds and uses thereof |
ES2744304B2 (es) | 2018-08-24 | 2020-06-22 | Consejo Superior Investigacion | Compuestos inhibidores de LRRK2 y su uso para el tratamiento de enfermedades neurodegenerativas |
WO2020068729A1 (en) | 2018-09-25 | 2020-04-02 | Incyte Corporation | Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators |
WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
KR20220059480A (ko) | 2019-08-06 | 2022-05-10 | 인사이트 코포레이션 | 고체 형태의 hpk1 억제제 |
TW202128685A (zh) | 2019-10-14 | 2021-08-01 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
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WO2006077319A1 (fr) * | 2005-01-19 | 2006-07-27 | Aventis Pharma S.A. | Pyrazolo pyridines substituees, compositions les contenant, procede de fabrication et utilisation |
WO2007100295A1 (en) * | 2006-03-03 | 2007-09-07 | Torrent Pharmaceuticals Ltd | Novel dual action receptors antagonists (dara) at the ati and eta receptors |
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WO2010106333A1 (en) * | 2009-03-19 | 2010-09-23 | Medical Research Council Technology | Compounds |
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-
2010
- 2010-05-14 GB GBGB1008134.7A patent/GB201008134D0/en not_active Ceased
-
2011
- 2011-05-16 EP EP11720847A patent/EP2569293A1/en not_active Withdrawn
- 2011-05-16 AU AU2011251733A patent/AU2011251733A1/en not_active Abandoned
- 2011-05-16 US US13/697,878 patent/US20130267513A1/en not_active Abandoned
- 2011-05-16 JP JP2013509631A patent/JP2013529196A/ja not_active Withdrawn
- 2011-05-16 CN CN201180033483XA patent/CN102971306A/zh active Pending
- 2011-05-16 CA CA2798222A patent/CA2798222A1/en not_active Abandoned
- 2011-05-16 WO PCT/GB2011/050937 patent/WO2011141756A1/en active Application Filing
Patent Citations (5)
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WO2006077319A1 (fr) * | 2005-01-19 | 2006-07-27 | Aventis Pharma S.A. | Pyrazolo pyridines substituees, compositions les contenant, procede de fabrication et utilisation |
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Title |
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VLADIMIR I. TYVORSKII, ET AL.,: ""Synthesis of 5-alkyl-4-amino-2-(trifuoromethyl)pyridines and their transformation into trifuoromethylated 1H-pyrazolo[4,3-c]pyridines", 《TETRAHEDRON》 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103819396A (zh) * | 2014-02-26 | 2014-05-28 | 四川大学 | 一种手性的1-(3,5-二氯吡啶-4-基)-乙醇的合成方法 |
CN103819396B (zh) * | 2014-02-26 | 2016-06-15 | 四川大学 | 一种手性的1-(3,5-二氯吡啶-4-基)-乙醇的合成方法 |
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EP2569293A1 (en) | 2013-03-20 |
WO2011141756A1 (en) | 2011-11-17 |
JP2013529196A (ja) | 2013-07-18 |
AU2011251733A1 (en) | 2012-12-20 |
CA2798222A1 (en) | 2011-11-17 |
US20130267513A1 (en) | 2013-10-10 |
GB201008134D0 (en) | 2010-06-30 |
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