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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- 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
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- 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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1008134.7A GB201008134D0 (en) | 2010-05-14 | 2010-05-14 | Compounds |
| GB1008134.7 | 2010-05-14 | ||
| PCT/GB2011/050937 WO2011141756A1 (en) | 2010-05-14 | 2011-05-16 | Pyrazolopyridines as inhibitors of the kinase lrrk2 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| 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)
| Country | Link |
|---|---|
| US (1) | US20130267513A1 (https=) |
| EP (1) | EP2569293A1 (https=) |
| JP (1) | JP2013529196A (https=) |
| CN (1) | CN102971306A (https=) |
| AU (1) | AU2011251733A1 (https=) |
| CA (1) | CA2798222A1 (https=) |
| GB (1) | GB201008134D0 (https=) |
| WO (1) | WO2011141756A1 (https=) |
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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| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | 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 |
| EP2844660B1 (en) * | 2012-05-02 | 2017-11-01 | 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 |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| WO2014001973A1 (en) | 2012-06-29 | 2014-01-03 | Pfizer Inc. | NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| MD20150037A2 (ro) | 2012-11-08 | 2015-11-30 | Pfizer Inc. | Compuşi heteroaromatici şi utilizarea lor ca liganzi de dopamină D1 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| 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 |
| US9440952B2 (en) | 2013-03-04 | 2016-09-13 | 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 |
| TW201444850A (zh) * | 2013-03-15 | 2014-12-01 | Ipsen Pharma Sas | 巨環lrrk2激酶抑制劑 |
| 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 |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
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| JP6487921B2 (ja) * | 2013-12-17 | 2019-03-20 | ファイザー・インク | LRRK2阻害薬としての新規の3,4−二置換−1H−ピロロ[2,3−b]ピリジンおよび4,5−二置換−7H−ピロロ[2,3−c]ピリダジン |
| EP3134405B1 (en) | 2014-04-25 | 2019-08-28 | 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 |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| AU2016295604B2 (en) * | 2015-07-23 | 2019-08-01 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
| KR102161364B1 (ko) | 2015-09-14 | 2020-09-29 | 화이자 인코포레이티드 | LRRK2 억제제로서 이미다조[4,5-c]퀴놀린 및 이미다조[4,5-c][1,5]나프티리딘 유도체 |
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| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
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| 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 |
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Citations (5)
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2010
- 2010-05-14 GB GBGB1008134.7A patent/GB201008134D0/en not_active Ceased
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2011
- 2011-05-16 WO PCT/GB2011/050937 patent/WO2011141756A1/en not_active Ceased
- 2011-05-16 AU AU2011251733A patent/AU2011251733A1/en not_active Abandoned
- 2011-05-16 CA CA2798222A patent/CA2798222A1/en not_active Abandoned
- 2011-05-16 JP JP2013509631A patent/JP2013529196A/ja not_active Withdrawn
- 2011-05-16 US US13/697,878 patent/US20130267513A1/en not_active Abandoned
- 2011-05-16 EP EP11720847A patent/EP2569293A1/en not_active Withdrawn
- 2011-05-16 CN CN201180033483XA patent/CN102971306A/zh active Pending
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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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Cited By (2)
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| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20130267513A1 (en) | 2013-10-10 |
| GB201008134D0 (en) | 2010-06-30 |
| CA2798222A1 (en) | 2011-11-17 |
| AU2011251733A1 (en) | 2012-12-20 |
| JP2013529196A (ja) | 2013-07-18 |
| WO2011141756A1 (en) | 2011-11-17 |
| EP2569293A1 (en) | 2013-03-20 |
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