CN106008523B - 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 - Google Patents
作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 Download PDFInfo
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- CN106008523B CN106008523B CN201610388362.1A CN201610388362A CN106008523B CN 106008523 B CN106008523 B CN 106008523B CN 201610388362 A CN201610388362 A CN 201610388362A CN 106008523 B CN106008523 B CN 106008523B
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- -1 pyrazolo [1,5-a] pyrimidine compound Chemical class 0.000 title claims description 310
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- 125000001424 substituent group Chemical group 0.000 claims description 346
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- 238000002360 preparation method Methods 0.000 claims description 154
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- 150000002367 halogens Chemical class 0.000 claims description 119
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 105
- 125000005842 heteroatom Chemical group 0.000 claims description 103
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 77
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- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 58
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 55
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Classifications
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
- C07D453/04—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems having a quinolyl-4, a substituted quinolyl-4 or a alkylenedioxy-quinolyl-4 radical linked through only one carbon atom, attached in position 2, e.g. quinine
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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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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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- 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
- C07D471/22—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 systems contains four or more hetero rings
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
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- Rheumatology (AREA)
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- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22419609P | 2009-07-09 | 2009-07-09 | |
| US61/224,196 | 2009-07-09 | ||
| US34676710P | 2010-05-20 | 2010-05-20 | |
| US61/346,767 | 2010-05-20 | ||
| CN201080040095.XA CN102596957B (zh) | 2009-07-09 | 2010-07-09 | 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN201080040095.XA Division CN102596957B (zh) | 2009-07-09 | 2010-07-09 | 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN106008523A CN106008523A (zh) | 2016-10-12 |
| CN106008523B true CN106008523B (zh) | 2019-01-25 |
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| CN201610388362.1A Expired - Fee Related CN106008523B (zh) | 2009-07-09 | 2010-07-09 | 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 |
| CN201811635133.0A Expired - Fee Related CN110003214B (zh) | 2009-07-09 | 2010-07-09 | 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 |
| CN201080040095.XA Expired - Fee Related CN102596957B (zh) | 2009-07-09 | 2010-07-09 | 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201811635133.0A Expired - Fee Related CN110003214B (zh) | 2009-07-09 | 2010-07-09 | 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 |
| CN201080040095.XA Expired - Fee Related CN102596957B (zh) | 2009-07-09 | 2010-07-09 | 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物 |
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| CN (3) | CN106008523B (https=) |
| AR (1) | AR077468A1 (https=) |
| AU (1) | AU2010271270C1 (https=) |
| CA (2) | CA2767648C (https=) |
| CL (1) | CL2012000059A1 (https=) |
| CO (1) | CO6612183A2 (https=) |
| CR (2) | CR20120065A (https=) |
| ES (2) | ES2774654T3 (https=) |
| IL (1) | IL217414A (https=) |
| MX (2) | MX364157B (https=) |
| MY (1) | MY162180A (https=) |
| NZ (1) | NZ598086A (https=) |
| RU (2) | RU2016114128A (https=) |
| SG (2) | SG10201603095TA (https=) |
| TW (1) | TWI503321B (https=) |
| UY (1) | UY32782A (https=) |
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