AR073055A1 - Derivados biciclicos de triazol - Google Patents
Derivados biciclicos de triazolInfo
- Publication number
- AR073055A1 AR073055A1 ARP090103142A ARP090103142A AR073055A1 AR 073055 A1 AR073055 A1 AR 073055A1 AR P090103142 A ARP090103142 A AR P090103142A AR P090103142 A ARP090103142 A AR P090103142A AR 073055 A1 AR073055 A1 AR 073055A1
- Authority
- AR
- Argentina
- Prior art keywords
- nar
- nhet
- hal
- nhet1
- conr5
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D403/10—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 aromatic rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Los compuestos de la formula (1) en donde X1, X2, X3, X4, X5 son cada uno de modo independiente entre sí, CH o N, R1, R2, R7 son cada uno, de modo independiente entre si, H, Hal, A, [C(R5)2]nOR5, N=CR5N(R5)2, SR5, NO2, CN, {C(R5)2]nCOOR5, CON(R5)2, NR5COA, NR5SO2A, SO2N(R5)2, S(O)mA, [C(R5)2]nN(R5)2, [C(R5)2]nHet, O[C(R5)2]pOR5, O[C(R5)2]pN(R5)2, O[C(R5)2]pN+O-(R5)2, O[C(R5)2]nHet, S[C(R5)2]pN(R5)2, S[C(R5)2]pHet, NR5[C(R5)2]nN(R5)2, NR5[C(R5)2]nHet, NHCON(R5)2, NHCONH[C(R5)2]pN(R5)2, NHCONH[C(R5)2]nHet, NHCO[C(R5)2]nN(R5)2, NHCO[C(R5)2]nHet, [C(R5)2]nCON(R5)2, CONR5[C(R5)2]nN(R5)2, CONR5[C(R5)2]nNR5COOA, [C(R5)2]nNR5COOA, CONR5[C(R5)2]nOR5, CONR5[C(R5)2]nHet, COHet, COA, CH=CH-COOR5, CH=CH-N(R5)2, CH=CH-CON(R5)2, O-[C(R5)2]n-cicloalquilen-[C(R5)2]n-Het, O-[C(R5)2]n-cicloalquilen-[C(R5)2]n-N(R5)2, O-[C(R5)2]n-cicloalquilen-[C(R5)2]n-OR5, [C(R5)2]nAr, O[C(R5)2]nAr, S[C(R5)2]nAr, NR5[C(R5)2]nAr, NHCONH[C(R5)2]nAr, NHCO[C(R5)2]nAR o CONR5[C(R5)2]nAr o COAr, R3, R3' son cada uno, de modo independiente entre sí, H, F o R8; R3 y R3' son juntos también una cadena de alquileno con 2-5 átomos de C, en donde 1 o 2 grupos CH2 no adyacentes pueden estar reemplazados por O, NH y/o NR5, R4, R6 son cada uno, de modo independiente entre sí, H, A o Hal, R5 es H o R8; R8 es alquilo no ramificado o ramificado C1-6, A es alquilo no ramificado o ramificado C1-10 en donde 1-7 átomos de H pueden estar reemplazados por OH, F, Cl y/o Br, y/o en donde uno o dos grupos CH2 pueden estar reemplazados por O, NR8, NH, S, SO, SO2 y/o grupo CH=CH, o alquilo cíclico C3-7, que puede estar monosustituido con OH, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR5, N(R5)2, SR5, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, SO2N(R5)2 y/o S(O)mA, Het es un heterociclo saturado, insaturado o aromático mono-, di- o tricíclico con 1 a 4 átomos de N, O y/o S, que no está sustituido o que está mono-, di- o trisustituido con Hal, A, OR5, N(R5)2, SR5, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, SO2N(R5)2, S(O)mA, CO-Het1, Het1, [C(R5)2]nN(R5)2, [C(R5)2]nOR5, [C(R5)2]nHet1, O[C(R5)2]pN(R5)2, O[C(R5)2]pOR5, O[C(R5)2]nHet1, NHCOOA, NHCON(R5)2, NHCOO[C(R5)2]pN(R5)2, NHCOO[C(R5)2]nHet1, NHCONH[C(R5)2]nN(R5)2, NHCONH[C(R5)2]nHet1, OCONH[C(R5)2]nN(R5)2, OCONH[C(R5)2]nHet1, CO-Het1, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo); Het1 es un heterociclo saturado monocíclico con 1 a 2 átomos de N y/u O, que puede estar mono- o disustituido con A, COOA, OA, OH, Hal y/u =O (oxigeno del carbonilo); Hal es F, Cl, Br o I, m es 0, 1, o 2; n es 0 1, 2, 3 o 4, p es 1, 2, 3 o 4, así como sus sales, tautomeros y estereoisomeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de las tirosina quinasas, en especial de la Met-quinasa, y pueden utilizarse, por ejemplo, para el tratamiento de tumores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102008037790A DE102008037790A1 (de) | 2008-08-14 | 2008-08-14 | Bicyclische Triazolderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073055A1 true AR073055A1 (es) | 2010-10-13 |
Family
ID=41138729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103142A AR073055A1 (es) | 2008-08-14 | 2009-08-14 | Derivados biciclicos de triazol |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8435986B2 (es) |
| EP (1) | EP2310013B1 (es) |
| JP (1) | JP5475778B2 (es) |
| KR (1) | KR20110051243A (es) |
| CN (1) | CN102123710B (es) |
| AR (1) | AR073055A1 (es) |
| AU (1) | AU2009281491B2 (es) |
| BR (1) | BRPI0914555A2 (es) |
| CA (1) | CA2733941C (es) |
| DE (1) | DE102008037790A1 (es) |
| EA (1) | EA201100334A1 (es) |
| ES (1) | ES2648233T3 (es) |
| HK (1) | HK1159989A1 (es) |
| IL (1) | IL211193A0 (es) |
| MX (1) | MX2011001511A (es) |
| WO (1) | WO2010017870A1 (es) |
| ZA (1) | ZA201101899B (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009111354A2 (en) * | 2008-03-03 | 2009-09-11 | Tiger Pharmatech | Tyrosine kinase inhibitors |
| CU24167B1 (es) | 2009-12-31 | 2016-03-31 | Hutchison Medipharma Ltd | Derivados de triazolopirazinas sustituidas como inhibidores del receptor c-met o hgf para tratar el cáncer |
| DK2571878T3 (en) * | 2010-05-17 | 2019-02-11 | Indian Incozen Therapeutics Pvt Ltd | Hitherto unknown 3,5-DISUBSTITUTED-3H-IMIDAZO [4,5-B] PYRIDINE AND 3,5- DISUBSTITUTED -3H- [1,2,3] TRIAZOL [4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN CHINES |
| KR20130109122A (ko) * | 2010-09-23 | 2013-10-07 | 베링거 인겔하임 인터내셔날 게엠베하 | 류코트리엔 생성에 대한 옥사디아졸 억제제 |
| CN104703988B (zh) * | 2013-09-30 | 2017-04-12 | 韩国化学研究院 | 新的三唑并吡嗪衍生物及其用途 |
| CA2925129C (en) * | 2013-10-04 | 2023-04-04 | Novartis Ag | 3' end caps for rnai agents for use in rna interference |
| WO2015050871A2 (en) | 2013-10-04 | 2015-04-09 | Novartis Ag | Organic compounds to treat hepatitis b virus |
| GB201321740D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| KR102379517B1 (ko) * | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| WO2017136727A2 (en) | 2016-02-05 | 2017-08-10 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| DK3552017T3 (da) | 2016-12-09 | 2022-05-16 | Denali Therapeutics Inc | Forbindelser, der er anvendelige som ripk1-inhibitorer |
| KR20180092096A (ko) * | 2017-02-08 | 2018-08-17 | 에이비온 주식회사 | 트리아졸로 피라진 유도체의 신규한 다형체 및 이의 제조 방법 |
| CN108570053A (zh) * | 2017-03-13 | 2018-09-25 | 中国科学院上海药物研究所 | 五元并六元杂环化合物、制备方法、中间体、组合和应用 |
| KR102708681B1 (ko) | 2018-02-13 | 2024-09-26 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| SG11202012425QA (en) | 2018-07-13 | 2021-01-28 | Gilead Sciences Inc | Pd-1/pd-l1 inhibitors |
| KR102635333B1 (ko) | 2018-10-24 | 2024-02-15 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| IL314082A (en) | 2022-01-12 | 2024-09-01 | Denali Therapeutics Inc | Crystal forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazapin-3-yl)- H4- 1,2,4-triazole-3-carboxamide |
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-
2008
- 2008-08-14 DE DE102008037790A patent/DE102008037790A1/de not_active Withdrawn
-
2009
- 2009-07-16 CA CA2733941A patent/CA2733941C/en active Active
- 2009-07-16 CN CN2009801314380A patent/CN102123710B/zh active Active
- 2009-07-16 AU AU2009281491A patent/AU2009281491B2/en not_active Ceased
- 2009-07-16 MX MX2011001511A patent/MX2011001511A/es not_active Application Discontinuation
- 2009-07-16 EA EA201100334A patent/EA201100334A1/ru unknown
- 2009-07-16 BR BRPI0914555A patent/BRPI0914555A2/pt not_active IP Right Cessation
- 2009-07-16 EP EP09777234.7A patent/EP2310013B1/de active Active
- 2009-07-16 ES ES09777234.7T patent/ES2648233T3/es active Active
- 2009-07-16 JP JP2011522392A patent/JP5475778B2/ja active Active
- 2009-07-16 US US13/059,016 patent/US8435986B2/en active Active
- 2009-07-16 WO PCT/EP2009/005172 patent/WO2010017870A1/de active Application Filing
- 2009-07-16 KR KR1020117005525A patent/KR20110051243A/ko not_active Application Discontinuation
- 2009-08-14 AR ARP090103142A patent/AR073055A1/es unknown
-
2011
- 2011-02-10 IL IL211193A patent/IL211193A0/en active IP Right Grant
- 2011-03-11 ZA ZA2011/01899A patent/ZA201101899B/en unknown
-
2012
- 2012-01-12 HK HK12100381.3A patent/HK1159989A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2733941A1 (en) | 2010-02-18 |
| AU2009281491A1 (en) | 2010-02-18 |
| CN102123710B (zh) | 2012-11-07 |
| US20110135600A1 (en) | 2011-06-09 |
| BRPI0914555A2 (pt) | 2015-12-15 |
| ZA201101899B (en) | 2011-11-30 |
| JP5475778B2 (ja) | 2014-04-16 |
| MX2011001511A (es) | 2011-03-15 |
| CN102123710A (zh) | 2011-07-13 |
| JP2011530545A (ja) | 2011-12-22 |
| ES2648233T3 (es) | 2017-12-29 |
| AU2009281491B2 (en) | 2014-02-20 |
| DE102008037790A1 (de) | 2010-02-18 |
| US8435986B2 (en) | 2013-05-07 |
| IL211193A0 (en) | 2011-04-28 |
| HK1159989A1 (en) | 2012-08-10 |
| CA2733941C (en) | 2016-10-04 |
| KR20110051243A (ko) | 2011-05-17 |
| EA201100334A1 (ru) | 2011-08-30 |
| WO2010017870A1 (de) | 2010-02-18 |
| EP2310013B1 (de) | 2017-08-23 |
| EP2310013A1 (de) | 2011-04-20 |
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