MXPA01002175A - Derivados de quinazolina como medicamentos. - Google Patents
Derivados de quinazolina como medicamentos.Info
- Publication number
- MXPA01002175A MXPA01002175A MXPA01002175A MXPA01002175A MXPA01002175A MX PA01002175 A MXPA01002175 A MX PA01002175A MX PA01002175 A MXPA01002175 A MX PA01002175A MX PA01002175 A MXPA01002175 A MX PA01002175A MX PA01002175 A MXPA01002175 A MX PA01002175A
- Authority
- MX
- Mexico
- Prior art keywords
- quinazoline
- alkyl
- pyridylamino
- substituents
- independently
- Prior art date
Links
- 239000003814 drug Substances 0.000 title claims description 10
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title description 19
- 150000001875 compounds Chemical class 0.000 claims abstract description 103
- 125000001424 substituent group Chemical group 0.000 claims abstract description 64
- 102000004887 Transforming Growth Factor beta Human genes 0.000 claims abstract description 44
- 108090001012 Transforming Growth Factor beta Proteins 0.000 claims abstract description 44
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 claims abstract description 41
- 125000003118 aryl group Chemical group 0.000 claims abstract description 39
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 18
- 238000000034 method Methods 0.000 claims abstract description 17
- 150000003839 salts Chemical class 0.000 claims abstract description 11
- 125000004122 cyclic group Chemical group 0.000 claims abstract description 8
- -1 aryl alkylaryl Chemical group 0.000 claims description 65
- 125000000217 alkyl group Chemical group 0.000 claims description 47
- 230000000694 effects Effects 0.000 claims description 43
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 238000011282 treatment Methods 0.000 claims description 22
- 125000003342 alkenyl group Chemical group 0.000 claims description 19
- 125000000304 alkynyl group Chemical group 0.000 claims description 19
- 239000000203 mixture Substances 0.000 claims description 17
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 13
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 11
- 125000005842 heteroatom Chemical group 0.000 claims description 11
- 125000002252 acyl group Chemical group 0.000 claims description 10
- 125000003435 aroyl group Chemical group 0.000 claims description 10
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 7
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 7
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 125000001931 aliphatic group Chemical group 0.000 claims description 6
- 125000001041 indolyl group Chemical group 0.000 claims description 6
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 5
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 5
- 125000000623 heterocyclic group Chemical group 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 125000002950 monocyclic group Chemical group 0.000 claims description 5
- 229910052717 sulfur Inorganic materials 0.000 claims description 5
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 4
- 239000011230 binding agent Substances 0.000 claims description 4
- 230000002452 interceptive effect Effects 0.000 claims description 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 4
- ISVKZMKGDXSOHM-UHFFFAOYSA-N 2-(4-fluorophenyl)-n-pyridin-4-ylquinazolin-4-amine Chemical compound C1=CC(F)=CC=C1C1=NC(NC=2C=CN=CC=2)=C(C=CC=C2)C2=N1 ISVKZMKGDXSOHM-UHFFFAOYSA-N 0.000 claims description 3
- QGWNGFYEPGNYNY-UHFFFAOYSA-N 2-phenyl-n-pyridin-4-ylquinazolin-4-amine Chemical compound N=1C(C=2C=CC=CC=2)=NC2=CC=CC=C2C=1NC1=CC=NC=C1 QGWNGFYEPGNYNY-UHFFFAOYSA-N 0.000 claims description 3
- 125000005251 aryl acyl group Chemical group 0.000 claims description 3
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 3
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 3
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims description 3
- 125000002541 furyl group Chemical group 0.000 claims description 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 3
- 125000002883 imidazolyl group Chemical group 0.000 claims description 3
- 125000005956 isoquinolyl group Chemical group 0.000 claims description 3
- 125000002971 oxazolyl group Chemical group 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 125000004076 pyridyl group Chemical group 0.000 claims description 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 3
- 125000005493 quinolyl group Chemical group 0.000 claims description 3
- 125000000335 thiazolyl group Chemical group 0.000 claims description 3
- 125000001544 thienyl group Chemical group 0.000 claims description 3
- ZVGAQVAHOPFEJQ-UHFFFAOYSA-N 2-(2-fluorophenyl)-n-pyridin-4-ylquinazolin-4-amine Chemical compound FC1=CC=CC=C1C1=NC(NC=2C=CN=CC=2)=C(C=CC=C2)C2=N1 ZVGAQVAHOPFEJQ-UHFFFAOYSA-N 0.000 claims description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- UKTAMAPHRYOUJF-UHFFFAOYSA-N 2-(2,6-dibromophenyl)-n-pyridin-4-ylquinazolin-4-amine Chemical compound BrC1=CC=CC(Br)=C1C1=NC(NC=2C=CN=CC=2)=C(C=CC=C2)C2=N1 UKTAMAPHRYOUJF-UHFFFAOYSA-N 0.000 claims 1
- YOOMHBKQLQDQNP-UHFFFAOYSA-N 2-(2,6-dichlorophenyl)-n-pyridin-4-ylquinazolin-4-amine Chemical compound ClC1=CC=CC(Cl)=C1C1=NC(NC=2C=CN=CC=2)=C(C=CC=C2)C2=N1 YOOMHBKQLQDQNP-UHFFFAOYSA-N 0.000 claims 1
- NZFSBHMJKSDUJJ-UHFFFAOYSA-N 2-(2-bromophenyl)-n-pyridin-4-ylquinazolin-4-amine Chemical compound BrC1=CC=CC=C1C1=NC(NC=2C=CN=CC=2)=C(C=CC=C2)C2=N1 NZFSBHMJKSDUJJ-UHFFFAOYSA-N 0.000 claims 1
- GFAMVEXIOQUVBP-UHFFFAOYSA-N 2-(2-chlorophenyl)-n-pyridin-4-ylquinazolin-4-amine Chemical compound ClC1=CC=CC=C1C1=NC(NC=2C=CN=CC=2)=C(C=CC=C2)C2=N1 GFAMVEXIOQUVBP-UHFFFAOYSA-N 0.000 claims 1
- HVFQVBSNHDYUFU-UHFFFAOYSA-N 2-(2-fluorophenyl)-4-n-pyridin-4-ylquinazoline-4,6-diamine Chemical compound C12=CC(N)=CC=C2N=C(C=2C(=CC=CC=2)F)N=C1NC1=CC=NC=C1 HVFQVBSNHDYUFU-UHFFFAOYSA-N 0.000 claims 1
- KWBWEHKATKLMFL-UHFFFAOYSA-N 2-(2-fluorophenyl)-4-n-pyridin-4-ylquinazoline-4,7-diamine Chemical compound N=1C(C=2C(=CC=CC=2)F)=NC2=CC(N)=CC=C2C=1NC1=CC=NC=C1 KWBWEHKATKLMFL-UHFFFAOYSA-N 0.000 claims 1
- URDICAFRQWPDGT-UHFFFAOYSA-N 2-(2-fluorophenyl)-6,7-dimethoxy-n-pyridin-4-ylquinazolin-4-amine Chemical compound C=12C=C(OC)C(OC)=CC2=NC(C=2C(=CC=CC=2)F)=NC=1NC1=CC=NC=C1 URDICAFRQWPDGT-UHFFFAOYSA-N 0.000 claims 1
- FREPRBGKBRCENL-UHFFFAOYSA-N 2-(2-fluorophenyl)-6-n-[(3-methoxyphenyl)methyl]-4-n-pyridin-4-ylquinazoline-4,6-diamine Chemical compound COC1=CC=CC(CNC=2C=C3C(NC=4C=CN=CC=4)=NC(=NC3=CC=2)C=2C(=CC=CC=2)F)=C1 FREPRBGKBRCENL-UHFFFAOYSA-N 0.000 claims 1
- VZEZHGMMOHNBQJ-UHFFFAOYSA-N 2-(2-fluorophenyl)-6-n-[(4-methoxyphenyl)methyl]-4-n-pyridin-4-ylquinazoline-4,6-diamine Chemical compound C1=CC(OC)=CC=C1CNC1=CC=C(N=C(N=C2NC=3C=CN=CC=3)C=3C(=CC=CC=3)F)C2=C1 VZEZHGMMOHNBQJ-UHFFFAOYSA-N 0.000 claims 1
- VSDBMQKTNZZXMO-UHFFFAOYSA-N 2-(2-fluorophenyl)-6-n-[(4-methylsulfanylphenyl)methyl]-4-n-pyridin-4-ylquinazoline-4,6-diamine Chemical compound C1=CC(SC)=CC=C1CNC1=CC=C(N=C(N=C2NC=3C=CN=CC=3)C=3C(=CC=CC=3)F)C2=C1 VSDBMQKTNZZXMO-UHFFFAOYSA-N 0.000 claims 1
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Landscapes
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/141,916 US6184226B1 (en) | 1998-08-28 | 1998-08-28 | Quinazoline derivatives as inhibitors of P-38 α |
| PCT/US1999/019846 WO2000012497A2 (en) | 1998-08-28 | 1999-08-27 | Quinazoline derivatives as medicaments |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA01002175A true MXPA01002175A (es) | 2003-07-14 |
Family
ID=22497802
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA01002175A MXPA01002175A (es) | 1998-08-28 | 1999-08-27 | Derivados de quinazolina como medicamentos. |
Country Status (14)
| Country | Link |
|---|---|
| US (7) | US6184226B1 (https=) |
| EP (1) | EP1107959B1 (https=) |
| JP (1) | JP2002523502A (https=) |
| KR (1) | KR20010083874A (https=) |
| CN (1) | CN1152867C (https=) |
| AT (1) | ATE342256T1 (https=) |
| AU (1) | AU771947B2 (https=) |
| BR (1) | BR9913648A (https=) |
| CA (1) | CA2342250A1 (https=) |
| DE (1) | DE69933573T2 (https=) |
| ES (1) | ES2274642T3 (https=) |
| IL (1) | IL141723A0 (https=) |
| MX (1) | MXPA01002175A (https=) |
| WO (1) | WO2000012497A2 (https=) |
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-
1998
- 1998-08-28 US US09/141,916 patent/US6184226B1/en not_active Expired - Lifetime
-
1999
- 1999-08-27 ES ES99949568T patent/ES2274642T3/es not_active Expired - Lifetime
- 1999-08-27 WO PCT/US1999/019846 patent/WO2000012497A2/en not_active Ceased
- 1999-08-27 IL IL14172399A patent/IL141723A0/xx unknown
- 1999-08-27 BR BR9913648-1A patent/BR9913648A/pt not_active Application Discontinuation
- 1999-08-27 CN CNB998116599A patent/CN1152867C/zh not_active Expired - Lifetime
- 1999-08-27 DE DE69933573T patent/DE69933573T2/de not_active Revoked
- 1999-08-27 US US09/383,825 patent/US6476031B1/en not_active Expired - Lifetime
- 1999-08-27 AU AU62413/99A patent/AU771947B2/en not_active Expired
- 1999-08-27 MX MXPA01002175A patent/MXPA01002175A/es not_active Application Discontinuation
- 1999-08-27 EP EP99949568A patent/EP1107959B1/en not_active Revoked
- 1999-08-27 CA CA002342250A patent/CA2342250A1/en not_active Abandoned
- 1999-08-27 JP JP2000567525A patent/JP2002523502A/ja active Pending
- 1999-08-27 KR KR1020017002716A patent/KR20010083874A/ko not_active Ceased
- 1999-08-27 AT AT99949568T patent/ATE342256T1/de not_active IP Right Cessation
-
2000
- 2000-03-14 US US09/525,034 patent/US6277989B1/en not_active Expired - Lifetime
-
2001
- 2001-10-02 US US09/969,936 patent/US20030069248A1/en not_active Abandoned
- 2001-10-05 US US09/972,582 patent/US6903096B2/en not_active Expired - Lifetime
-
2005
- 2005-02-07 US US11/053,121 patent/US7345045B2/en not_active Expired - Fee Related
- 2005-05-23 US US11/136,242 patent/US20050220784A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU6241399A (en) | 2000-03-21 |
| IL141723A0 (en) | 2002-03-10 |
| DE69933573D1 (de) | 2006-11-23 |
| WO2000012497A2 (en) | 2000-03-09 |
| US6277989B1 (en) | 2001-08-21 |
| US20050220784A1 (en) | 2005-10-06 |
| WO2000012497B1 (en) | 2000-09-08 |
| EP1107959B1 (en) | 2006-10-11 |
| US6903096B2 (en) | 2005-06-07 |
| CN1333757A (zh) | 2002-01-30 |
| CA2342250A1 (en) | 2000-03-09 |
| WO2000012497A3 (en) | 2000-06-29 |
| AU771947B2 (en) | 2004-04-08 |
| US6476031B1 (en) | 2002-11-05 |
| BR9913648A (pt) | 2002-01-02 |
| ATE342256T1 (de) | 2006-11-15 |
| US7345045B2 (en) | 2008-03-18 |
| US6184226B1 (en) | 2001-02-06 |
| US20020161010A1 (en) | 2002-10-31 |
| JP2002523502A (ja) | 2002-07-30 |
| HK1035897A1 (en) | 2001-12-14 |
| US20050171123A1 (en) | 2005-08-04 |
| EP1107959A2 (en) | 2001-06-20 |
| DE69933573T2 (de) | 2007-05-03 |
| US20030069248A1 (en) | 2003-04-10 |
| KR20010083874A (ko) | 2001-09-03 |
| ES2274642T3 (es) | 2007-05-16 |
| CN1152867C (zh) | 2004-06-09 |
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| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |