AR043057A1 - Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasa - Google Patents
Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasaInfo
- Publication number
- AR043057A1 AR043057A1 ARP030103973A ARP030103973A AR043057A1 AR 043057 A1 AR043057 A1 AR 043057A1 AR P030103973 A ARP030103973 A AR P030103973A AR P030103973 A ARP030103973 A AR P030103973A AR 043057 A1 AR043057 A1 AR 043057A1
- Authority
- AR
- Argentina
- Prior art keywords
- phenyl
- hydrogen
- och3
- unsubstituted
- optionally substituted
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 12
- 239000003112 inhibitor Substances 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
- -1 thiophene-2-yl Chemical group 0.000 abstract 25
- 229910052739 hydrogen Inorganic materials 0.000 abstract 17
- 239000001257 hydrogen Substances 0.000 abstract 17
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 14
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 7
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 3
- 125000001118 alkylidene group Chemical group 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000001624 naphthyl group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 239000001301 oxygen Chemical group 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 229910052717 sulfur Chemical group 0.000 abstract 3
- 239000011593 sulfur Chemical group 0.000 abstract 3
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 abstract 2
- 125000001931 aliphatic group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 abstract 1
- HPARLNRMYDSBNO-UHFFFAOYSA-N 1,4-benzodioxine Chemical compound C1=CC=C2OC=COC2=C1 HPARLNRMYDSBNO-UHFFFAOYSA-N 0.000 abstract 1
- KLIDCXVFHGNTTM-UHFFFAOYSA-N 2,6-dimethoxyphenol Chemical group COC1=CC=CC(OC)=C1O KLIDCXVFHGNTTM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 abstract 1
- 125000006275 3-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C([H])C(*)=C1[H] 0.000 abstract 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 abstract 1
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- KNMAZUXTEPXPOM-UHFFFAOYSA-N 5-methoxy-6-(trifluoromethyl)-1h-indole Chemical group C1=C(C(F)(F)F)C(OC)=CC2=C1NC=C2 KNMAZUXTEPXPOM-UHFFFAOYSA-N 0.000 abstract 1
- 125000006519 CCH3 Chemical group 0.000 abstract 1
- 125000006414 CCl Chemical group ClC* 0.000 abstract 1
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Divinylene sulfide Natural products C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 abstract 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 1
- 125000004190 benzothiazol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N=C(*)SC2=C1[H] 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- OTAFHZMPRISVEM-UHFFFAOYSA-N chromone Chemical compound C1=CC=C2C(=O)C=COC2=C1 OTAFHZMPRISVEM-UHFFFAOYSA-N 0.000 abstract 1
- ZYGHJZDHTFUPRJ-UHFFFAOYSA-N coumarin Chemical compound C1=CC=C2OC(=O)C=CC2=C1 ZYGHJZDHTFUPRJ-UHFFFAOYSA-N 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 150000002475 indoles Chemical class 0.000 abstract 1
- LPAGFVYQRIESJQ-UHFFFAOYSA-N indoline Chemical class C1=CC=C2NCCC2=C1 LPAGFVYQRIESJQ-UHFFFAOYSA-N 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 abstract 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 239000003909 protein kinase inhibitor Substances 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000004159 quinolin-2-yl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C([H])C(*)=NC2=C1[H] 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 abstract 1
- 229930192474 thiophene Natural products 0.000 abstract 1
- 150000003577 thiophenes Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42244102P | 2002-10-30 | 2002-10-30 | |
| US47643303P | 2003-06-06 | 2003-06-06 | |
| US47669103P | 2003-06-06 | 2003-06-06 | |
| US47990303P | 2003-06-19 | 2003-06-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR043057A1 true AR043057A1 (es) | 2005-07-13 |
Family
ID=32314959
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030103973A AR043057A1 (es) | 2002-10-30 | 2003-10-30 | Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasa |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20040122016A1 (https=) |
| EP (1) | EP1558607B1 (https=) |
| JP (1) | JP2006514684A (https=) |
| KR (1) | KR20050088283A (https=) |
| AR (1) | AR043057A1 (https=) |
| AT (1) | ATE466855T1 (https=) |
| AU (1) | AU2003288956A1 (https=) |
| CA (1) | CA2504320A1 (https=) |
| DE (1) | DE60332475D1 (https=) |
| MX (1) | MXPA05004689A (https=) |
| NO (1) | NO20052595L (https=) |
| NZ (1) | NZ540161A (https=) |
| TW (1) | TW200416221A (https=) |
| WO (1) | WO2004041813A1 (https=) |
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| GB9823871D0 (en) * | 1998-10-30 | 1998-12-23 | Pharmacia & Upjohn Spa | 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents |
| GB9823873D0 (en) | 1998-10-30 | 1998-12-30 | Pharmacia & Upjohn Spa | 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents |
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| DE60023926T2 (de) * | 1999-09-10 | 2006-07-20 | Merck & Co., Inc. | Tyrosin kinase inhibitoren |
| JP2002053566A (ja) | 2000-08-11 | 2002-02-19 | Japan Tobacco Inc | チアゾール化合物及びその医薬用途 |
| US20020173507A1 (en) * | 2000-08-15 | 2002-11-21 | Vincent Santora | Urea compounds and methods of uses |
| EP1256578B1 (en) * | 2001-05-11 | 2006-01-11 | Pfizer Products Inc. | Thiazole derivatives and their use as cdk inhibitors |
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| AR040123A1 (es) * | 2002-05-31 | 2005-03-16 | Upjohn Co | Compuestos tiofeno, antihelminticos e insecticidas |
-
2003
- 2003-10-30 EP EP03781448A patent/EP1558607B1/en not_active Expired - Lifetime
- 2003-10-30 AU AU2003288956A patent/AU2003288956A1/en not_active Abandoned
- 2003-10-30 WO PCT/US2003/034319 patent/WO2004041813A1/en not_active Ceased
- 2003-10-30 AR ARP030103973A patent/AR043057A1/es unknown
- 2003-10-30 US US10/696,862 patent/US20040122016A1/en not_active Abandoned
- 2003-10-30 MX MXPA05004689A patent/MXPA05004689A/es unknown
- 2003-10-30 NZ NZ540161A patent/NZ540161A/en unknown
- 2003-10-30 TW TW092130255A patent/TW200416221A/zh unknown
- 2003-10-30 KR KR1020057007702A patent/KR20050088283A/ko not_active Withdrawn
- 2003-10-30 DE DE60332475T patent/DE60332475D1/de not_active Expired - Lifetime
- 2003-10-30 AT AT03781448T patent/ATE466855T1/de not_active IP Right Cessation
- 2003-10-30 CA CA002504320A patent/CA2504320A1/en not_active Abandoned
- 2003-10-30 JP JP2005502202A patent/JP2006514684A/ja not_active Withdrawn
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2005
- 2005-05-30 NO NO20052595A patent/NO20052595L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| JP2006514684A (ja) | 2006-05-11 |
| TW200416221A (en) | 2004-09-01 |
| DE60332475D1 (de) | 2010-06-17 |
| AU2003288956A1 (en) | 2004-06-07 |
| WO2004041813A1 (en) | 2004-05-21 |
| EP1558607B1 (en) | 2010-05-05 |
| NZ540161A (en) | 2008-03-28 |
| US20040122016A1 (en) | 2004-06-24 |
| EP1558607A1 (en) | 2005-08-03 |
| NO20052595D0 (no) | 2005-05-30 |
| NO20052595L (no) | 2005-06-27 |
| KR20050088283A (ko) | 2005-09-05 |
| MXPA05004689A (es) | 2005-12-05 |
| CA2504320A1 (en) | 2004-05-21 |
| ATE466855T1 (de) | 2010-05-15 |
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