AR032637A1 - Compuestos de pirrolotriazina, utiles como inhibidores de la actividad de la cinasa p38 y las composiciones farmaceuticas que los contienen - Google Patents
Compuestos de pirrolotriazina, utiles como inhibidores de la actividad de la cinasa p38 y las composiciones farmaceuticas que los contienenInfo
- Publication number
- AR032637A1 AR032637A1 ARP010105381A ARP010105381A AR032637A1 AR 032637 A1 AR032637 A1 AR 032637A1 AR P010105381 A ARP010105381 A AR P010105381A AR P010105381 A ARP010105381 A AR P010105381A AR 032637 A1 AR032637 A1 AR 032637A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- aryl
- heterocycle
- hydrogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 230000000694 effects Effects 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 19
- 125000000623 heterocyclic group Chemical group 0.000 abstract 16
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 229910052739 hydrogen Inorganic materials 0.000 abstract 13
- 239000001257 hydrogen Substances 0.000 abstract 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 13
- 125000004432 carbon atom Chemical group C* 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical group 0.000 abstract 9
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 7
- -1 -OH Chemical group 0.000 abstract 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 6
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000003107 substituted aryl group Chemical group 0.000 abstract 5
- 229930194542 Keto Natural products 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 4
- 125000000468 ketone group Chemical group 0.000 abstract 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 239000011203 carbon fibre reinforced carbon Substances 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 150000001721 carbon Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 239000011593 sulfur Substances 0.000 abstract 2
- RBIIKVXVYVANCQ-CUWPLCDZSA-N (2s,4s,5s)-5-amino-n-(3-amino-2,2-dimethyl-3-oxopropyl)-6-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]-4-hydroxy-2-propan-2-ylhexanamide Chemical compound C1C(C)(C)N(C[C@H](N)[C@@H](O)C[C@@H](C(C)C)C(=O)NCC(C)(C)C(N)=O)CC(=O)N1C1=CC=CC=C1Cl RBIIKVXVYVANCQ-CUWPLCDZSA-N 0.000 abstract 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 abstract 1
- KYMQCBPHCXAPDE-UHFFFAOYSA-N 90594-15-3 Chemical compound N1=C2C=CC=CN2C2=C1C(C)=C(NO)C=N2 KYMQCBPHCXAPDE-UHFFFAOYSA-N 0.000 abstract 1
- 101100478290 Arabidopsis thaliana SR30 gene Proteins 0.000 abstract 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 abstract 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 101100054666 Streptomyces halstedii sch3 gene Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical group [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 230000002491 angiogenic effect Effects 0.000 abstract 1
- 150000004982 aromatic amines Chemical class 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 230000002458 infectious effect Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 150000003921 pyrrolotriazines Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 abstract 1
- 125000003396 thiol group Chemical class [H]S* 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 230000003612 virological effect Effects 0.000 abstract 1
Classifications
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P25/28—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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Transplantation (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
Abstract
Un método de tratamiento de una o más condiciones asociadas con la actividad de la cinasa p38 que comprende la administracion a un paciente en necesidad del mismo de al menos un compuesto que tiene la formula (1): o una sal, profármaco o solvato farmacéuticamente aceptable del mismo, en donde: R3 es hidrogeno, metilo, perfluorometilo, metoxi, halogeno, ciano o NH2; X se selecciona de ûO-, -OC(=O)-, -S-, S(=O)-, SO2-, -C(=O)-, -CO2-, NR10, -NR10C(=O)-, -NR10C(=O)NR11-, -NR10CO2-, NR10SO2-, NR10SO2NR11-, -SO2NR10-, -C(=O)NR10-, halogeno, nitro y ciano, o X está ausente; Z se selecciona de oxígeno, azufre, nitrogeno y CR20, en donde, cuando Z es CR20, dicho átomo de carbono puede formar un arilo o heteroarilo bicíclico opcionalmente sustituido con R4 y R5; R1 es hidrogeno, -CH3, -OH, -OCH3, -SH, SCH3, -OC(=O)R21, -S(=O)R22, -SO2R22, -SO2NR24R25, -CO2R21, -C(=O)NR24R25, -NH2, -NR24R25,-NR21SO2NR24R25, -NR21SO2R22, -NR24C(=O)R25, -NR24CO2R25, -NR21 C(=O) NR24R25 halogeno, nitro o ciano; R2 se selecciona de: a) hidrogeno, con la condicion de que R2, no sea hidrogeno cuando X es ûS(=O)-, -SO2- -NR10CO2-, o NR10SO2-; b) alquilo, alquenilo y alquinilo opcionalmente sustituidos con hasta cuatro R26 pentafluoroalquilo; c) arilo y heteroarilo opcionalmente sustituido con hasta tres R27; y d) heterociclo y cicloalquilo opcionalmente sustituido con ceto (=O), hasta tres R27 y/o que tiene un puente carbono-carbono de 3 a 4 átomos de carbono; o e) R2 está ausente si X es halogeno, nitro o ciano; i) R4 es arilo sustituido, arilo sustituido con NHSO2alquilo, heteroarilo sustituido o un anillo carbocíclico o heterocíclico saturado o insaturado, de 7 a 11 miembros, bicíclico, opcionalmente sustituido, R5 es hidrogeno, alquilo o alquilo sustituido, excepto cuando Z es oxígeno o azufre, R5 está ausente, o alternativamente, ii) R4 y R5 tomados conjuntamente con Z forman u arilo o heteroarilo de 7 a 11 miembros bicíclico, opcionalmente sustituido; R6 es hidrogeno, alquilo, alquilo sustituido, arilo, arilo sustituido, heterociclo, heterociclo sustituido, -NR7R8, -OR7, o halogeno; R10 y R11 son independientemente seleccionados de hidrogeno, alquilo, alquilo sustituido, arilo, arilo sustituido cicloalquilo, cicloalquilo sustituido, heterociclo y heterociclo sustituido; R7, R8, R21, R24 y R25 se seleccionan independientemente de hidrogeno, alquilo, alquilo sustituido, arilo, arilo sustituido, heterociclo y heterociclo sustituido; R20 es hidrogeno, alquilo inferior, o alquilo sustituido o R20 puede estar ausente si el átomo de carbono al cual está unido junto con R4 y R5 es parte de un arilo o heteroarilo bicíclico insaturado; R22 es alquilo, alquilo sustituido, arilo, arilo sustituido, heterociclo, o heterociclo sustituido; R26 se selecciona de halogeno, trifluorometilo, haloalcoxi, ceto (=O), nitro, ciano, -SR28, -OR28, -NR28R29, -NR28SO2R29, -SO2R28, -SO2R8, -SO2NR28R29, -CO2R28, -C(=O)R28, -C(=O)R2, -C(=O)NR28R29, -OC(=O)R8, -OC(=O)NR28R29, -NR28C(=O)R29, -NR28CO2R9, =N-OH, =N-O-, alquilo; arilo opcionalmente sustituido con uno a tres R27; cicloalquilo opcionalmente sustituido con ceto (=O), uno a tres R27; o que tiene un puente carbono-carbono de 3 a 4 átomos de carbono; y heterociclo opcionalmente sustituido con ceto (=O), uno a tres R27, o que tiene un puente carbono-carbono de 3 a 4 átomos de carbono, en donde R28 y R29 son cada uno independientemente seleccionados de hidrogeno, alquilo, alquenilo, arilo, aralquilo, cicloalquilo de 3 a 7 átomos de carbono y heterociclo de 3 a 7 átomos de carbono, o pueden ser tomados conjuntamente para formar un heterociclo de 3 a 7 átomos de carbono; y en donde cada R28 y R29 a su vez esta opcionalmente sustituido con hasta dos de alquilo, alquenilo, halogeno, haloalquilo, haloalcoxi, ciano, nitro amino, hidroxilo, alcoxi, alquiltio, fenilo, bencilo, feniloxi y benciloxi; y R27 se selecciona de alquilo, R32, y alquilo de 1 a 4 átomos de carbono sustituido con uno a tres R32, en donde cada grupo R32 se selecciona independientemente de halogeno, haloalquilo, haloalcoxi, nitro, ciano, SR30, - OR30, -NR30R31, -NR30SO2, -NR30SO2R31-SO2R30, -SO2NR30R31, -CO2R30, ûC(=O)R30, -C(=O)NR30R31, -OC(=O)R30, -OC(=O)NR30R31, -NR30C(=O)R31, -NR30CO2R31, y un anillo carbocíclico o heterocíclico de 3 a 7 miembros opcionalmente sustituido con alquilo, halogeno, hidroxilo, alcoxi, haloalquilo, haloalcoxi, nitro, amino, o ciano, en donde R30 y R31 son cada uno independientemente seleccionados de hidrogeno, alquilo, alquenilo, arilo, aralquilo, cicloalquilo de 3 a 7 átomos de carbono, y heterociclo, o pueden ser tomados conjuntamente para formar un heterociclo de 3 a 7 átomos de carbono. Los compuestos de pirrolotriazina utiles como inhibidores de cinasa y las composiciones farmacéuticas que los contienen en la formula (2)o una sal, profármaco o solvato farmacéuticamente aceptable del mismo, en donde: R3 es metilo, CF3, o CH3; R5 es hidrogeno o alquilo; Y es ûC(=O)NR23-, -NR23C(=O)NR23-, SO2NR23, o NR23SO2; R18 y R23 se seleccionan de hidrogeno, alquilo, alcoxi, arilo, y arilo sustituido con uno a tres R9, excepto cuando Y es ûNR23SO2-, R18 es alquilo de 1 a 4 átomos de carbono o arilo opcionalmente sustituido con uno a tres R19; R13 y R19 en cada aparicion se seleccionan independientemente de alquilo, halo, trifluorometoxi, trifluorometilo, hidroxilo, alcoxi, alcanoilo, alcanoiloxi, tiol, alquitio, ureido, nitro, ciano, carboxilo, carboxilaquilo, carbamilo, alcoxicarbonilo, alquiltiono, ariltiono, arilsulfonilamina, alquilsulfonilamina, ácido sulfonico, alquilsulfonilo, sulfonamido y ariloxi, en donde cada grupo R13 y/o R19 puede estar además sustituido con hidroxilo, alquilo, alcoxi, arilo, o aralquilo; y X, R1, R2 y R6 son como se definen anteriormente para los compuestos de la formula (1). Los compuestos son utiles para tratar enfermedades inflamatorias, autoinmunes, desordenes proliferativos, desordenes angiogénicos y enfermedades infecciosas, neurodegenerativas y virales.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24987700P | 2000-11-17 | 2000-11-17 | |
| US31056101P | 2001-08-07 | 2001-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR032637A1 true AR032637A1 (es) | 2003-11-19 |
Family
ID=26940426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010105381A AR032637A1 (es) | 2000-11-17 | 2001-11-16 | Compuestos de pirrolotriazina, utiles como inhibidores de la actividad de la cinasa p38 y las composiciones farmaceuticas que los contienen |
Country Status (31)
| Country | Link |
|---|---|
| EP (1) | EP1363910B1 (es) |
| JP (1) | JP2004522713A (es) |
| KR (1) | KR100847605B1 (es) |
| CN (1) | CN1622946A (es) |
| AR (1) | AR032637A1 (es) |
| AT (1) | ATE318820T1 (es) |
| AU (2) | AU3276002A (es) |
| BG (1) | BG107750A (es) |
| BR (1) | BR0115446A (es) |
| CA (1) | CA2429628A1 (es) |
| CY (1) | CY1105250T1 (es) |
| CZ (1) | CZ20031370A3 (es) |
| DE (1) | DE60117607T2 (es) |
| DK (1) | DK1363910T3 (es) |
| EE (1) | EE200300227A (es) |
| ES (1) | ES2259051T3 (es) |
| GE (1) | GEP20063915B (es) |
| HR (1) | HRP20030485A2 (es) |
| HU (1) | HUP0303897A2 (es) |
| IL (1) | IL155570A0 (es) |
| IS (1) | IS6816A (es) |
| MX (1) | MXPA03004290A (es) |
| MY (1) | MY127066A (es) |
| NO (1) | NO20032229L (es) |
| NZ (1) | NZ525334A (es) |
| PE (1) | PE20020819A1 (es) |
| PL (1) | PL366376A1 (es) |
| PT (1) | PT1363910E (es) |
| SK (1) | SK5402003A3 (es) |
| WO (1) | WO2002040486A2 (es) |
| YU (1) | YU37903A (es) |
Families Citing this family (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20020506A1 (es) | 2000-08-22 | 2002-07-09 | Glaxo Group Ltd | Derivados de pirazol fusionados como inhibidores de la proteina cinasa |
| US6867300B2 (en) | 2000-11-17 | 2005-03-15 | Bristol-Myers Squibb Company | Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors |
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| CA2163399A1 (en) * | 1994-11-24 | 1996-05-25 | Katsuhiro Kawano | Triazine derivative, chymase activity inhibitor and nitric oxide production inhibitor |
| WO1999024033A1 (en) * | 1997-11-12 | 1999-05-20 | Shionogi & Co., Ltd. | Method for the treatment of disorders associated with apoptosis using n-heterocyclic glyoxylamide compounds |
| AU770377B2 (en) * | 1999-05-21 | 2004-02-19 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
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