AR062785A1 - Compuestos de 4-metilpiridopirimidinona, composiciones farmaceuticas que los contienen y usos en estados patologicos asociados al crecimiento anormal celular,tal como cancer. - Google Patents
Compuestos de 4-metilpiridopirimidinona, composiciones farmaceuticas que los contienen y usos en estados patologicos asociados al crecimiento anormal celular,tal como cancer.Info
- Publication number
- AR062785A1 AR062785A1 ARP070104059A ARP070104059A AR062785A1 AR 062785 A1 AR062785 A1 AR 062785A1 AR P070104059 A ARP070104059 A AR P070104059A AR P070104059 A ARP070104059 A AR P070104059A AR 062785 A1 AR062785 A1 AR 062785A1
- Authority
- AR
- Argentina
- Prior art keywords
- cycloalkyl
- alkyl
- aryl
- cycloheteroalkyl
- heteroaryl
- Prior art date
Links
Classifications
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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
- C07D471/02—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 system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
Abstract
Y su uso como inhibidores de la fosfoinositido 3-quinasa alfa (PI3-Kalfa). Reivindicacion 1: Un compuesto de formula (1) o una sal del mismo, lo en la que R1 es H o alquilo C1-6 opcionalmente sustituido con al menos un grupo R5; A es un grupo cicloalquilo de 3 a 10 miembros; R2 es alquilo C1-6 sustituido con al menos un grupo R6, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14, heteroarilo C2-9, -NR7aR7b, o -N=CR8aR8b en los que cada uno de dichos cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-4, y heteroarilo C2-9 está opcionalmente sustituido con al menos un grupo R9; R3 es alquilo C1-6, cicloalquilo C3-10, cicloheteroalquilo C2-9, alquenilo C2-8, alquinilo C2-8, halogeno, ciano, -(CH2)nC(O)OR10, - (CH2)nC(O)N(R11aR11b), COR12, arilo C6-14 o heteroarilo C2-9, en los que dichos alquilo C1-6, cicloalquilo C3-10, cicloheteroalquilo C2-9, alquenilo C2-8, alquinilo C2-8, arilo C6-14 y heteroarilo C2-9, están opcionalmente sustituidos con al menos un grupo R9; cada R4 es independientemente -OH, halogeno, CF3, NR11aR11b, alquilo C1-6, alquenilo C1-6, alquinilo C1-6, alcoxi C1-6, ciano, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14, heteroarilo C2-9, -C(O)R12, -C(O)NR11aR11b, - S(O)mR12, -S(O)mNR11aR11b, -NR11aS(O)mR12, -(CH2)nC(O)OR10, -(CH2)nC(O)N(R11aR11b), -OC(O)R12, -NR11aC(O)R12 o -NR11aC(O)N(R11aR11b) en los que cada uno de dichos alquilo C1-6, alquenilo C1-6, alquinilo C1-6, alcoxi C1-6), cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-12, y heteroarilo C2-9 está opcionalmente sustituido con al menos un grupo R13; cada R5 es independientemente -OH, halogeno, CF3, -NR11aR11b, alquilo C1-6, alcoxi C1-6, ciano, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14, heteroarilo C2-9, -S(O)mR12, -S(O)mNR11aR11b, -C(O)R12 o -C(O)NR11aR11b en los que cada uno de dichos alquilo C1-6, alcoxi C1-6, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14 y heteroarilo C2-9 está opcionalmente sustituido con al menos un grupo R9, cada R6 es independientemente -OH, alquinilo C1-6, ciano, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14, heteroarilo C2-9, -C(O)R12, -C(O)NR11aR11b, -S(O)mR12, -S(O)mNR11aR11b, -NR11aS(O)mR12, - (CH2)nC(O)OR10, -(CH2)nC(O)N(R11aR11b), -OC(O)R12, -NR11aC(O)R12 o -NR11aC(O)N(R11aR11b) en los que cada uno de dichos alquinilo C1-6, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14 y heteroarilo C2-9 está opcionalmente sustituido con al menos un grupo R13; R7a y R7b son cada uno de ellos independientemente H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10), o arilo C6-10, en los que cada uno de dichos alquilo C1-6), alquenilo C2-6, alquinilo C2-6, cicloalquilo C3- 10, y arilo C6-10, está opcionalmente sustituido con al menos un grupo R9: o R7a y R7b se pueden tomar junto con el átomo de nitrogeno para formar un anillo heterociclilo de 5 a 8 miembros, en el que dicho anillo heterociclilo tiene de 1 a 3 heteroátomos de anillo seleccionados entre el grupo constituido por N, O, y S y en el que dicho anillo cicloheteroalquilo de 5 a 8 miembros está opcionalmente sustituido con al menos un grupo R9; R8a y R8b son cada uno de ellos independientemente H, alquilo C1-6, o cicloalquilo C3-10, en los que cada uno de dichos alquilo C1-6, y cicloalquilo C3-10, está opcionalmente sustituido con al menos un grupo R9; cada R9 es independientemente -OH, halogeno, CF3, -NR11aR11b, alquilo C1-6, alquenilo C1-6, alquinilo C1-6, alcoxi C1-6, ciano, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14, heteroarilo C2-9, -C(O)R12, -C(O)NR11aR11b, -S(O)mR12, -S(O)mNR11aR11b, -NR11aS(O)mR12, -(CH2)nC(O)OR10, -(CH2)nC(O)N(R11aR11b), -OC(O)R12, -NR11aC(O)R12 o -NR11aC(O)N(R11aR11b) en los que cada uno de dichos alquilo C1-6, alquenilo C1-6, alquinilo C1-6, alcoxi C1-6, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14 y heteroarilo C2-9, está opcionalmente sustituido con al menos un grupo R13; cada R10 es independientemente H, o alquilo C1-6; R11a y R11b es cada uno independientemente H, alquilo C1-6, cicloheteroalquilo C2-9, heteroarilo C2-9, o arilo C6-12, en los que cada uno de dichos alquilo C1-6, cicloheteroalquilo C2-9, heteroarilo C2-9, y arilo C6-12, está opcionalmente sustituido con al menos un grupo R13; cada uno de R12 es independientemente alquilo C1-6, cicloalquilo C3-10, cicloheteroalquilo C2-9, heteroarilo C2-9, o arilo C6-14, en los que cada uno de dichos alquilo C1-6, cicloalquilo C3-10, cicloheteroalquilo C2-9, heteroarilo C2-9, y arilo C6-14, está opcionalmente sustituido con al menos un grupo R13; cada R13 es independientemente -OH, halogeno, CF3, alquilo C1-6, alquenilo C1-6, alquinilo C1-6, alcoxi C1-6, ciano, cicloalquilo C3-10, cicloheteroalquilo C2-9, arilo C6-14, heteroarilo C2-9, amino, carbonilo, C-amido, sulfinilo, S-sulfonamido, C-carboxilo, N-amido, o N-carbamilo; cada m es independientemente 1 o 2; cada n es independientemente 0, 1, 2, 3, o 4; y cada z es un numero entero seleccionado independientemente entre 0, 1, 2, 3, 4, 5, 6, 7, u 8.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US84506506P | 2006-09-15 | 2006-09-15 | |
| US94785207P | 2007-07-03 | 2007-07-03 | |
| US95262807P | 2007-07-30 | 2007-07-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR062785A1 true AR062785A1 (es) | 2008-12-03 |
Family
ID=38859750
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104059A AR062785A1 (es) | 2006-09-15 | 2007-09-13 | Compuestos de 4-metilpiridopirimidinona, composiciones farmaceuticas que los contienen y usos en estados patologicos asociados al crecimiento anormal celular,tal como cancer. |
Country Status (42)
Families Citing this family (36)
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| WO2006050501A2 (en) | 2004-11-03 | 2006-05-11 | University Of Kansas | Novobiocin analogues as anticancer agents |
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| PL1940839T3 (pl) * | 2005-10-07 | 2013-12-31 | Exelixis Inc | Pirydopirymidynonowe inhibitory PI3Kalfa |
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