ECSP055988A - Compuestos de aminoheteroarilo como inhibidores de las proteinquinasas - Google Patents
Compuestos de aminoheteroarilo como inhibidores de las proteinquinasasInfo
- Publication number
- ECSP055988A ECSP055988A EC2005005988A ECSP055988A ECSP055988A EC SP055988 A ECSP055988 A EC SP055988A EC 2005005988 A EC2005005988 A EC 2005005988A EC SP055988 A ECSP055988 A EC SP055988A EC SP055988 A ECSP055988 A EC SP055988A
- Authority
- EC
- Ecuador
- Prior art keywords
- cr6r7
- aryl
- cycloalkyl
- membered
- nr4r5
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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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
- A61K31/4965—Non-condensed pyrazines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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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
- A61P35/00—Antineoplastic agents
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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
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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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Physical Education & Sports Medicine (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Un compuesto de la formula 1en donde: Y es N o CR12: R1 es seleccionado de arilo C6- 12, heterarilo de 5- 12 miembros, cicloalquilo C3- 12, heteroalicíclico de 3- 12 miembros, - O(CR6R7)nR4, - C(O)R4, - C(O)OR4, - CN, - NO2, - S(O)mR4, - SO2NR4R5, - C(O)NR4R5, - NR4(C(O)R5, - C(=NR6)NR4R5, alquilo C1- 8, alquenilo C2- 8, y alquinilo C2- 8; y cada hidrógeno en R1 es opcionalmente substituido por uno o más grupos R3; R2 es hidrogeno, halógeno, alquilo C1- 12, alquenilo C2- 12, alquinilo C2- 12, cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico de 3- 12 miembros, heteroarilo de 5- 12 miembros, - S(O)mR4, - SO2NR4R5, - S(O)2OR4, - NO2, - NR4R5, - (CR6R7)nOR4, - CN, - C(O)R4, - OC(O)R4, - O(CR6R7)nR4, - NR4C(O)R5, - (CR6R7)nC(O)OR4, - (CR6R7)nNCR4R5, - C(=NR6)NR4R5, - NR4C(O)NR5R6, - NR4S(O)pR5 o - C(O)NR4R5, y cada hidrógeno en R2 es opcionalmente sustituido por uno o más grupos R8; R3 es halógeno, alquilo C1- 12, alquenilo C2- 12, alquinilo C2- 12, cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico 3- 12 miembros, heteroarilo de 5- 12 miembros, - S(O)mR4, - SO2NR4R5, - S(O)2OR4, - NO2, - NR4R5, - (CR6R7)nOR4, - CN, - C(O)R4, - OC(O)R4, - O(CR6R7)nR4, - NR4C(O)R5, - (CR6R7)nC(O)OR4, - (CR6R7)nNCR4R5, - C(=NR6)NR4R5, - NR4C(O)NR5R6, - NR4S(O)pR5 o - C(O)NR4R5, cada hidrógeno en R3 es opcionalmente sustituido por uno o más grupos R8, y grupos los R3 sobre átomos adyacentes se pueden combinar para formar un arilo C6- 12, heteroarilo de 5- 12 miembros, cicloalquilo C3- 12 o grupo heteroalicíclico de 3- 12 miembros; Cada uno de R4, R5, R6 y R7 es independientemente hidrógeno, halógeno, alquilo C1- 12, alquenilo C2- 12, alquinilo C2- 12, cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico de 3- 12 miembros, heteroarilo de 5- 12 miembros; o cualquiera dos entre R4, R5, R6 y R7 unidos al mismo átomo de nitrógeno pueden junto con el nitrógeno al cual están unidos ser combinados para formar un heteroalicíclico de 13 a 12 miembros o grupo heteroarilo de 5- 12 miembros opcionalmente conteniendo de 1 a 3 heteroátomos adicionales seleccionados de N. O y S; o cualquiera dos entre R4, R5, R6 y R7 unidos al mismo átomo de carbono puede ser combinados para formar un cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico de 3 - 12 miembros, o grupo heteroarilo de 5- 12 miembros; y cada hidrógeno en R4, R5, R6 y R7 es opcionalmente sustituido por uno o más grupos R8; cada R8 es independientemente halógeno, alquilo C1- 12, alquenilo C2- 12, alquinilo C2- 12, cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico de 3 - 12 miembros, heteroarilo de 5 - 12 miembros, - CN, alquilo - O- C1- 12, cicloalquilo - O- (CH2)nC3- 12, arilo - O- (CH2)nC6- 12, - O- (CH2)n(heteroalicíclico de 3- 12 miembros) o - O- (CH2)n(heteroarilo de 5- 12 miembros); y cada hidrógeno en R8 es opcionalmente sustituido por uno o más grupos R11; A1 es - (CR9R10)n- A2 excepto que: (i) cuando Y es N y R1 es arilo sustituido o no sustituido o heteroarilo sustituido o no sustituido, A1 es - (CR9R10)n- A2 y n no es cero; y (ii) cuando Y es N y R2 es H y A1 es m- clorobencilo, R1 es piperazina no sustituida; cada R9 y R10 es independientemente hidrógeno, halógeno, alquilo C1- 12, cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico de 3- 12 miembros, heteroarilo de 5- 12 miembros, - S(O)mR4, - SO2NR4R5, - S(O)2OR4, - NO2, - NR4R5, - (CR6R7)nOR4, - CN, - C(O)R4, - OC(O)R4, - NR4C(O)R5, - (CR6R7)nC(O)OR4, - (CR6R7)nNCR4R5, - NR4C(O)NR5R6, - NR4S(O)pR5 o - C(O)NR4R5; R9 y R10 se pueden combinar para formar un cicloalquilo C3- 12, heteroalicíclico de 3- 12 miembros, arilo C6- 12 o anillo de heteroarilo de 5- 12 miembros; y cada hidrógeno en R9 y R10 es opcionalmente sustituido por uno o más grupos R3; A2 es arilo C6- 12, heteroarilo de 5- 12 miembros, cicloalquilo C3- 12 o heteroalicíclico de 3 - 12 miembros, y A2 es opcionalmente sustituido por uno o más grupos R3; cada R11 es independientemente halógeno, alquilo C1- 12, alcoxilo C1- 12, cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico de 3 - 12 miembros, heteroarilo de 5- 12 miembros, alquilo - O- C1- 12, cicloalquilo - O- (CH2)nC3- 12, arilo - O- (CH2)nC6- 12, - O_(CH2)n(heteroalicíclico de 3- 12 miembros), - O- (CH2)n(heteroarilo de 5- 12 miembros) o - CN, y cada hidrógeno en R11 es un generalmente sustituido por uno o más grupos seleccionados de halógeno - OH, - CN, alquilo C1- 12, el cual puede ser parcial o totalmente halogenado, alquilo - O- C1- 12 el cual puede ser total o parcialmente halogenado, - CO, - SO y - SO2; R12 es hidrógeno, halógeno, alquilo C1- 12, alquenilo C2- 12, alquinilo C2- 12, cicloalquilo C3- 12, arilo C6- 12, heteroalicíclico de 3- 12 miembros, heteroarilo de 5- 12 miembros, S(O)mR4, - SO2NR4R5, - S(O)2OR4, - NO2, - NR4R5, - (CR6R7)nOR4, - CN, - C(O)R4, - OC(O)R4, - O(CR6R7)nR4, - NR4C(O)R5, - (CR6R7)nC(O)OR4, - (CR6R7)nNCR4R5, - C(=NR6)NR4R5, - NR4C(O)NR5R6, - NR4S(O)pR5 o - C(O)NR4R5 y cada hidrogeno en R12 es opcionalmente sustituido por uno o más grupos R3; R1 y R2 o R1 y R2 se pueden combinar juntos para formar arilo C6- 12, heteroarilo de 5- 12 miembros, cicloalquilo C3- 12, o grupo heteroalicíclico de 3- 12 miembros; m es 0, 1 o 2; n es 0, 1, 2, 3 o 4; y p es 1 o 2; o una sal, solvato o hidrato farmaceuticamente aceptable del mismo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US44958803P | 2003-02-26 | 2003-02-26 | |
US54022904P | 2004-01-29 | 2004-01-29 |
Publications (1)
Publication Number | Publication Date |
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ECSP055988A true ECSP055988A (es) | 2006-01-16 |
Family
ID=32930516
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EC2005005988A ECSP055988A (es) | 2003-02-26 | 2005-08-26 | Compuestos de aminoheteroarilo como inhibidores de las proteinquinasas |
Country Status (29)
Country | Link |
---|---|
US (2) | US7230098B2 (es) |
EP (2) | EP2476667B1 (es) |
JP (1) | JP4695588B2 (es) |
KR (1) | KR101106905B1 (es) |
CN (1) | CN103265477B (es) |
AP (1) | AP2114A (es) |
AU (1) | AU2004215428B2 (es) |
BR (1) | BRPI0407827B8 (es) |
CA (1) | CA2517256C (es) |
CY (2) | CY1113837T1 (es) |
DK (2) | DK2476667T3 (es) |
EA (1) | EA010727B1 (es) |
EC (1) | ECSP055988A (es) |
ES (2) | ES2502490T3 (es) |
GE (1) | GEP20084341B (es) |
HR (1) | HRP20050714B1 (es) |
IL (1) | IL170291A (es) |
IS (1) | IS2910B (es) |
MA (1) | MA27713A1 (es) |
ME (1) | MEP52808A (es) |
MX (1) | MXPA05009063A (es) |
NO (1) | NO332188B1 (es) |
NZ (1) | NZ541861A (es) |
OA (1) | OA13151A (es) |
PL (1) | PL216368B1 (es) |
PT (2) | PT2476667E (es) |
RS (1) | RS53118B (es) |
TN (1) | TNSN05208A1 (es) |
WO (1) | WO2004076412A2 (es) |
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PE20070978A1 (es) * | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
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