AR044499A1 - Pirimidinas sustituidas con indano inhibidoras de la replicacion del hiv - Google Patents
Pirimidinas sustituidas con indano inhibidoras de la replicacion del hivInfo
- Publication number
- AR044499A1 AR044499A1 ARP040100548A ARP040100548A AR044499A1 AR 044499 A1 AR044499 A1 AR 044499A1 AR P040100548 A ARP040100548 A AR P040100548A AR P040100548 A ARP040100548 A AR P040100548A AR 044499 A1 AR044499 A1 AR 044499A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cyano
- nr13r14
- optionally substituted
- halo
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- 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
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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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
-
- 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
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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
-
- 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
- A61P31/18—Antivirals for RNA viruses for HIV
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuesto, proceso para su preparación, composición farmacéutica y uso como medicamento en el tratamiento de las infecciones por HIV. Reivindicación 1: Un compuesto de fórmula (1), un N-óxido, una sal de adición farmacéuticamente aceptable, una amina cuaternaria o una forma estereoquímicamente isomérica del mismo, en el cual a1=a2=a3=a4 representa un radical bivalente de fórmula -CH=CH-CH=CH- (a-1); -N=CH-CH=CH- (a-2); -N=CH-N=CH- (a-3); -N=CH-CH=N- (a-4); -N=N-CH=CH- (a-5); -b1-b2-b3- representa un radical bivalente de fórmula -CH2-CH2-CH2- (b-1); n es 0, 1, 2, 3 ó 4; y en el caso en que -a1=a2-a3=a4- es (a-1), luego n también puede ser 5; m es 0, 1, 2, 3; q es 0, 1 ó 2; p es 1 ó 2; R1 es hidrógeno; arilo; formilo; alquilcarbonilo C1-6; alquilo C1-6; alquiloxicarbonilo C1-6; alquilo C1-6 substituido con formilo, alquilcarbonilo C1-6, alquiloxicarbonilo C1-6, alquilcarboniloxi C1-6; alquiloxi C1-6alquilcarbonilo C1-6 substituido con alquiloxicarbonilo C1-6; cada R2 representa independientemente hidroxi, halo, alquilo C1-6 optativamente substituido con ciano o con -C(=O)R6, cicloalquilo C3-7, alquenilo C2-6 optativamente substituido con uno o más átomos de halógeno o ciano, alquinilo C2-6 optativamente substituido con uno o más átomos de halógeno o ciano, alquiloxicarbonilo C1-6, carboxilo, ciano, nitro, NR13R14, polihalometilo, polihalometiltio, -S(=O)pR6, -NH-S(=O)pR6, -C(=O)R6, -NHC(=O)H, -C(=O)NHNH2,-NHC(=O)R6,-C(=NH)R6 o un radical de fórmula (2) en la cual cada A1, es independientemente N, CH o CR6; y A2 es NH, O, S o NR6; X1 es -NR5-, -NH-NH-, -N=N-, -O-, -C(=O)-, alcanodiilo C1-4, -CHOH-, -S-, -S(=O)p-, -NR13-C(=O)-, -C(=O)-NR13-, -X2-alcanodiilo C1-4- o -alcanodiilo C1-4-X2-; X2 es - NR5-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)p; R3 es hidrógeno, halo, alquilo C1-6, NR13R14, -C(=O)-NR13R14, -C(=O)-R15, -CH=N-NH-C(=O)-R16, -C(N=O-R8)-alquilo C1-4, R7 o -X3-R7; o bien alquilo C1-6 substituido con uno o más substituyentes cada uno de los cuales es independientemente seleccionado entre halo, hidroxi, ciano, NR9R10, -C(=O)-NR9R10, -C(=O)-alquilo C1-6 o R7, y además de la mencionada lista de substituyentes, dos átomos de hidrógeno geminales de dicho alquilo C1-6 también pueden ser reemplazados por un alcanodiilo C2-5 formando así un anillo de espiro; alquiloxi C1-6alquilo C1-6 optativamente substituido con uno o más substituyentes cada uno de los cuales es seleccionado entre hidroxi, ciano, NR9R10, -C(=O)-NR9R10, -C(=O)-alquilo C1-6 o R7; alquenilo C2-6 substituido con uno o más substituyentes cada uno de los cuales es seleccionado entre halo, hidroxi, ciano, NR9R10, -C(=O)-NR9R10, -C(=O)-alquilo C1-6 o R7; alquinilo C2-6 substituido con uno o más substituyentes cada uno de los cuales es seleccionado entre halo, hidroxi, ciano, NR9R10, -C(=O)-NR9R10, -C(=O)-alquilo C1-6 o R7; X3 es -NR5-, -NH-NH-, -N=N-, -O-, -C(=O)-, -S-, -S(=O)p-, -X2-alcanodiilo C1-4-, -alcanodiilo C1-4-X2a-,- alcanodiilo C1-4-X2b-alcanodiilo C1-4, -C(=N-OR8)-alcanodiilo C1-4-;donde X2a es -NH-NH-, -N=N-, -O-, -C(=O)-, -S-, -S(=O)p-; donde X2b es -NH-NH-, -N=N-, -C(=O)-, -S-, -S(=O)p-; R4 es halo, hidroxi, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, alquiloxi C1-6, ciano, nitro, polihaloalquilo C1-6, polihaloalquiloxi C1-6, -C(=O)-NR13R14, alquiloxicarbonilo C1-6, alquilcarbonilo C1-6, formilo, -NR13R14 o R7; R5 es hidrógeno; arilo; formilo; alquilcarbonilo C1-6; alquilo C1- 6; alquiloxicarbonilo C1-6; alquilo C1-6 substituido con formilo, alquilcarbonilo C1-6, alquiloxicarbonilo C1-6 o alquilcarboniloxi C1-6; alquiloxi C1-6alquilcarbonilo C1-6 substituido con alquiloxicarbonilo C1-6; R6 es alquilo C1-4, NR13R14 o polihaloalquilo C1-4; R7 es un carbociclo monocíclico, bicíclico o tricíclico saturado, parcialmente saturado o aromático o un heterociclo monocíclico, bicíclico o tricíclico saturado, parcialmente saturado o aromático, donde cada uno de dichos sistemas de anillos carbocíclicos o heterocíclicos puede estar optativamente substituido con uno, dos, tres, cuatro o cinco substituyentes cada uno de los cuales es independientemente seleccionado entre halo, hidroxi, mercapto, alquilo C1-6, hidroxialquilo C1-6, aminoalquilo C1-6, mono o di(alquil C1-6)aminoalquilo C1-6, formilo, alquilcarbonilo C1-6, cicloalquilo C3-7, alquiloxi C1-6, alquiloxicarbonilo C1-6, alquiltio C1-6, ciano, nitro, polihaloalquilo C1-6, polihaloalquiloxi C1-6, aminocarbonilo, -CH(=N-O-R8), R7a, -X3-R7a o R7a-alquilo C1-4; R7a es carbociclo monocíclico, bicíclico o tricíclico saturado, parcialmente saturado o aromático o un heterociclo monocíclico, bicíclico o tricíclico saturado, parcialmente saturado o aromático, donde cada uno de dichos sistemas de anillos carbocíclicos o heterocíclicos puede estar optativamente substituido con uno, dos, tres, cuatro o cinco substituyentes cada uno de los cuales es independientemente seleccionado entre halo, hidroxi, mercapto, alquilo C1-6, hidroxialquilo C1-6, aminoalquilo C1-6, mono o di (alquil C1-6)aminoalquilo C1-6, formilo, alquilcarbonilo C1-6, cicloalquilo C3-7, alquiloxi C1-6, alquiloxicarbonilo C1-6, alquiltio C1-6, ciano, nitro, polihaloalquilo C1-6, polihaloalquiloxi C1-6, -C(=O)-NR13R14, -CH(=N-O-R8); R8 es hidrógeno, alquilo C1-4, arilo o arilalquilo C1-4; R9 y R10 cada uno independientemente es hidrógeno; hidroxi; alquilo C1-6; alquiloxi C1-6; alquilcarbonilo C1-6; alquiloxicarbonilo C1-6; NR13R14; -C(=O)-NR13R14; -CH(=NR11) o R7, donde cada uno de los grupos alquilo C1-6 antes mencionados puede estar individual y optativamente substituido con uno o dos substituyentes cada uno de los cuales es independientemente seleccionado entre hidroxi, alquiloxi C1-6, hidroxialquiloxi C1-6, carboxilo, alquiloxicarbonilo C1-6, ciano, imino, NR13R14, polihalometilo, polihalometiloxi, polihalometiltio, -S(=O)pR6, -NH-S(=O)pR6, -C(=O)R6, -NHC(=O)H, - C(=O)NHNH2, -NHC(=O)R6,-C (=NH)R6,R7; o bien R9 yR10 pueden ser tomados en conjunto para formar un radical bivalente o trivalente de las fórmulas -CH2-CH2-CH2-CH2- (d-1); -CH2-CH2-CH2-CH2-CH2- (d-2); -CH2-CH2-O-CH2-CH2- (d-3); -CH2-CH2-S-CH2-CH2- (d- 4); -CH2-CH2-NR12-CH2-CH2- (d-5); -CH2-CH=CH-CH2- (d-6), =CH-CH=CH-CH=CH- (d-7); R11 es ciano; alquilcarbonilo C1-4; alquiloxicarbonilo C1-4; -C(=O)-NR13R14; o alquilo C1-4 optativamente substituido con alquiloxi C1-4, ciano, NR13R14 o -C(=O)- NR13R14; R12 es hidrógeno o alquilo C1-4; cada uno de R13 y R14 es independientemente hidrógeno, Het, alquilo C1-6 optativamente substituido con ciano o aminocarbonilo, alquenilo C2-6 optativamente substituido con ciano o aminocarbonilo, alquinilo C2-6 optativamente substituido con ciano o aminocarbonilo; R15 es alquilo C1-6 optativamente substituido con ciano o -C(=O)-NR13R14; R16 es R7 o alquilo C1-6 optativamente substituido con ciano o -C(=O)-NR13R14; R17, en caso de estar presente, es independientemente en cada caso ciano, halo, hidroxi,-C(=O)-NR13R14, alquilo C1-6 optativamente substituido con uno o más substituyentes independientemente seleccionados entre ciano, -C(=O)-NR13R14 o halo; alquenilo C2-6 optativamente substituido con uno o más substituyentes independientemente seleccionados entre ciano,-C(=O)-NR13R14 o halo; alquinilo C2-6 optativamente substituido con uno o más substituyentes independientemente seleccionados entre ciano, -C (=O)-NR13R14 o halo; y, en lo posible, R17 también puede estar unido a la porción -b1-b2-b3- por un doble enlace, por lo cual R17 es entonces =O, =S, =NH, =N-R15, =N-R7, =N-O-R15, =N-O-R7, =CH2, =CH-C(=O)-NR13R14, =CH-R7, o =CH-R15; donde =CH2 puede estar optativamente substituido con ciano, hidroxi, halo, nitro; Q representa hidrógeno, alquilo C1-6, halo, polihaloalquilo C1-6, -C(=O)-NR13R14, o -NR9R10; Z es C-Y, donde, Y representa hidrógeno, hidroxi, halo, alquilo C1-6, cicloalquilo C3-7, alquiloxi C1- 6,alquiloxicarbonilo C1-6, carbonilo, ciano, nitro, NR13R14, polihalometilo, polihalometiloxi, polihalometiltio, -S(=O)pR8, -NH-S(=O)R8, -NH-SO2-R8, -NH-SO2-(alcanodiilo C1-4)-CO-N(R8)2-, -C(=O)R8, -NHC(=O)H, -C(=O)NHNH2, -NHC(=O)R8, -C(=O)-NH-R8, - C(=NH)R8, arilo o alquenilo C2-6 optativamente substituido con uno o más átomos de halo; alquinilo C2-6 optativamente substituido con uno o más átomos de halo; alquilo C1-6 substituido con ciano o con -C(=O)R8; arilo es fenilo o fenilo substituido con uno, dos, tres, cuatro o cinco substituyentes cada uno de los cuales es independientemente seleccionado entre halo, hidroxi, mercapto, alquilo C1-6, hidroxialquilo C1-6, alquilo C1-6NR13R14, alquilcarbonilo C1-6, cicloalquilo C3-7, alquiloxi C1- 6, alquiloxi C1-6-carbonilo, alquiltio C1-6, ciano, nitro, polihaloalquilo C1-6, polihaloalquiloxi C1-6, -C(=O)-NR13R14, R7 o -X3-R7; Het es un heterociclo monocíclico, bicíclico o tricíclico saturado, parcialmente saturado o aromático, donde cada uno de dichos sistemas de anillos carbocíclicos o heterocíclicos puede estar optativamente substituido con uno, dos, tres, cuatro o cinco substituyentes cada uno de los cuales es independientemente seleccionado entre halo, hidroxi, mercapto, alquilo C1-6, hidroxialquilo C1-6, aminoalquilo C1-6, mono o di(alquil C1-6)aminoalquilo C1-6, formilo, alquilcarbonilo C1-6, cicloalquilo C3-7, alquiloxi C1-6, alquiloxicarbonilo C1-6, alquiltio C1-6, ciano, nitro, polihaloalquilo C1-6, polihaloalquiloxi C1-6, -C(=O)-NR13R14, -CH(=N-O-R8).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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EP03100411 | 2003-02-20 | ||
US47501203P | 2003-06-02 | 2003-06-02 |
Publications (1)
Publication Number | Publication Date |
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AR044499A1 true AR044499A1 (es) | 2005-09-14 |
Family
ID=32910137
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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ARP040100549A AR044500A1 (es) | 2003-02-20 | 2004-02-20 | Pirimidinas y triazinas inhibidoras de la replicacion del hiv |
ARP040100548A AR044499A1 (es) | 2003-02-20 | 2004-02-20 | Pirimidinas sustituidas con indano inhibidoras de la replicacion del hiv |
Family Applications Before (1)
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ARP040100549A AR044500A1 (es) | 2003-02-20 | 2004-02-20 | Pirimidinas y triazinas inhibidoras de la replicacion del hiv |
Country Status (27)
Country | Link |
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US (2) | US7585870B2 (es) |
EP (2) | EP1603887B1 (es) |
JP (2) | JP4586013B2 (es) |
KR (2) | KR20050094896A (es) |
CN (2) | CN100572364C (es) |
AP (1) | AP2005003373A0 (es) |
AR (2) | AR044500A1 (es) |
AT (2) | ATE506353T1 (es) |
AU (2) | AU2004213186B2 (es) |
BR (2) | BRPI0407741B8 (es) |
CA (2) | CA2516699C (es) |
CL (2) | CL2004000306A1 (es) |
CY (1) | CY1106788T1 (es) |
DE (2) | DE602004032321D1 (es) |
DK (1) | DK1597238T3 (es) |
EA (2) | EA011256B1 (es) |
ES (1) | ES2287734T3 (es) |
HR (2) | HRP20050820A2 (es) |
IL (2) | IL169596A (es) |
MX (2) | MXPA05008866A (es) |
MY (1) | MY138308A (es) |
NO (2) | NO20054312L (es) |
NZ (2) | NZ542428A (es) |
PL (2) | PL226954B1 (es) |
PT (1) | PT1597238E (es) |
TW (2) | TW200510339A (es) |
WO (2) | WO2004074261A1 (es) |
Families Citing this family (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
EP1534286B1 (en) | 2002-07-29 | 2009-12-09 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
CL2004000306A1 (es) * | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa. |
DK1656372T3 (da) | 2003-07-30 | 2013-07-01 | Rigel Pharmaceuticals Inc | 2,4-pyrimidindiaminforbindelser til anvendelse til behandling eller forebyggelse af autoimmunsygdomme |
KR20070011458A (ko) | 2004-04-08 | 2007-01-24 | 탈자진 인코포레이티드 | 키나제의 벤조트리아진 억제제 |
WO2006024034A1 (en) | 2004-08-25 | 2006-03-02 | Targegen, Inc. | Heterocyclic compounds and methods of use |
WO2006068770A1 (en) | 2004-11-24 | 2006-06-29 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
CA2591948C (en) | 2005-01-19 | 2013-11-12 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
JP5225079B2 (ja) | 2005-06-08 | 2013-07-03 | ライジェル ファーマシューティカルズ, インコーポレイテッド | Jak経路の阻害のための組成物および方法 |
US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
US8604042B2 (en) | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
EP1951684B1 (en) | 2005-11-01 | 2016-07-13 | TargeGen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
EP1991532B1 (en) | 2006-02-24 | 2017-01-11 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
EP2781510B1 (en) * | 2006-12-29 | 2016-12-14 | Janssen Sciences Ireland UC | Hiv inhibiting 5,6-substituted pyrimidines |
BRPI0720858B8 (pt) * | 2006-12-29 | 2021-05-25 | Janssen R & D Ireland | pirimidinas 6-substituídas inibidoras de hiv e composição farmacêutica que as compreende |
MX2010012703A (es) | 2008-05-21 | 2010-12-21 | Ariad Pharma Inc | Derivados fosforosos como inhibidores de cinasa. |
US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
US7737157B2 (en) * | 2008-08-29 | 2010-06-15 | Hutchison Medipharma Enterprises Limited | Pyrimidine compounds |
AU2009290474A1 (en) | 2008-09-11 | 2010-03-18 | Pfizer Inc. | Heteroaryls amide derivatives and their use as glucokinase activators |
TW201024281A (en) | 2008-11-24 | 2010-07-01 | Boehringer Ingelheim Int | New compounds |
TWI491605B (zh) * | 2008-11-24 | 2015-07-11 | Boehringer Ingelheim Int | 新穎化合物 |
SI2406253T1 (sl) | 2009-03-11 | 2013-09-30 | Pfizer Inc. | Derivati benzofuranila, uporabljeni kot inhibitorji glukokinaze |
CA2816957A1 (en) | 2010-11-07 | 2012-05-10 | Targegen, Inc. | Compositions and methods for treating myelofibrosis |
US9249124B2 (en) | 2011-03-30 | 2016-02-02 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Aurora kinase inhibitors and methods of making and using thereof |
AU2012250517B2 (en) | 2011-05-04 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
GB201119358D0 (en) | 2011-11-10 | 2011-12-21 | Lewi Paulus J | Disubstituted triazine dimers for treatment and/or prevention of infectious diseases |
GB201204756D0 (en) | 2012-03-19 | 2012-05-02 | Lewi Paulus J | Triazines with suitable spacers for treatment and/or prevention of HIV infections |
AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
WO2014072419A1 (en) | 2012-11-08 | 2014-05-15 | Universiteit Antwerpen | Novel anti-hiv compounds |
US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
WO2018019204A1 (zh) * | 2016-07-26 | 2018-02-01 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
CN106749203B (zh) * | 2016-11-28 | 2020-04-10 | 洛阳聚慧医药科技有限公司 | 一种嘧啶类杂环化合物、嘧啶类杂环化合物盐以及制备方法和应用 |
PL3966207T3 (pl) | 2019-05-10 | 2024-03-04 | Deciphera Pharmaceuticals, Llc | Fenyloaminopirymidynoamidowe inhibitory autofagii i sposoby ich zastosowania |
CN114072397A (zh) | 2019-05-10 | 2022-02-18 | 德西费拉制药有限责任公司 | 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法 |
AU2020297422B2 (en) | 2019-06-17 | 2024-03-21 | Deciphera Pharmaceuticals, Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
Family Cites Families (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3459731A (en) * | 1966-12-16 | 1969-08-05 | Corn Products Co | Cyclodextrin polyethers and their production |
US5691364A (en) * | 1995-03-10 | 1997-11-25 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
NZ322907A (en) | 1995-11-23 | 1998-12-23 | Janssen Pharmaceutica Nv | Solid mixtures of cyclodextrins prepared via melt-extrusion |
NO311614B1 (no) | 1996-10-01 | 2001-12-17 | Janssen Pharmaceutica Nv | Substituerte diamino-1,3,5-triazinderivater |
GB9705361D0 (en) | 1997-03-14 | 1997-04-30 | Celltech Therapeutics Ltd | Chemical compounds |
EP0945447A1 (en) | 1998-03-27 | 1999-09-29 | Janssen Pharmaceutica N.V. | Trisubstituted 1,3,5-triazine derivatives for treatment of HIV infections |
CZ299380B6 (cs) * | 1998-03-27 | 2008-07-09 | Janssen Pharmaceutica N. V. | Pyrimidinová sloucenina, použití této slouceniny pro prípravu léciva, farmaceutický prostredek tutoslouceninu obsahující, zpusob prípravy tohoto prostredku a uvedené slouceniny a kombinace a produktuvedenou slouceninu obsahující |
HU230394B1 (hu) * | 1998-11-10 | 2016-04-28 | Janssen Pharmaceutica N.V. | HIV-vírus szaporodását gátló pirimidin-származékok |
GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
ES2391550T3 (es) | 1999-04-15 | 2012-11-27 | Bristol-Myers Squibb Company | Inhibidores cíclicos de la proteína tirosina quinasa |
GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
BRPI0014271B1 (pt) * | 1999-09-24 | 2021-06-22 | Janssen Pharmaceutica N.V. | Partícula consistindo em uma dispersão de sólidos, uso da dita partícula, dispersão de sólidos, forma de dosagem farmacêutica, bem como processos de preparação de dita partícula, dispersão e forma de dosagem |
WO2001025220A1 (en) * | 1999-10-07 | 2001-04-12 | Amgen Inc. | Triazine kinase inhibitors |
CA2406562C (en) | 2000-05-08 | 2009-09-15 | Janssen Pharmaceutica N.V. | Hiv replication inhibiting pyrimidines and triazines |
AU2002216650A1 (en) | 2000-10-31 | 2002-05-15 | Lynn Bonham | Triazine derivatives as lpaat-b inhibitors and uses thereof |
JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
WO2003066099A1 (fr) * | 2002-02-05 | 2003-08-14 | Yamanouchi Pharmaceutical Co., Ltd. | Derives de 2,4,6-triamino-1,3,5-triazine |
AR039540A1 (es) * | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
CN1665789A (zh) * | 2002-06-28 | 2005-09-07 | 山之内制药株式会社 | 二氨基嘧啶酰胺衍生物 |
EP1534286B1 (en) * | 2002-07-29 | 2009-12-09 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
CL2004000306A1 (es) | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa. |
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