AR056865A1 - Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas - Google Patents
Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticasInfo
- Publication number
- AR056865A1 AR056865A1 ARP060102462A ARP060102462A AR056865A1 AR 056865 A1 AR056865 A1 AR 056865A1 AR P060102462 A ARP060102462 A AR P060102462A AR P060102462 A ARP060102462 A AR P060102462A AR 056865 A1 AR056865 A1 AR 056865A1
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- Prior art keywords
- ring
- cycloalkenyl
- cycloalkyl
- heterocyclyl
- group
- Prior art date
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- 229910052757 nitrogen Inorganic materials 0.000 title abstract 11
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 title 2
- 102000035195 Peptidases Human genes 0.000 title 1
- 108091005804 Peptidases Proteins 0.000 title 1
- 239000004365 Protease Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 20
- 125000000623 heterocyclic group Chemical group 0.000 abstract 18
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 17
- 125000001072 heteroaryl group Chemical group 0.000 abstract 15
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 229910052760 oxygen Inorganic materials 0.000 abstract 9
- 125000005842 heteroatom Chemical group 0.000 abstract 8
- 229910052717 sulfur Inorganic materials 0.000 abstract 8
- 125000003342 alkenyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000000304 alkynyl group Chemical group 0.000 abstract 6
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 6
- 229910052799 carbon Inorganic materials 0.000 abstract 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 6
- -1 heterocyclynyl Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 125000004043 oxo group Chemical group O=* 0.000 abstract 6
- 125000004350 aryl cycloalkyl group Chemical group 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 5
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 4
- 125000005015 aryl alkynyl group Chemical group 0.000 abstract 4
- 125000004367 cycloalkylaryl group Chemical group 0.000 abstract 4
- 125000005215 cycloalkylheteroaryl group Chemical group 0.000 abstract 4
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 abstract 4
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 3
- 229910003849 O-Si Inorganic materials 0.000 abstract 3
- 229910003872 O—Si Inorganic materials 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- 150000001721 carbon Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 102000004580 Aspartic Acid Proteases Human genes 0.000 abstract 1
- 108010017640 Aspartic Acid Proteases Proteins 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 230000001149 cognitive effect Effects 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
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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
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
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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
- 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
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
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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
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
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- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
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- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Peptides Or Proteins (AREA)
Abstract
Composiciones farmacéuticas que comprenden los compuestos de la formula (1) y el método para inhibir aspartil proteasas y, en particular, los métodos para tratar enfermedades cardiovasculares, enfermedades cognitivas y neuroedegenerativas. Reivindicacion 1: Un compuesto que presenta la formula estructural (1), o un estereoisomero, tautomero o sal o solvato del mismo aceptable para uso farmacéutico, donde Q es un enlace o -N(R5)-; T es un enlace, -O-, -C(O)-; -S-, -N(R5)-, -S(O)-, -S(O)2- o -C(R6'R7')-; U es un enlace o -C(R6)(R7)-; Y es C o N; Z es C o N; el anillo A, que incluye las variables Y y Z, es un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo y heteroarilo de tres a nueve miembros que tiene 0 a 7, con preferencia 0 a 4, heteroátomos seleccionados independientemente del grupo que consiste en O, S, N y -N(R)-, donde el anillo A está no sustituido o sustituido con 1 a 5 residuos R1 seleccionados independientemente y/u oxo cuando el anillo A es cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; donde R se selecciona independientemente del grupo que consiste en hidrogeno alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, -OR15, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12) y -S(O)2N(R11)(R12); R1 se selecciona independientemente del grupo que consiste en H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halo, -CN, -OR15, -C(O)R15, -C(O)OR15, - C(O)N(R15)(R16), -S(O)0-2R15, -S(O)N(R15)(R16), -S(O)1-2-N(15)(R16), S(O)2N(R15)(R16), -C(=NOR15)R16, -P(O)(OR15)(OR16), -N(R15)(R16), -N(R15)C(O)R16, -N(R15)S(O)R16, -N(R15)S(O)2R16, -N(R15)S(O)2N(R16)(R17), -N(R15)S(O)N(R16)(R17), - N(R15)C(O)N(R16)(R17) y -N(R15)C(O)OR16; y opcionalmente, iii) cuando el anillo A está disustituido con dos grupos en el mismo átomo de carbono, los dos grupos R1 junto con el átomo de carbono del anillo forman un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2, heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos o iv) cuando el anillo A está disustituido con: a) dos grupos R1; o b) un grupo R y un grupo R1, los dos grupos o el grupo R y el grupo R1 junto con los átomos del anillo A al cual están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14; R2 se selecciona independientemente del grupo que consiste en H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, -OR15, -CN, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -NO2, -N=C(R8)2 y -N(R8)2; R3, R4, R6 y R7 se seleccionan independientemente del grupo que consiste en H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, halo, -CH2-O-Si(R9)(R10)(R19), -SH, -CN, -OR9, -C(O)R5, -C(O)OR9, -C(O)N(R11)(R12), -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, - N(R11)S(O)2R10-, -N(R11)C(O)N(R12)(R13), -N(R11)C(O)OR9 y -C(=NOH)R8; y opcionalmente, (i) R3 y R4, junto con el átomo al cual están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 8 miembros que tiene 0 a 3 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S y -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo, cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (ii) R6 y R7, junto con el carbono al cual están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 8 miembros que tiene 0 a 3 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo, cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (iii) cuando U es - C(R6)(R7)-, R3 y R6 junto con los átomos de carbono a los cuales están unidos forman un anillo de cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (iv) cuando T es -C(R6')(R7'), R3 y R6' junto con los átomos de carbono a los cuales están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilarilo o heteroarilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (v) cuando T es -N(R5)-, R3 y R5 junto con los átomos a los cuales están unidos forman un anillo heterociclilo, heterociclenilo, heteroarilo de 3 a 7 miembros que tiene 1 a 4, con preferencia 1 a 2, heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/o con oxo cuando dicho anillo es un anillo heterociclilo o un anillo heterociclenilo; o (vi) a) R3 y R4, junto con el carbono al cual están unidos, o b) R6 y R7 junto con el carbono al cual están unidos, forman uno de los grupos multicíclicos (2), donde: M es independientemente -(CH2)-, -S-, -N(R19)-, -O-, -S(O)-, -S(O)2- o -C(O)-; q es 0, 1 o 2; A y B son independientemente arilo, heteroarilo, cicloalquilo, cicloalquenilo o heterociclilo; E es arilo o heteroarilo; y F es cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo, con la condicion de que no haya ningun átomo de oxigeno y/o azufre adyacente presente en el sistema anular y además con la condicion de que ambos (a) R3 y R4; y (b) R6 y R7 no se puedan combinar para formar dichos grupos multicíclicos (2), al mismo tiempo; R5 se selecciona del grupo que consiste en H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, - CH2-O-Si(R9)(R10)(R19), -CN, -C(O)R8, -C(O)OR9, -C(O)N(R11)(R12), -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)S(O)2R10-, -N(R11)C(O)N(R12)(R13), -N(R11)C(O)OR9 y -C(=NOH)R8; R6' y R7' se seleccionan independientemente del grupo que consiste en H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquil-heteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, -halo, -CH2-O-Si(9)(R10)(R19), -SH, -CN, -OR9, -C(O)R8, -C(O)OR9, -C(O)N(R11)(P12), -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)S(O)2R10-, -N(R11)C(O)N(R12)(R13), -N(R11)C(O)OR9 y -C(=NOH)R8; u opcionalmente R6' y R7' jun
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-
2006
- 2006-06-12 ES ES11157371.3T patent/ES2436795T3/es active Active
- 2006-06-12 AR ARP060102462A patent/AR056865A1/es not_active Application Discontinuation
- 2006-06-12 US US11/451,065 patent/US8722708B2/en active Active
- 2006-06-12 BR BRPI0612545-0A patent/BRPI0612545A2/pt not_active IP Right Cessation
- 2006-06-12 AU AU2006259573A patent/AU2006259573A1/en not_active Abandoned
- 2006-06-12 EP EP06784808A patent/EP1896032B1/en active Active
- 2006-06-12 KR KR1020077029569A patent/KR20080028881A/ko not_active Withdrawn
- 2006-06-12 CA CA002610828A patent/CA2610828A1/en not_active Abandoned
- 2006-06-12 RU RU2008100164/04A patent/RU2008100164A/ru not_active Application Discontinuation
- 2006-06-12 CN CNA2006800209186A patent/CN101394852A/zh active Pending
- 2006-06-12 JP JP2008516998A patent/JP4896972B2/ja not_active Expired - Fee Related
- 2006-06-12 WO PCT/US2006/022919 patent/WO2006138265A2/en not_active Ceased
- 2006-06-12 EP EP11157371.3A patent/EP2345411B1/en active Active
- 2006-06-12 MX MX2007016183A patent/MX2007016183A/es active IP Right Grant
- 2006-06-13 PE PE2006000660A patent/PE20070321A1/es not_active Application Discontinuation
- 2006-06-13 TW TW095120997A patent/TW200716643A/zh unknown
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2007
- 2007-11-18 IL IL187455A patent/IL187455A0/en unknown
- 2007-11-29 ZA ZA200710385A patent/ZA200710385B/xx unknown
- 2007-12-12 EC EC2007008004A patent/ECSP078004A/es unknown
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2008
- 2008-01-11 NO NO20080186A patent/NO20080186L/no not_active Application Discontinuation
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Also Published As
| Publication number | Publication date |
|---|---|
| ES2436795T3 (es) | 2014-01-07 |
| IL187455A0 (en) | 2008-02-09 |
| JP4896972B2 (ja) | 2012-03-14 |
| EP1896032B1 (en) | 2012-10-31 |
| CN101394852A (zh) | 2009-03-25 |
| AU2006259573A1 (en) | 2006-12-28 |
| WO2006138265A2 (en) | 2006-12-28 |
| BRPI0612545A2 (pt) | 2010-11-23 |
| US9382242B2 (en) | 2016-07-05 |
| NO20080186L (no) | 2008-03-14 |
| PE20070321A1 (es) | 2007-04-16 |
| JP2008546696A (ja) | 2008-12-25 |
| US8722708B2 (en) | 2014-05-13 |
| WO2006138265A3 (en) | 2007-03-01 |
| EP2345411B1 (en) | 2013-10-02 |
| US20140206715A1 (en) | 2014-07-24 |
| JP2011251978A (ja) | 2011-12-15 |
| TW200716643A (en) | 2007-05-01 |
| KR20080028881A (ko) | 2008-04-02 |
| ECSP078004A (es) | 2008-01-23 |
| MX2007016183A (es) | 2008-03-10 |
| JP5454956B2 (ja) | 2014-03-26 |
| EP1896032A2 (en) | 2008-03-12 |
| RU2008100164A (ru) | 2009-07-20 |
| EP2345411A1 (en) | 2011-07-20 |
| CA2610828A1 (en) | 2006-12-28 |
| US20080176868A1 (en) | 2008-07-24 |
| ZA200710385B (en) | 2008-11-26 |
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