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
- Authority
- AR
- Argentina
- Prior art keywords
- ring
- cycloalkenyl
- cycloalkyl
- heterocyclyl
- group
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
-
- 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
-
- 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
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
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US69054105P | 2005-06-14 | 2005-06-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR056865A1 true AR056865A1 (es) | 2007-10-31 |
Family
ID=37467438
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP060102462A AR056865A1 (es) | 2005-06-14 | 2006-06-12 | Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas |
Country Status (19)
Country | Link |
---|---|
US (2) | US8722708B2 (es) |
EP (2) | EP1896032B1 (es) |
JP (2) | JP4896972B2 (es) |
KR (1) | KR20080028881A (es) |
CN (1) | CN101394852A (es) |
AR (1) | AR056865A1 (es) |
AU (1) | AU2006259573A1 (es) |
BR (1) | BRPI0612545A2 (es) |
CA (1) | CA2610828A1 (es) |
EC (1) | ECSP078004A (es) |
ES (1) | ES2436795T3 (es) |
IL (1) | IL187455A0 (es) |
MX (1) | MX2007016183A (es) |
NO (1) | NO20080186L (es) |
PE (1) | PE20070321A1 (es) |
RU (1) | RU2008100164A (es) |
TW (1) | TW200716643A (es) |
WO (1) | WO2006138265A2 (es) |
ZA (1) | ZA200710385B (es) |
Families Citing this family (71)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
KR20080031189A (ko) * | 2005-06-14 | 2008-04-08 | 쉐링 코포레이션 | 아스파르틸 프로테아제 억제제 |
US7868000B2 (en) | 2005-06-14 | 2011-01-11 | Schering Corporation | Aspartyl protease inhibitors |
CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
AR061264A1 (es) | 2006-06-12 | 2008-08-13 | Schering Corp | Inhibidores de aspartil-proteasas derivados de pirimidina, composiciones farmaceuticas que los contienen y usos para tratar enfermedades cognitivas o neurodegenerativas, y como inhibidores del virus vih. |
TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
EP2061771A1 (en) * | 2006-12-12 | 2009-05-27 | Schering Corporation | Aspartyl protease inhibitors containing a tricyclic ring system |
US8093254B2 (en) | 2006-12-12 | 2012-01-10 | Schering Corporation | Aspartyl protease inhibitors |
MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
WO2009005470A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
WO2009005471A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
JP2010538068A (ja) | 2007-09-06 | 2010-12-09 | シェーリング コーポレイション | ガンマセクレターゼモジュレーター |
MX2010005028A (es) | 2007-11-05 | 2010-05-27 | Schering Corp | Moduladores de gamma secretasa. |
MX2010006378A (es) | 2007-12-11 | 2010-09-07 | Schering Corp | Moduladores de gamma secretasa. |
US8071766B2 (en) | 2008-02-01 | 2011-12-06 | Takeda Pharmaceutical Company Limited | HSP90 inhibitors |
KR20130018370A (ko) | 2008-06-13 | 2013-02-20 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
US8426447B2 (en) | 2008-09-11 | 2013-04-23 | Amgen Inc. | Spiro-tricyclic ring compounds as beta-secretase modulators and methods of use |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
AU2009314049B2 (en) | 2008-11-13 | 2015-03-05 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
US20100125087A1 (en) * | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
TW201020244A (en) * | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
WO2010056194A1 (en) * | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use |
EP2379566A2 (en) | 2008-12-22 | 2011-10-26 | Schering Corporation | Gamma secretase modulators |
AU2009330233A1 (en) | 2008-12-22 | 2011-07-07 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
US20120238546A1 (en) | 2009-06-16 | 2012-09-20 | Zhaoning Zhu | Gamma secretase modulators |
EP2443119A1 (en) | 2009-06-16 | 2012-04-25 | Schering Corporation | Gamma secretase modulators |
WO2010147973A1 (en) | 2009-06-16 | 2010-12-23 | Schering Corporation | Gamma secretase modulators |
EP2281824A1 (en) | 2009-08-07 | 2011-02-09 | Noscira, S.A. | Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders |
WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
WO2011071135A1 (ja) | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
US8883782B2 (en) | 2010-03-15 | 2014-11-11 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
JP5584352B2 (ja) | 2010-03-15 | 2014-09-03 | アムジエン・インコーポレーテツド | β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途 |
KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체 |
US8921363B2 (en) | 2010-08-05 | 2014-12-30 | Amgen Inc. | Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors |
MY160138A (en) * | 2010-09-22 | 2017-02-28 | Janssen Pharmaceutica Nv | 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
WO2012069428A1 (en) | 2010-11-22 | 2012-05-31 | Noscira, S.A. | Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions |
EP2643325A1 (en) | 2010-11-23 | 2013-10-02 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
SG191097A1 (en) | 2010-12-22 | 2013-08-30 | Janssen Pharmaceutica Nv | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
EP2673279A1 (en) | 2011-02-07 | 2013-12-18 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use |
US8962859B2 (en) | 2011-02-15 | 2015-02-24 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
KR102012671B1 (ko) | 2011-03-01 | 2019-08-21 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(BACE)의 억제제로서 유용한 6,7-디하이드로-피라졸로[1,5-a]피라진-4-일아민 유도체 |
MX340031B (es) | 2011-03-09 | 2016-06-21 | Janssen Pharmaceutica Nv | Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina utiles como inhibidores de beta-secretasa (bace). |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
US9181236B2 (en) | 2011-08-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
WO2013142370A1 (en) | 2012-03-19 | 2013-09-26 | Varghese John | APP SPECIFIC BACE INHIBITORS (ASBIs) AND USES THEREOF |
US9422277B2 (en) | 2012-10-17 | 2016-08-23 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
CN104995176B (zh) | 2013-02-12 | 2019-02-22 | 巴克老龄化研究所 | 调节bace所介导的app加工的乙内酰脲 |
CA2902080A1 (en) * | 2013-02-25 | 2014-08-28 | Merck Patent Gmbh | 2-amino-3,4-dihydroquinazoline derivatives and the use thereof as cathepsin d inhibitors |
EA032662B1 (ru) | 2013-06-12 | 2019-06-28 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 4-АМИНО-6-ФЕНИЛ-5,6-ДИГИДРОИМИДАЗО[1,5-а]ПИРАЗИН-3(2H)-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) |
CN105324383B (zh) | 2013-06-12 | 2017-10-31 | 詹森药业有限公司 | 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物 |
AU2014280124B2 (en) | 2013-06-12 | 2018-11-01 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (BACE) |
CA2967164A1 (en) | 2014-12-18 | 2016-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase |
RU2642246C2 (ru) * | 2014-12-30 | 2018-01-24 | Федеральное государственное бюджетное научное учреждение "Институт экспериментальной медицины" (ФГБНУ "ИЭМ") | Применение пробиотического штамма микроорганизма enterococcus faecium l-3 для лечения нейродегенеративных заболеваний |
WO2018118829A1 (en) * | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heterocyclic compounds as hiv protease inhibitors |
KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
CN110563631B (zh) * | 2018-06-05 | 2023-05-23 | 爱斯特(成都)生物制药股份有限公司 | 一种抑制ido的化合物及其应用 |
Family Cites Families (93)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US1077204A (en) | 1912-11-20 | 1913-10-28 | John Bonner Semple | Tracer for projectiles. |
US3632814A (en) * | 1968-11-25 | 1972-01-04 | Velsicol Chemical Corp | Phosphoramidate esters |
JPS5013951B1 (es) * | 1969-05-23 | 1975-05-23 | ||
DE2430354A1 (de) | 1974-06-25 | 1976-01-15 | Basf Ag | Neue substituierte 1-amino-isoindole, verfahren zu deren herstellung sowie diese enthaltende pharmazeutische zubereitungen |
DE2757982C2 (de) * | 1977-12-24 | 1980-02-21 | Basf Ag, 6700 Ludwigshafen | Verbindungen der Isoindolinreihe und Verfahren zur Herstellung von in den anwendungstechnischen Eigenschaften verbesserten Pigmenten |
DE3371618D1 (en) * | 1982-02-27 | 1987-06-25 | Asahi Chemical Ind | Coloring method and color-forming material |
IL92011A0 (en) * | 1988-10-19 | 1990-07-12 | Abbott Lab | Heterocyclic peptide renin inhibitors |
WO1993004047A1 (en) | 1991-08-16 | 1993-03-04 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
DE4419849A1 (de) * | 1994-06-07 | 1995-12-14 | Hoechst Ag | Isoindolinpigmente |
US5629322A (en) | 1994-11-15 | 1997-05-13 | Merck & Co., Inc. | Cyclic amidine analogs as inhibitors of nitric oxide synthase |
JP3666922B2 (ja) * | 1995-02-21 | 2005-06-29 | 山本化成株式会社 | カルボン酸塩、その製造方法および該塩化合物を用いる感熱記録材料 |
IL117149A0 (en) | 1995-02-23 | 1996-06-18 | Schering Corp | Muscarinic antagonists |
US5889006A (en) | 1995-02-23 | 1999-03-30 | Schering Corporation | Muscarinic antagonists |
DE19516804A1 (de) * | 1995-05-08 | 1996-11-14 | Hoechst Ag | Isoindolinpigmente auf Basis von Aminochinoxalindionen |
US5935958A (en) | 1996-07-01 | 1999-08-10 | Schering Corporation | Muscarinic antagonists |
US5952349A (en) | 1996-07-10 | 1999-09-14 | Schering Corporation | Muscarinic antagonists for treating memory loss |
US5977138A (en) | 1996-08-15 | 1999-11-02 | Schering Corporation | Ether muscarinic antagonists |
AU9298098A (en) | 1997-09-03 | 1999-03-22 | Guilford Pharmaceuticals Inc. | Amino-substituted compounds, methods, and compositions for inhibiting parp activity |
WO1999033795A1 (en) * | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
US6066636A (en) | 1998-06-30 | 2000-05-23 | Schering Corporation | Muscarinic antagonists |
US6420364B1 (en) * | 1999-09-13 | 2002-07-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compound useful as reversible inhibitors of cysteine proteases |
SK286463B6 (sk) * | 1999-09-13 | 2008-10-07 | Boehringer Ingelheim Pharmaceuticals, Inc. | Spiroheterocyklické zlúčeniny, spôsob ich výroby,farmaceutický prostriedok s ich obsahom a ich použitie |
US6294554B1 (en) | 1999-09-22 | 2001-09-25 | Schering Corporation | Muscarinic antagonists |
PE20020276A1 (es) * | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
EP1343760B1 (en) | 2000-12-22 | 2009-08-12 | Schering Corporation | Muscarinic antagonists |
AU2002306734A1 (en) | 2001-03-15 | 2002-10-03 | The Johns Hopkins University | Inhibitors of plasmepsins |
KR20040019094A (ko) * | 2001-08-03 | 2004-03-04 | 쉐링 코포레이션 | 신규한 감마 세크레타제 억제제 |
CA2462861A1 (en) | 2001-10-10 | 2003-04-17 | Yuguang Wang | Piperidine compounds as muscarinic antagonists |
EP1699455B1 (en) | 2003-12-15 | 2013-05-08 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
KR20070026811A (ko) | 2004-06-16 | 2007-03-08 | 와이어쓰 | 베타-세크리타제 억제제로서의 디페닐이미다조피리미딘 및디페닐이미다졸 아민 |
EP1756087B1 (en) * | 2004-06-16 | 2009-10-07 | Wyeth | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
JP5046932B2 (ja) | 2004-08-06 | 2012-10-10 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | β−セクレターゼ(BACE)のインヒビターとして有用な新規の2−アミノ−キナゾリン誘導体 |
US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
PT1789398E (pt) | 2004-08-06 | 2010-10-21 | Janssen Pharmaceutica Nv | Derivados de 2-amino- quinazolina úteis como inibidores de β-secretase (bace) |
CA2583342A1 (en) | 2004-10-13 | 2006-04-27 | Merck And Co., Inc. | Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzhermer's disease |
WO2006044492A2 (en) | 2004-10-14 | 2006-04-27 | Ingenious Targeting Laboratory, Inc. | Methods for generating rat embryo-derived cell lines and genetic modification of rat genome |
WO2006041404A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-compounds and uses thereof |
US20090062282A1 (en) * | 2004-10-15 | 2009-03-05 | Astrazeneca Ab | Substituted Amino-Pyrimidones and Uses Thereof |
WO2006076284A2 (en) | 2005-01-14 | 2006-07-20 | Wyeth | AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE |
AU2006259574A1 (en) * | 2005-06-14 | 2006-12-28 | Schering Corporation | The preparation and use of compounds as aspartyl protease inhibitors |
US7868000B2 (en) * | 2005-06-14 | 2011-01-11 | Schering Corporation | Aspartyl protease inhibitors |
PE20070078A1 (es) * | 2005-06-14 | 2007-03-08 | Schering Corp | Compuestos heterociclicos macrociclicos como inhibidores de aspartil proteasa |
AU2006266167A1 (en) * | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation |
TW200738683A (en) * | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
TW200730523A (en) * | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
JP2009509957A (ja) * | 2005-09-26 | 2009-03-12 | ワイス | β−セクレターゼ阻害剤としてのアミノ−5−[4−(ジフルオロメトキシ)フェニル]−5−フェニルイミダゾロン化合物 |
CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
ES2360957T3 (es) * | 2005-10-25 | 2011-06-10 | Janssen Pharmaceutica Nv | Derivados de 2-amino-3,4-dihidro-pirido(3,4-d)-pirimidina utiles como inhibidores de la beta-secretasa (bace). |
DE602006016314D1 (de) | 2005-10-27 | 2010-09-30 | Schering Corp | Heterozyklische aspartyl-proteasehemmer |
US7560451B2 (en) * | 2005-10-31 | 2009-07-14 | Schering Corporation | Aspartyl protease inhibitors |
TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
AR058381A1 (es) * | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
US7776882B2 (en) | 2006-02-06 | 2010-08-17 | Baxter Ellen W | 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
US7868022B2 (en) | 2006-02-06 | 2011-01-11 | Janssen Pharmaceutica Nv | 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
WO2007092839A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | Macrocycle derivatives useful as inhibitors of beta-secretase (bace) |
WO2007100536A1 (en) * | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
JP2009532464A (ja) | 2006-04-05 | 2009-09-10 | アストラゼネカ・アクチエボラーグ | 2−アミノピリミジン−4−オン及びAβ−関連の病理を治療又は予防するためのその使用 |
AR061264A1 (es) * | 2006-06-12 | 2008-08-13 | Schering Corp | Inhibidores de aspartil-proteasas derivados de pirimidina, composiciones farmaceuticas que los contienen y usos para tratar enfermedades cognitivas o neurodegenerativas, y como inhibidores del virus vih. |
TW200815447A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
TW200808796A (en) * | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
US20080051420A1 (en) * | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
TW200815443A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
TW200815349A (en) * | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
TW200817406A (en) | 2006-08-17 | 2008-04-16 | Wyeth Corp | Imidazole amines as inhibitors of β-secretase |
WO2008063114A1 (en) | 2006-11-20 | 2008-05-29 | Astrazeneca Ab | Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia |
EP2061771A1 (en) | 2006-12-12 | 2009-05-27 | Schering Corporation | Aspartyl protease inhibitors containing a tricyclic ring system |
US8093254B2 (en) | 2006-12-12 | 2012-01-10 | Schering Corporation | Aspartyl protease inhibitors |
TW200831484A (en) * | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
TW200902499A (en) * | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
UY31083A1 (es) * | 2007-05-15 | 2009-01-05 | Astrazeneca Ab | Derivados de sulfoximinas para la inhibicion de b-secretasa |
WO2009005470A1 (en) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
WO2009005471A1 (en) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
US8222264B2 (en) | 2007-07-06 | 2012-07-17 | Boehringer Ingelheim International Gmbh | Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture |
RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
JP2011510030A (ja) | 2008-01-22 | 2011-03-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換アミノ−ベンゾイミダゾール類、該化合物を含む医薬、これらの使用及びこれらの製造方法 |
BRPI0906625A2 (pt) | 2008-01-28 | 2015-07-14 | Janssen Pharmaceutica Nv | Derivados de tio-2-amino-quinolina-6-substituída úteis como inibidores da beta-secretase (bace) |
AU2009209147B2 (en) | 2008-01-29 | 2013-03-14 | Janssen Pharmaceutica Nv | 2-amino-quinoline derivatives useful as inhibitors of beta-secretase (BACE) |
BRPI0907563A2 (pt) * | 2008-02-18 | 2015-08-04 | Hoffmann La Roche | Derivados de 4,5-di-hidro-xazol-2-il amina |
JP2011514342A (ja) | 2008-02-28 | 2011-05-06 | メルク・シャープ・エンド・ドーム・コーポレイション | アルツハイマー病治療用2−アミノイミダゾールベータ−セクレターゼ阻害剤 |
JP2011518225A (ja) | 2008-04-22 | 2011-06-23 | シェーリング コーポレイション | Bace−1阻害剤としてのフェニル置換2−イミノ−3−メチルピロロピリミジノン化合物、組成物、およびそれらの使用 |
TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
KR20130018370A (ko) | 2008-06-13 | 2013-02-20 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
AU2009277485B2 (en) | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
WO2010013302A1 (ja) | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
EP2332943B1 (en) | 2008-09-30 | 2015-04-22 | Eisai R&D Management Co., Ltd. | Novel fused aminodihydrothiazine derivative |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
US20100125087A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
WO2010056194A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use |
EP2376083A4 (en) | 2008-11-20 | 2012-06-20 | Purdue Research Foundation | CHINAZOLIN INHIBITORS OF BACE 1 AND METHOD OF USE |
-
2006
- 2006-06-12 ES ES11157371.3T patent/ES2436795T3/es active Active
- 2006-06-12 WO PCT/US2006/022919 patent/WO2006138265A2/en active Application Filing
- 2006-06-12 JP JP2008516998A patent/JP4896972B2/ja not_active Expired - Fee Related
- 2006-06-12 EP EP06784808A patent/EP1896032B1/en active Active
- 2006-06-12 KR KR1020077029569A patent/KR20080028881A/ko not_active Application Discontinuation
- 2006-06-12 CA CA002610828A patent/CA2610828A1/en not_active Abandoned
- 2006-06-12 EP EP11157371.3A patent/EP2345411B1/en active Active
- 2006-06-12 BR BRPI0612545-0A patent/BRPI0612545A2/pt not_active IP Right Cessation
- 2006-06-12 RU RU2008100164/04A patent/RU2008100164A/ru not_active Application Discontinuation
- 2006-06-12 AR ARP060102462A patent/AR056865A1/es not_active Application Discontinuation
- 2006-06-12 AU AU2006259573A patent/AU2006259573A1/en not_active Abandoned
- 2006-06-12 US US11/451,065 patent/US8722708B2/en active Active
- 2006-06-12 MX MX2007016183A patent/MX2007016183A/es active IP Right Grant
- 2006-06-12 CN CNA2006800209186A patent/CN101394852A/zh active Pending
- 2006-06-13 TW TW095120997A patent/TW200716643A/zh unknown
- 2006-06-13 PE PE2006000660A patent/PE20070321A1/es not_active Application Discontinuation
-
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
-
2008
- 2008-01-11 NO NO20080186A patent/NO20080186L/no not_active Application Discontinuation
-
2011
- 2011-07-11 JP JP2011153202A patent/JP5454956B2/ja not_active Expired - Fee Related
-
2014
- 2014-03-26 US US14/226,338 patent/US9382242B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
RU2008100164A (ru) | 2009-07-20 |
PE20070321A1 (es) | 2007-04-16 |
TW200716643A (en) | 2007-05-01 |
EP2345411B1 (en) | 2013-10-02 |
WO2006138265A3 (en) | 2007-03-01 |
ES2436795T3 (es) | 2014-01-07 |
EP2345411A1 (en) | 2011-07-20 |
WO2006138265A2 (en) | 2006-12-28 |
CN101394852A (zh) | 2009-03-25 |
KR20080028881A (ko) | 2008-04-02 |
US8722708B2 (en) | 2014-05-13 |
JP4896972B2 (ja) | 2012-03-14 |
JP2011251978A (ja) | 2011-12-15 |
NO20080186L (no) | 2008-03-14 |
EP1896032A2 (en) | 2008-03-12 |
ZA200710385B (en) | 2008-11-26 |
MX2007016183A (es) | 2008-03-10 |
JP2008546696A (ja) | 2008-12-25 |
AU2006259573A1 (en) | 2006-12-28 |
US9382242B2 (en) | 2016-07-05 |
BRPI0612545A2 (pt) | 2010-11-23 |
US20140206715A1 (en) | 2014-07-24 |
EP1896032B1 (en) | 2012-10-31 |
IL187455A0 (en) | 2008-02-09 |
JP5454956B2 (ja) | 2014-03-26 |
ECSP078004A (es) | 2008-01-23 |
US20080176868A1 (en) | 2008-07-24 |
CA2610828A1 (en) | 2006-12-28 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR056865A1 (es) | Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas | |
AR054618A1 (es) | Compuestos de azetidina y su uso como inhibidores de proteasas | |
AR054510A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas y composiciones farmaceuticas que los comprenden. | |
AR054620A1 (es) | Inhibidores de aspartil proteasas | |
AR056211A1 (es) | Derivados de [1,4,6]oxadiazepinas, composiciones farmaceuticas que los contienen en combinacion con otros agentes terapeuticos y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de aspartil-proteasas | |
AR054619A1 (es) | Inhibidores de aspartil proteasas | |
AR061264A1 (es) | Inhibidores de aspartil-proteasas derivados de pirimidina, composiciones farmaceuticas que los contienen y usos para tratar enfermedades cognitivas o neurodegenerativas, y como inhibidores del virus vih. | |
AR057983A1 (es) | Inhibidores hterociclicos de aspartil proteasas | |
AR065421A1 (es) | Inhibidores heterociclicos de la aspartil proteasa | |
AR064287A1 (es) | Inhibidores de aspartil protesa | |
AR062640A1 (es) | Compuestos de azolcarboxamidas y composiciones herbicidas | |
NO20065830L (no) | Substituerte 2-kinolyloksazoler som er anvendbare som PDE4-inhibitorer. | |
AR066459A1 (es) | Derivados de oxadiazol como moduladores de gamma-secretasa. composiciones farmaceuticas | |
CO6251251A2 (es) | Derivados de pirazinona y su uso en el tratamiento de enfermedades pulmonares | |
AR054617A1 (es) | Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden | |
ES2655028T3 (es) | Proceso para la síntesis de inhibidores de enzima de activación de E1 | |
CO6140059A2 (es) | Derivados de imidazol-pirimidina para el tratamiento de enfermedades relacionadas con la glicogeno sintasa quinasa (gsk3) | |
RS52883B (en) | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS | |
AR056863A1 (es) | Compuestos sulfoximino-macrociclicos y sus sales, composiciones farmaceuticas, metodos de preparacion y usos de los mismos | |
MY153045A (en) | Oxopyrazine derivative and herbicide | |
CO5580746A2 (es) | Derivados de fenil-piperazina como inhibidores de la reabsorcion de la serotonina | |
PE20070318A1 (es) | Metodo para purificar tigeciclina | |
WO2006004880A3 (en) | Substituted n-arylsulfonylheterocyclic amines as gamma-secretase inhibitors | |
DE602007002176D1 (de) | Mikropartikel, umfassend ein vernetztes polymer | |
AR046775A1 (es) | Procedimiento para preparar derivados de piridina, y compuestos intermediarios utiles en dicho proceso |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Abandonment or withdrawal |