CO5300387A1 - Moduladores de ccr5 tratamiento del virus de inmunodeficiencia humana (vih) - Google Patents
Moduladores de ccr5 tratamiento del virus de inmunodeficiencia humana (vih)Info
- Publication number
- CO5300387A1 CO5300387A1 CO99075874A CO99075874A CO5300387A1 CO 5300387 A1 CO5300387 A1 CO 5300387A1 CO 99075874 A CO99075874 A CO 99075874A CO 99075874 A CO99075874 A CO 99075874A CO 5300387 A1 CO5300387 A1 CO 5300387A1
- Authority
- CO
- Colombia
- Prior art keywords
- group
- alkyl
- alkoxy
- substituents
- independently selected
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
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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
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
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- 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
- C07D405/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/08—Bridged systems
Abstract
Un compuesto, de Fórmula (I) que comprende las regiones: [Región a] [Región ß] [Región ?] [Región d] en la que [Región a] se selecciona entre el grupo compuesto por: A. Componentes sustituyentes arilheterocíclicos que comprenden: 1. restos hetero-fenilmetileno de Fórmula parcial (1.0.0.) <EMI FILE="99075874_1" ID="1" IMF=JPEG >En la que: el símbolo " * " indica el punto de unión del resto de Fórmula parcial (1.0.0.) a la Región ß, como se define más adelante; R5 es un miembro seleccionado entre el grupo compuesto por un enlace directo; -O-, -C(=O)-, -NR4- y -S (=O)p-; en el que:R4 es hidrógeno o alquilo (C1-C2); R6 es un miembro seleccionado entre el grupo compuesto por hidrógeno; alquilo (C1-C2); alcoxi (C1-C2); -CH; -OH;y -C(=O)NH2;- - - j es un número entero seleccionado entre 0, 1 y 2;- - - m es un número entero seleccionado entre 0, 1 y 2; - - - cada uno de R7 y R8 es un miembro seleccionado entre el grupo compuesto por -F; -Cl; -C02R4; -OH; -CN; -CONR4aR4b; -NR4aR4b -; -NR4aC(=O)R4b; -NR4aC(=O)OR4b; -NR4aS(=O)pR4b; -S(=O)PNR4aR4b; alquilo (C1-C4) y alcoxi (C1-C4) en los que cada uno de dichos alquilo y alcoxi está sustituido con 0 a 3 sustituyentes seleccionados independientemente entre F y Cl; alcoxicarbonilo (C1-C2); alquilcarbonilo (C1-C2); y alquilcarboniloxi (C1-C2); en los que: - 2 -- - - - p es un número entero seleccionado entre 0, 1 y 2; - - - - cada uno de R4a y R4b se selecciona independientemente entre hidrógeno y alquilo (C1-C2); - - - el resto representado por la Fórmula parcial (1. 0.1):<EMI FILE="99075874_2" ID="2" IMF=JPEG >en la Fórmula parcial (1.0.0) representa un grupo heterocíclico monocíclico, o un sistema de anillo bicíclico benzo-condensado que contiene dicho grupo heterocíclico, en el que dicho grupo heterocíclico contiene un total de 5 ó 6 miembros de los cuales uno o dos de dichos miembros es nitrógeno, estando representada la presencia del segundo átomo de nitrógeno opcional por: "(N]"; en el que dicho grupo heterocíclico o sistema de anillo se selecciona entre el grupo compuesto por pirrolilo; pirazolilo; imidazolilo; piridinilo; pirazinilo; pirimidinilo; piridazinilo; piperazinilo; indolilo; indazolinilo; benzoimidazolilo; quinolinilo; iso-quinolinilo; y quinazolinilo; en el que:- - - - R12a es un miembro seleccionado entre el grupo compuesto por hidrógeno; F; Cl; -CO2R4; oxo; -OH; CN; NH2; NH-alquilo (C1-C2); N-dialquilo (C1-C2)2; -CF3; alquilo (C1-C4); alquenilo (C2-C4); alcoxi (C1-C4); cicloalquilo (C3-C7); y fenilo; en el que dicho alquilo, alquenilo, alcoxi, cicloalquilo y fenilo están sustituidos con 0 a 2 sustituyentes R9 en los que:- - - - R9 es un miembro seleccionado independientemente entre el grupo compuesto por F; Cl; -CO2R4; -OH; ciano; -C0NR4aR4b; -NR4aR4b; NR4aC(=O)R4b; -NR4aC(=O)OR4b; -NR4aS(=O)PR4b; -S(=O)pR4aR4b; alquilo (C1-C4) incluyendo dimetilo, y alcoxi (C1-C4), en el que dicho alquilo y alcoxi están sustituidos independientemente con 0 a 3 sustituyentes seleccionados independientemente entre F y Cl; alcoxicarbonilo (C1-C2); alquilcarbonilo (C1-C2); y alquilcarboniloxi (C1-C2); y- R12b está ausente o es un miembro seleccionado entre el grupo compuesto por hidrógeno; alquilo (C1-C4); alquenilo (C2-C4); alcoxi (C1-C2); cicloalquilo (C3-C7); y fenilo; en el que dichos alquilo, alquenilo, alcoxi, cicloalquilo y fenilo están sustituidos con 0 a 2 sustituyentes R9, en el que R9 tiene los mismos significados que anteriormente, con la excepción de que se selecciona independientemente de entre ellos; y restos hetero-fenilmetileno de Fórmula parcial (1.1.0):<EMI FILE="99075874_3" ID="3" IMF=JPEG >- - - en la que: el símbolo "*"; R5; R6; R7; R8; j y m son como se han definido con detalle anteriormente, con la excepción de que todos los sustituyentes mencionados anteriormente se seleccionan independientemente de su selección anterior;- - - el resto representado por la Fórmula parcial (1.1.1): <EMI FILE="99075874_4" ID="4" IMF=JPEG > en la Fórmula parcial (1.1.0) representa: - - - - a. un grupo heterocíclico monocíclico que contiene un total de 5 ó 6 miembros de los cuales uno de dichos miembros es nitrógeno y Q se selecciona entre O y S, en el que S puede estar opcionalmente en la forma sulfonato, -S(=O)2; en el que dicho grupo heterocíclico se selecciona entre el grupo compuesto por oxazolilo; oxazolidinilo; isoxazolilo; tiazolilo; tiazolidinilo; iso-tiazolilo; morfolinilo; y tiomorfolinilo; o - - - - b. un grupo heterocíclico monocíclico que contiene un total de 5 ó 6 miembros de los cuales dos de dichos miembros son nitrógeno y un tercer o cuarto de dichos miembros se selecciona independientemente entre N, O y S, en el que dicho S puede estar opcionalmente en la forma sulfonato, -S(=O)2; - 3 -en el que dicho grupo heterocíclico se selecciona entre el grupo compuesto por triazolilo, triazinilo; tetrazolilo; oxadiazolilo; tiadiazolilo; y- - - - R13a se selecciona entre el grupo compuesto por hidrógeno; F, Cl; -CO2R4; oxo; -OH; -CN; NH2; NH-alquilo (C1-C2); N-dialquilo (C1-C2)2; -CF3; alquilo (C1-C4); alquenilo (C2-C4); alcoxi (C1-C2); cicloalquilo (C3-C7); y fenilo; en el que dichos alquilo, alquenilo, alcoxi, cicloalquilo y fenilo están sustituidos con 0 a 2 sustituyentes R11, en el que: - - - - R11 es un miembro seleccionado entre el grupo compuesto por F; Cl; -CO2R4; -OH; -CN; -CONR4aR4b; -NR4aR4b; -NR4aC(=O)R4b; -NR4aC(=O)OR4b; NR4aS(=O)PR4b; -S(=O)pNR4aR4b; alquilo (C1-C4) incluyendo dimetilo, y alcoxi (C1-C4), en el que cada uno de dichos alquilo y alcoxi está independientemente sustituido con 0 a 3 sustituyentes seleccionados independientemente entre F y Cl; alcoxicarbonilo (C1-C2); alquilcarbonilo (C1-C2); y alquilcarboniloxi (C1-C2); y- - - - R13b es un miembro seleccionado entre el grupo compuesto por hidrógeno; alquilo (C1-C4); alquenilo (C2-C4); alcoxi (C1-C2); cicloalquilo (C3-C7); C(=O)alquilo (C1-C4); S(=O)2alquilo (C1-C4) y fenilo; en el que dichos alquilo, alquenilo, alcoxi, cicloalquilo y fenilo están sustituidos con 0 a 2 sustituyentes R11, donde R11 tiene el mismo significado que anteriormente, con la excepción de que se selecciona independientemente; -B. un resto amido-arilo o heterociclico (sustituido) seleccionado entre el grupo compuesto por - - 1. restos amido-arilo alquil-, y alquenil- y alquinil sustituidos de Fórmula parcial (2.0.0):<EMI FILE="99075874_5" ID="5" IMF=JPEG >- - - en la que: el símbolo " * "; R4 y R6 son como se han definido anteriormente, con la excepción de que todos los sustituyentes mencionados anteriormente se seleccionan independientemente de su selección anterior;- - - A es un miembro seleccionado entre el grupo compuesto por:- - - - 1. el resto de fórmula parcial (2.0.3)<EMI FILE="99075874_6" ID="6" IMF=JPEG >- - - - en la que: los símbolos R7; R8 y m son como se han definido anteriormente, con la excepción de que todos los sustituyentes mencionados anteriormente se seleccionan independientemente de su selección anterior; y el símbolo " * " indica el punto de unión del resto A a las porciones restantes de Fórmula parcial (2.0.0);- - - - 2. el resto de Fórmula parcial (2.0.4)<EMI FILE="99075874_7" ID="7" IMF=JPEG > que representa un grupo heterocíclico monocíclico, seleccionado entre el grupo compuesto por pirrolilo; pirazolilo; imidazolilo; piridinilo; pirazinilo; o pirimidinilo; en la que: los símbolos R12a y R12b son como se han definido anteriormente, con la excepción de que todos los sustituyentes mencionados anteriormente se seleccionan independientemente de su selección anterior; y el símbolo " * " indica el punto de unión del resto A a las otras porciones restantes de Fórmula parcial (2.0.0);- - - - 3. el resto de Fórmula parcial (2.0.5)<EMI FILE="99075874_8" ID="8" IMF=JPEG > - 4 -que representa- - - - - a. un grupo heteroaromático monocíclico que contiene un total de 5 miembros, de los cuales uno de dichos miembros es nitrógeno y Q se selecciona entre O y S, en el que dicho S puede estar opcionalmente en la forma sulfonato, -S(=O)2; seleccionado entre el grupo compuesto por oxazolilo; isoxazolilo; tiazolilo; e iso-tiazolilo; o- - - - - b. un grupo heterocíclico monocíclico que contiene un total de 5 ó 6 miembros, de los cuales dos de dichos miembros son nitrógeno y un tercer o cuarto de dichos miembros se selecciona independientemente entre N, O y S, en el que dicho S puede estar opcionalmente en la forma sulfonato, -S(=O)2; seleccionado entre el grupo compuesto por triazolilo; triazinilo; tetrazolilo; oxadiazolilo; y tiadiazolilo; y- - - - - en el que: R13a, R13b y j son como se han definido anteriormente, con la excepción de que todos los sustituyentes mencionados se seleccionan independientemente de su selección anterior; y el símbolo " * " indica el punto de unión del resto A a las otras porciones restantes de Fórmula parcial (2.0.2); - - - R5a es un miembro seleccionado entre el grupo compuesto por un enlace directo; -C(=0)-; y -S(=O)2-;- - - W1 es (1.) un enlace directo; (2.) en el caso en el que R5a es -C(=O)- o -S(=O)2, W1 es un enlace directo o -alquileno (C1-C3)-, en el que cualquier átomo de carbono sencillo del mismo se sustituye con 0 a 2 sustituyentes R23, en el que R23 es un miembro seleccionado entre el grupo compuesto por -F; -Cl; -CO2R4; -OH; -CN; alcoxi (C1-C4); cicloalquilo (C3-C7); y fenilo; en el que dicho alcoxi, cicloalquilo y fenilo están sustituidos con 0 a 2 sustituyentes R11, en el que dicho R11, es como se ha definido anteriormente, con la excepción de que todos los sustituyentes mencionados anteriormente se seleccionan independientemente de su selección anterior; o (3.) es un miembro seleccionado independientemente entre el grupo compuesto por los restos de Fórmulas parciales (2.0.6) a (2.0.16), inclusive:<EMI FILE="99075874_9" ID="9" IMF=JPEG ><EMI FILE="99075874_10" ID="10" IMF=JPEG >- - - - en las que: el símbolo "->" indica el punto de unión del resto W1 al átomo de nitrógeno en la Fórmula parcial (2.0.0), y el símbolo " * " indica el punto de unión del
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9828420.1A GB9828420D0 (en) | 1998-12-23 | 1998-12-23 | CCR5 antagonists useful as anti-hiv agents |
GBGB9921375.3A GB9921375D0 (en) | 1999-09-10 | 1999-09-10 | CCR5 Modulators |
Publications (1)
Publication Number | Publication Date |
---|---|
CO5300387A1 true CO5300387A1 (es) | 2003-07-31 |
Family
ID=26314899
Family Applications (1)
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CO99075874A CO5300387A1 (es) | 1998-12-23 | 1999-12-02 | Moduladores de ccr5 tratamiento del virus de inmunodeficiencia humana (vih) |
Country Status (48)
Families Citing this family (63)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1013276A1 (en) * | 1998-12-23 | 2000-06-28 | Pfizer Inc. | Aminoazacycloalkanes as CCR5 modulators |
US7217714B1 (en) * | 1998-12-23 | 2007-05-15 | Agouron Pharmaceuticals, Inc. | CCR5 modulators |
US6399619B1 (en) | 1999-04-06 | 2002-06-04 | Merck & Co., Inc. | Pyrrolidine modulators of chemokine receptor activity |
US6248755B1 (en) | 1999-04-06 | 2001-06-19 | Merck & Co., Inc. | Pyrrolidine modulators of chemokine receptor activity |
SE9903544D0 (sv) | 1999-10-01 | 1999-10-01 | Astra Pharma Prod | Novel compounds |
EP1118858A3 (en) * | 2000-01-12 | 2003-07-09 | Pfizer Limited | Assay method |
GB2359078A (en) | 2000-02-11 | 2001-08-15 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
GB2359081A (en) | 2000-02-11 | 2001-08-15 | Astrazeneca Uk Ltd | Pharmaceutically active thiazolopyrimidines |
GB2359551A (en) | 2000-02-23 | 2001-08-29 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
GB0005642D0 (en) * | 2000-03-10 | 2000-05-03 | Astrazeneca Uk Ltd | Chemical compounds |
TR200400541T4 (tr) * | 2000-05-26 | 2004-04-21 | Pfizer Inc. | Terapide faydalı tropan türevleri. |
US6667314B2 (en) * | 2000-05-26 | 2003-12-23 | Pfizer, Inc. | Tropane derivatives useful in therapy |
GB0015562D0 (en) * | 2000-06-23 | 2000-08-16 | Pfizer Ltd | Heterocycles |
US6511994B2 (en) | 2000-10-11 | 2003-01-28 | Merck & Co., Inc. | Modulators of CCR5 chemokine receptor activity |
US6531484B2 (en) | 2000-10-11 | 2003-03-11 | Merck & Co., Inc. | Pyrrolidine modulators of CCR5 chemokine receptor activity |
SE0003828D0 (sv) | 2000-10-20 | 2000-10-20 | Astrazeneca Ab | Novel compounds |
CA2432527A1 (en) * | 2000-12-22 | 2002-07-04 | Takeda Chemical Industries, Ltd. | Medicinal compositions for oral use |
SE0101322D0 (sv) | 2001-04-12 | 2001-04-12 | Astrazeneca Ab | Novel compounds |
SE0103818D0 (sv) * | 2001-11-15 | 2001-11-15 | Astrazeneca Ab | Chemical compounds |
AR041786A1 (es) * | 2002-03-15 | 2005-06-01 | Novartis Ag | Derivados de azetidina como antagonistas del receptor ccr-3, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la elaboracion de un medicamento |
CN1324025C (zh) * | 2002-04-08 | 2007-07-04 | 美国辉瑞有限公司 | 作为ccr5调节剂的托烷衍生物 |
US6855724B2 (en) | 2002-04-08 | 2005-02-15 | Agouron Pharmaceuticals, Inc. | Tropane derivatives useful in therapy |
JP2005533999A (ja) * | 2002-05-23 | 2005-11-10 | ファイザー・インク | 受容体滞留時間を測定するリガンドの同定方法 |
GB0221828D0 (en) | 2002-09-20 | 2002-10-30 | Astrazeneca Ab | Novel compound |
US7202259B2 (en) | 2002-11-18 | 2007-04-10 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
US7759336B2 (en) * | 2002-12-10 | 2010-07-20 | Ono Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic compounds and medicinal use thereof |
CA2509711A1 (en) | 2002-12-13 | 2004-07-01 | Smithkline Beecham Corporation | Piperidine derivatives as ccr5 antagonists |
JP2006514950A (ja) | 2002-12-13 | 2006-05-18 | スミスクライン ビーチャム コーポレーション | Ccr5拮抗薬としてのシクロプロピル化合物 |
AU2004220225B2 (en) | 2003-03-14 | 2010-06-17 | Ono Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient |
JP4710606B2 (ja) | 2003-04-18 | 2011-06-29 | 小野薬品工業株式会社 | スピロピペリジン化合物およびその医薬用途 |
EP1654229B1 (en) * | 2003-07-31 | 2007-05-09 | AstraZeneca AB | Piperidine derivatives as ccr5 receptor modulators |
US7220772B2 (en) | 2003-09-05 | 2007-05-22 | Pfizer, Inc. | Pyrazole derivatives |
CA2579609A1 (en) | 2003-09-10 | 2005-03-17 | Virochem Pharma Inc. | Spirohydantoin compounds and methods for the modulation of chemokine receptor activity |
SI1682545T1 (sl) * | 2003-10-03 | 2008-04-30 | Pfizer | Derivati tropana, substituirani z imidazopiridinom, z antagonisticno aktivnostjo receptorja CCR5 zazdravljenje HIV in vnetja |
GB0328243D0 (en) | 2003-12-05 | 2004-01-07 | Astrazeneca Ab | Methods |
CA2552087C (en) * | 2004-01-30 | 2011-01-25 | Euro-Celtique S.A. | Methods for making 4-tetrazolyl-4-phenylpiperidine compounds |
TW200533348A (en) | 2004-02-18 | 2005-10-16 | Theravance Inc | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
WO2005100322A1 (en) * | 2004-04-14 | 2005-10-27 | Pfizer Limited | Sulphur-linked imidazole compounds for the treament of hiv |
TW200610761A (en) * | 2004-04-23 | 2006-04-01 | Astrazeneca Ab | Chemical compounds |
EP1761542B1 (en) | 2004-06-09 | 2008-01-02 | F.Hoffmann-La Roche Ag | Octahydropyrrolo[3,4-c]pyrrole derivatives an their use as antiviral agents |
PE20090123A1 (es) | 2004-09-13 | 2009-03-10 | Ono Pharmaceutical Co | Un derivado heterociclico conteniendo nitrogeno y un farmaco conteniendo el mismo como el ingrediente activo |
KR20070116867A (ko) * | 2005-04-08 | 2007-12-11 | 뉴로서치 에이/에스 | (+)- 및(-)-8-알킬-3-(트리플루오르알킬설포닐옥시)-8-아자바이사이클(3.2.1)옥트-2-엔 |
CA2603204A1 (en) | 2005-04-14 | 2006-10-19 | F. Hoffmann-La Roche Ag | Aminopyrazole derivatives, their manufacture and use as pharmaceutical agents |
JPWO2006129679A1 (ja) | 2005-05-31 | 2009-01-08 | 小野薬品工業株式会社 | スピロピペリジン化合物およびその医薬用途 |
US7665658B2 (en) | 2005-06-07 | 2010-02-23 | First Data Corporation | Dynamic aggregation of payment transactions |
ES2277745B1 (es) * | 2005-06-14 | 2008-06-01 | Laboratorios Almirall S.A. | Derivados n-amida de 8-azabiciclo /3.2.1/oct-3-ilo como antagonistas de ccr1. |
WO2007049771A1 (ja) | 2005-10-28 | 2007-05-03 | Ono Pharmaceutical Co., Ltd. | 塩基性基を含有する化合物およびその用途 |
JP5217438B2 (ja) | 2005-11-18 | 2013-06-19 | 小野薬品工業株式会社 | 塩基性基を含有する化合物およびその用途 |
BRPI0708731A2 (pt) | 2006-03-10 | 2011-06-07 | Ono Pharmaceutical Co | derivado heterocìclico nitrogenado, e agente farmacêutico compreendendo o derivado como ingrediente ativo |
US20080015835A1 (en) * | 2006-07-13 | 2008-01-17 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Methods and systems for treating disease |
US20090082344A1 (en) * | 2006-07-13 | 2009-03-26 | Searete Llc | Methods and systems for treating disease |
US20080015833A1 (en) * | 2006-07-13 | 2008-01-17 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Methods and systems for molecular inhibition of protein misfolding |
US20080015787A1 (en) * | 2006-07-13 | 2008-01-17 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Methods and systems for treating disease |
WO2008016006A1 (en) | 2006-07-31 | 2008-02-07 | Ono Pharmaceutical Co., Ltd. | Compound having cyclic group bound thereto through spiro binding and use thereof |
US20080146605A1 (en) * | 2006-12-19 | 2008-06-19 | Auspex Pharmaceuticals, Inc. | Preparation and utility of ccr5 inhibitors |
RU2488585C2 (ru) | 2007-08-31 | 2013-07-27 | Пэдью Фарма Л.П. | Замещенные пиперидиновые соединения хиноксалинового типа и их применение |
WO2010129351A1 (en) | 2009-04-28 | 2010-11-11 | Schepens Eye Research Institute | Method to identify and treat age-related macular degeneration |
WO2011011652A1 (en) | 2009-07-24 | 2011-01-27 | Glaxosmithkline Llc | Therapeutic compounds |
BR112012024522A2 (pt) | 2010-04-02 | 2017-08-08 | Phivco 1 Llc | combinação, uso de uma combinação, composição farmacêutica, forma de dosagem única , kit, e, método para tratar um distúrbio |
CN104169425A (zh) | 2011-03-09 | 2014-11-26 | 理查德·G·佩斯泰尔 | ***癌细胞系、遗传标志及其用途 |
US20140271680A1 (en) | 2011-08-12 | 2014-09-18 | Universite Paris-Est Creteil Val De Marne | Methods and pharmaceutical compositions for treatment of pulmonary hypertension |
US9453836B2 (en) | 2012-05-14 | 2016-09-27 | Richard G. Pestell | Use of modulators of CCR5 in the treatment of cancer and cancer metastasis |
US9090618B2 (en) * | 2012-12-27 | 2015-07-28 | Purdue Pharma L.P. | Substituted benzimidazole-type piperidine compounds and uses thereof |
Family Cites Families (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9125900D0 (en) | 1991-12-05 | 1992-02-05 | Wyeth John & Brother Ltd | Piperazine derivatives |
PH30413A (en) | 1992-03-26 | 1997-05-09 | Boehringer Ingelheim Italia | Crystalline forms of endo-2,3-dihydro-n-(8-methyl)-8-azabicyclo-(3,2,1)oct-3-yl)-2-oxo-1h-benzimidazole-1-carboxamides |
GB9310713D0 (en) * | 1993-05-24 | 1993-07-07 | Zeneca Ltd | Aryl substituted heterocycles |
FR2728166A1 (fr) | 1994-12-19 | 1996-06-21 | Oreal | Composition topique contenant un antagoniste de substance p |
SK1296A3 (en) * | 1995-01-04 | 1996-08-07 | Bayer Ag | Acyled pseudopeptides with trifluoromethyl-substituted 2-azabicyklooctane, manufacturing process thereof and medicaments containing these substances |
GB9502644D0 (en) * | 1995-02-10 | 1995-03-29 | Zeneca Ltd | Heterocyclic derivatives |
GB9523526D0 (en) * | 1995-11-17 | 1996-01-17 | Zeneca Ltd | Therapeutic compounds |
WO1997024325A1 (en) * | 1995-12-28 | 1997-07-10 | Takeda Chemical Industries, Ltd. | DIPHENYLMETHANE DERIVATIVES AS MIP-1α/RANTES RECEPTOR ANTAGONISTS |
CN1168719C (zh) * | 1996-03-29 | 2004-09-29 | 辉瑞大药厂 | 6-苯基吡啶-2-基胺衍生物以及药物组合物和用途 |
JP2000516210A (ja) * | 1996-07-12 | 2000-12-05 | ロイコサイト,インコーポレーテッド | ケモカインレセプターアンタゴニストとその使用方法 |
US6323206B1 (en) * | 1996-07-12 | 2001-11-27 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
WO1998004554A1 (fr) * | 1996-07-29 | 1998-02-05 | Banyu Pharmaceutical Co., Ltd. | Antagonistes de recepteurs de chemokines |
AU5522498A (en) | 1996-12-13 | 1998-07-03 | Merck & Co., Inc. | Substituted aryl piperazines as modulators of chemokine receptor activity |
WO1998025604A1 (en) | 1996-12-13 | 1998-06-18 | Merck & Co., Inc. | Spiro-substituted azacycles as modulators of chemokine receptor activity |
AU5803398A (en) | 1996-12-13 | 1998-07-03 | Merck & Co., Inc. | Spiro-substituted azacycles as modulators of chemokine receptor activity |
JP2001508798A (ja) | 1997-01-21 | 2001-07-03 | メルク エンド カンパニー インコーポレーテッド | ケモカインレセプター活性のモジュレーターとしての3,3−二置換ピペリジン類 |
CA2296314A1 (en) | 1997-07-25 | 1999-02-04 | Merck & Co., Inc. | Cyclic amine modulators of chemokine receptor activity |
IL125658A0 (en) * | 1997-08-18 | 1999-04-11 | Hoffmann La Roche | Ccr-3 receptor antagonists |
JP2001526178A (ja) | 1997-08-28 | 2001-12-18 | メルク エンド カムパニー インコーポレーテッド | ピロリジン系およびピペリジン系ケモカイン受容体活性調節剤 |
AR013669A1 (es) * | 1997-10-07 | 2001-01-10 | Smithkline Beecham Corp | Compuestos y metodos |
EP1047675A1 (en) * | 1998-01-21 | 2000-11-02 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
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