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AR082508A1 - Derivados de bencimidazoles utiles como inhibidores de prostaglandina esintasa-1 microsomica - Google Patents

Derivados de bencimidazoles utiles como inhibidores de prostaglandina esintasa-1 microsomica

Info

Publication number
AR082508A1
AR082508A1 ARP110103037A ARP110103037A AR082508A1 AR 082508 A1 AR082508 A1 AR 082508A1 AR P110103037 A ARP110103037 A AR P110103037A AR P110103037 A ARP110103037 A AR P110103037A AR 082508 A1 AR082508 A1 AR 082508A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
groups
cycloalkyl
fluorine atoms
Prior art date
Application number
ARP110103037A
Other languages
English (en)
Inventor
Henri Doods
Raimund Kuelzer
Roland Pfau
Dirk Stenkamp
Benjamin Pelcman
Robert Roenn
Henning Priepke
Original Assignee
Boehringer Ingelheim Int
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Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43332838&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR082508(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR082508A1 publication Critical patent/AR082508A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/29—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/43—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C211/44—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring
    • C07C211/52—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/36—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/62—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/20—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C331/00—Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/16—Isothiocyanates
    • C07C331/28—Isothiocyanates having isothiocyanate groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/82—Nitrogen atoms
    • 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
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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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    • C07—ORGANIC CHEMISTRY
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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
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  • Physical Education & Sports Medicine (AREA)
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Abstract

Usos como inhibidores de la prostaglandina E2 sintasa-1 microsómica (mPGES-1), composiciones farmacéuticas que los contienen, y sus usos como medicamentos para el tratamiento y/o prevención de enfermedades inflamatorias y condiciones asociadas. Intermediarios.Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1) en la que R1 y R2 representan independientemente halo, -alquilo C1-3, y este último grupo alquilo está opcionalmente sustituido con uno o más átomos de flúor; W representa -C(O)-, -C(O)O-, y estos grupos están unidos al nitrógeno del resto -NH- por medio del átomo de carbono; M representa -alquilo C1-6, -cicloalquilo C3-7, y ambos grupos están opcionalmente sustituidos con uno o más grupos seleccionados de -F, -OH, -CN, -NH2, -NH(alquilo C1-2), -N(alquil C1-2)2, -O-alquilo C1-3, -alquilo C1-5, -cicloalquilo C3-4, en cuyos tres últimos grupos los grupos alquilo o cicloalquilo están opcionalmente sustituidos con uno o más átomos de flúor; u oxetanilo-, tetrahidrofuranilo-, tetrahidropiranilo-, azetidinilo-, pirrolidinilo-, piperidinilo-, y todos estos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, -alquilo C1-3 y este último grupo alquilo está opcionalmente sustituido con uno o más átomos de flúor; o fenilo-, piridilo-, tienilo-, pirrolilo-, pirazolilo-, imidazolilo-, tiazolilo-, oxazolilo-, o isoxazolilo-, y todos estos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, -CN o -alquilo C1-3, y este último grupo alquilo está opcionalmente sustituido además con uno o más átomos de flúor; R8 representa -H, halógeno, -alquilo C1-3, y este último grupo alquilo está opcionalmente sustituido con uno o más átomos de flúor; R6 representa -H, -alquilo C1-5, -cicloalquil C3-5-alquilo C0-2, en cuyos tres últimos grupos los fragmentos alquilo o cicloalquilo están opcionalmente sustituidos con uno o más átomos de flúor; R7 representa halo, alquil C1-5-O-, cicloalquil C3-7-alquil C0-2-O-, (heterocicloalquil de 4 - 7-miembros)-alquil C0-2-O-, en cuyos tres últimos grupos los fragmentos alquilo, cicloalquilo o heterocicloalquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de -F y -O-alquilo C1-3 y este último grupo alquilo está opcionalmente sustituido además con uno o más átomos de flúor; A representa alquilo C1-8-, fenilo-, indanilo-, naftilo-, 1,2,3,4-tetrahidronaftilo-, piridilo-, tienilo-, benzotienilo-, pirrolilo-, indolil-pirazolilo-, indazolilo-, tiazolilo-, benzotiazolilo-, oxazolilo-, benzoxazolilo-, isoxazolilo-, bencisoxazolilo-, fenilalquilo C1-3-, tienil-alquilo C1-3-, piridil-alquilo C1-3-, cicloalquil C3-7-alquilo C0-3-, oxetanil-alquilo C0-3, tetrahidrofuranil-alquilo C0-3, tetrahidropiranil-alquilo C0-3, en cuyos grupos los fragmentos alquilo-, cicloalquilo- y heterocicloalquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de R9a y los fragmentos arilo y heteroarilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de R9b; cada R9a representa independientemente -F, -Cl, -alquilo C1-3 que está opcionalmente sustituido con uno o más sustituyentes seleccionados de -F, -O-alquilo C1-3; cada R9b representa independientemente -halo, -CN; -alquilo C1-3 que está opcionalmente sustituido con uno o más átomos de flúor; o una sal de los mismos.
ARP110103037A 2010-08-20 2011-08-19 Derivados de bencimidazoles utiles como inhibidores de prostaglandina esintasa-1 microsomica AR082508A1 (es)

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Application Number Priority Date Filing Date Title
EP10173501 2010-08-20

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AR082508A1 true AR082508A1 (es) 2012-12-12

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ARP110103037A AR082508A1 (es) 2010-08-20 2011-08-19 Derivados de bencimidazoles utiles como inhibidores de prostaglandina esintasa-1 microsomica

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US (1) US8759537B2 (es)
EP (1) EP2606036B1 (es)
JP (1) JP5650844B2 (es)
KR (1) KR101891494B1 (es)
CN (1) CN103097359B (es)
AP (1) AP2012006641A0 (es)
AR (1) AR082508A1 (es)
AU (1) AU2011290725C1 (es)
CA (1) CA2804575C (es)
CL (1) CL2013000304A1 (es)
CO (1) CO6680683A2 (es)
CY (1) CY1116034T1 (es)
DK (1) DK2606036T3 (es)
EA (1) EA021433B1 (es)
EC (1) ECSP13012499A (es)
ES (1) ES2528751T3 (es)
GE (1) GEP20146197B (es)
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PE (1) PE20131117A1 (es)
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TW (1) TW201302716A (es)
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