AR073920A1 - Derivados urea de nortropanos sustituidos, medicamentos que contienen dichos compuestos , su uso en el tratamiento de enfermedades mediadas por la inhibicion de la enzima 11beta-hidroxiesteroide deshidrogenasa y proceso para su preparacion. - Google Patents
Derivados urea de nortropanos sustituidos, medicamentos que contienen dichos compuestos , su uso en el tratamiento de enfermedades mediadas por la inhibicion de la enzima 11beta-hidroxiesteroide deshidrogenasa y proceso para su preparacion.Info
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- AR073920A1 AR073920A1 ARP090104073A ARP090104073A AR073920A1 AR 073920 A1 AR073920 A1 AR 073920A1 AR P090104073 A ARP090104073 A AR P090104073A AR P090104073 A ARP090104073 A AR P090104073A AR 073920 A1 AR073920 A1 AR 073920A1
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- Prior art keywords
- alkyl
- piperazin
- het
- oxo
- aryl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title abstract 3
- 230000005764 inhibitory process Effects 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical class NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- -1 cyano, carboxy Chemical group 0.000 abstract 48
- 125000003118 aryl group Chemical group 0.000 abstract 15
- 125000003545 alkoxy group Chemical group 0.000 abstract 10
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 abstract 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 6
- 125000006563 (C1-3) alkylaminocarbonyl group Chemical group 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 125000003830 C1- C4 alkylcarbonylamino group Chemical group 0.000 abstract 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 5
- 125000006576 di-(C1-C3-alkyl)-aminocarbonyl group Chemical group 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 4
- 125000004104 aryloxy group Chemical group 0.000 abstract 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 4
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 abstract 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 4
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 abstract 3
- 125000006595 (C1-C3) alkylsulfinyl group Chemical group 0.000 abstract 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000004658 aryl carbonyl amino group Chemical group 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 229910052731 fluorine Inorganic materials 0.000 abstract 3
- 239000011737 fluorine Substances 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 3
- VFKHECGAEJNAMV-HETMPLHPSA-N (1s,2r,3s,4r)-4-(6-aminopurin-9-yl)cyclopentane-1,2,3-triol Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1C[C@H](O)[C@@H](O)[C@H]1O VFKHECGAEJNAMV-HETMPLHPSA-N 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 abstract 2
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 abstract 2
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000005100 aryl amino carbonyl group Chemical group 0.000 abstract 2
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract 2
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 abstract 2
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 abstract 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 abstract 2
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 2
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000002541 furyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000001041 indolyl group Chemical group 0.000 abstract 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical group C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 abstract 1
- 102000004277 11-beta-hydroxysteroid dehydrogenases Human genes 0.000 abstract 1
- 108090000874 11-beta-hydroxysteroid dehydrogenases Proteins 0.000 abstract 1
- DGGKXQQCVPAUEA-UHFFFAOYSA-N 8-azabicyclo[3.2.1]octane Chemical group C1CCC2CCC1N2 DGGKXQQCVPAUEA-UHFFFAOYSA-N 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 abstract 1
- 125000006598 aminocarbonylamino group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 1
- QWPPOHNGKGFGJK-UHFFFAOYSA-N hypochlorous acid Chemical group ClO QWPPOHNGKGFGJK-UHFFFAOYSA-N 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Particularmente, los compuestos son inhibidores de la 11b-hidroxiesteroide deshidrogenasa (HSD) 1 y por lo tanto son adecuados para el tratamiento y la prevencion de enfermedades que pueden estar influenciadas por la inhibicion de esta enzima, tales como enfermedades metabolicas, en particular diabetes tipo 2, obesidad y dislipidemia. Se provee además, un proceso para la obtencion del mismo. Reivindicacion 1: Compuestos caracterizados porque tienen la formula (1) en la que R1 representa arilo o heteroarilo, mientras que por arilo se entiende fenilo o naftilo, y heteroarilo representa pirrolilo, furanilo, tienilo, piridinilo, indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo, o pirrolilo, imidazolilo, furanilo, tienilo, piridinilo en cada uno de Io cuales uno o dos grupos CH están reemplazados por N, o indolilo, benzofuranilo, benzotiofenilo, quinolinilo o isoquinolinilo donde, en cada uno de ellos de 1 a 3 grupos CH son reemplazados por N, mientras que en el N anteriormente mencionado, incluyendo los grupos heteroarilo, uno o dos grupos -N=CH- son opcionalmente reemplazados por -NH-CO- y/o -N(alquil C1-4)-CO-, y mientras que los grupos heteroarilo y arilo policíclico anteriormente mencionados opcionalmente están parcialmente saturados, aunque retienen una subestructura aromática o heteroaromática unida al grupo carbonilo en la formula (1), en la que en los anillos parcialmente saturados uno o dos grupos CH opcionalmente están reemplazados, independientemente entre si, por O, S, NH, N(alquil C1-4), carbonilo o sulfonilo, donde los grupos arilo, heteroarilo, arilo y heteroarilo parcialmente saturados antes mencionados están opcionalmente sustituidos con uno o más, preferiblemente uno a cuatro sustituyentes R2, donde todos los grupos heteroarilo están unidos a la estructura de nortropano de formula (1) mediante un átomo de carbono; RN, independientemente entre sí, representan hidrogeno, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, cicloalquilo C3-6, (het)arilo, alquilcarbonilo C1-4, alquiloxicarbonilo C1-4, alquilsulfonilo C1-4, (het)arilcarbonilo, (het)arilsulfonilo, donde cada grupo alquilo, alquenilo y alquinilo opcionalmente está además mono o polisustituido con fluor, y está opcionalmente monosustituido con hidroxi, alcoxi C1-4, alquilsulfanilo C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, amino, alquilamino C1-4, di-(alquil C1-4)amino, alquilcarbonilamino C1-4, ciano, carboxi, alcoxicarbonilo C1-4, aminocarbonilo, alquilaminocarbonilo C1-4, di-(alquil C1-4)aminocarbonilo o (het)arilo; R2, independientemente entre sí, representan halogeno, nitro, ciano, hidroxi, cicloalquilo C3-6, cicloalquiloxi C3-6, tetrahidrofuran-3-iloxi, tetrahidropiran-3-iIoxi, tetrahidropiran-4-iloxi, tetrahidrofuranil-alquiloxi C1-3, tetrahidropiranil-alquiloxi C1-3, (het)arilo, (het)ariloxi, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquiloxi C1-6, alquilamino C1-6, donde en cada grupo un grupo CH2 está opcionalmente reemplazado por carbonilo o sulfonilo, y donde cada grupo está opcionalmente mono o polifluorado, y donde cada grupo está opcionalmente sustituido adicionalmente con hidroxi, cloro, alquiloxi C1-3, amino, alquilamino C1-3, di-(alquil C1-3)-amino, pirrolidin-1-ilo, 2-oxo-pirrolidin-1-ilo, piperidin-1-ilo, 2-oxo-piperidin-1-ilo, morfolin-4-ilo, 3-oxo-morfolin-4-ilo, piperazin-1-ilo, 2-oxo-piperazin-1-ilo, 3-oxo-piperazin-1-ilo, 4-(alquil C1-3)-piperazin-1-ilo, 2-oxo-4-(alquil C1-3)-piperazin-1-ilo, 3-oxo-4-(alquil C1-3)-piperazin-1-ilo, carboxi, alquiloxicarbonilo C1-3,, ciano, aminocarbonilo, alquilaminocarbonilo C1-3, di-(alquil C1-3)-aminocarbonilo, pirrolidin-1-ilcarbonilo, piperidin-1-ilcarbonilo, morfolin-4-ilcarbonilo, piperazin-1-il-carbonilo, 4-(alquil C1-3)-piperazin-1-il-carbonilo, alquil C1-4-carbonilamino, N-(alquil C1-3)-alquilcarbonilamino C1-4, arilcarbonilamino, alquilsulfanilo C1-3, alquilsulfinilo C1-3, alquilsulfonilo C1-3, cicloalquilo C3-6, tetrahidrofuranilo, tetrahidropiranilo, (het)arilo o (het)ariloxi, amino, di-(alquil C1-3)amino, pirrolidin-1-ilo, 2-oxo-pirrolidin-1-ilo, piperidin-1-ilo, 2-oxo-piperidin-1-ilo, morfolin-4-ilo, 3-oxo-morfolin-4-ilo, piperazin-1-ilo, 2-oxo-piperazin-1-ilo, 3-oxo-piperazin-1-ilo, 4-(alquil C1-3)-piperazin-1-ilo, 4-(alquilcarbonil C1-4)-piperazin-1-ilo, 4-(cicloalquilcarbonil C3-6)-piperazin-1-ilo, 4-(alquiloxicarbonil C1-4)-piperazin-1-ilo, 4-(alquilsulfonil C1-4)-piperazin-1-ilo, 2-oxo-4(alquil C1-3)-piperazin-1-ilo, 3-oxo-4-(alquil C1-3)-piperazin-1-ilo, (het)arilcarbonibamino, alquiloxicarbonilamino C1-4, aminocarboniIamino, alquil C1-4-aminocarbonilamino (het)arilaminocarbonilamino, di-(alquil C1-3)aminocarbonilamino, pirrolidin-1-ilcarbonilamino, piperidin-1-ilcarbonilamino, morfolin-4-il-carbonilamino, piperazin-1-ilcarbonilamino, 4-(alquil C1-3)-pirerazin-1-ilcarbonilamino, aminosulfonilamino, alquilaminosulfonilamino C1-3, di-(alquil C1-3)amino-sulfonilamino, pirrolidin-1-ilsulfonilamino, piperidin-1-ilsulfonilamino, morfolin-4-ilsulfonilanino, piperazin-1-ilsulfoniIamino, 4-(alquil C1-3)-piperazin-1-ilsulfonilamino, (alquiloxicarbonilamino C1-3)carbonilamino, (het)arilsulfonilamino, N-(alquil C1-3)-alquilcarbonilamino C1-4, N-(alquil C1-3)-(het)arilcarbonilamino, N-(alquil C1-3)-(het)aril-alquilcarbonilamino C1-3, N-(alquil C1-3)-alquiloxicarbonil C1-3amino, N-(aminocarbonilo)-alquilamino C1-3, N-(alquilamino C1-3carbonil)-alquilamino C1-3, N-[di-(alquil C1-3)aminocarbonil]-alquilamino C1-3, N-(alquil C1-3)-alquilsulfonilamino C1-3, N-(alquil C1-3)-(het)arilsulfonilamino, N-(alquil C1-3)-(het)aril-alquilsulfonilamino C1-3, carboxi, alquiloxicarbonilo C1-3, aminocarbonilo, alquilamino C1-3carbonilo, di(alquil C1-3)-aminocarbonilo, azetidin-1-ilcarbonilo, pirrolidin-1-ilcarbonilo, piperidin-1-il-carbonilo, morfoIin-4-ilcarbonilo, piperazin-1-ilcarbonilo, 4-(alquil C1-3)-piperazin-1-il-carbonilo, (het)arilaminocarbonilo, N-(alquil C1-3)-(het)aril-aminocarbonilo, (het)aril-alquilaminocarbonilo C1-3, N-(alquil C1-3)-(het)aril-alquilaminocarbonilo C1-3, (het)arilcarbonilo, alquilsulfanilo C1-3, alquilsulfinilo C1-3, (het)arilsulfonilo, tritluorometilsulfanilo, trifluorometilsulfinilo, aminosulfonilo, alquilaminosulfonilo C1-3, di-(alquil C1-3)-aminosulfonilo, pirrolidin-1-il-sulfonilo, piperidin-1-ilsulfonilo, morfolin-4-ilsulfonilo, piperazin-1-ilsulfonilo, 4-(alquil C1-3)-piperazin-1-ilsulfonilo, en donde todos los anillos heterocicloalquilo y cicloalquilo saturados anteriormente mencionados están opcionalmente sustituidos con uno o dos grupos independientemente seleccionados entre fluor, alquilo C1-3, alcoxi C1-3, alcoxi C1-3-alquilo C1-3 e hidroxi; V es CY5Y6, O o NRN; W está ausente o es CY7Y8 o (CY7Y8)-(CY9Y10); X está ausente o es CY11Y12 o (CY11Y12)-(CY13Y14); V y W pueden también combinarse para formar un grupo cicloalquilo C3-6 que está hibridado vía dos átomos de carbono adyacentes al aza-ciclo y en donde uno o dos grupos CH2 están opcionalmente reemplazados, independientemente entre si por O, S, NRN, carbonilo o sulfonilo y que opcionalmente está parcialmente insaturado y opcionalmente mono- o polisustituido, preferiblemente mono a tetrasustituido, con sustituyentes seleccionados, independientemente entre si, de R3; V y W pueden también combinarse para formar un grupo (het)arilo hibridado mediante dos átomos de carbono adyacentes al aza-ciclo; R3 representa halogeno, alquilo C1-4, ciano, carboxi, alquiloxicarbonilo C1-4, aminocarbonilo, alquilaminocarbonilo C1-3, di-(alquil C1-3)-aminocarbonilo, hidroxi, alcoxi C1-4, amino, alquilamino C1-3, di-(alquil C1-3)-amino, alquilcarbonilamino C1-4, N-alquil C1-3-alquil C1-4-carbonilamino y (het)arilo, donde cada grupo alquilo anteriormente mencionado está opcionalmente mono o poli sustituido con fluor, y opcionalmente monosustituido con hidroxi, alcoxi C1-4, alquilsulfanilo C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, amino, alquilamino C1-3, di-(alquil C1-3)amino, alquilcarbonilamino C1-4, ciano, carboxi, alcoxi C1-4-carbonilo, aminocarbonilo, alquilaminocarbonilo C1-4, di-(alquil C1-4)-aminocarbonilo o (het)arilo; Y1 a Y14, que pueden ser idénticos y/o diferentes, independientemente entre si, representan hidrogeno, halogeno, nitro, ciano, hidroxi, cicloalquilo C3-6, cicloalquiloxi C3-6, tetrahidrofuran-3-iloxi, tetrahidropiran-3-iloxi, tetrahidropiran-4-iloxi, tetrahidrofuranil-alquiloxi C1-3, tetrahidropiranil-alquiloxi C1-3, (het)arilo, (het)ariloxi, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquiloxi C1-6, alquilamino C1-6, donde en cada grupo, un grupo CH2 está opcionalmente reemplazado por carbonilo o sulfonilo, y donde cada grupo está opcionalmente mono o polifluorado, y donde cada grupo está opcionalmente sustituido adicionalmente con hidroxi, cloro, alquiloxi C1-3, amino, alquil C1-3-amino, di-(alquil C1-3)-amino, pirrolidin-1-ilo, 2-oxo-pirrolidin-1-ilo, piperidin-1-ilo, 2-oxo-piperidin-1-ilo, morfolin-4-ilo, 3-oxo-morfolin-4-ilo, piperazin-1-ilo, 2-oxo-piperazin-1-ilo, 3-oxo-piperazin-1-ilo, 4-(alquil C1-3)-piperazin-1-ilo, 2-oxo-4-(alquil C1-3)-piperazin-1-ilo, 3-oxo-4-(alquil C1-3)-piperazin-1-ilo, carboxi, alquiloxi C1-3-carbonilo, ciano, aminocarbonilo, alquilaminocarbonilo C1-3, di-(alquil C1-3)-aminocarbonilo, pirrolidin-1-ilcarbonilo, piperidin-1-ilcarbonilo, morfolin-4-ilcarbonilo, piperazin-1-ilcarbonilo, 4-(alquil C1-3)-piperazin-1-ilcarbonilo, alquilcarbonil C1-3-amino, (het)arilcarbonilamino, alquilsulfanilo C1-3, alquilsulfinilo C1-3, alquil C1-3-sulfonilo, cicloalquilo C3-6, (het)arilo o (het)ariloxi; amino, di-(alquil C1-3)amino, pirrolidin-1-ilo, 2-oxo-pirrolidin-1-ilo, piperidin-1-ilo, 2-oxo-piperidin-1-ilo, morfolin-4-ilo, 3-oxo-morfolin-4-ilo, piperazin-1-ilo, 2-oxo-piperazin-1-ilo, 3-oxo-piperazin-1-ilo, 4-(alquil C1-3)-piperazin-1-ilo, 4-(alquilcarbonil C1-4)-piperazin-1-ilo, 4-(cicloalquilcarbonil C3-6)-piperazin-1-ilo, 4-(alquiloxicarbonil C1-4)-piperazin-1-ilo, 4-(alquilsulfonil C1-4)-piperazin-1-ilo, 2-oxo-4-(alquil C1-3)-piperazin-1-
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| TW200811170A (en) | 2006-06-27 | 2008-03-01 | Sanofi Aventis | Urea derivatives of tropane, their preparation and their therapeutic application |
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| CL2009001151A1 (es) | 2008-05-13 | 2010-08-13 | Boehringer Ingelheim Int | Compuestos derivados de acidos carbociclicos aliciclicos de benzomorfanos, procedimiento de preparacion, composicion farmaceutica, utiles para tratar enfermedades influenciadas por la inhibicion de la enzima 11beta-hidroxiesteroide deshidrogenasa, como trastornos metabolicos. |
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| EP2318355B1 (en) | 2008-07-25 | 2018-09-12 | Boehringer Ingelheim International GmbH | 1,1'-diadamantyl carboxylic acids, medicaments containing such compounds and their use |
| EP2318403B1 (en) | 2008-08-25 | 2015-12-23 | Boehringer Ingelheim International GmbH | Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| TW201022266A (en) | 2008-10-23 | 2010-06-16 | Boehringer Ingelheim Int | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| EP2438049B1 (en) | 2009-06-02 | 2014-05-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| TWI531571B (zh) | 2009-11-06 | 2016-05-01 | 維它藥物公司 | 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜芳基羰基衍生物 |
-
2009
- 2009-10-22 TW TW098135826A patent/TW201022266A/zh unknown
- 2009-10-22 JP JP2011532637A patent/JP5544366B2/ja active Active
- 2009-10-22 WO PCT/EP2009/063913 patent/WO2010046445A2/en not_active Ceased
- 2009-10-22 EP EP09740684.7A patent/EP2350068B1/en active Active
- 2009-10-22 CA CA2738453A patent/CA2738453C/en active Active
- 2009-10-22 AR ARP090104073A patent/AR073920A1/es unknown
- 2009-10-22 US US13/124,259 patent/US8829027B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP2350068B1 (en) | 2017-08-30 |
| CA2738453A1 (en) | 2010-04-29 |
| US20110275595A1 (en) | 2011-11-10 |
| TW201022266A (en) | 2010-06-16 |
| CA2738453C (en) | 2017-07-04 |
| US8829027B2 (en) | 2014-09-09 |
| JP2012506405A (ja) | 2012-03-15 |
| WO2010046445A3 (en) | 2010-07-01 |
| EP2350068A2 (en) | 2011-08-03 |
| JP5544366B2 (ja) | 2014-07-09 |
| WO2010046445A2 (en) | 2010-04-29 |
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