Tricyclic compounds for use in the treatment and/or control of obesityThe invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Compound, is selected from:(1ar, 7bs)-5-[2-(2-diethylamino methylcyclopropyl groups) the fluoro-phenylsulfonamido of-4-]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid, or its enantiomorph;the fluoro-2-of (1ar, 7bs)-5-{4-[2-(pyrrolidin-1-yl methyl) cyclopropyl]-phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-(3-diethylamino-2,2-dimethyl propyl)-4-fluorobenzene sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[the fluoro-2-of 4-((r)-pyrrolidin-3-yl methyl) benzene-sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[the fluoro-2-of 4-((s)-pyrrolidin-3-yl methyl) benzene-sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also [c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5-{4-[(r)-1-(2-hydroxy-2-methyl propyl group)-pyrrolidin-3-yl methyl] phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-(1-azabicyclic [2.2.2] oct-3-yl methyl) the fluoro-phenylsulfonamido of-4-]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-(pungent-3-ylidenylmethyl of (z)-1-azabicyclic [2.2.2])-4-fluorobenzene sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-(pungent-3-ylidenylmethyl of (e)-1-azabicyclic [2.2.2])-4-fluorobenzene sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;(1ar, 7bs)-5-{2-[(e)-(1-ethyl piperidine-3-subunit) methyl]-4-fluorobenzene sulfonamido }-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;(1ar, 7bs)-5-{2-[(z)-(1-ethyl piperidine-3-subunit) methyl]-4-fluorobenzene sulfonamido }-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid, or its enantiomorph;(1ar, 7bs)-5-{2-[2-((s)-1-ethyl pyrrolidine-2-base) ethyl] the fluoro-phenylsulfonamido of-4-}-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5-{4-[(r)-1-(2-hydroxyethyl) pyrrolidin-3-yl methyl] phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene-cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-((inner mold)-8-ethyl-8-azabicyclic [3.2.1] oct-3-yl) methyl-4-fluorobenzene sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-((external form)-8-ethyl-8-azabicyclic [3.2.1] oct-3-yl) methyl-4-fluorobenzene sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also [c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5-{4-[(z)-3-(3-hydroxy-3-methyl pyrrolidin-1-yl) the third-1-thiazolinyl] phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene cyclopropylene also [c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5{4-[(z)-3-(4-hydroxy piperidine-1-base) the third-1-thiazolinyl] phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5-{4-[(z)-3-(4-hydroxy-4-methyl piperidin-1-yl) the third-1-thiazolinyl] phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene-cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-(own-6-base of 3-ethyl-3-azabicyclic [3.1.0]) the fluoro-phenylsulfonamido of-4-]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5-{4-[(z)-2-((s)-pyrrolidin-2-yl) vinyl]-phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene cyclopropylene also-[c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5-{4-[(z)-3-((s)-3-hydroxymethyl-pyrrolidine-1-base) the third-1-thiazolinyl] phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene-cyclopropylene also [c] chromene-4-carboxylic acid;the fluoro-2-of (1ar, 7bs)-5-{4-[(z)-3-((r)-3-hydroxymethyl-pyrrolidine-1-base) the third-1-thiazolinyl] phenylsulfonamido }-1,1a, 2,7b-tetrahydrochysene-cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-(the fluoro-2-{ of 4-(z)-3-[(s)-3-(2-hydroxyl third-2-base) pyrrolidin-1-yl] the third-1-thiazolinyl } phenylsulfonamido)-1,1a, 2,7b-tetrahydrochysene cyclopropylene is [c] chromene-4-carboxylic acid also;(1ar, 7bs)-5-(the fluoro-2-{ of 4-(z)-3-[(r)-3-(2-hydroxyl third-2-base) pyrrolidin-1-yl] the third-1-thiazolinyl } phenylsulfonamido)-1,1a, 2,7b-tetrahydrochysene cyclopropylene is [c] chromene-4-carboxylic acid also;(1ar, 7bs)-5-[the fluoro-2-of 4-(the thick pyrroles's piperazine of six hydrogen-1h--2-ylmethyl) phenylsulfonamido]-1,1a, 2,7b-tetrahydrochysene-cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-{2-[((s)-1-ethyl pyrrolidine-3-base formamyl) methyl] the fluoro-phenylsulfonamido of-4-}-1,1a, 2,7b-tetrahydrochysene-cyclopropylene also [c] chromene-4-carboxylic acid;(1ar, 7bs)-5-[2-((3r)-1-ethyl pyrrolidine-3-ylmethyl) benzene-sulfonamido]-1,1a, 2,7b-tetrahydrochysene cyclopropylene also [c] c...
비만의 치료 및/또는 제어에서 사용하기 위한 트리시클릭 화합물본 발명은 트리시클릭 화합물, 및 의학적 장애, 예컨대 비만을 치료하는데 있어서의 그의 용도를 제공한다. 제약 조성물 및 다양한 트리시클릭 화합물의 제조 방법이 제공된다. 상기 화합물은 메티오닐 아미노펩티다제 2에 대한 활성을 갖는 것으로 여겨진다.(1aR,7bS)-5-[2-(2-디에틸아미노메틸시클로프로필)-4-플루오로-벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산, 또는 그의 거울상이성질체; (1aR,7bS)-5-{4-플루오로-2-[2-(피롤리딘-1-일메틸)시클로프로필]-벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-(3-디에틸아미노-2,2-디메틸프로필)-4-플루오로벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로-[c]크로멘-4-카르복실산; (1aR,7bS)-5-[4-플루오로-2-((R)-피롤리딘-3-일메틸)벤젠-술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-[4-플루오로-2-((S)-피롤리딘-3-일메틸)벤젠-술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(R)-1-(2-히드록시-2-메틸프로필)-피롤리딘-3-일메틸]벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-(1-아자비시클로[2.2.2]옥트-3-일메틸)-4-플루오로-벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-((Z)-1-아자비시클로[2.2.2]옥트-3-일리덴메틸)-4-플루오로벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-((E)-1-아자비시클로[2.2.2]옥트-3-일리덴메틸)-4-플루오로벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-{2-[(E)-(1-에틸피페리딘-3-일리덴)메틸]-4-플루오로벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-{2-[(Z)-(1-에틸피페리딘-3-일리덴)메틸]-4-플루오로벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산, 또는 그의 거울상이성질체; (1aR,7bS)-5-{2-[2-((S)-1-에틸피롤리딘-2-일)에틸]-4-플루오로-벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(R)-1-(2-히드록시에틸)피롤리딘-3-일메틸]벤젠술포닐아미노}-1,1a,2,7b-테트라히드로-시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-((엔도)-8-에틸-8-아자비시클로[3.2.1]옥트-3-일)메틸-4-플루오로벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-((엑소)-8-에틸-8-아자비시클로[3.2.1]옥트-3-일)메틸-4-플루오로벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(Z)-3-(3-히드록시-3-메틸피롤리딘-1-일)프로프-1-에닐]벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(Z)-3-(4-히드록시피페리딘-1-일)프로프-1-에닐]벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(Z)-3-(4-히드록시-4-메틸피페리딘-1-일)프로프-1-에닐]벤젠술포닐아미노}-1,1a,2,7b-테트라히드로-시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-(3-에틸-3-아자비시클로[3.1.0]헥스-6-일)-4-플루오로-벤젠술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(Z)-2-((S)-피롤리딘-2-일)에테닐]-벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(Z)-3-((S)-3-히드록시메틸피롤리딘-1-일)프로프-1-에닐]벤젠술포닐아미노}-1,1a,2,7b-테트라히드로-시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-{4-플루오로-2-[(Z)-3-((R)-3-히드록시메틸피롤리딘-1-일)프로프-1-에닐]벤젠술포닐아미노}-1,1a,2,7b-테트라히드로-시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-(4-플루오로-2-{(Z)-3-[(S)-3-(2-히드록시프로판-2-일)피롤리딘-1-일]프로프-1-에닐}벤젠술포닐아미노)-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-(4-플루오로-2-{(Z)-3-[(R)-3-(2-히드록시프로판-2-일)피롤리딘-1-일]프로프-1-에닐}벤젠술포닐아미노)-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-[4-플루오로-2-(헥사히드로-1H-피롤리진-2-일메틸)벤젠술포닐아미노]-1,1a,2,7b-테트라히드로-시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-{2-[((S)-1-에틸피롤리딘-3-일카르바모일)메틸]-4-플루오로-벤젠술포닐아미노}-1,1a,2,7b-테트라히드로-시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-[2-((3R)-1-에틸피롤리딘-3-일메틸)벤젠-술포닐아미노]-1,1a,2,7b-테트라히드로시클로프로파[c]크로멘-4-카르복실산; (1aR,7bS)-5-{2-[((S)-1-에틸피롤리딘-3-카르보닐)아미노-메틸]-4-플루오로벤젠술포닐아미노}-1,1a,2,7b-테트라히드로-시클로프로파[c]크로멘-4-카르복실산 - 포름산 (1:1); (1aR,7bS)-5-{2-[2-((R)-1-에틸피롤리딘-3-일아미노)에틸]-4-플루오로벤젠술포닐아미노}-1,1a,2,7b-테트라히드로시클로프로파-[c]크로멘-4-카르복실산 - 포름산 (1:1)으로 이루어진 군으로부터 선택된 화합물, 및 그의 제약상 허용되는 염, 입체이성질체, 에스테르 및 전구약물.