JP2000501117A - ムスカリン様アンタゴニスト - Google Patents
ムスカリン様アンタゴニストInfo
- Publication number
- JP2000501117A JP2000501117A JP10508038A JP50803898A JP2000501117A JP 2000501117 A JP2000501117 A JP 2000501117A JP 10508038 A JP10508038 A JP 10508038A JP 50803898 A JP50803898 A JP 50803898A JP 2000501117 A JP2000501117 A JP 2000501117A
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- JP
- Japan
- Prior art keywords
- alkyl
- added
- mixture
- solution
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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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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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- 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
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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
- C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/24—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by sulfur atoms to which a second hetero atom is attached
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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
- C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/30—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
- C07D211/32—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
- C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
- C07D295/03—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- C07—ORGANIC CHEMISTRY
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/092—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
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- C07—ORGANIC CHEMISTRY
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
- C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D295/116—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings with the doubly bound oxygen or sulfur atoms directly attached to a carbocyclic ring
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- C—CHEMISTRY; METALLURGY
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
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- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- 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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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.以下の構造式を有する化合物(その全ての異性体、ならびに薬学的に受容可 能な塩、エステル、および溶媒和物を含む): ここで、YおよびZのうちの1つは、Nであり、そして他方は、N、CH、また はC-アルキルであり; Xは、-O-、-S-、-SO-、-SO2-、-NR6-、-CO-、-CH2-、-CS-、-C(OR5)2-、-C(S R5)2-、-CONR20-、-C(アルキル)2-、-C(H)(アルキル)-、-NR20-SO2-、-SO2-NR20 -、-NR20CO-、-O-CO-NH-、-NH-CO-O-、 であり; Rは、 水素、アシル、アルキル、アルコキシ、アルケニル、シクロアルキル、アルキル およびカルボニルからなる群から選択される1つまたは2つの基で置換されたシ クロアルキル、シクロアルケニル、ビシクロアルキル、アリールアルケニル、ベ ンジル、独立して選択された3つまでのR3基で置換されたベンジル、シクロアル キルアルキル、ポリハロアシル、ベンジルオキシアルキル、ヒドロキシC2-C20ア ルキル、アルケニルカルボニル、アルキルアリールスルホニル、アルコキシカル ボニルアミノアシル、アルキルスルホニル、またはアリールスルホニルであり、 さらに、Xが-CH2-である場合、Rはまた-OHであり得;さらに、XがNでない場 合、Rはまたヒドロキシメチルであり得、さらに、RおよびXは結合してProt-( NOAA)r-NH-基を形成し得、ここでrは1〜4の整数であり、Protは窒素保護基で あり、そしてrが1の場合、NOAAは天然に存在するアミノ酸またはそのエナンチ オマーであり、あるいはrが2〜4の場合、各NOAAは、独立して選択された天然 に存在するアミノ酸またはそのエナンチオマーのペプチドであり; R1およびR21は、独立して、H、アルキル、アルケニル、シクロアルキル、シ クロアルケニル、ビシクロアルキル、アルキニル、シアノ、アミノアルキル、ア ルコキシカルボニル、アミノカルボニル、ヒドロキシアミジノ、アルコキシカル ボニルアルキル、フェニルアルキル、アルキルカルボニルオキシアルキル、 H、-OH、(但し、R1およびR21は、両方が-OHではなく、かつYはNではない) 、ホルミル、-COアルキル、-COアシル、-COアリール、およびヒドロキシアルキ ル からなる群から選択され;さらに、R1およびR21は一緒になって基=CH2、=N-OR5 、=さらに、R1およびR21は、それらが結合する炭素原子と一緒になって基 を形成し得るか、あるいはR1およびR21は、それらが結合する炭素原子と一緒に なって3〜7の炭素原子を含む飽和ヘテロ環式環を形成し得、これらの1つ以上 は必要に応じてアルキルで置換され得、そして1つまたは2つの基は、独立して S、OおよびN-R20から選択され; R2は、 であり; R3、R4、R22、R24、およびR25は、独立して、アルキル、H、ハロ、アルコキ シ、ベンジルオキシ、ニトロまたはアミノアルキルにより置換されたベンジルオ キシ、ハロアルキル、ポリハロアルキル、ニトロ、シアノ、スルホニル、ヒドロ キシ、アミノ、アルキルアミノ、ホルミル、アルキルチオ、ポリハロアルコキシ 、アシルオキシ、トリアルキルシリル、アルキルスルホニル、アリールスルホニ ル、アシル、アルコキシカルボニル、アルキルスルフィニル;-OCONH2、-OCONH- アルキル、アルキルアミノアルキル、ジアルキルアミノアルキル、-COOH、-CON( R20)2、-OCON(アルキル)2、-NHCOO-アルキル、-NHCO-アルキル、フェニル、ヒド ロキシアルキル、またはモルホリノからなる群から選択され; 各R5およびR6は、独立して、Hおよびアルキルからなる群から選択され、但し 、 XがC(OR5)2またはC(SR5)2である場合、両方のR5基がHであり得ず、そしてさら に、XがC(OR5)2またはC(SR5)2である場合、X中の2つのR5基は結合して-(CR20 2 )p-を形成し得、ここでpは2〜4の整数であり; R7は、独立して、H、アルキル、アリールアルキル、シクロアルキル、アリー ルおよび本明細書中で定義した通りのR3およびR4で置換されたアリールからなる 群から選択され; 各R8は、独立して、H、ヒドロキシアルキルまたはアルキルからなる群から選 択されるか、あるいは、2つのR8基が結合してアルキレン基を形成し得; R9は、H、アルキル、アラルキル、またはアシルであり; R20は、H、アリールまたはアルキルであり; R27およびR28は、独立して、H、アルキル、ヒドロキシアルキル、アリールア ルキル、アミノアルキル、ハロアルキル、チオアルキル、アルキルチオアルキル 、カルボキシアルキル、イミダゾリルアルキル(imidazolyalkyl)、およびインド リルアルキル(indolyalkyl)からなる群から選択されるか;あるいはR27およびR2 8 は結合してアルキレン基を形成し得; R29は、H、アルキル、-CO-アルキル、-CO-シクロアルキル、アルコキシカル ボニル、アミノカルボニル、アリールオキシカルボニル、アルキルアミノカルボ ニル、ジアルキルアミノカルボニル、アルキルスルホニル、アリールスルホニル または-SO2-NH-R20であり; R30は、H、アルキル、アリール、シクロアルキル、ヒドロキシアルキル、ア ミノアルキル、-COOR20、-CON(R20)2またはシアノであり; R31およびR32は、R30と同じであり、さらに、2つのR30,R31およびR32基は、 基-(CH2)r-(ここでrは1〜6である)を形成し得、さらに、R31およびR32はま た、ヒドロキシ、-N(R20)2、-O-アシル、-N(R20)アシル、-OCOOR20、または-OCO N(R20)2であり得; R33は、アリールまたはヘテロアリールであり、但し、R33がヘテロアリールで ある場合、CO-R33結合はR33基中の炭素原子へのものであり; R34は、アルキル、シクロアルキルまたはアリールであり、そしてさらに、R1 およびR21が、それらが結合している炭素原子と一緒になって3〜7の炭素原子 を 含む飽和ヘテロ環式環を形成し、そして2つの基が独立してS、O、およびN-R2 0 から選択される場合、R34はまたHであり得; R35は、-CH2-、-NR20-または-O-であり; R36は、-NH2-、アルキルまたはアルコキシであり; R37は、独立して、Hおよびアルキルからなる群から選択され; R38は、-CO-(CH2)0-5-OR5、-SO2-(アルキル)、または であり、ここでq1およびq2は、独立して、1〜5であり、但し、q1とq2との合計 は2〜5であり;そして R39およびR40は、独立して、=Oおよび(H,H)からなる群から選択される。 2.以下の化合物番号からなる群から選択される、請求項1に記載の化合物: 本明細書に現れる化合物の表からの17 ,18,25,30,31,32,34,35,36,37 ,41,43,44,49,53,54,56,57,58,59,80,82,84,85,94,98,100 ,108 ,121,126,127,137,145,151,152,154,155,162,166,178,179, 181,185,190,191,194,199,214,215,216,225,247,253,256,257,33 7,339,340,341,349,351,367,409,459,479,488,489,490,500,501 ,502,503,505,506,507,515,516,517,555 および562 3.薬学的に受容可能なキャリアと組み合わせて請求項1に記載の化合物を含有 する、薬学的組成物。 4.単一パッケージ中の別々の容器中に、組み合わせて使用するための薬学的化 合物を含む、認知疾患または神経退化疾患を処置するためのキットであって、1 つの容器中に、請求項1に記載の化合物を含み、そして別の容器中にアセチルコ リンエステラーゼインヒビターを含み、該化合物およびインヒビターの各々が、 薬学的に受容可能なキャリア中に存在し、そしてそれらの組み合わせた量が有効 量である、キット。
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US08/700,628 | 1996-08-08 | ||
US08/700,628 US5889006A (en) | 1995-02-23 | 1996-08-08 | Muscarinic antagonists |
PCT/US1997/013383 WO1998005292A2 (en) | 1996-08-08 | 1997-08-06 | Piperidine and piperazine derivatives and their use as muscarinic antagonists |
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JP2003509494A (ja) * | 1999-09-22 | 2003-03-11 | シェーリング コーポレイション | ムスカリン拮抗薬 |
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USRE42327E1 (en) | 2002-06-14 | 2011-05-03 | Toyama Chemical Co., Ltd. | Medicinal compositions improving brain function and method for improving brain function |
US7834053B2 (en) | 2002-06-14 | 2010-11-16 | Toyama Chemical Co., Ltd. | Medicinal compositions improving brain function and method for improving brain function |
JPWO2003105830A1 (ja) * | 2002-06-14 | 2005-10-13 | 富山化学工業株式会社 | 脳機能を改善する医薬組成物および脳機能を改善するための方法 |
JP2008526860A (ja) * | 2005-01-06 | 2008-07-24 | シェーリング コーポレイション | ケトンアミドの調製 |
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US11793817B2 (en) | 2011-11-18 | 2023-10-24 | Heptares Therapeutics Limited | Muscarinic M1 receptor agonists |
US11834407B2 (en) | 2016-10-14 | 2023-12-05 | Heptares Therapeutics Limited | Substituted cyclohexanes as muscarinic M1 receptor and/or M4 receptor agonists |
US11773090B2 (en) | 2018-06-22 | 2023-10-03 | Heptares Therapeutics Limited | Pharmaceutical compounds |
US11945801B2 (en) | 2018-12-07 | 2024-04-02 | Heptares Therapeutics Limited | Bicyclic aza compounds as muscarinic M1 and/or M4 receptor agonists |
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