JP2001506231A - ヘテロ環式チオエステルおよびケトン - Google Patents
ヘテロ環式チオエステルおよびケトンInfo
- Publication number
- JP2001506231A JP2001506231A JP51566798A JP51566798A JP2001506231A JP 2001506231 A JP2001506231 A JP 2001506231A JP 51566798 A JP51566798 A JP 51566798A JP 51566798 A JP51566798 A JP 51566798A JP 2001506231 A JP2001506231 A JP 2001506231A
- Authority
- JP
- Japan
- Prior art keywords
- dimethyl
- phenyl
- propyl
- pyrrolidinecarbothioate
- oxopentanoyl
- 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.)
- Ceased
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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
- C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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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
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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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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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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- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
- C07D207/06—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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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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
- C07D207/16—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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- 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
- C07D211/22—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 oxygen atoms
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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
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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
- 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
- C07D211/60—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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
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- 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
- C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D277/06—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
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- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
- C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
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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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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- 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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- 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
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- Chemical & Material Sciences (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. 次式II [式中、 nは1または2を表し、 XはOまたはSを表し、 ZはS、CH2、CHR1およびC(R1)2からなる群より選択され、 R1は炭素原子数1ないし5の直鎖または分岐鎖アルキル基、炭素原子数2 ないし5の直鎖または分岐鎖アルケニル基、Ar1およびそれらの混合物から なる群より選択され、ここで前記R1は未置換であるかまたはハロゲン原子、 ニトロ基、炭素原子数1ないし6の直鎖もしくは分岐鎖アルキル基、炭素原子 数2ないし6の直鎖もしくは分岐鎖アルケニル基、ヒドロキシ基、炭素原子数 1ないし4のアルコキシ基、炭素原子数2ないし4のアルケニルオキシ基、フ ェノキシ基、ベンジルオキシ基、アミノ基、Ar1またはそれらの混合物で置 換されており、 R2は炭素原子数1ないし9の直鎖または分岐鎖アルキル基、炭素原子数2 ないし9の直鎖または分岐鎖アルケニル基、炭素原子数3ないし8のシクロア ルキル基、炭素原子数5ないし7のシクロアルケニル基およびAr1からなる 群より選択され、 Ar1はフェニル基、ベンジル基、ピリジル基、フルオレニル基、チオイン ドリル基またはナフチル基を表し、ここで前記Ar1は未置換であるかまたは ハロゲン原子、ヒドロキシ基、ニトロ基、炭素原子数1ないし6の直鎖もしく は分岐鎖アルキル基、炭素原子数2ないし6の直鎖もしくは分岐鎖アルケニル 基、炭素原子数1ないし4のアルコキシ基、炭素原子数2ないし4のアルケニ ルオキシ基、フェノキシ基、ベンジルオキシ基、アミノ基またはそれらの混合 物で置換されている。]で表される化合物またはその医薬的に許容可能な塩。 2. 式中、 nは1を表し、また XはOを表すところの、請求項1記載の化合物。 3. 式中、ZはCH2を表すところの、請求項2記載の化合物。 4. (2S)−2−({1−オキソ−5−フェニル}−ペンチル−1−(3, 3−ジメチル−1,2−ジオキソペンチル)ピロリジン、 3,3−ジメチル−1−[(2S)−2−(5−(3−ピリジル)ペンタノ イル)−1−ピロリジン]−1,2−ペンタンジオン、 (2S)−2−({1−オキソ−4−フェニル}−ブチル−1−(3,3− ジメチル−1,2−ジオキソブチル)ピロリジン、 (2S)−2−({1−オキソ−4−フェニル}−ブチル−1−(2−シク ロヘキシル−1,2−ジオキソエチル)ピロリジン、 2−({1−オキソ−4−フェニル}−ブチル−1−(3,3−ジメチル− 1,2−ジオキソブチル)ピロリジン、および 1−{(2S)−2−[5,5−ジ(4−フルオロフェニル)ペンタノイル ]−2−ピロリジン}−3,3−ジメチル−1,2−ペンタンジオン からなる群より選択される、請求項3記載の化合物。 5. 式中、ZはSを表すところの、請求項2記載の化合物。 6. 2−フェニル−1−エチル 1−(3,3−ジメチル−1,2−ジオキソ ペンチル)−2−ピペリジンカルボチオエート、 (3−チオインドリル)メチル(2S)−1−(3,3−ジメチル−1,2 −ジオキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル(2S)−1−(2−シクロヘキシル−1,2− ジオキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル(2S)−1−(1−シクロペンチル−1,2− ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−フェニル−1−プロピル(2S)−1−(3,3−ジメチル−1,2− ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−(3−ピリジル)−1−プロピル(2S)−1−(3,3−ジメチル− 1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−フェニル−1−プロピル(2S)−1−(2−シクロヘキシル−1,2 −ジオキソエチル)−2−ピロリジンカルボチオエート、 4−フェニル−1−ブチル(2S)−1−(2−シクロヘキシル−1,2− ジオキソエチル)−2−ピロリジンカルボチオエート、 4−フェニル−1−ブチル(2S)−1−(3,3−ジメチル−1,2−ジ オキソペンチル)−2−ピロリジンカルボチオエート、 3−(3−ピリジル)−1−プロピル(2S)−1−(2−シクロヘキシル −1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジフェニル−1−プロピル(2S)−1−(3,3−ジメチル−1 ,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジフェニル−1−プロピル(2S)−1−(2−シクロヘキシル− 1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル(2S)−1−(3,3− ジメチル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジ(パラ−フルオロ)フェニル−1−プロピル(2S)−1−(3 ,3−ジメチル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエ ート、 4,4−ジ(パラ−フルオロフェニル)ブチル 1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(1−ナフチル)プロピル(2S)−1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピロリジンカルボチオエート、 2,2−ジフェニルエチル(2S)−1−(3,3−ジメチル−2−オキソ ペンタノイル)テトラヒドロ−1H−2−ピロールカルボチオエート、 3−[4−(トリフルオロメチル)フェニル]プロピル(2S)−1−( 3,3−ジメチル−2−オキソペンタノイル)−2−ピロリジンカルボチオ エート、 3−(2−ナフチル)プロピル(2S)−1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピロリジンカルボチオエート、 3−(3−クロロフェニル)プロピル(2S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−[3−(トリフルオロメチル)フェニル]プロピル(2S)−1−(3 ,3−ジメチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエー ト、 3−(1−ビフェニル)プロピル(2S)−1−(3,3−ジメチル−2− オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(2−フルオロフェニル)プロピル(2S)−1−(3,3−ジメチル −2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(3−フルオロフェニル)プロピル(2S)−1−(3,3−ジメチル −2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(2−クロロフェニル)プロピル(2S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、および 3−(3,4−ジメトキシフェニル)プロピル(2S)−1−(3,3−ジ メチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエート からなる群より選択される、請求項5記載の化合物。 7. 式中、 nは1を表し、また XはSを表すところの、請求項1記載の化合物。 8. 式中、ZはCH2を表すところの、請求項7記載の化合物。 9. 式中、ZはSを表すところの、請求項7記載の化合物。 10. 式中、 nは2を表し、また XはOを表すところの、請求項1記載の化合物。 11. 式中、ZはCH2を表すところの、請求項10記載の化合物。 12. 2−({1−オキソ−6−フェニル}−ヘキシル−1−(3,3−ジメ チル−1,2−ジオキソブチル)ピペリジン、および 3,3−ジメチル−1−[2−(4−フェニルペンタノイル)ピペリジノ] −1,2−ペンタンジオン からなる群より選択される、請求項11記載の化合物。 13. 式中、ZはSを表すところの、請求項10記載の化合物。 14. 2−フェニル−1−エチル(2S)−1−(3,3−ジメチル−1,2 −ジオキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル 1−(2−フェニル−1,2−ジオキソエチル )−2−ピペリジンカルボチオエート、 3−フェニル−1−プロピル 1−(3,3−ジメチル−1,2−ジオキソ ブチル)−2−ピペリジンカルボチオエート、 4−フェニル−1−ブチル 1−(1,2−ジオキソ−3,3−ジメチルブ チル)−2−ピペリジンカルボチオエート、 1,5−ジフェニル−3−ペンチル 1−(3,3−ジメチル−1,2−ジ オキソペンチル)−2−ピペリジンカルボチオエート、 1,5−ジフェニル−3−メルカプトペンチル 1−(3−フェニル−1, 2−ジオキソエチル)−2−ピペリジンカルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル 1−(1,2−ジオキソ −3,3−ジメチルペンチル)ピペリジン−2−カルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル 1−(2−フェニル−1 ,2−ジオキソエチル)ピペリジン−2−カルボチオエート、 3−(1−ナフチル)−1−プロピル 1−(3,3−ジメチル−1,2− ジオキソペンチル)ピペリジン−2−カルボチオエート、 2,2−ジフェニルエチル(2S)−1−(3,3−ジメチル−2−オキソ ペンタノイル)−2−ピペリジンカルボチオエート、 3,3−ジフェニルプロピル 1−(3,3−ジメチル−2−オキソペンタ ノイル)−2−ピペリジンカルボチオエート 3−(2−ナフチル)プロピル(2R,S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピペリジンカルボチオエート、 4−フェニルブチル 1−(3,3−ジメチル−2−オキソペンタノイル) −2−ピペリジンカルボチオエート、 3−フェニルプロピル 1−(3,3−ジメチル−2−オキソペンタノイル )−2−ピペリジンカルボチオエート、 3−(2−クロロフェニル)プロピル 1−(3,3−ジメチル−2−オキ ソペンタノイル)−2−ピペリジンカルボチオエート、 3−(2−フルオロフェニル)プロピル 1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピペリジンカルボチオエート、および 3−(3−フルオロフェニル)プロピル 1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピペリジンカルボチオエート からなる群より選択される、請求項13記載の化合物。 15. 式中、 nは2を表し、また XはSを表すところの、請求項1記載の化合物。 16. 式中、ZはCH2を表すところの、請求項15記載の化合物。 17. 式中、ZはSを表すところの、請求項15記載の化合物。 18. 式中、ZはCHR1を表すところの、請求項15記載の化合物。 19. 2−({1−オキソー[2−{2’−フェニル}エチル]−4−フェニ ル}−ブチル−1−(3,3−ジメチル−1,2−ジオキソブチル)ピペリジ ン である、請求項18記載の化合物。 20. (i)神経活性を奏するのに有効な量の請求項1記載の化合物、および (ii)医薬的に許容可能なキャリア からなる医薬組成物。 21. 前記化合物において、 nは1を表し、また XはOを表すところの、請求項20記載の医薬組成物。 22. 前記化合物において、ZはCH2を表すところの、請求項21記載の医 薬組成物。 23. 前記化合物は、 (2S)−2−({1−オキソ−5−フェニル}−ペンチル−1−(3,3 −ジメチル−1,2−ジオキソペンチル)ピロリジン、 3,3−ジメチル−1−[(2S)−2−(5−(3−ピリジル)ペンタノ イル)−1−ピロリジン]−1,2−ペンタンジオン、 (2S)−2−({1−オキソ−4−フェニル}−ブチル−1−(3,3− ジメチル−1,2−ジオキソブチル)ピロリジン、 (2S)−2−({1−オキソ−4−フェニル}−ブチル−1−(2−シク ロヘキシル−1,2−ジオキソエチル)ピロリジン、 2−({1−オキソ−4−フェニル}−ブチル−1−(3,3−ジメチル− 1,2−ジオキソブチル)ピロリジン、および 1−{(2S)−2−[5,5−ジ(4−フルオロフェニル)ペンタノイル ]−2−ピロリジン}−3,3−ジメチル−1,2−ペンタンジオン からなる群より選択されるところの、請求項22記載の医薬組成物。 24. 前記化合物において、ZはSを表すところの、請求項21記載の医薬組 成物。 25. 前記化合物は、 2−フェニル−1−エチル 1−(3,3−ジメチル−1,2−ジオキソペ ンチル)−2−ピペリジンカルボチオエート、 (3−チオインドリル)メチル(2S)−1−(3,3−ジメチル−1,2 −ジオキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル(2S)−1−(2−シクロヘキシル−1,2− ジオキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル(2S)−1−(1−シクロペンチル−1,2− ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−フェニル−1−プロピル(2S)−1−(3,3−ジメチル−1,2− ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−(3−ピリジル)−1−プロピル(2S)−1−(3,3−ジメチ ル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−フェニル−1−プロピル(2S)−1−(2−シクロヘキシル−1,2 −ジオキソエチル)−2−ピロリジンカルボチオエート、 4−フェニル−1−ブチル(2S)−1−(2−シクロヘキシル−1,2− ジオキソエチル)−2−ピロリジンカルボチオエート 4−フェニル−1−ブチル(2S)−1−(3,3−ジメチル−1,2−ジ オキソペンチル)−2−ピロリジンカルボチオエート、 3−(3−ピリジル)−1−プロピル(2S)−1−(2−シクロヘキシル −1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジフェニル−1−プロピル(2S)−1−(3,3−ジメチル−1 ,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジフェニル−1−プロピル(2S)−1−(2−シクロヘキシル− 1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル(2S)−1−(3,3− ジメチル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジ(パラ−フルオロ)フェニル−1−プロピル(2S)−1−(3 ,3−ジメチル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエ ート、 4,4−ジ(パラ−フルオロフェニル)ブチル 1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(1−ナフチル)プロピル(2S)−1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピロリジンカルボチオエート、 2,2−ジフェニルエチル(2S)−1−(3,3−ジメチル−2−オキソ ペンタノイル)テトラヒドロ−1H−2−ピロールカルボチオエート、 3−[4−(トリフルオロメチル)フェニル]プロピル(2S)−1−(3 ,3−ジメチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエー ト、 3−(2−ナフチル)プロピル(2S)−1−(3,3−ジメチル−2− オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(3−クロロフェニル)プロピル(2S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−[3−(トリフルオロメチル)フェニル]プロピル(2S)−1−(3 ,3−ジメチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエー ト、 3−(1−ビフェニル)プロピル(2S)−1−(3,3−ジメチル−2− オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(2−フルオロフェニル)プロピル(2S)−1−(3,3−ジメチル −2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(3−フルオロフェニル)プロピル(2S)−1−(3,3−ジメチル −2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(2−クロロフェニル)プロピル(2S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、および 3−(3,4−ジメトキシフェニル)プロピル(2S)−1−(3,3−ジ メチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエート からなる群より選択されるところの、請求項24記載の医薬組成物。 26. 前記化合物において、 nは1を表し、また XはSを表すところの、請求項20記載の医薬組成物。 27. 前記化合物において、ZはCH2を表すところの、請求項26記載の医 薬組成物。 28. 前記化合物において、ZはSを表すところの、請求項26記載の医薬組 成物。 29. 前記化合物において、 nは2を表し、また XはOを表すところの、請求項20記載の医薬組成物。 30. 前記化合物において、ZはCH2を表すところの、請求項29記載の医 薬組成物。 31. 前記化合物は、 2−({1−オキソ−6−フェニル}−ヘキシル−1−(3,3−ジメチル −1,2−ジオキソブチル)ピペリジン、および 3,3−ジメチル−1−[2−(4−フェニルペンタノイル)ピペリジノ] −1,2−ペンタンジオン からなる群より選択されるところの、請求項30記載の医薬組成物。 32. 前記化合物において、ZはSを表すところの、請求項29記載の医薬組 成物。 33. 前記化合物は、 2−フェニル−1−エチル(2S)−1−(3,3−ジメチル−1,2−ジ オキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル 1−(2−フェニル−1,2−ジオキソエチル )−2−ピペリジンカルボチオエート、 3−フェニル−1−プロピル 1−(3,3−ジメチル−1,2−ジオキソ ブチル)−2−ピペリジンカルボチオエート、 4−フェニル−1−ブチル 1−(1,2−ジオキソ−3,3−ジメチルブ チル)−2−ピペリジンカルボチオエート、 1,5−ジフェニル−3−ペンチル 1−(3,3−ジメチル−1,2−ジ オキソペンチル)−2−ピペリジンカルボチオエート、 1,5−ジフェニル−3−メルカプトペンチル 1−(3−フェニル−1, 2−ジオキソエチル)−2−ピペリジンカルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル 1−(1,2−ジオキソ −3,3−ジメチルペンチル)ピペリジン−2−カルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル 1−(2−フェニル−1 ,2−ジオキソエチル)ピペリジン−2−カルボチオエート、 3−(1−ナフチル)−1−プロピル 1−(3,3−ジメチル−1,2− ジオキソペンチル)ピペリジン−2−カルボチオエート、 2,2−ジフェニルエチル (2S)−1−(3,3−ジメチル−2−オキ ソペンタノイル)−2−ピペリジンカルボチオエート、 3,3−ジフェニルプロピル 1−(3,3−ジメチル−2−オキソペンタ ノイル)−2−ピペリジンカルボチオエート、 3−(2−ナフチル)プロピル (2R,S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピペリジンカルボチオエート、 4−フェニルブチル 1−(3,3−ジメチル−2−オキソペンタノイル) −2−ピペリジンカルボチオエート 3−フェニルプロピル 1−(3,3−ジメチル−2−オキソペンタノイル )−2−ピペリジンカルボチオエート、 3−(2−クロロフェニル)プロピル 1−(3,3−ジメチル−2−オキ ソペンタノイル)−2−ピペリジンカルボチオエート、 3−(2−フルオロフェニル)プロピル 1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピペリジンカルボチオエート、および 3−(3−フルオロフェニル)プロピル 1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピペリジンカルボチオエート からなる群より選択されるところの、請求項32記載の医薬組成物。 34. 前記化合物において、 nは2を表し、また XはSを表すところの、請求項20記載の医薬組成物。 35. 前記化合物において、ZはCH2を表すところの、請求項34記載の医 薬組成物。 36. 前記化合物において、ZはSを表すところの、請求項34記載の医薬組 成物。 37. 前記化合物において、ZはCHR1を表すところの、請求項34記載の 医薬組成物。 38. 前記化合物は、 2−({1−オキソ−[2−{2’−フェニル}エチル]−4−フェニル} −ブチル−1−(3,3−ジメチル−1,2−ジオキソブチル)ピペリジン であるところの、請求項37記載の医薬組成物。 39. 動物に神経活性を奏するに有効な量の請求項1記載の化合物を投与する ことからなる、動物において神経活性を生ずる方法。 40. 神経活性は、損傷したニューロンの刺激、ニューロン再生の促進、神経 変性の予防および神経学的障害の治療からなる群より選択されるところの、請 求項39記載の方法。 41. 神経学的障害は、物理的損傷または疾病状態による末梢神経障害、脳へ の外的損傷、脊髄への物理的損傷、脳損傷と関連する発作、および神経変性に 関連する神経学的障害からなる群より選択されるところの、請求項40記載の 方法。 42. 神経変性に関連する神経学的障害はアルツハイマー病、パーキンソン病 、および筋萎縮側索硬化からなる群から選択されるところの請求項41記載の 方法。 43. 前記化合物において、 nは1を表し、また XはOを表すところの、請求項39記載の方法。 44. 前記化合物において、ZはCH2を表すところの、請求項43記載の方 法。 45. 前記化合物は、 (2S)−2−({1−オキソ−5−フェニル}−ペンチル−1−(3,3 −ジメチル−1,2−ジオキソペンチル)ピロリジン、 3,3−ジメチル−1−[(2S)−2−(5−(3−ピリジル)ペンタノ イル)−1−ピロリジン]−1,2−ペンタンジオン、 (2S)−2−({1−オキソ−4−フェニル}−ブチル−1−(3,3− ジメチル−1,2−ジオキソブチル)ピロリジン、 (2S)−2−({1−オキソ−4−フェニル}−ブチル−1−(2−シク ロヘキシル−1,2−ジオキソエチル)ピロリジン、 2−({1−オキソ−4−フェニル}−ブチル−1−(3,3−ジメチル− 1,2−ジオキソブチル)ピロリジン、および 1−{(2S)−2−[5,5−ジ(4−フルオロフェニル)ペンタノイ ル]−2−ピロリジン}−3,3−ジメチル−1,2−ペンタンジオン からなる群より選択されるところの、請求項44記載の方法。 46. 前記化合物において、ZはSを表すところの、請求項43記載の方法。 47. 前記化合物は、 2−フェニル−1−エチル 1−(3,3−ジメチル−1,2−ジオキソペ ンチル)−2−ピペリジンカルボチオエート (3−チオインドリル)メチル (2S)−1−(3,3−ジメチル−1, 2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル (2S)−1−(2−シクロヘキシル−1,2 −ジオキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル (2S)−1−(1−シクロペンチル−1,2 −ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−フェニル−1−プロピル (2S)−1−(3,3−ジメチル−1,2 −ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−(3−ピリジル)−1−プロピル (2S)−1−(3,3−ジメチル −1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−フェニル−1−プロピル (2S)−1−(2−シクロヘキシル−1, 2−ジオキソエチル)−2−ピロリジンカルボチオエート、 4−フェニル−1−ブチル (2S)−1−(2−シクロヘキシル−1,2 −ジオキソエチル)−2−ピロリジンカルボチオエート、 4−フェニル−1−ブチル (2S)−1−(3,3−ジメチル−1,2− ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−(3−ピリジル)−1−プロピル (2S)−1−(2−シクロヘキシ ル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジフェニル−1−プロピル (2S)−1−(3,3−ジメチル− 1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3,3−ジフェニル−1−プロピル (2S)−1−(2−シクロヘキシル −1,2−ジオキソペンチル)−2−ピロリジンカルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル (2S)−1−(3, 3−ジメチル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエー ト、 3,3−ジ(パラ−フルオロ)フェニル−1−プロピル (2S)−1−( 3,3−ジメチル−1,2−ジオキソペンチル)−2−ピロリジンカルボチオエ ート、 4,4−ジ(パラ−フルオロフェニル)ブチル 1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(1−ナフチル)プロピル (2S)−1−(3,3−ジメチル−2− オキソペンタノイル)−2−ピロリジンカルボチオエート、 2,2−ジフェニルエチル (2S)−1−(3,3−ジメチル−2−オキソ ペンタノイル)テトラヒドロ−1H−2−ピロールカルボチオエート、 3−[4−(トリフルオロメチル)フェニル]プロピル (2S)−1−( 3,3−ジメチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエ ート、 3−(2−ナフチル)プロピル (2S)−1−(3,3−ジメチル−2− オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(3−クロロフェニル)プロピル (2S)−1−(3,3−ジメチル −2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−[3−(トリフルオロメチル)フェニル]プロピル (2S)−1−( 3,3−ジメチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエ ート、 3−(1−ビフェニル)プロピル (2S)−1−(3,3−ジメチル−2 −オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(2−フルオロフェニル)プロピル (2S)−1−(3,3−ジメチ ル−2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(3−フルオロフェニル)プロピル (2S)−1−(3,3−ジメチ ル−2−オキソペンタノイル)−2−ピロリジンカルボチオエート、 3−(2−クロロフェニル)プロピル (2S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピロリジンカルボチオエート、および 3−(3,4−ジメトキシフェニル)プロピル (2S)−1−(3,3− ジメチル−2−オキソペンタノイル)−2−ピロリジンカルボチオエート からなる群より選択されるところの、請求項46記載の方法。 48. 前記化合物において、 nは1を表し、また XはSを表すところの、請求項39記載の方法。 49. 前記化合物において、ZはCH2を表すところの、請求項48記載の方 法。 50. 前記化合物において、ZはSを表すところの、請求項48記載の方法。 51. 前記化合物において、 nは2を表し、また XはOを表すところの、請求項39記載の方法。 52. 前記化合物において、ZはCH2を表すところの、請求頂51記載の方 法。 53. 前記化合物は、 2−({1−オキソ−6−フェニル}−ヘキシル−1−(3,3−ジメチル −1,2−ジオキソブチル)ピペリジン、および 3,3−ジメチル−1−[2−(4−フェニルペンタノイル)ピペリジノ] −1,2−ペンタンジオン からなる群より選択されるところの、請求項52記載の方法。 54. 前記化合物において、ZはSを表すところの、請求項51記載の方法。 55. 前記化合物は、 2−フェニル−1−エチル(2S)−1−(3,3−ジメチル−1,2−ジ オキソペンチル)−2−ピロリジンカルボチオエート、 2−フェニル−1−エチル 1−(2−フェニル−1,2−ジオキソエチル )−2−ピペリジンカルボチオエート、 3−フェニル−1−プロピル 1−(3,3−ジメチル−1,2−ジオキソ ブチル)−2−ピペリジンカルボチオエート、 4−フェニル−1−ブチル 1−(1,2−ジオキソ−3,3−ジメチルブ チル)−2−ピペリジンカルボチオエート、 1,5−ジフェニル−3−ペンチル 1−(3,3−ジメチル−1,2−ジ オキソペンチル)−2−ピペリジンカルボチオエート、 1,5−ジフェニル−3−メルカプトペンチル 1−(3−フェニル−1, 2−ジオキソエチル)−2−ピペリジンカルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル 1−(1,2−ジオキソ −3,3−ジメチルペンチル)ピペリジン−2−カルボチオエート、 3−(パラ−メトキシフェニル)−1−プロピル 1−(2−フェニル−1 ,2−ジオキソエチル)ピペリジン−2−カルボチオエート、 3−(1−ナフチル)−1−プロピル 1−(3,3−ジメチル−1,2− ジオキソペンチル)ピペリジン−2−カルボチオエート、 2,2−ジフェニルエチル (2S)−1−(3,3−ジメチル−2−オキ ソペンタノイル)−2−ピペリジンカルボチオエート、 3,3−ジフェニルプロピル 1−(3,3−ジメチル−2−オキソペンタ ノイル)−2−ピペリジンカルボチオエート、 3−(2−ナフチル)プロピル (2R,S)−1−(3,3−ジメチル− 2−オキソペンタノイル)−2−ピペリジンカルボチオエート、 4−フェニルブチル 1−(3,3−ジメチル−2−オキソペンタノイル) −2−ピペリジンカルボチオエート、 3−フェニルプロピル 1−(3,3−ジメチル−2−オキソペンタノイル )−2−ピペリジンカルボチオエート、 3−(2−クロロフェニル)プロピル 1−(3,3−ジメチル−2−オキ ソペンタノイル)−2−ピペリジンカルボチオエート、 3−(2−フルオロフェニル)プロピル 1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピペリジンカルボチオエート、および 3−(3−フルオロフェニル)プロピル 1−(3,3−ジメチル−2−オ キソペンタノイル)−2−ピペリジンカルボチオエート からなる群より選択されるところの、請求項54記載の方法。 56. 前記化合物において、 nは2を表し、また XはSを表すところの、請求項39記載の方法。 57. 前記化合物において、ZはCH2を表すところの、請求項56記載の方 法。 58. 前記化合物において、ZはSを表すところの、請求項56記載の方法。 59. 前記化合物において、ZはCHR1を表すところの、請求項56記載の 方法。 60. 前記化合物は、 2−({1−オキソー[2−{2’−フェニル}エチル]−4−フェニル} −ブチル−1−(3,3−ジメチル−1,2−ジオキソブチル)ピペリジン であるところの、請求項59記載の方法。
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US08/904,461 | 1997-08-01 | ||
US08/904,461 US5990131A (en) | 1996-09-25 | 1997-08-01 | Heterocyclic thioesters and ketones |
PCT/US1997/015832 WO1998013343A1 (en) | 1996-09-25 | 1997-09-09 | Heterocyclic thioesters and ketones |
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BR (1) | BR9713202A (ja) |
CA (1) | CA2263927C (ja) |
CZ (1) | CZ298120B6 (ja) |
DE (2) | DE69738382T2 (ja) |
EA (2) | EA002982B1 (ja) |
ES (1) | ES2298912T3 (ja) |
ID (1) | ID19615A (ja) |
IL (2) | IL128792A (ja) |
NO (1) | NO313939B1 (ja) |
NZ (3) | NZ334315A (ja) |
PA (1) | PA8438401A1 (ja) |
PE (1) | PE110498A1 (ja) |
PL (1) | PL194249B1 (ja) |
SG (1) | SG109418A1 (ja) |
SK (1) | SK26599A3 (ja) |
WO (1) | WO1998013343A1 (ja) |
ZA (1) | ZA977900B (ja) |
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- 1997-09-09 AT AT97940917T patent/ATE310722T1/de not_active IP Right Cessation
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-
1999
- 1999-03-02 IL IL128792A patent/IL128792A/en not_active IP Right Cessation
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- 1999-03-24 NO NO19991432A patent/NO313939B1/no not_active IP Right Cessation
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2002
- 2002-04-19 NZ NZ518473A patent/NZ518473A/en unknown
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2005500270A (ja) * | 2001-05-29 | 2005-01-06 | ギルフォード ファーマシュウティカルズ インコーポレイテッド | 手術の結果として発生した神経損傷を治療するための方法 |
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