JP2001511781A - スルホンアミド誘導体 - Google Patents
スルホンアミド誘導体Info
- Publication number
- JP2001511781A JP2001511781A JP53314498A JP53314498A JP2001511781A JP 2001511781 A JP2001511781 A JP 2001511781A JP 53314498 A JP53314498 A JP 53314498A JP 53314498 A JP53314498 A JP 53314498A JP 2001511781 A JP2001511781 A JP 2001511781A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- group
- mmol
- alkenyl
- 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
Links
Classifications
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
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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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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- A—HUMAN NECESSITIES
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- 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
- A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C307/04—Diamides of sulfuric acids
- C07C307/08—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to carbon atoms of rings other than six-membered aromatic rings
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- C—CHEMISTRY; METALLURGY
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C311/04—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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- C—CHEMISTRY; METALLURGY
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
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- C—CHEMISTRY; METALLURGY
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C311/06—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/09—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton the carbon skeleton being further substituted by at least two halogen atoms
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- C—CHEMISTRY; METALLURGY
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/14—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
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- C—CHEMISTRY; METALLURGY
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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- C—CHEMISTRY; METALLURGY
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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- C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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- C07C311/53—X and Y not being nitrogen atoms, e.g. N-sulfonylcarbamic acid
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- 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
- C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
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- 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
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.グルタメート受容体機能を増強するための薬剤の製造のための、式: R1−L−NHSO2R2 I [式中、 R1は、置換されていない芳香族もしくはヘテロ芳香族基、または置換されて いる芳香族もしくはヘテロ芳香族基を表し; R2は、(1−6C)アルキル、(3−6C)シクロアルキル、(1−6C)フルオロ アルキル、(1−6C)クロロアルキル、(2−6C)アルケニル、(1−4C)アル コキシ(1−4C)アルキル、置換されていないフェニル、もしくはハロゲン、( 1−4C)アルキル、もしくは(1−4C)アルコキシで置換されているフェニル 、または式R3R4N(式中、R3およびR4は各々独立して、(1−4C)アルキル を表すか、またはそれらが結合している窒素原子と一緒になって、アゼチジニル 、ピロリジニル、ピペリジニル、モルホリノ、ピペラジニル、ヘキサヒドロアゼ ピニル、もしくはオクタヒドロアゾシニル基を形成する。)の基を表し;および Lは、置換されていない(2−4C)アルキレン鎖、もしくは(1−6C)アルキ ル、アリール(1−6C)アルキル、(2−6C)アルケニル、アリール(2−6C) アルケニル、およびアリールから独立して選択される1つもしくは2つの置換基 で置換されている(2−4C)アルキレン鎖を表すか、またはこの2つの置換基が 、それらが結合する炭素原子と一緒になって、(3−8C)炭素環式環を形成する 。] の化合物またはその医薬的に許容され得る塩の使用。 2.R2が、(1−6C)アルキル、(1−6C)フルオロアルキル、(2−6C)ア ルケニル、または式R3R4N(式中、R3およびR4は各々独立して、(1−4C) アルキルを表すか、またはそれらが結合している窒素原子と一緒になって、アゼ チジニル、ピロリジニル、ピペリジニル、モルホリノ、ピペラジニル、ヘキサヒ ドロアゼピニル、もしくはオクタヒドロアゾシニル基を形成する。)の基を表す 、請求項1に記載の使用。 3.Lが、式:[式中、R5、R6、R7、およびR8の2つは、水素を表して、残りのものは独立 して、水素、(1−6C)アルキル、アリール(1−6C)アルキル、(2−6C)ア ルケニル、アリール(2−6C)アルケニル、もしくはアリールを表すか、または それらが結合している炭素原子と一緒になって、(3−8C)炭素環式環を形成す る。] の基を表す、請求項1または請求項2に記載の使用。 4.R6およびR7が、水素を表し;およびR5およびR8が各々独立して、水素も しくは(1−4C)アルキルを表すか、またはそれらが結合している炭素原子と一 緒になって、(3−8C)炭素環式環を形成する、請求項3に記載の使用。 5.R8が、(1−4C)アルキルを表すか、またはR5およびR8が、それらが結 合している炭素原子と一緒になって、シクロプロピル環を形成する、請求項4に 記載の使用。 6.R2が、メチル、エチル、プロピル、2−プロピル、ブチル、2−メチルプ ロピル、シクロヘキシル、トリフルオロメチル、2,2,2−トリフルオロエチル 、クロロメチル、エテニル、プロプ−2−エニル、メトキシエチル、フェニル、 4−フルオロフェニル、またはジメチルアミノを表す、請求項1〜5のいずれか に記載の使用。 7.R2が、エチル、2−プロピル、またはジメチルアミノを表す、請求項6に 記載の使用。 8.R1が、置換されていないナフチル基、もしくはフェニル、フリル、チエニ ル、もしくはピリジル基、または ハロゲン;ニトロ;シアノ;ヒドロキシイミノ;(1−10C)アルキル;(2 −10C)アルケニル;(2−10C)アルキニル;(3−8C)シクロアルキル ;ヒドロキシ(3−8C)シクロアルキル;オキソ(3−8C)シクロアルキル; ハロ(1−10C)アルキル;(CH2)yX1R9(式中、yは、0または1 〜4の整数であり、X1は、O、S、NR10、CO、COO、OCO、CON R11、NR12CO、NR12COCOO、またはOCONR13を表し、R9は、 水素、(1−10C)アルキル、(3−10C)アルケニル、(3−10C)アルキ ニル、ピロリジニル、テトラヒドロフリル、モルホリノ、または(3−8C)シ クロアルキルを表し、およびR10、R11、R12、およびR13は各々独立して、 水素または(1−10C)アルキルを表すか、またはR9およびR10、R11、R1 2、もしくはR13は、それらが結合している窒素原子と一緒になって、アゼチ ジニル、ピロリジニル、ピペリジニル、もしくはモルホリノ基を形成する。) ;N−(1−4C)アルキルピペラジニル;N−フェニル(1−4C)アルキルピ ペラジニル;チエニル;フリル;オキサゾリル;イソオキサゾリル;ピラゾリ ル;イミダゾリル;チアゾリル;ピリジル;ピリダジニル;ピリミジニル;ジ ヒドロチエニル;ジヒドロフリル;ジヒドロチオピラニル;ジヒドロピラニル ;ジヒドロチアゾリル;(1−4C)アルコキシカルボニル ジヒドロチアゾリ ル;(1−4C)アルコキシカルボニル ジメチルジヒドロチアゾリル;テトラ ヒドロチエニル;テトラヒドロフリル;テトラヒドロチオピラニル;テトラヒ ドロピラニル;インドリル;ベンゾフリル;ベンゾチエニル;ベンゾイミダゾ リル;および式R14−(La)n−X2−(Lb)m(式中、X2は、結合、O、NH、 S、SO、SO2、CO、CH(OH)、CONH、NHCO、NHCONH、 NHCOO、COCONH、OCH2CONH、またはCH=CHを表し、La およびLbは各々、(1−4C)アルキレンを表し、nおよびmの一方は0また は1であって、他方は0であり、およびR14は、置換されていないフェニルも しくはヘテロ芳香族基、または1つもしくは2つのハロゲン、ニトロ、シアノ 、ヒドロキシイミノ、(1−10C)アルキル、(2−10C)アルケニル、(2 −10C)アルキニル、(3−8C)シクロアルキル、4−(1,1−ジオキソテ トラヒドロ−1,2−チアジニル)、ハロ(1−10C)アルキル、シアノ(2− 10C)アルケニル、フェニル、および(CH2)zX3R15(式中、zは、0また は1〜4の整数であり、X3は、O、S、NR16、CO、CH(OH)、COO 、OCO、CONR17、NR18CO、NHSO2、NHSO2NR17、NHCO NH、OCONR19、またはNR19COOを表し、R15は、 水素、(1−10C)アルキル、フェニル(1−4C)アルキル、(1−10C)ハ ロアルキル、(1−4C)アルコキシカルボニル(1−4C)アルキル、(1−4 C)アルキルスルホニルアミノ(1−4C)アルキル、(N−(1−4C)アルコキ シカルボニル)(1−4C)アルキルスルホニルアミノ(1−4C)アルキル、(3 −10C)アルケニル、(3−10C)アルキニル、(3−8C)シクロアルキル 、カンホリル、または置換されていない芳香族もしくはヘテロ芳香族基、もし くは1つもしくは2つのハロゲン、(1−4C)アルキル、ハロ(1−4C)アル キル、ジ(1−4C)アルキルアミノ、および(1−4C)アルコキシで置換され ている芳香族もしくはヘテロ芳香族基を表し、およびR16、R17、R18、およ びR19は各々独立して、水素または(1−10C)アルキルを表すか、またはR 15およびR16、R17、R18、もしくはR19は、それらが結合している窒素原子 と一緒になって、アゼチジニル、ピロリジニル、ピペリジニル、もしくはモル ホリノ基を形成する。)で置換されているフェニルもしくはヘテロ芳香族基を 表す。)の基から独立して選択される1つもしくは2つの置換基で置換されて いるナフチル基、もしくはフェニル、フリル、チエニル、もしくはピリジル基 を表す、請求項1〜7のいずれかに記載の使用。 9.R1が、置換されていないナフチル基もしくはフェニル基、または ハロゲン;ニトロ;シアノ;(1−10C)アルキル;(V2−10C)アルケニ ル;(2−10C)アルキニル;(3−8C)シクロアルキル;ハロ(1−10C) アルキル;(CH2)yX1R9(式中、yは、0または1〜4の整数であり、X1 は、O、S、NR10、CO、COO、OCO、CONR11、NR12CO、OC ONR13を表し、R9は、水素、(1−10C)アルキル、(3−10C)アルケ ニル、(3−10C)アルキニル、または(3−8C)シクロアルキルを表し、お よびR10、R11、R12、およびR13は各々独立して、水素または(1−10C) アルキルを表すか、またはR9およびR10、R11、R12、もしくはR13は、そ れらが結合している窒素原子と一緒になって、アゼチジニル、ピロリジニル、 ピペリジニル、もしくはモルホリノ基を形成する。);チエニル;フリル;オ キサゾリル;イソオキサゾリル;ピラゾリル;イミダゾリル;チアゾリ ル;ピリジル;ピリダジニル;ピリミジニル;ジヒドロチエニル;ジヒドロフ リル;ジヒドロチオピラニル;ジヒドロピラニル;テトラヒドロチエニル;テ トラヒドロフリル;テトラヒドロチオピラニル;テトラヒドロピラニル;イン ドリル;ベンゾフリル;ベンゾチエニル;ベンゾイミダゾリル;および式R14 −(La)n−X2−(Lb)m(式中、X2は、結合、O、NH、S、SO、SO2、 CO、CONH、またはNHCOを表し、LaおよびLbは各々、(1−4C)ア ルキレンを表し、nおよびmの一方は0または1であって、他方は0であり、 およびR14は、置換されていないフェニル基、または1つもしくは2つのハロ ゲン、ニトロ、シアノ、(1−10C)アルキル、(2−10C)アルケニル、( 2−10C)アルキニル、(3−8C)シクロアルキル、ハロ(1−10C)アル キル、および(CH2)zX3R15(式中、zは、0または1〜4の整数であり、 X3は、O、S、NR16、CO、COO、OCO、CONR17、NR18CO、 OCONR19を表し、R15は、水素、(1−10C)アルキル、(3−10C)ア ルケニル、(3−10C)アルキニル、または(3−8C)シクロアルキルを表し 、およびR16、R17、R18、およびR19は各々独立して、水素または(1−1 0C)アルキルを表すか、またはR15およびR16、R17、R18、もしくはR19 は、それらが結合している窒素原子と一緒になって、アゼチジニル、ピロリジ ニル、ピペリジニル、もしくはモルホリノ基を形成する。)で置換されている フェニル基を表す。)の基から独立して選択される1つもしくは2つの置換基 で置換されているナフチル基もしくはフェニル基 を表す、請求項1〜8のいずれかに記載の使用。 10.R1が、2−ナフチル、または式: [式中、 R20は、ハロゲン;ニトロ;シアノ;ヒドロキシイミノ;(1−10C)アルキ ル;(2−10C)アルケニル;(2−10C)アルキニル;(3−8C)シクロアル キル;ヒドロキシ(3−8C)シクロアルキル;オキソ(3−8C)シクロアルキル ;ハロ(1−10C)アルキル;(CH2)yX1R9(式中、yは、0または1〜4の 整数であり、X1は、O、S、NR10、CO、COO、OCO、CONR11、N R12CO、NR12COCOO、またはOCONR13を表し、R9は、水素、(1− 10C)アルキル、(3−10C)アルケニル、(3−10C)アルキニル、ピロリ ジニル、テトラヒドロフリル、モルホリノ、または(3−8C)シクロアルキルを 表し、およびR10、R11、R12、およびR13は各々独立して、水素または(1− 10C)アルキルを表すか、またはR9およびR10、R11、R12、もしくはR13は 、それらが結合している窒素原子と一緒になって、アゼチジニル、ピロリジニル 、ピペリジニル、もしくはモルホリノ基を形成する。);N−(1−4C)アルキ ルピペラジニル;N−フェニル(1−4C)アルキルピペラジニル;チエニル;フ リル;オキサゾリル;イソオキサゾリル;ピラゾリル;イミダゾリル;チアゾリ ル;ピリジル;ピリダジニル;ピリミジニル;ジヒドロチエニル;ジヒドロフリ ル;ジヒドロチオピラニル;ジヒドロピラニル;ジヒドロチアゾリル;(1−4 C)アルコキシカルボニル ジヒドロチアゾリル;(1−4C)アルコキシカルボニ ル ジメチルジヒドロチアゾリル;テトラヒドロチエニル;テトラヒドロフリル ;テトラヒドロチオピラニル;テトラヒドロピラニル;インドリル;ベンゾフリ ル;ベンゾチエニル;ベンゾイミダゾリル;および式R14−(La)n−X2−(Lb)m (式中、X2は、結合、O、NH、S、SO、SO2、CO、CH(OH)、C ONH、NHCO、NHCONH、NHCOO、COCONH、OCH2CON H、またはCH=CH、NHCOを表し、LaおよびLbは各々、(1−4C)アル キレンを表し、nおよびmの一方は0または1であって、他方は0であり、およ びR14は、置換されていないフェニルもしくはヘテロ芳香族基、または1つもし くは2つのハロゲン;ニトロ;シアノ;ヒドロキシイミノ;(1−10C)アルキ ル;(2−10C)アルケニル;(2−10C)アルキニル;(3−8C)シクロアル キル;4−(1,1−ジオキソテトラヒドロ−1,2− チアジニル);ハロ(1−10C)アルキル;シアノ(2−10C)アルケニル;フ ェニル;(CH2)zX3R15(式中、zは、0または1〜4の整数であり、X3は、 O、S、NR16、CO、CH(OH)、COO、OCO、CONR17、NR18CO 、NHSO2、NHSO2NR17、NHCONH、OCONR19、またはNR19C OOを表し、R15は、水素、(1−10C)アルキル、フェニル(1−4C)アルキ ル、(1−10C)ハロアルキル、(1−4C)アルコキシカルボニル(1−4C)ア ルキル、(1−4C)アルキルスルホニルアミノ(1−4C)アルキル、(N−(1− 4C)アルコキシカルボニル)(1−4C)アルキルスルホニルアミノ(1−4C)ア ルキル、(3−10C)アルケニル、(3−10C)アルキニル、(3−8C)シクロ アルキル、カンホリル、または置換されていない芳香族もしくはヘテロ芳香族基 、もしくは1つもしくは2つのハロゲン、(1−4C)アルキル、および(1−4 C)アルコキシで置換されている芳香族もしくはヘテロ芳香族基を表し、および R16、R17、R18、およびR19は各々独立して、水素または(1−10C)アルキ ルを表すか、またはR15およびR16、R17、R18、もしくはR19は、それらが結 合している窒素原子と一緒になって、アゼチジニル、ピロリジニル、ピペリジニ ル、もしくはモルホリノ基を形成する。)で置換されているフェニルもしくはヘ テロ芳香族基を表す。)の基を表し;および R21は、水素原子、ハロゲン原子、(1−4C)アルキル基、または(1−4C) アルコキシ基を表す。] の基を表す、請求項8に記載の使用。 11.R1が、2−ナフチル、または式: [式中、 R20は、ハロゲン;ニトロ;シアノ;(1−10C)アルキル;(2−10C)ア ルケニル;(2−10C)アルキニル;(3−8C)シクロアルキル;ハロ(1− 10C)アルキル;(CH2)yX1R9(式中、yは、0または1〜4の整数であり 、X1は、O、S、NR10、CO、COO、OCO、CONR11、NR12CO、 またはOCONR13を表し、R9は、水素、(1−10C)アルキル、(3−10C )アルケニル、(3−10C)アルキニル、または(3−8C)シクロアルキルを表 し、およびR10、R11、R12、およびR13は各々独立して、水素または(1−1 0C)アルキルを表すか、またはR9およびR10、R11、R12、もしくはR13は、 それらが結合している窒素原子と一緒になって、アゼチジニル、ピロリジニル、 ピペリジニル、もしくはモルホリノ基を形成する。);チエニル;フリル;オキ サゾリル;イソオキサゾリル;ピラゾリル;イミダゾリル;チアゾリル;ピリジ ル;ピリダジニル;ピリミジニル;ジヒドロチエニル;ジヒドロフリル;ジヒド ロチオピラニル;ジヒドロピラニル;テトラヒドロチエニル;テトラヒドロフリ ル;テトラヒドロチオピラニル;テトラヒドロピラニル;インドリル;ベンゾフ リル;ベンゾチエニル;ベンゾイミダゾリル;および式R14−(La)n−X2−(Lb )m(式中、X2は、結合、O、NH、S、SO、SO2、CO、CONH、また はNHCOを表し、LaおよびLbは各々、(1−4C)アルキレンを表し、nおよ びmの一方は0または1であって、他方は0であり、およびR14は、置換されて いないフェニル基、または1つもしくは2つのハロゲン;ニトロ;シアノ;(1 −10C)アルキル;(2−10C)アルケニル;(2−10C)アルキニル;(3− 8C)シクロアルキル;ハロ(1−10C)アルキル;(CH2)zX3R15(式中、z は、0または1〜4の整数であり、X3は、O、S、NR16、CO、COO、O CO、CONR17、NR18CO、OCONR19を表し、R15は、水素、(1−1 0C)アルキル、(3−10C)アルケニル、(3−10C)アルキニル、または(3 −8C)シクロアルキルを表し、およびR16、R17、R18、およびR19は各々独 立して、水素または(1−10C)アルキルを表すか、またはR15およびR16、R17 、R18、もしくはR19は、それらが結合している窒素原子と一緒になって、ア ゼチジニル、ピロリジニル、ピペリジニル、もしくはモルホリノ基を形成する。 )で置換されているフェニル基を表す。)の基を表し;および R21は、水素原子、ハロゲン原子、(1−4C)アルキル基、または(1−4 C)アルコキシ基を表す。] の基を表す、請求項9に記載の使用。 12.R1が、2−ナフチル、4−ブロモフェニル、4−ベンズアミドフェニル 、4−メチルフェニル、4−イソプロピルフェニル、4−イソブチルフェニル、 4−t−ブチルフェニル、4−メトキシフェニル、4−イソプロポキシフェニル 、4−シクロペンチルフェニル、4−シクロヘキシルフェニル、4−(2−ヒド ロキシメチルフェニル)フェニル、4−(4−ヒドロキシメチルフェニル)フェニ ル、4−(2−フリル)フェニル、4−(3−フリル)フェニル、4−(2−チエニ ル)フェニル、4−(3−チエニル)フェニル、4−(ピロリジン−1−イル)フェ ニル、4−(ピペリジン−1−イル)フェニル、3−クロロ−4−ピペリジン−1 −イルフェニル、4−ベンジルオキシフェニル、4−(2−フルオロフェニル)フ ェニル、4−(3−フルオロフェニル)フェニル、4−(2−ホルミルフェニル)フ ェニル、4−(3−ホルミルフェニル)フェニル、4−(4−ホルミルフェニル)フ ェニル、4−(4−メチルフェニル)フェニル、または4−(2−メトキシフェニ ル)フェニルを表す、請求項11に記載の使用。 13.認識障害;神経変性障害;加齢と関係のある痴呆;加齢により誘発される 記憶障害;運動障害;薬物により誘発される状態の反転;うつ病;注意欠陥障害 ;注意欠陥多動障害;精神病;精神病と関連のある認識欠陥;または薬物により 誘発される精神病の処置のための薬剤の製造のための、式: R1−L−NHSO2R2 I [式中、 R1は、置換されていない芳香族もしくはヘテロ芳香族基、または置換されて いる芳香族もしくはヘテロ芳香族基を表し; R2は、(1−6C)アルキル、(3−6C)シクロアルキル、(1−6C)フルオ ロアルキル、(1−6C)クロロアルキル、(2−6C)アルケニル、(1−4C)ア ルコキシ(1−4C)アルキル、置換されていないフェニル、もしくはハロゲン、 (1−4C)アルキル、もしくは(1−4C)アルコキシで置換されているフェニル 、または式R3R4N(式中、R3およびR4は各々独立して、(1−4C)アルキル を表すか、またはそれらが結合している窒素原子と一緒になって、アゼチジニル 、 ピロリジニル、ピペリジニル、モルホリノ、ピペラジニル、ヘキサヒドロアゼピ ニル、もしくはオクタヒドロアゾシニル基を形成する。)の基を表し;および Lは、置換されていない(2−4C)アルキレン鎖、もしくは(1−6C)アルキ ル、アリール(1−6C)アルキル、(2−6C)アルケニル、アリール(2−6C) アルケニル、およびアリールから独立して選択される1つもしくは2つの置換基 で置換されている(2−4C)アルキレン鎖を表すか、またはこの2つの置換基が 、それらが結合する炭素原子と一緒になって、(3−8C)炭素環式環を形成する 。] の化合物またはその医薬的に許容され得る塩の使用。 14.記憶または学習能力を改善するための薬剤の製造のための、式: R1−L−NHSO2R2 I [式中、 R1は、置換されていない芳香族もしくはヘテロ芳香族基、または置換されて いる芳香族もしくはヘテロ芳香族基を表し; R2は、(1−6C)アルキル、(3−6C)シクロアルキル、(1−6C)フルオ ロアルキル、(1−6C)クロロアルキル、(2−6C)アルケニル、(1−4C)ア ルコキシ(1−4C)アルキル、置換されていないフェニル、もしくはハロゲン、 (1−4C)アルキル、もしくは(1−4C)アルコキシで置換されているフェニル 、または式R3R4N(式中、R3およびR4は各々独立して、(1−4C)アルキル を表すか、またはそれらが結合している窒素原子と一緒になって、アゼチジニル 、ピロリジニル、ピペリジニル、モルホリノ、ピペラジニル、ヘキサヒドロアゼ ピニル、もしくはオクタヒドロアゾシニル基を形成する。)の基を表し;および Lは、置換されていない(2−4C)アルキレン鎖、もしくは(1−6C)アルキ ル、アリール(1−6C)アルキル、(2−6C)アルケニル、アリール(2−6C) アルケニル、およびアリールから独立して選択される1つもしくは2つの置換基 で置換されている(2−4C)アルキレン鎖を表すか、またはこの2つの置換基が 、それらが結合する炭素原子と一緒になって、(3−8C)炭素環式環を形成する 。] の化合物またはその医薬的に許容され得る塩の使用。 15.式: [式中、 R1は、置換されていないナフチル基、もしくはフェニル、フリル、チエニル 、もしくはピリジル基、または ハロゲン;ニトロ;シアノ;ヒドロキシイミノ;(1−10C)アルキル;(2 −10C)アルケニル;(2−10C)アルキニル;(3−8C)シクロアルキル ;ヒドロキシ(3−8C)シクロアルキル;オキソ(3−8C)シクロアルキル; ハロ(1−10C)アルキル;(CH2)yX1R9(式中、yは、0または1〜4の 整数であり、X1は、O、S、NR10、CO、COO、OCO、CONR11、 NR12CO、NR12COCOO、またはOCONR13を表し、R9は、水素、( 1−10C)アルキル、(3−10C)アルケニル、(3−10C)アルキニル、 ピロリジニル、テトラヒドロフリル、モルホリノ、または(3−8C)シクロア ルキルを表し、およびR10、R11、R12、およびR13は各々独立して、水素ま たは(1−10C)アルキルを表すか、またはR9およびR10、R11、R12、も しくはR13は、それらが結合している窒素原子と一緒になって、アゼチジニル 、ピロリジニル、ピペリジニル、もしくはモルホリノ基を形成する。);N− (1−4C)アルキルピペラジニル;N−フェニル(1−4C)アルキルピペラジ ニル;チエニル;フリル;オキサゾリル;イソオキサゾリル;ピラゾリル;イ ミダゾリル;チアゾリル;ピリジル;ピリダジニル;ピリミジニル;ジヒドロ チエニル;ジヒドロフリル;ジヒドロチオピラニル;ジヒドロピラニル;ジヒ ドロチアゾリル;(1−4C)アルコキシカルボニル ジヒドロチアゾリル;(1 −4C)アルコキシカルボニル ジメチルジヒドロチアゾリル;テトラヒドロチ エニル;テトラヒドロフリル;テトラヒドロチオピラニル;テトラヒドロピラ ニル;インドリル;ベンゾフリル;ベンゾチエニル;ベンゾイミダゾリル;お よび式R14−(La)n−X2−(Lb)m(式中、X2は、結合、 O、NH、S、SO、SO2、CO、CH(OH)、CONH、NHCO、NH CONH、NHCOO、COCONH、OCH2CONH、またはCH=CH を表し、LaおよびLbは各々、(1−4C)アルキレンを表し、nおよびmの一 方は0または1であって、他方は0であり、およびR14は、置換されていない フェニルもしくはヘテロ芳香族基、または1つもしくは2つのハロゲン、ニト ロ、シアノ、ヒドロキシイミノ、(1−10C)アルキル、(2−10C)アルケ ニル、(2−10C)アルキニル、(3−8C)シクロアルキル、4−(1,1−ジ オキソテトラヒドロ−1,2−チアジニル)、ハロ(1−10C)アルキル、シア ノ(2−10C)アルケニル、フェニル、および(CH2)zX3R15(式中、zは 、0または1〜4の整数であり、X3は、O、S、NR16、CO、CH(OH) 、COO、OCO、CONR17、NR18CO、NHSO2、NHSO2NR17、 NHCONH、OCONR19、またはNR19COOを表し、R15は、水素、( 1−10C)アルキル、フェニル(1−4C)アルキル、(1−10C)ハロアル キル、(1−4C)アルコキシカルボニル(1−4C)アルキル、(1−4C)アル キルスルホニルアミノ(1−4C)アルキル、(N−(1−4C)アルコキシカル ボニル)(1−4C)アルキルスルホニルアミノ(1−4C)アルキル、(3−10 C)アルケニル、(3−10C)アルキニル、(3−8C)シクロアルキル、カン ホリル、または置換されていない芳香族もしくはヘテロ芳香族基、もしくは1 つもしくは2つのハロゲン、(1−4C)アルキル、および(1−4C)アルコキ シで置換されている芳香族もしくはヘテロ芳香族基を表し、およびR16、R17 、R18、およびR19は各々独立して、水素または(1−10C)アルキルを表す か、またはR15およびR16、R17、R18、もしくはR19は、それらが結合して いる窒素原子と一緒になって、アゼチジニル、ピロリジニル、ピペリジニル、 もしくはモルホリノ基を形成する。)で置換されているフェニルもしくはヘテ ロ芳香族基を表す。)の基から独立して選択される1つもしくは2つの置換基 で置換されているナフチル基、もしくはフェニル、フリル、チエニル、もしく はピリジル基 を表し; R2は、(1−6C)アルキル、(3−6C)シクロアルキル、(1−6C)フルオ ロアルキル、(1−6C)クロロアルキル、(2−6C)アルケニル、(1−4C)ア ルコキシ(1−4C)アルキル、置換されていないフェニル、もしくはハロゲン、 (1−4C)アルキル、もしくは(1−4C)アルコキシで置換されているフェニル 、または式R3R4N(式中、R3およびR4は各々独立して、(1−4C)アルキル を表すか、またはそれらが結合している窒素原子と一緒になって、アゼチジニル 、ピロリジニル、ピペリジニル、モルホリノ、ピペラジニル、ヘキサヒドロアゼ ピニル、もしくはオクタヒドロアゾシニル基を形成する。)の基を表し;および R5、R6、R7、およびR8のいずれか1つは、(1−6C)アルキル;アリール (1−6C)アルキル;(2−6C)アルケニル;アリール(2−6C)アルケニル; もしくはアリールを表すか、またはR5、R6、R7、およびR8の2つは、それら が結合している炭素原子と一緒になって、(3−8C)炭素環式環を形成して;R5 、R6、R7、およびR8の残りのものは、水素を表す。] (但し、N−(2,2−ジフェニルエチル)メタンスルホンアミド、並びにR7がメ チルを表し;R5、R6、およびR8が水素を表し;および (a)R1がフェニルを表し;およびR2がメチル、ブチル、フルオロメチル、 ジフルオロメチル、トリフルオロメチル、ジメチルアミノ、またはピペリジニル を表すか;または (b)R1が4−クロロフェニル、4−ニトロフェニル、または3−メトキシ フェニルを表し;およびR2がメチルを表すか;または (c)R1が4−ニトロフェニルを表し;およびR2がトリフルオロメチルを表 す; 式Iの化合物を除く。) の化合物またはその医薬的に許容され得る塩。 16.R1が、置換されていないナフチル基もしくはフェニル基、または ハロゲン;ニトロ;シアノ;(1−10C)アルキル;(2−10C)アルケニル ;(2−10C)アルキニル;(3−8C)シクロアルキル;ハロ(1−10C)ア ルキル;(CH2)yX1R9(式中、yは、0または1〜4の整数であり、X1は 、O、S、NR10、CO、COO、OCO、CONR11、NR12CO、OCO NR13を表し、R9は、水素、(1−10C)アルキル、(3−10C)アル ケニル、(3−10C)アルキニル、または(3−8C)シクロアルキルを表し、 およびR10、R11、R12、およびR13は各々独立して、水素または(1−10 C)アルキルを表すか、またはR9およびR10、R11、R12、もしくはR13は、 それらが結合している窒素原子と一緒になって、アゼチジニル、ピロリジニル 、ピペリジニル、もしくはモルホリノ基を形成する。);チエニル;フリル; オキサゾリル;イソオキサゾリル;ピラゾリル;イミダゾリル;チアゾリル; ピリジル;ピリダジニル;ピリミジニル;ジヒドロチエニル;ジヒドロフリル ;ジヒドロチオピラニル;ジヒドロピラニル;テトラヒドロチエニル;テトラ ヒドロフリル;テトラヒドロチオピラニル;テトラヒドロピラニル;インドリ ル;ベンゾフリル;ベンゾチエニル:ベンゾイミダゾリル;および式R14−( La)n−X2−(Lb)m(式中、X2は、結合、O、NH、S、SO、SO2、CO 、CONH、またはNHCOを表し、LaおよびLbは各々、(1−4C)アルキ レンを表し、nおよびmの一方は0または1であって、他方は0であり、およ びR14は、置換されていないフェニル基、または1つもしくは2つのハロゲン 、ニトロ、シアノ、(1−10C)アルキル、(2−10C)アルケニル、(2− 10C)アルキニル、(3−8C)シクロアルキル、ハロ(1−10C)アルキル 、および(CH2)zX3R15(式中、zは、0または1〜4の整数であり、X3は 、O、S、NR16、CO、COO、OCO、CONR17、NR18CO、OCO NR19を表し、R15は、水素、(1−10C)アルキル、(3−10C)アルケニ ル、(3−10C)アルキニル、または(3−8C)シクロアルキルを表し、およ びR16、R17、R18、およびR19は各々独立して、水素または(1−10C)ア ルキルを表すか、またはR15およびR16、R17、R18、もしくはR19は、それ らが結合している窒素原子と一緒になって、アゼチジニル、ピロリジニル、ピ ペリジニル、もしくはモルホリノ基を形成する。)で置換されているフェニル 基を表す。)の基から独立して選択される1つもしくは2つの置換基で置換さ れているナフチル基もしくはフェニル基 を表し;および R2が、(1−6C)アルキル、(1−6C)フルオロアルキル、(2−6C)アル ケニル、または式R3R4N(式中、R3およびR4は各々独立して、(1−4C) アルキルを表すか、またはそれらが結合している窒素原子と一緒になって、アゼ チジニル、ピロリジニル、ピペリジニル、モルホリノ、ピペラジニル、ヘキサヒ ドロアゼピニル、もしくはオクタヒドロアゾシニル基を形成する。)の基を表す ; 請求項15に記載の化合物。 17.R6およびR7が、水素を表す、請求項15または請求項16に記載の化合 物。 18.R5およびR8が各々独立して、水素もしくは(1−4C)アルキルを表すか 、またはそれらが結合している炭素原子と一緒になって、(3−8C)炭素環式環 を形成する、請求項17に記載の化合物。 19.R8が、メチルもしくはエチルを表すか、またはR5およびR8が、それら が結合している炭素原子と一緒になって、シクロプロピル環を形成する、請求項 18に記載の化合物。 20.R1が、2−ナフチル、または式: [式中、 R20は、ハロゲン;ニトロ;シアノ;ヒドロキシイミノ;(1−10C)アルキ ル;(2−10C)アルケニル;(2−10C)アルキニル;(3−8C)シクロアル キル;ヒドロキシ(3−8C)シクロアルキル;オキソ(3−8C)シクロアルキル ;ハロ(1−10C)アルキル;(CH2)yX1R9(式中、yは、0または1〜4の 整数であり、X1は、O、S、NR10、CO、COO、OCO、CONR11、N R12CO、NR12COCOO、OCONR13を表し、R9は、水素、(1−10C )アルキル、(3−10C)アルケニル、(3−10C)アルキニル、ピロリジ ニル、テトラヒドロフリル、モルホリノ、または(3−8C)シクロアルキルを表 し、およびR10、R11、R12、およびR13は各々独立して、水素または(1−1 0C)アルキルを表すか、またはR9およびR10、R11、R12、もしくはR13は、 それらが結合している窒素原子と一緒になって、アゼチジニル、ピロリジニル、 ピペリジニル、もしくはモルホリノ基を形成する。);N−(1−4C)アルキル ピペラジニル;N−フェニル(1−4C)アルキルピペラジニル;チエニル;フリ ル;オキサゾリル;イソオキサゾリル;ピラゾリル;イミダゾリル;チアゾリル ;ピリジル;ピリダジニル;ピリミジニル;ジヒドロチエニル;ジヒドロフリル ;ジヒドロチオピラニル;ジヒドロピラニル;ジヒドロチアゾリル;(1−4C) アルコキシカルボニル ジヒドロチアゾリル;(1−4C)アルコキシカルボニル ジメチルジヒドロチアゾリル;テトラヒドロチエニル;テトラヒドロフリル;テ トラヒドロチオピラニル;テトラヒドロピラニル;インドリル;ベンゾフリル; ベンゾチエニル;ベンゾイミダゾリル;および式R14−(La)n−X2−(Lb)m( 式中、X2は、結合、O、NH、S、SO、SO2、CO、CONH、NHCO、 NHCONH、NHCOO、COCONH、OCH2CONH、またはCH=C H、NHCOを表し、LaおよびLbは各々、(1−4C)アルキレンを表し、nお よびmの一方は0または1であって、他方は0であり、およびR14は、置換され ていないフェニルもしくはヘテロ芳香族基、または1つもしくは2つのハロゲン ;ニトロ;シアノ;ヒドロキシイミノ;(1−10C)アルキル;(2−10C)ア ルケニル;(2−10C)アルキニル;(3−8C)シクロアルキル;4−(1,1− ジオキソテトラヒドロ−1,2−チアジニル);ハロ(1−10C)アルキル;シア ノ(2−10C)アルケニル;フェニル;(CH2)zX3R15(式中、zは、0また は1〜4の整数であり、X3は、O、S、NR16、CO、CH(OH)、COO、 OCO、CONR17、NR18CO、NHSO2、NHSO2NR17、NHCONH 、OCONR19、またはNR19COOを表し、R15は、水素、(1−10C)アル キル、フェニル(1−4C)アルキル、(1−10C)ハロアルキル、(1−4C)ア ルコキシカルボニル(1−4C)アルキル、(1−4C)アルキルスルホニルアミノ (1−4C)アルキル、(N−(1−4C)アルコキシカルボニル)(1−4C)アルキ ルスルホニルアミノ(1−4C)アルキル、(3−10 C)アルケニル、(3−10C)アルキニル、(3−8C)シクロアルキル、カンホ リル、または置換されていない芳香族もしくはヘテロ芳香族基、もしくは1つも しくは2つのハロゲン、(1−4C)アルキル、および(1−4C)アルコキシで置 換されている芳香族もしくはヘテロ芳香族基を表し、およびR16、R17、R18、 およびR19は各々独立して、水素または(1−10C)アルキルを表すか、または R15およびR16、R17、R18、もしくはR19は、それらが結合している窒素原子 と一緒になって、アゼチジニル、ピロリジニル、ピペリジニル、もしくはモルホ リノ基を形成する。)で置換されているフェニルもしくはヘテロ芳香族基を表す 。)の基を表し;および R21は、水素原子、ハロゲン原子、(1−4C)アルキル基、または(1−4C) アルコキシ基を表す。] の基を表す、請求項15〜19のいずれかに記載の化合物。 21.R1が、2−ナフチル、または式: [式中、 R20は、ハロゲン;ニトロ;シアノ;(1−10C)アルキル;(2−10C)ア ルケニル;(2−10C)アルキニル;(3−8C)シクロアルキル;ハロ(1−1 0C)アルキル;(CH2)yX1R9(式中、yは、0または1〜4の整数であり、 X1は、O、S、NR10、CO、COO、OCO、CONR11、NR12CO、O CONR13を表し、R9は、水素、(1−10C)アルキル、(3−10C)アルケ ニル、(3−10C)アルキニル、または(3−8C)シクロアルキルを表し、およ びR10、R11、R12、およびR13は各々独立して、水素または(1−10C)アル キルを表すか、またはR9およびR10、R11、R12、もしくはR13は、それらが 結合している窒素原子と一緒になって、アゼチジニル、ピロリジニル、ピペリジ ニル、もしくはモルホリノ基を形成する。);チエニル;フリル;オキサ ゾリル;イソオキサゾリル;ピラゾリル;イミダゾリル;チアゾリル;ピリジル ;ピリダジニル;ピリミジニル;ジヒドロチエニル;ジヒドロフリル;ジヒドロ チオピラニル;ジヒドロピラニル;テトラヒドロチエニル;テトラヒドロフリル ;テトラヒドロチオピラニル;テトラヒドロピラニル;インドリル;ベンゾフリ ル;ベンゾチエニル;ベンゾイミダゾリル;および式R14−(La)n−X2−(Lb)m (式中、X2は、結合、O、NH、S、SO、SO2、CO、CONH、または NHCOを表し、LaおよびLbは各々、(1−4C)アルキレンを表し、nおよび mの一方は0または1であって、他方は0であり、およびR14は、置換されてい ないフェニル基、または1つもしくは2つのハロゲン;ニトロ;シアノ;(1− 10C)アルキル;(2−10C)アルケニル;(2−10C)アルキニル;(3−8 C)シクロアルキル;ハロ(1−10C)アルキル;(CH2)zX3R15(式中、zは 、0または1〜4の整数であり、X3は、O、S、NR16、CO、COO、OC O、CONR17、NR18CO、OCONR19を表し、R15は、水素、(1−10 C)アルキル、(3−10C)アルケニル、(3−10C)アルキニル、または(3− 8C)シクロアルキルを表し、およびR16、R17、R18、およびR19は各々独立 して、水素または(1−10C)アルキルを表すか、またはR15およびR16、R17 、R18、もしくはR19は、それらが結合している窒素原子と一緒になって、アゼ チジニル、ピロリジニル、ピペリジニル、もしくはモルホリノ基を形成する。) で置換されているフェニル基を表す。)の基を表し;および R21は、水素原子、ハロゲン原子、(1−4C)アルキル基、または(1−4C) アルコキシ基を表す。] の基を表す、請求項15〜19のいずれかに記載の化合物。 22.R1が、2−ナフチル、4−ブロモフェニル、4−ベンズアミドフェニル 、4−メチルフェニル、4−イソプロピルフェニル、4−イソブチルフェニル、 4−t−ブチルフェニル、4−メトキシフェニル、4−イソプロポキシフェニル 、4−シクロペンチルフェニル、4−シクロヘキシルフェニル、4−(4−(ヒド ロキシメチル)フェニル)フェニル、4−(2−(ヒドロキシメチル)フェニル)フェ ニル、4−(2−フリル)フェニル、4−(3−フリル)フェニル、4−(2−チエ ニル)フェニル、4−(3−チエニル)フェニル、4−(ピロリジン−1−イル)フ ェ ニル、4−(ピペリジン−1−イル)フェニル、3−クロロ−4−ピペリジン−1 −イルフェニル、4−ベンジルオキシフェニル、4−(2−フルオロフェニル)フ ェニル、4−(3−フルオロフェニル)フェニル、4−(2−ホルミルフェニル)フ ェニル、4−(3−ホルミルフェニル)フェニル、4−(4−ホルミルフェニル)フ ェニル、4−(4−メチルフェニル)フェニル、または4−(2−メトキシフェニ ル)フェニルを表す、請求項21に記載の化合物。 23.R2が、メチル、エチル、プロピル、2−プロピル、2−メチルプロピル 、シクロヘキシル、トリフルオロメチル、2,2,2−トリフルオロエチル、クロ ロメチル、エテニル、プロプ−2−エニル、メトキシエチル、フェニル、4−フ ルオロフェニル、またはジメチルアミノを表す、請求項15〜22のいずれかに 記載の化合物。 24.R2が、エチル、2−プロピル、またはジメチルアミノを表す、請求項2 3に記載の化合物。 25.N−2−(4−(3−チエニル)フェニル)プロピル 2−プロパンスルホン アミド; N−2−(4−(3−チエニル)フェニル)プロピル ジメチルスルファミド; N−2−(4−シクロペンチルフェニル)プロピル 2−プロパンスルホンアミ ド; N−2−(4−(4−(2−メタンスルホンアミドエチル)フェニル)フェニル)プ ロピル 2−プロパンスルホンアミド; N−2−(4−(5−ブロモ−[1,2,4]オキサジアゾール−3−イル)フェニ ル)プロピル 2−プロパンスルホンアミド; N−2−(4−(5−(2−メチル)テトラゾリル)フェニル)プロピル 2−プロ パンスルホンアミド; N−2−(4−(4−アミノフェニル)フェニル)プロピル 2−プロパンスルホ ンアミド; N−2−(4−(3−(5−(2−ヒドロキシ)エチル)イソオキサゾリル)フェニ ル)プロピル 2−プロパンスルホンアミド; N−2−(4−(5−(3−ブロモ)イソオキサゾリル)フェニル)プロピル 2− プロパンスルホンアミド; N−2−(4−(2−ピリジル)フェニル)プロピル 2−プロパンスルホンアミ ド; N−2−(4−(4−(2−(アセトアミド)エチル)フェニル)フェニル)プロピル 2−プロパンスルホンアミド; N−2−(4−N−(ベンズアミド)フェニル)プロピル 2−プロパンスルホン アミド; N−2−(4−N−(4−エチルベンズアミド)フェニル)プロピル 2−プロパ ンスルホンアミド; N−2−(4−N−(シクロブチルカルボキシアミド)フェニル)プロピル 2− プロパンスルホンアミド; N−2−(4−N−(5−イソオキサゾリルカルボキシアミド)フェニル)プロピ ル 2−プロパンスルホンアミド; N−2−(4−N−(6−クロロニコチニルカルバミド)フェニル)プロピル 2 −プロパンスルホンアミド; N−2−(4−N−(ピコニオイルカルバミド)フェニル)プロピル 2−プロパ ンスルホンアミド; N−2−(4−N−(ベンズアミド)フェニル)プロピル 2−ジメチルスルファ ミド; N−2−(2−チエン−3−イル−5−チエニル)プロピル 2−プロパンスル ホンアミド; (+)−N−2R−(4−(3−チエニル)フェニル)プロピル 2−プロパンスル ホンアミド; およびその医薬的に許容され得る塩から選択される、請求項15に記載の化合物 。 26.請求項15〜25のいずれかに記載の化合物、および医薬的に許容され得 る希釈剤または担体を含んでなる医薬組成物。 27.式: の化合物を、式: R2SO2X III [式中、Xは、脱離原子または基を表す。] の化合物と反応させた後、必要および/または所望である場合には、医薬的に許 容され得る塩を形成することを含んでなる、請求項15〜26のいずれかに記載 の化合物の製造方法。
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JP2001525844A (ja) * | 1997-05-16 | 2001-12-11 | ローディア シミ | ペルフルオロスルホンアミド、ペルスルホンイミド及びそれらの塩の合成方法並びにスルホニル化試薬 |
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- 1998-01-30 CA CA002278790A patent/CA2278790A1/en not_active Abandoned
- 1998-01-30 NZ NZ336559A patent/NZ336559A/xx unknown
- 1998-01-30 IL IL13097098A patent/IL130970A/xx not_active IP Right Cessation
- 1998-01-30 TR TR1999/02368T patent/TR199902368T2/xx unknown
- 1998-01-30 HU HU0002208A patent/HUP0002208A3/hu unknown
- 1998-01-30 KR KR1019997007012A patent/KR20000070753A/ko not_active Application Discontinuation
- 1998-01-30 UA UA99084464A patent/UA71892C2/uk unknown
- 1998-02-02 ZA ZA9800842A patent/ZA98842B/xx unknown
- 1998-02-02 CO CO98004892A patent/CO5080767A1/es unknown
- 1998-02-03 EP EP98300759A patent/EP0860428B1/en not_active Expired - Lifetime
- 1998-02-03 ES ES98300759T patent/ES2232914T3/es not_active Expired - Lifetime
- 1998-02-03 SI SI9830743T patent/SI0860428T1/xx unknown
- 1998-02-03 EP EP04104929A patent/EP1528055A2/en not_active Withdrawn
- 1998-02-03 DE DE69827984T patent/DE69827984T2/de not_active Expired - Lifetime
- 1998-02-03 AT AT98300759T patent/ATE284385T1/de not_active IP Right Cessation
- 1998-02-03 DK DK98300759T patent/DK0860428T3/da active
- 1998-02-03 PT PT98300759T patent/PT860428E/pt unknown
- 1998-02-04 AR ARP980100477A patent/AR011623A1/es unknown
- 1998-02-04 PE PE1998000078A patent/PE72899A1/es not_active Application Discontinuation
-
1999
- 1999-07-28 NO NO993667A patent/NO993667L/no not_active Application Discontinuation
-
2001
- 2001-07-25 US US09/912,809 patent/US6596716B2/en not_active Expired - Fee Related
-
2003
- 2003-05-29 US US10/447,619 patent/US7135487B2/en not_active Expired - Fee Related
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JP2001525844A (ja) * | 1997-05-16 | 2001-12-11 | ローディア シミ | ペルフルオロスルホンアミド、ペルスルホンイミド及びそれらの塩の合成方法並びにスルホニル化試薬 |
JP4865115B2 (ja) * | 1997-05-16 | 2012-02-01 | ローディア シミ | (ペルフルオロ)スルホニル化方法 |
JP2002338538A (ja) * | 2001-05-21 | 2002-11-27 | Takeda Schering-Plough Animal Health Kk | 新規スルホンアミド誘導体およびそれを含む魚類用抗寄生虫薬 |
WO2009057515A1 (ja) * | 2007-11-01 | 2009-05-07 | Ube Industries, Ltd. | スルホン酸フェニル化合物、それを用いた非水電解液及びリチウム電池 |
US8512897B2 (en) | 2007-11-01 | 2013-08-20 | Ube Industries, Ltd. | Phenyl sulfonate compound, nonaqueous electrolyte solution using the same, and lithium battery |
JP5375616B2 (ja) * | 2007-11-01 | 2013-12-25 | 宇部興産株式会社 | スルホン酸フェニル化合物、それを用いた非水電解液及びリチウム電池 |
JP2013509376A (ja) * | 2009-10-28 | 2013-03-14 | ドムペ・ソチエタ・ペル・アツィオーニ | ブラジキニン受容体アンタゴニストとして有用な2−アリール−プロピオンアミド誘導体およびそれらを含有する医薬組成物 |
JP2017206507A (ja) * | 2011-12-27 | 2017-11-24 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | 殺菌剤としてのヘテロアリールピペリジン誘導体及びヘテロアリールピペラジン誘導体 |
JP2015519308A (ja) * | 2012-04-10 | 2015-07-09 | ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア | 癌治療用組成物および方法 |
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