JP2000513735A - 5−アロイルナフタレン誘導体 - Google Patents
5−アロイルナフタレン誘導体Info
- Publication number
- JP2000513735A JP2000513735A JP10531568A JP53156898A JP2000513735A JP 2000513735 A JP2000513735 A JP 2000513735A JP 10531568 A JP10531568 A JP 10531568A JP 53156898 A JP53156898 A JP 53156898A JP 2000513735 A JP2000513735 A JP 2000513735A
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- alkyl
- hydroxy
- compound
- cyano
- 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.)
- Granted
Links
Classifications
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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
- C07D207/18—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07C311/15—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
- C07—ORGANIC CHEMISTRY
- 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
- C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
- C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
- C07C311/51—Y being a hydrogen or a carbon atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C317/22—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/24—Sulfones; Sulfoxides having sulfone or sulfoxide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/22—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and doubly-bound oxygen atoms bound to the same carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
- C07C323/67—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfonamide groups, bound to the carbon skeleton
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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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
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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
- C07D295/04—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
- C07D295/12—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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- 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
- C07D295/22—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 hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/40—Radicals substituted by oxygen atoms
- C07D307/46—Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/22—Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D405/02—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
- C07D405/06—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 carbon chain containing only aliphatic carbon atoms
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Luminescent Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式(I): [式中、 Aは、結合、−CH2−、−CH(OH)−、−C=NOR4−、−C(O)− 、−NR5−、−O−、又は−S(O)n−であり、ここにおいてnは0〜2の整 数であり、R4は水素又はアルキルであり、並びにR5は水素、アルキル又はアシ ルであり; Zは、式(B)、(C)、(D)、又は(E) により表される基であり: ここにおいて: n1は、0〜3であり; Xは、O又はSであり; R6及びR7は、独立して水素、アルキル、ハロゲンアルキル、シクロアルキル、 シクロアルキルアルキル、アシル、アルキルチオ、シクロアルキルチオ、シクロ アルキルアルキルチオ、アルコキシ、シクロアルキルオキシ、シクロアルキルア ルキルオキシ、ハロゲンアルキルオキシ、アルケニル、ハロゲン、シアノ、ニト ロ、ヒドロキシ、又はR9及びR10が独立して水素、アルキル又はアシルである −NR9R10から選択されるか;あるいはR6及びR7はこれらが互いに隣接する 場合にメチレンジオキシ又はエチレンジオキシを形成し; R8は、水素、アルキル、ハロゲンアルキル、アルコキシ、シクロアルキルオキ シ、ハロゲンアルキルオキシ、アルキルチオ、シクロアルキルチオ、ニトロ、シ アノ、ヒドロキシ、又はハロゲンであり; R1は、水素、アルキル、アルケニル、アルキニル、ハロゲンアルキル、シク ロアルキル、シクロアルキルアルキル、アルコキシ、アルケニルオキシ、シクロ アルキルオキシ、シクロアルキルアルキルオキシ、ハロゲンアルキルオキシ、ヒ ドロキシアルキルオキシ、アルコキシアルキルオキシ、アルキルチオ、シクロア ルキルチオ、シクロアルキルアルキルチオ、ヒドロキシ、ハロゲン、シアノ、カ ルボキシ、アルコキシカルボニル、アシル、−C=NOR4、−NR9R10、−C ONR9R10、−OCONR9R10、又は−OSO2R11であり、ここにおいて、 R4、R9、及びR10は前記に定義されるとおりであり、R11はアルキル、シクロ アルキル、又はハロゲンアルキルであり; R2は、水素、アルキル、アルコキシ、ハロゲン、ニトロ、又は−NR9R10で あり;並びに R3は、−SO2R12又は−SO2NR13R14であり、ここにおいて: R12はアルキル、ヒドロキシアルキル、アルコキシアルキル、カルボキシアルキ ル、又はアルコキシカルボニルアルキルであり; R13は水素、アルキル、又はアシルであり;並びに R14は水素、アルキル、ハロゲンアルキル、シクロアルキル、シクロアルキルア ルキル、アルケニル、ヒドロキシアルキル、アルコキシアルキル、アルコキシカ ルボニルアルキル、アミノ、アミノアルキル、アリール、アラルキル、ヘテロア ラルキル、ヘテロシクロ、ヘテロシクロアルキル、アシル、ヒドロキシ、又はア ルコキシであるか;あるいはR13及びR14は、それらが結合する窒素原子と一緒 になって場合によりヘテロシクロアミノ基を形成する] を有する化合物、その医薬的に許容される塩、プロドラッグ、個々の異性体又は 異性体の混合物。 2.Aが、−C=NOR4−、−O−、−S−、−NR5−、又は−C(O)−で ある請求項1に記載の化合物。 3.Zが、式(B)又は(D)により表される基である請求項1又は2に記載の 化合物。 4.Aが、−C(O)−である請求項1〜3のいずれか1項に記載の化合物。 5.R3が、−SO2R12であるか、又はR3が−SO2NR13R14である請求項1 〜4のいずれか1項に記載の化合物。 6.Zが、式(B)により表される基であり、ここにおいてR6及びR7は、独立 して水素、アルキル、シクロアルキル、アルコキシ、エテニル、ハロゲン、又は R9及びR10がアルキルである−NR9R10から選択され、並びにR2が、水素で ある請求項5に記載の化合物。 7.R3は、−SO2−(アルキル)−であるか、あるいはR3が−SO2NR13R14 である場合にR3はR14が水素、アルキル、ヒドロキシ又は2−ヒドロキシエ チルである−SO2NR13R14である請求項5又は6に記載の化合物。 8.R1が、水素、アルキル、アルコキシ、シクロアルコキシ、2−ヒドロキシ エチルオキシ、ヒドロキシ、ハロゲン、又はシアノであり;R6及びR7が、独立 して水素、アルキル、アルコキシ又はハロゲンである請求項5〜7のいずれか1 項に記載の化合物。 9.R1が、水素、メチル、ヒドロキシ、メトキシ、クロロ、又はシアノであり ;R3が−SO2Me又は−SO2NH2である請求項8に記載の化合物。 10.R6及びR7が、独立して水素、メチル、メトキシ、フルオロ、又はクロロ から選択される請求項5〜9のいずれか1項に記載の化合物。 11.R6が2位であり、かつR7が4位であるか、又はR6が3位であり、かつ R7が4位である請求項6〜10のいずれか1項に記載の化合物。 12.R1がシアノであり、R6及びR7が水素である、すなわち5−ベンゾイル −6−シアノ−2−メチルスルホニルナフタレンである請求項1に記載の化合物 。 13.R1がシアノであり、R6が水素であり、及びR7がフルオロである、すな わち5−(4−フルオロベンゾイル)−6−シアノ−2−メチルスルホニルナフ タレンである請求項1に記載の化合物。 14.R1がメトキシであり、R6が水素であり、及びR7がフルオロである、す なわち5−(4−フルオロベンゾイル)−6−メトキシ−2−ナフタレンスルホ ンアミドである請求項1に記載の化合物。 15.R1がシアノであり、R6が水素であり、及びR7がフルオロである、すな わち5−(4−フルオロベンゾイル)−6−シアノ−2−ナフタレンスルホンア ミドである請求項1に記載の化合物。 16.R1がメトキシであり、R6がフルオロであり、及びR7が水素である、す なわち5−(3−フルオロベンゾイル)−6−メトキシ−2−ナフタレンスルホ ンアミドである請求項1に記載の化合物。 17.Zが、式(D)(式中、XはSであって、かつ式(D)の2位においてA と結合する)により表される基であり;R2及びR8は水素である請求項1〜4の いずれか1項に記載の化合物。 18.R3が、−SO2R12、又は−SO2NR13R14であり;ここにおいてR12 はアルキルであり;R13は水素であり;及びR14は水素、アルキル、ヒドロキシ 、又は2−ヒドロキシエチルである請求項17に記載の化合物。 19.R1が、水素、アルキル、アルコキシ、シクロアルコキシ、2−ヒドロキ シエチルオキシ、ヒドロキシ、クロロ、又はシアノである請求項17又は18に 記載の化合物。 20.R3が−SO2Me、又は−SO2NH2であり、R1が水素、メチル、ヒド ロキシ、メトキシ、又はシアノである請求項19に記載の化合物。 21.医薬的に有効量の請求項1〜20のいずれか1項に記載の化合物、及び医 薬的に許容される非毒性賦形剤を含んでなる医薬組成物。 22.Aが−C(O)−である請求項1に記載の化合物の製造方法であって、 (1)式 (式中、R1、R2及びR12は請求項1に記載のとおりである) の化合物を、式ZC(O)L(式中、Lはアシル化条件下で脱離基であり、Zは 請求項1に記載のとおりである)のアシル化剤と反応させること、及び、 (2)場合により、基R1、R2、R6、R7、R8、及びR12のいずれかを修飾 すること、 を含んでなる製造方法。 23.治療活性物質として使用するための請求項1〜20のいずれか1項に記載 の化合物。 24.炎症性疾患、特には筋炎、滑膜炎、痛風、強直性脊椎炎、滑液包炎並びに 関節炎、好ましくはリューマチ性関節炎、及び変形性関節炎の治療に使用するた めの請求項1〜20のいずれか1項に記載の化合物。 25.自己免疫疾患、特に全身性狼瘡、紅斑性及びI型糖尿病の治療に使用する ための請求項1〜20のいずれか1項に記載の化合物。 26.炎症性又は自己免疫疾患の治療における請求項1〜20のいずれか1項に 記載の化合物の使用。 27.炎症性又は自己免疫疾患治療のための医薬の調製における請求項1〜20 のいずれか1項に記載の化合物の使用。
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US3646697P | 1997-01-28 | 1997-01-28 | |
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PCT/EP1998/000306 WO1998032732A1 (en) | 1997-01-28 | 1998-01-21 | 5-aroylnaphthalene derivatives |
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AU2001277560A1 (en) | 2000-08-09 | 2002-02-18 | F. Hoffmann-La Roche Ag | Quinolene derivatives as anti-inflammation agents |
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CN1675154A (zh) * | 2002-06-07 | 2005-09-28 | 科蒂科股份有限公司 | 抑制巨噬细胞移动抑制因子(mif)的细胞因子或生物活性的萘衍生物 |
EP1692101B1 (en) * | 2003-03-31 | 2011-07-06 | Council of Scientific and Industrial Research | Mercapto-phenyl-naphthyl-methane derivatives and preparation thereof |
DE602004002832T2 (de) | 2003-05-07 | 2007-06-06 | Osteologix A/S | Behandlung von knorpel/knochen-erkrankungen mit wasserlöslichen strontiumsalzen |
JP2009541219A (ja) * | 2006-06-12 | 2009-11-26 | メルク エンド カムパニー インコーポレーテッド | 高眼圧治療のための眼科組成物 |
WO2013086229A1 (en) * | 2011-12-07 | 2013-06-13 | Amgen Inc. | Bicyclic aryl and heteroaryl sodium channel inhibitors |
WO2014201173A1 (en) | 2013-06-12 | 2014-12-18 | Amgen Inc. | Bicyclic sulfonamide compounds as sodium channel inhibitors |
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