RU2001106631A - Производные бензола и их фармацевтическое применение - Google Patents
Производные бензола и их фармацевтическое применениеInfo
- Publication number
- RU2001106631A RU2001106631A RU2001106631/04A RU2001106631A RU2001106631A RU 2001106631 A RU2001106631 A RU 2001106631A RU 2001106631/04 A RU2001106631/04 A RU 2001106631/04A RU 2001106631 A RU2001106631 A RU 2001106631A RU 2001106631 A RU2001106631 A RU 2001106631A
- Authority
- RU
- Russia
- Prior art keywords
- group
- substituent
- chr
- general formula
- benzene
- Prior art date
Links
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical class C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 15
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 125000005842 heteroatom Chemical group 0.000 claims 7
- -1 R 21 Chemical compound 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 239000004480 active ingredient Substances 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000004423 acyloxy group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 102000005741 Metalloproteases Human genes 0.000 claims 1
- 108010006035 Metalloproteases Proteins 0.000 claims 1
- 102000003945 NF-kappa B Human genes 0.000 claims 1
- 108010057466 NF-kappa B Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002257 antimetastatic agent Substances 0.000 claims 1
- 239000003435 antirheumatic agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000021164 cell adhesion Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 210000004969 inflammatory cell Anatomy 0.000 claims 1
- 239000011159 matrix material Substances 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000000770 proinflammatory effect Effects 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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- A—HUMAN NECESSITIES
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A61P35/00—Antineoplastic agents
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- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- 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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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C233/60—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
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- C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C233/61—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
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- C07C233/62—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
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- C07C233/63—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
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- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/56—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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- C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
- C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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- C07C247/00—Compounds containing azido groups
- C07C247/02—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton
- C07C247/08—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being unsaturated
- C07C247/10—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being unsaturated and containing rings
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- C07C251/34—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C251/48—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
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- C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
- C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
- C07C255/44—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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- C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
- C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
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- 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
- C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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- C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
- C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
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- C07C323/39—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 nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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- 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
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- C07D209/58—[b]- or [c]-condensed
- C07D209/72—4,7-Endo-alkylene-iso-indoles
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Claims (15)
1. Производные бензола следующей общей формулы (I) или их фармацевтически приемлемые соли
где R1 представляет собой циклоалкильную группу, имеющую заместитель, или циклоалкенильную группу, имеющую заместитель;
R2 представляет атом водорода или алкильную группу;
R3-R10, которые могут быть одинаковыми или отличными друг от друга, представляют собой атом водорода, атом галогена, гидроксильную группу, меркаптогруппу, нитрогруппу, цианогруппу, трифторметильную группу, алкильную группу, алкоксильную группу, алкилтиогруппу, аминогруппу, которая может быть замещена алкильной группой или аминозащитной группой, ацилоксигруппу, ацильную группу, карбоксильную группу, алкоксикарбонильную группу или карбамоильную группу;
Y представляет собой группу следующей общей формулы (II), (III) или (IV)
где R11 и R13, каждый, представляют атом водорода или алкильную группу, R12 и R14, каждый, представляют алкильную группу, которая может иметь заместитель, циклоалкильную группу, которая может иметь заместитель, циклоалкенильную группу, которая может иметь заместитель, арильную группу, которая может иметь заместитель, ароматическую гетероциклическую группу, содержащую один или несколько гетероатомов, которая может иметь заместитель, или насыщенную гетероциклическую группу, содержащую один или несколько гетероатомов, которая может иметь заместитель, и R15 и R16, каждый, представляют алкильную группу или арильную группу, которые могут образовывать цикл вместе, и n и m, каждый, являются целым, выбранным 0 - 6;
Х- представляет собой межатомную связь, или является любым из -О-, -O-CHR17-, -O-CHR18-O-, -O-СО-, -СО-O-, -O-CS-, -CS-O-, -S-, -SO-, -SO2-, -S-CHR19-, -CHR20-S-, -S-CO-,-CO-S-, -S-CS-, -CS-S-, -SO2-NR21-, -NR22-SO2-, -NR23-, -NR24-CHR25-, -CHR26-NR27-, -CO-, -C(=NOR28), -C(=CHR29), -CO-CHR30-, -CHR31-CO-, -CO-NR32-, -NR33-CO-, -CR34R35-, -CHR36-CHR37- и -CR38=CR39-, где R17, R18, R19, R20, R21, R22, R25, R26, R29, R30, R31, R32, R33, R34, R38 и R39, каждый, представляют собой атом водорода или алкильную группу, R23, R24, R27 и R28, каждый, представляют атом водорода, алкильную группу или ацильную группу, R36 и R37, каждый, представляют собой атом водорода, гидроксильную группу или алкильную группу, и R35 представляет собой атом водорода, гидроксильную группу, меркаптогруппу, цианогруппу, алкильную группу, которая может иметь заместитель, алкоксильную группу, алкилтиогруппу, ацилоксигруппу, аминогруппу, которая может быть замещена алкильной группой или аминозащитной группой, карбоксильную группу, алкоксикарбонильную группу или карбамоильную группу.
2. Производные бензола или их фармацевтически приемлемые соли по п.1, где R1 в общей формуле (I) является циклоалкильной группой, имеющей заместитель.
3. Производные бензола или их фармацевтически приемлемые соли по п.1, где R1 в общей формуле (I) является циклопропильной группой, имеющей заместитель.
4. Производные бензола или их фармацевтически приемлемые соли по п.1, где R1 в общей формуле (I) является 2,2-диметилциклопропильной группой или 2,2-дихлорциклопропильной группой.
5. Производные бензола или их фармацевтически приемлемые соли по п.4, где R12 в общей формуле (II) является 2,2-диметилциклопропильной группой или 2,2-дихлорциклопропильной группой, и n = 0.
6. Производные бензола или их фармацевтически приемлемые соли по п.1, где R3-R10 в общей формуле (I), каждый, является атомом водорода.
7. Производные бензола или их фармацевтически приемлемые соли по п.6, где Y в общей формуле (I) представлен общей формулой (II)
где R11 представляет атом водорода или алкильную группу;
R12 представляет алкильную группу, которая может иметь заместитель, циклоалкильную группу, которая может иметь заместитель, циклоалкенильную группу, которая может иметь заместитель, арильную группу, которая может иметь заместитель, ароматическую гетероциклическую группу, имеющую один или более гетероатомов, которая может иметь заместитель, или насыщенную гетероциклическую группу, имеющую один или более гетероатомов, которая может иметь заместитель, а n является целым числом, выбранным из 0-6.
8. Производные бензола или их фармацевтически приемлемые соли по.6, где Y в общей формуле (I) представлен общей формулой (II)
где R13 представляет атом водорода или алкильную группу;
R14 представляет алкильную группу, которая может иметь заместитель, циклоалкильную группу, которая может иметь заместитель, циклоалкенильную группу, которая может иметь заместитель, арильную группу, которая может иметь заместитель, ароматическую гетероциклическую группу, имеющую один или более гетероатомов, которая может иметь заместитель, или насыщенную гетероциклическую группу, имеющую один или несколько гетероатомов, которая может иметь заместитель, и n является целым числом, выбранным из 0-6.
10. Производные бензола или их фармацевтически приемлемые соли по любому из пп.3-9, где R1 в общей формуле (I) является циклопропильной группой, имеющей заместитель, и атом углерода, соседний с карбонильной группой в циклопропильной группе, имеет абсолютную конфигурацию S.
11. Производные бензола или их фармацевтически приемлемые соли по любому из пп.3-9, где R1 в общей формуле (I) является циклопропильной группой, имеющей заместитель, и атом углерода, соседний с карбонильной группой в циклопропильной группе, имеет абсолютную конфигурацию R.
12. Производные бензола или их фармацевтически приемлемые соли по п.1, где производные бензола общей формулы (I) представлены нижеследующей общей формулой (Iа)
где R1 и R2 такие, как указано для общей формулы (I);
Y1 такой, как указано для общих формул (II) и (III), R11, R13, n и m такие, как указано для общих формул (II) и (III), R12 и R14, каждый, представляют алкильную группу, которая может иметь заместитель, циклоалкильную группу, которая может иметь заместитель, циклоалкенильную группу, которая может иметь заместитель, арильную группу, которая может иметь заместитель, или ароматическую гетероциклическую группу, имеющую один или более гетероатомов, которая может иметь заместитель;
X1- представляет собой -О-, -O-CHR17-, -CHR18-O-, -O-СО-, -СО-O-, -O-CS-, -CS-O-, -S-, -SO-, -SO2-, -S-CHR19-, -CHR20-S-, -S-CO-, -CO-S-, -S-CS-, -CS-S-, -SO2-NR21-, -NR22-SO2-, -NR23-, -NR24-CHR25-, -CHR26-NR27-, -CO-, -C(=NOR28), -C(=CHR29), -CO-CHR30-, -CHR31-CO-, -CO-NR32-, -NR33-CO-, -CR34R35-, -CHR36-CHR37- и -CR38=CR39-, где заместители с R17 по R39 определены в формуле (I).
13. Ингибитор активации АР-1 или NF-каппа В, который содержит производное бензола или его фармацевтически приемлемую соль по любому из пп.1-12 в качестве активного ингредиента.
14. Ингибитор продукции провоспалительных цитокинов, ингибитор продукции матриксных металлопротеаз или ингибитор экспрессии фактора воспалительной клеточной адгезии, который содержит производное бензола или его фармацевтически приемлемую соль по любому из пп.1-12 в качестве активного ингредиента.
15. Противовоспалительный агент, противоревматический агент, иммунодепрессант, ингибитор метастазирования злокачественных опухолей, средство против артериосклероза и противовирусный агент, который содержит производное бензола или его фармацевтически приемлемую соль по любому из пп.1-12 в качестве активного ингредиента.
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2443671C2 (ru) * | 2006-07-28 | 2012-02-27 | Клариант Спешиалти Файн Кемикалз (Фрэнс) | Новый способ синтеза (е)-стильбеновых производных, который позволяет получить ресвератрол и писатаннол |
RU2451664C2 (ru) * | 2006-09-07 | 2012-05-27 | Чжэцзян Даде Фармасьютикал Груп Ко.Лтд | Способы производства и использования этоксикомбретастатинов и пролекарства на их основе |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU5570600A (en) * | 1999-07-01 | 2001-01-22 | Ajinomoto Co., Inc. | Heterocyclic compounds and medicinal use thereof |
EP1211240A4 (en) | 1999-09-01 | 2003-02-12 | Ajinomoto Kk | BISCYCLOPROPANOCARBOXYLIC ACID AMIDE COMPOUNDS AND MEDICINAL USE THEREOF |
EP1174129A1 (en) * | 2000-07-17 | 2002-01-23 | Zenner, Hans Peter, Prof. Dr. med. | Use of a matrix-metalloprotease inhibitor for the treatment of cancer |
WO2002036547A1 (fr) * | 2000-11-01 | 2002-05-10 | Ajinomoto Co.,Inc. | Composes amides d'acide cyclopropanecarboxylique et utilisations medicales |
DE10059418A1 (de) * | 2000-11-30 | 2002-06-20 | Aventis Pharma Gmbh | Ortho, meta-substituierte Bisarylverbindungen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen |
CN101125138A (zh) | 2000-12-18 | 2008-02-20 | 株式会社医药分子设计研究所 | 炎症性细胞因子产生游离抑制剂 |
EP1378237A4 (en) | 2001-04-10 | 2009-03-25 | Nippon Shinyaku Co Ltd | THERAPEUTIC AGENT FOR CHRONIC JOINT RHEUMATISM |
PE20030701A1 (es) | 2001-12-20 | 2003-08-21 | Schering Corp | Compuestos para el tratamiento de trastornos inflamatorios |
TW200402291A (en) | 2002-06-06 | 2004-02-16 | Inst Med Molecular Design Inc | Antiallergic |
EA009051B1 (ru) | 2002-06-06 | 2007-10-26 | Инститьют Оф Медисинал Молекьюлар Дизайн. Инк. | О-замещенные гидроксиарильные производные |
US20060089395A1 (en) * | 2002-06-10 | 2006-04-27 | Susumu Muto | Nf-kb activation inhibitors |
US20040142993A1 (en) * | 2002-07-01 | 2004-07-22 | Carlo Battistini | Inhibitors of HCV NS5B polymerase |
US8088737B2 (en) | 2003-04-04 | 2012-01-03 | Incyte Corporation | Compositions, methods and kits relating to Her-2 cleavage |
EP1735268B1 (en) | 2004-03-15 | 2012-02-15 | Eli Lilly And Company | Opioid receptor antagonists |
ZA200700811B (en) * | 2004-08-06 | 2008-10-29 | Otsuka Pharma Co Ltd | Aromatic compound |
US20070258428A1 (en) * | 2006-04-24 | 2007-11-08 | Interdigital Technology Corporation | Method and apparatus for coordinating timing in a wireless local area network |
US7671058B2 (en) | 2006-06-21 | 2010-03-02 | Institute Of Medicinal Molecular Design, Inc. | N-(3,4-disubstituted phenyl) salicylamide derivatives |
CN101472597B (zh) * | 2006-06-22 | 2012-10-03 | 爱科来株式会社 | 核转录因子ap-1的表达抑制剂及使用其的药品和制品 |
ES2601856T3 (es) | 2007-06-08 | 2017-02-16 | Mannkind Corporation | Inhibidores de la IRE-1A |
WO2012112956A2 (en) * | 2011-02-19 | 2012-08-23 | The Broad Institute, Inc | Compounds and methods for targeting leukemic stem cells |
EP2810066B1 (en) * | 2012-01-24 | 2019-07-31 | Millennium Pharmaceuticals, Inc. | Methods of treatment of cancer |
JP5783380B2 (ja) * | 2012-03-23 | 2015-09-24 | Jsr株式会社 | 液晶配向剤および液晶配向膜の形成方法 |
WO2014074715A1 (en) * | 2012-11-07 | 2014-05-15 | Genentech, Inc. | Cyclopropyl amide derivatives |
CN115787126B (zh) * | 2022-12-02 | 2024-07-09 | 安徽威驰化工有限责任公司 | 一种基于吡啶盐酸盐制备高性能有机纤维的方法 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CH489198A (de) * | 1967-10-19 | 1970-04-30 | Ciba Geigy | Schädlingsbekämpfungsmittel |
US4181519A (en) * | 1977-01-21 | 1980-01-01 | Shell Oil Company | Diphenylamine derivative herbicides |
JPH0314835A (ja) | 1989-06-12 | 1991-01-23 | New Japan Chem Co Ltd | 芳香族環状ポリイミドの製造方法 |
ES2220929T3 (es) * | 1995-05-11 | 2004-12-16 | Applied Research Systems Ars Holding N.V. | Inhibidor de la actividad il-6. |
GB9520092D0 (en) * | 1995-10-02 | 1995-12-06 | Hoechst Roussel Ltd | Chemical compounds |
DE19624155A1 (de) * | 1996-06-18 | 1998-01-08 | Hoechst Ag | Substituierte Benzoesäurederivate, Verfahren zu ihrer Herstellung und die Anwendung der Verbindungen zur Behandlung von Krankheiten |
EP1079830A1 (en) * | 1998-05-22 | 2001-03-07 | Avanir Pharmaceuticals | BENZIMIDAZOLE ANALOGS AS DOWN-REGULATORS OF IgE |
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RU2443671C2 (ru) * | 2006-07-28 | 2012-02-27 | Клариант Спешиалти Файн Кемикалз (Фрэнс) | Новый способ синтеза (е)-стильбеновых производных, который позволяет получить ресвератрол и писатаннол |
RU2451664C2 (ru) * | 2006-09-07 | 2012-05-27 | Чжэцзян Даде Фармасьютикал Груп Ко.Лтд | Способы производства и использования этоксикомбретастатинов и пролекарства на их основе |
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US20050165114A1 (en) | 2005-07-28 |
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US7459585B2 (en) | 2008-12-02 |
WO2000015603A1 (fr) | 2000-03-23 |
US6703379B2 (en) | 2004-03-09 |
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