KR920701168A - 치환된 1-(알콕시-이미노알킬)이미다졸 유도체 - Google Patents
치환된 1-(알콕시-이미노알킬)이미다졸 유도체Info
- Publication number
- KR920701168A KR920701168A KR1019910701434A KR910701434A KR920701168A KR 920701168 A KR920701168 A KR 920701168A KR 1019910701434 A KR1019910701434 A KR 1019910701434A KR 910701434 A KR910701434 A KR 910701434A KR 920701168 A KR920701168 A KR 920701168A
- Authority
- KR
- South Korea
- Prior art keywords
- imidazol
- ethylidene
- acid
- phenyl
- formula
- Prior art date
Links
- 125000004666 alkoxyiminoalkyl group Chemical group 0.000 title 1
- 150000002460 imidazoles Chemical class 0.000 title 1
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 16
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 13
- 239000001257 hydrogen Substances 0.000 claims abstract 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 13
- 229910052736 halogen Inorganic materials 0.000 claims abstract 10
- 150000002367 halogens Chemical group 0.000 claims abstract 10
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 7
- 125000004953 trihalomethyl group Chemical group 0.000 claims abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 4
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 4
- 125000004414 alkyl thio group Chemical group 0.000 claims abstract 3
- 125000003118 aryl group Chemical group 0.000 claims abstract 3
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims abstract 3
- DSNBHJFQCNUKMA-SCKDECHMSA-N thromboxane A2 Chemical compound OC(=O)CCC\C=C/C[C@@H]1[C@@H](/C=C/[C@@H](O)CCCCC)O[C@@H]2O[C@H]1C2 DSNBHJFQCNUKMA-SCKDECHMSA-N 0.000 claims abstract 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 2
- 239000004215 Carbon black (E152) Substances 0.000 claims abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 230000015572 biosynthetic process Effects 0.000 claims abstract 2
- 201000010099 disease Diseases 0.000 claims abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 2
- 125000005678 ethenylene group Chemical group [H]C([*:1])=C([H])[*:2] 0.000 claims abstract 2
- 229910052731 fluorine Inorganic materials 0.000 claims abstract 2
- 239000011737 fluorine Substances 0.000 claims abstract 2
- 229930195733 hydrocarbon Natural products 0.000 claims abstract 2
- 238000003786 synthesis reaction Methods 0.000 claims abstract 2
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 45
- 125000000219 ethylidene group Chemical group [H]C(=[*])C([H])([H])[H] 0.000 claims 36
- 239000002253 acid Substances 0.000 claims 32
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 6
- -1 3-trifluoromethylphenyl Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims 4
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- 208000017169 kidney disease Diseases 0.000 claims 3
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 238000006317 isomerization reaction Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 2
- 150000002923 oximes Chemical class 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 claims 1
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 1
- 229930105110 Cyclosporin A Natural products 0.000 claims 1
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 1
- 108010036949 Cyclosporine Proteins 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical compound CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 229960001265 ciclosporin Drugs 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 150000002596 lactones Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- OSFBJERFMQCEQY-UHFFFAOYSA-N propylidene Chemical group [CH]CC OSFBJERFMQCEQY-UHFFFAOYSA-N 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006313 (C5-C8) alkyl group Chemical group 0.000 abstract 1
- 125000006314 C5-C8 alkoxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/61—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—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
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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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
- A61P3/06—Antihyperlipidemics
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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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.상기 식에서, R은 수소 또는 C1-C4알킬이고, A는 할로겐 및 트리플루오로메틸 중에서 독립적으로 선택된 1또는 2개의 치환체에 의해 치환되거나 비치환된 페닐환에 의해 치환되거나 비치환된 C1-C4알킬렌 쇄이며, R1은 (a) 수소 또는 직쇄 또는 측쇄의 포화 또는 불포화 C1-C10탄화수소 래디칼, (b) 아릴 그룹 또는 아일잔기가, 할로겐, 트리할로메틸, C1-C4알킬, C2-C3알케닐, C2-C6알키닐, C1-C4알콕시, C1-C4알킬티오 및 C1-C4알킬설포닐, 중에서 독립적으로 선택된 1내지 4개의 치환체, 또는 C5-C8알킬, C4-C8알케닐, C5-C8알콕시, C5-C8알킬티오 및 페닐환이 할로겐, 트리할로메틸 및 C1-C4알킬 중에서 선택된 치환체에 의해 치환되거나 비치환된 페닐중에서 선택된 치환체에 의해 치환되거나 비치환된, 아릴 또는 아릴-C1-C4알킬 그룹, 또는 c) 사이클로알킬 그룹 또는 잔기가 1내지 3개의 C1-C4알킬 그룹에 의해 치환되거나 비치환된 C5-C8사이클로알킬 또는 C5-C8사이클로알킬-C1-C4알킬 그룹이고, T는 직쇄 또는 측쇄의 포화 또는 불포화 C1-C6탄화수소쇄, 또는 페닐렌 래디칼이며, X는 단일결합이거나, -O-CH2-, -C(R'R″)-, -Si(R'R″)-(여기에서, R'및 R″는 각각 동일하거나 상이하며, 수소, 불소 또는 C1-C4알킬이다), 비닐렌 또는 이소프로페닐렌으로 이루어진 2가 그룹이고, R2는 일반식 -OR3또는 -N(R3R4)(여기서, R3및 R4는 각각 독립적으로 수소 C1-C6알킬, 페닐 또는 벤질이다)의 그룹이다.
- 제1항에 있어서, R이 수소 또는 메틸이고, A가 페닐에 의해 임의로 치환되거나, 또는 할로겐 및 트리플루오로메틸 중에서 독립적으로 선택된 1 또는 2개의 치환체에 의해 임의로 치환된 C1-C4알킬렌 쇄이며, R1이 a) C1-C8알킬 또는 C2-C8알케닐 b) 할로겐, 트리할로메틸, C1-C4알킬, C1-C4알콕시, C1-C4알킬설포닐 및 C1-C4알킬티오 중에서 독립적으로 선택된 1또는 2개의 치환체, 또는 C5-C8알킬, C4-C8알케닐, C5-C8알콕시, C5-C8알킬티오, 및 페닐환이 할로겐, 트리할로메틸 및 C1-C4알킬 중에서 선택된 치환체에 의해 치환되거나 비치환된 페닐중에서 선택된 치환체 의해 치환되거나 비치환된, 페닐, 나프틸, 티에닐 또는 피리딜 그룹, 또는 c) 1또는 2개의 C1-C4알킬 그룹에 의해 치환되거나 비치환된 사이클로헥실 또는 사이클로헵틸 그룹이고, T가 C1-C5알킬렌, C2-C5알케닐렌 또는 페닐렌 그룹이며, X가 단일결합 또는 -O-CH2-그룹이고, R2가 일반식 -OR3또는 -NR3(여기서, R3은 수소 또는 C1-C4알킬이다)의 그룹인 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.
- 제1항에 있어서, R이 수소이고, A가 -CH2-, -CH(CH3)-, -CH2CH2- 또는 -CH(CH2Ph)-(여기서, Ph는 할로겐 원자에 의해 임의로 치환된 페닐이다)이며, R1이 a) C5-C7알킬, b) 할로겐, C1-C4알킬, C1-C4알콕시 또는 트리플루오로메틸에 의해 치환되거나 비치환된 페닐, 피리딜 또는 티에틸 환, 또는 c) 사이클로헥실 또는 사이클로헵틸 환이고, T가 C2-C5알킬렌 또는 페닐렌 그룹이며, R2가 일반식 -OR3(여기서, R3은 수소 또는 C1-C4알킬이다)의 그룹인 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.
- 5-[1-페닐-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-페닐-2-(이미다졸-1-일)에 틸리덴]아민옥시펜탄아미드, 에틸 4-[1-페닐-2-(이미다졸-1-일)에틸리덴]아민옥시부타노에이트, 4-[1-페닐-2-(이미다졸-1-일)에틸리덴]아민옥시프로파노에이트, 메틸-3-[1-페닐-2-(이미다졸-1-일)에틸리덴]아민옥시프로파노에이트, 에틸5-[1-3-트리플루오로페틸페닐)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노에이트, 5-[1-3-트리플루오로페틸페닐)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-3-브로모페닐-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 4-[1-3-트리플루오로메틸페닐)-2-(이미다졸-1-일)에틸리덴]아민옥시부타노산, 5-[1-3-(n-부틸)페닐)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-(2-메톡시페닐)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 에틸 3-옥사-5-[1-페닐-2-(이미다졸-1-일)에티리덴]아민옥시펜타노에이트, 3-옥사-5-[1-페닐-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 3-옥사-5-[1-(3-트리플루오로메틸페닐)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 3급-부틸 5-[1-페닐-2-(이미다졸-1-일)-2-메틸에틸리덴]아민옥시펜타노에이트, 5-[1-페닐-2-(이미다졸-1-일)-2-메틸에틸리덴]아민옥시펜타노산, 3-[1-페닐-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 4-[1-페닐-3-(이미다졸-1-일)프로필리덴]아민옥시부타노산, 5-[1-(n-헥실)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 에틸 5-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시부타노산, 3급-부틸 5-[1-(n-헥실)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노에이트, 5-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 에틸 4-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시펜타에이트, 4-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시부타노산, 5-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시펜탄아미드, 3-옥사-5-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-(3,3-디메틸사이클로헥실)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-사이클로펜틸-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-(2-티에닐)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 에틸 5-[1-(3-피리딜)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노에이트, 5-[1-(3-피리딜)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 4-[1-(3-피리딜)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-(3-n-부틸옥시페닐)-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 에틸 5-[1-(3-n-부틸옥시페닐-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노에이트, 6-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시헥사노산, 3-옥사-6-[1-사이클로헥실-2-(이미다졸-1-일)에틸리덴]아민옥시헥사노산, 5-[1-사이클로헵틸-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 6-[1-사이클로헵틸-2-(이미다졸-1-일)에틸리덴]아민옥시헥사노산, 5-[1-n-헵틸-2-(이미다졸-1-일)에틸리덴]아민옥시펜타노산, 5-[1-페닐-2-(이미다졸-1-일)벤질에틸리덴]아민옥시펜타노산, 5-[1-사이클로헥실-2-(이미다졸-1-일)-2-벤질에틸리덴]아민옥시펜타노산, 에틸 5-[1-페닐-2-(이미다졸-1-일)-2-벤질에틸리덴]아민옥시펜타노에이트, 에틸 5-[1-사이클로헥실-2-(이미다졸-1-일)-2-벤질에틸리덴]아민옥시펜타노에이트, 6-[1-페닐-2-(이미다졸-1-일)-2-벤질에틸리덴]아민옥시헥사노산, 6-[1-사이클로헥실-2-(이미다졸-1-일)-2-벤질에틸리덴]아민옥시헥사노산, 5-[1-(4-플루오로페닐)-2-(이미다졸-1-일)-2-(4-플루오로벤질)에틸리덴]아민옥시펜타노산, 5[1-사이클로헥실-2-(이미다졸-1-일)-2-(4-플루오로벤질)에틸리덴]아민옥시펜타노산, 및 3-옥사-5-[1-페닐-2-(이미다졸-1-일)-2-벤질에틸리덴]아민옥시펜타노산, 및 약제학적으로 허용되는 이의 염으로 이루어진 그룹 중에서 선택되는 Z- 또는 E- 이성체 또는 이들 이성체의 Z,E-혼합물로서 존재하는 화합물.
- a) 일반식(Ⅱ)의 옥심 또는 이의 염을 일반식(Ⅲ)의 화합물과 반응시키거나, (b) 일반식(Ⅱ)의 옥심 또는 이의 염을 일반식(Ⅳ)의 락톤과 반응시킴으로써 R2가 -OH인 일반식(Ⅰ)의 화합물을 수득하거나, c) 일반식(Ⅴ)의 화합물을 일반식(Ⅳ)의 화합물과 반응시키거나, d) 일반식(Ⅴ)의 화합물을 일반식(Ⅶ)의 화합물과 반응시키거나, e) 일반식(Ⅷ)의 화합물 또는 이의 염을 일반식(Ⅸ)의 화합물과 반응시킴으로써 X가 -O-CH2-인 일반식(Ⅰ)의 화합물을 수득하고, 경우에 따라 일반식(Ⅰ)의 화합물로 전환시키고/시키거나, 경우에 따라 일반식(Ⅰ)의 화합물을 이의 염으로 전환시키고/시키거나, 경우에 따라 일반식(Ⅰ)의 화합물의 염을 유리 화합물로 전환시키고/시키거나, 경우에 따라 일반식(Ⅰ)의 화합물의 이성체들의 혼합물을 단일 이성체로 분리하고/하거나, 경우에 따라 옥심 이중결합상에서 이성체화시킴으로써 혼합상태의 일반식(Ⅰ)의 화합물의 E- 및 Z-이성체의 비율을 변화시켜 상기한 이성체들을 상이한 비율로 수득하고/하거나, 경우에 따라 옥심 이중결합상에서 이성체화 시킴으로써 일반식(Ⅰ)의 화합물의 순수한 E- 이성체를 순수한 Z- 이성체 또는 E- 및 Z- 이성체들의 혼합물로 전환시키고/시키거나, 경우에 따라 옥심 이중결합상에서 이성체화시킴으로써 일반식(Ⅰ)의 순수한 Z- 이성체를 순수한 E- 이성체 또는 E- 및 Z- 이성체들의 혼합물로 전환시킴을 특징으로 하여, 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 염을 제조하는 방법.상기식에서, R, A, R1, R2, T 및 X는 제1항에서 정의한 바와 같고, Y는 이탈 그룹이며, Q 및 Q'는 각각 독립적으로 수소, 저급 알킬 또는 페닐이다.
- 적합한 담체 및/또는 희석제, 및 활성 성분으로서의 제1항에 따른 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 이의 염을 함유하는 약제학적 조성물.
- 트롬복산 A2합성 증가와 관련된 질환의 치료에 사용하기 위한, 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 염.
- 신장병을 치료하는데 사용하기 위한 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 염.
- 사이클로스포린 A-유도된 신증을 예방하고/하거나 치료하는데 사용하기 위한 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 염.
- 신장질환의 합병증인 과유지질혈증을 치료하는데 사용하기 위한 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 염.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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GB9302599D0 (en) * | 1993-02-10 | 1993-03-24 | Erba Carlo Spa | 2-(imadazol-l-yl)-heteroaryl-propylidene-aminoxyalkanoic acid derivatives |
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US5665756A (en) * | 1994-08-03 | 1997-09-09 | Hoechst Marion Roussel, Inc. | Aminoalkyloximes useful in the treatment of depression and obsessive compulsive disorders |
AU2890899A (en) * | 1998-03-13 | 1999-09-27 | Pozen, Inc. | Prophylaxis and treatment of migraine headaches with thromboxane synthetase inhibitors and/or receptor antagonists |
KR20050119648A (ko) * | 2003-03-13 | 2005-12-21 | 오노 야꾸힝 고교 가부시키가이샤 | 이미노 에테르 유도체 화합물 및 그 화합물을 유효성분으로서 함유하는 약제 |
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DE3116888A1 (de) * | 1981-04-28 | 1982-11-11 | Bayer Ag, 5090 Leverkusen | "azolylpropyl-oximino-derivate, verfahren zu ihrer herstellung sowie ihre verwendung als fungizide und pflanzenwachstumsregulatoren" |
EP0132771A2 (de) * | 1983-07-22 | 1985-02-13 | Hoechst Aktiengesellschaft | Neue 1,2 Diaryl-3-azolyl-propan-Derivate, ihre Herstellung und Verwendung als Pflanzenbehandlungsmittel |
DE3334220A1 (de) * | 1983-09-22 | 1985-04-11 | Bayer Ag, 5090 Leverkusen | 1-azolyl-substituierte oximether |
DE3413365A1 (de) * | 1984-04-09 | 1985-12-19 | Merz + Co GmbH & Co, 6000 Frankfurt | Substituierte phenylethylderivate, verfahren zu ihrer herstellung und pharmazeutische mittel |
DE3545085A1 (de) * | 1985-12-19 | 1987-07-02 | Bayer Ag | Substituierte cyclopropyl-oximether |
-
1991
- 1991-02-04 IL IL9714491A patent/IL97144A/en not_active IP Right Cessation
- 1991-02-20 NZ NZ237168A patent/NZ237168A/en unknown
- 1991-02-26 EP EP91904730A patent/EP0469125B1/en not_active Expired - Lifetime
- 1991-02-26 IE IE64791A patent/IE67286B1/en not_active IP Right Cessation
- 1991-02-26 AU AU73043/91A patent/AU644632B2/en not_active Ceased
- 1991-02-26 DK DK91904730.8T patent/DK0469125T3/da active
- 1991-02-26 HU HU913625A patent/HU209471B/hu not_active IP Right Cessation
- 1991-02-26 DE DE69107137T patent/DE69107137T2/de not_active Expired - Fee Related
- 1991-02-26 US US07/768,568 patent/US5280033A/en not_active Expired - Fee Related
- 1991-02-26 WO PCT/EP1991/000351 patent/WO1991013062A2/en active IP Right Grant
- 1991-02-26 PT PT96895A patent/PT96895A/pt not_active Application Discontinuation
- 1991-02-26 CA CA002053256A patent/CA2053256A1/en not_active Abandoned
- 1991-02-26 ES ES91904730T patent/ES2074263T3/es not_active Expired - Lifetime
- 1991-02-26 AT AT91904730T patent/ATE117995T1/de active
- 1991-02-26 JP JP3504223A patent/JPH04505464A/ja active Pending
- 1991-02-26 KR KR1019910701434A patent/KR920701168A/ko active IP Right Grant
- 1991-02-27 MY MYPI91000318A patent/MY105343A/en unknown
- 1991-10-25 FI FI915056A patent/FI915056A0/fi not_active Application Discontinuation
-
1995
- 1995-04-17 GR GR950400950T patent/GR3015820T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
CA2053256A1 (en) | 1991-08-28 |
HUT59910A (en) | 1992-07-28 |
IE67286B1 (en) | 1996-03-20 |
DK0469125T3 (da) | 1995-03-27 |
EP0469125B1 (en) | 1995-02-01 |
NZ237168A (en) | 1992-07-28 |
HU913625D0 (en) | 1992-03-30 |
AU7304391A (en) | 1991-09-18 |
PT96895A (pt) | 1991-10-31 |
EP0469125A1 (en) | 1992-02-05 |
WO1991013062A2 (en) | 1991-09-05 |
US5280033A (en) | 1994-01-18 |
ES2074263T3 (es) | 1995-09-01 |
HU209471B (en) | 1994-06-28 |
ATE117995T1 (de) | 1995-02-15 |
GR3015820T3 (en) | 1995-07-31 |
IE910647A1 (en) | 1991-08-28 |
MY105343A (en) | 1994-09-30 |
WO1991013062A3 (en) | 1991-10-17 |
IL97144A0 (en) | 1992-05-25 |
IL97144A (en) | 1994-11-28 |
FI915056A0 (fi) | 1991-10-25 |
AU644632B2 (en) | 1993-12-16 |
DE69107137T2 (de) | 1995-06-01 |
DE69107137D1 (de) | 1995-03-16 |
JPH04505464A (ja) | 1992-09-24 |
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