KR890005147A - 펩티딜헤테로사이클 - Google Patents
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- KR890005147A KR890005147A KR1019880011966A KR880011966A KR890005147A KR 890005147 A KR890005147 A KR 890005147A KR 1019880011966 A KR1019880011966 A KR 1019880011966A KR 880011966 A KR880011966 A KR 880011966A KR 890005147 A KR890005147 A KR 890005147A
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- 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
- C07D213/40—Acylated substituent nitrogen atom
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- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/14—Angiotensins: Related peptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
- C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
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- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/20—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated the carbon skeleton being saturated and containing rings
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- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
- C07C217/08—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
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- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C229/36—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
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- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C233/11—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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
- C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/22—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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
- C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/40—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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
- C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/47—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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
- C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/51—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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- C07C239/00—Compounds containing nitrogen-to-halogen bonds; Hydroxylamino compounds or ethers or esters thereof
- C07C239/08—Hydroxylamino compounds or their ethers or esters
- C07C239/20—Hydroxylamino compounds or their ethers or esters having oxygen atoms of hydroxylamino groups etherified
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- C07C265/00—Derivatives of isocyanic acid
- C07C265/02—Derivatives of isocyanic acid having isocyanate groups bound to acyclic carbon atoms
- C07C265/04—Derivatives of isocyanic acid having isocyanate groups bound to acyclic carbon atoms of a saturated carbon skeleton
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- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/20—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
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- C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
- C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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- C07C317/00—Sulfones; Sulfoxides
- C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C317/28—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 acyclic carbon atoms of the carbon skeleton
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- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
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- C07C323/51—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/56—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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- C07C323/57—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
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- C07C323/59—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton with acylated amino groups bound to the carbon skeleton
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- 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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- C07D211/72—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 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, directly attached to ring carbon atoms
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- 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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- C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
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- C07D263/28—Nitrogen atoms not forming part of a nitro radical
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- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
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- C07D295/205—Radicals derived from carbonic acid
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- C07D295/16—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 acylated on ring nitrogen atoms
- C07D295/20—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 acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
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- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
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- C07D309/14—Nitrogen atoms not forming part of a nitro radical
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- C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
- C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0227—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the (partial) peptide sequence -Phe-His-NH-(X)2-C(=0)-, e.g. Renin-inhibitors with n = 2 - 6; for n > 6 see C07K5/06 - C07K5/10
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- C07K5/06—Dipeptides
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- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- C07C2601/14—The ring being saturated
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Abstract
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Claims (10)
- 일반식(I)의 화합물 또는 이의 약제학적으로 허용되는 염 또는 에스테르.상기식에서,A는 수소, 저급알킬, 아미노알킬, (알킬)아미노알킬, 디알킬아미노알킬, (알콕시)아미노알킬, (알콕시)(알킬)아미노알킬, 페닐알킬, (치환된 페닐) 알킬[여기에서, 페닐 환은 저급알콕시, 저급알킬, 아미노, 알킬아미노, 디알킬아미노, 하이드록시, 할로, 머캅토, 니트로, 티오알콕시, 카복스알데히드, 카복시, 알콕시 카보닐 및 카복스아미드 중에서 독립적으로 선택된 하나, 두개 또는 세개의 치환체로 치환된다], 나프틸 알킬, (치환된 나프틸)알킬[여기에서, 나프틸 환은 저급알콕시, 저급알킬, 아미노, 알킬아미노, 디알킬아미 노, 하이드록시, 할로, 머캅토, 니트로, 티오알콕시, 카복스알데히드, 카복시, 알콕시카보닐 및 카복스아미드 중에서 독립적으로 선택된 하나, 두개 또는 세개의 치환제로 치환된다], 치환되거나 비치환된 헤테로사이클[여기에서, 포화된 헤테로사이클은 비치환되거나, 하이드록시, 옥소, 아미노, 알킬아미노, 디알킬아미노, 알콕시, 폴리알콕시, 저급알킬, 할로알킬 또는 폴리할로알킬로 일치환되거나 이치환될 수 있고, 불포화된 헤테로사이클은 비치환되거나 하이드록시, 아미노, 알킬아미노, 디알킬아미노, 알콕시, 폴리알콕시, 저급알킬, 할로알킬 또는 폴리할로알킬로 일치환될 수 있다]이거나; (비치환된 헤테로사이클릭)알킬 또는 (치환된 헤테로사이클릭) 알킬[여기에서, 비치환되거나 치환된 세테로사이클은 상기 정의한 바와 같다]이거나; -OR7또는 -SR7[여기에서, R7은 수소, 저급알킬, 아미노알킬, (알킬)아미노알킬, 디알킬아미노알킬, (알콕시)아미노알킬, (알콕시)(알킬)아미노알킬, 페닐알킬, (치환된 페닐) 알킬(여기에서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알킬, (치환된 나프틸) 알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 치환되거나 비치환된 헤테로사이클(상기 정의한 바와 같다), (비치환된 헤테로사이클릭) 알킬 또는 (치환된 헤테로사이클릭) 알킬 또는 (여기서, 비치환되거나 치환된 헤테로사이클은 상기 정의한 바와 같다), (비치환된 헤테로사이클릭) C(O)- 또는 (치환된 헤테로사이클릭) C(O)-(여기서, 비치환거나 치환된 헤테로사이클은 상기 정의한 바와 같다)]이거나; NR8R9[여기에서, R8및 R9는 수소, 하이드록시, 알콕시, 저급알킬, 아미노알킬, 시아노알킬 및 하이드록시 알킬 중에서 독립적으로 선택된다]이거나 ;[여기에서, B는 NH, 알킬아미노, S,O,CH2NHC2또는 CH(OR52))(여기서, R52는 수소, 저급알킬 또는 저급알킬카보닐이다)이고, R10은 수소, 저급알킬, 사이클로알킬, 페닐, 치환된 페닐(상기 정의한 바와 같다), 나프틸, 치환된 나프틸(상기 정의한 바와 같다), 알콕시, 알케닐옥시, 하이드록시알콕시, 디하이드록시알콕시, 페닐알콕시, (치환된 페닐) 알콕시(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알콕시(치환된 나프틸) 알콕시알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 티오알콕시알킬, 저급알킬설피닐알킬, 저급알킬설포닐알킬, 페닐티오알킬, (치환된 페닐) 티오알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸티오알킬, (치환된 나프틸) 티오알킬 (여기서, 치환된 나프틸은 상기 정의한 바와 같다), 페닐설포닐알킬, (치환된 페닐), 설포닐알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸 설포닐알킬, (치환된 나프틸), 설포닐알킬, (치환된 나프틸) 설포닐알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 아미노, 알킬아미노, 디알킬아미노, (하이드록시알킬)(알킬)아미노, (디하이드록시알킬)(알킬)아미노, 아미노알킬, 알콕시카보닐알킬, 카복시알킬, (N-보호된)아미노알킬, 알킬아미노알킬, (N-보호된)(알킬)아미노알킬, 디알킬아미노알킬, (헤테로사이클릭)알킬, 치환되거나 비치환된 헤테로사이클(상기 정의한 바와 같다), 아미노사이클로알킬, 아미노알킬아미노, (디알킬아미노알킬)(알킬)아미노, 페닐알킬아미노, (치환된 페닐)알킬아미노(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알킬아미노, (치환된 나프틸) 알킬아미노(여기서, 치환된 나프틸은 상기 정의한 바와 같다), (페닐알킬)(알킬)아미노, ((치환된 페닐)알킬)(알킬), 아미노(여기서, 치환된 페닐은 상기 정의한 바와 같다), (나프틸알킬)(알킬)아미노, ((치환된 나프틸)알킬(알킬) 아미노(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 알콕시알킬(알킬)아미노, (폴리알콕시)알킬(알킬)아미노, 디-(알콕시알킬)아미노, 디-(하이드록시알킬)아미노, 디-((폴리알콕시)알킬)아미노, ((헤테로사이클릭)알킬)(알킬)아미노, ((헤테로사이클릭)알킬) 아미노, (헤테로사이클릭)(알킬)아미노, (알킬아미노알킬)(알킬)아미노, (디알킬아미노알킬)(알킬)아미노, ((알콕시)(알킬)아미노알킬)(알킬)아미노, ((알콕시)아미노알킬)(알킬)아미노, 폴리알콕시 또는 (폴리알콕시)알킬 이다]이거나;R41CH(OH)CH2- 또는 R41CH(OH)CH(OH)-[여기서, R41은 저급알킬, 사이클로알킬, 페닐, 치환된 페닐(상기 정의한 바와 같다), 나프틸, 치환된 나프틸(상기 정의한 바와 같다), 페닐알킬, (치환된 페닐) 알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알킬, (치환된 나프틸) 알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 페닐 알콕시알킬, (치환된 페닐) 알콕시알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알콕시알킬, (치환된 나프틸)알콕시알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 티오알콕시알킬, 저급알킬설피닐알킬, 저급알킬설포닐알킬, 페닐티오알킬, (치환된 페닐) 티오 알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다). 나프틸티오알킬, (치환된 나프틸) 티오알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 페닐설포닐알킬, (치환된 페닐) 설포닐알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸설포닐알킬, (치환된 나프틸) 설포닐알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 아미노알킬, 알콕시카보닐알킬, 카복시알킬, (N-보호된)아미노알킬, 알킬아미노알킬, (N-보호된)(알킬)아미노알킬, 디알킬아미노알킬, 헤테로사이클릭알킬, 치환되거나 비치환된 헤테로사이클(상기 정의한 바와 같다), 아미노사이클릭알킬, 치환된거나 비치환된 헤테로사이클(상기 정의한 바와 같다), 아미노사이클로알킬 또는(폴리알콕시)알킬 이다]이고,W는 C=O,CHOH 또는 NR2[여기서, R2는 수소 또는 저급알킬이다]이며,u는 C=O, CH2또는 NR2[여기서, R2는 수소 또는 저급알킬이다]이고, 단 W가 CHOH일 경우 u는 CH2이며, W가 NR2일 경우 u는 C=O 또는 CH2이고,V는 CH, C(OH) 또는 C(할로겐)이며, 단 u가 NR2일 경우 V는 CH이고,R1은 저급알킬, 사이클로알킬알킬, 벤질, (알파, 알파)-디메틸벤질, 4-메톡시벤질, 할로벤질, 4-하이드록시벤질, (1-나프틸)메틸, (2-나프틸)메틸, (비치환된 헤테로사이클릭)메틸, (치환된 헤테로사이클릭) 메틸(여기에서, 비치환되거나 치환된 헤테로사이클은 상기 정의한 바와 같다), 펜에틸, 1-벤질옥시에틸, 페녹시, 티오페녹시 또는 아닐리노이며, 단,R1이 페녹시, 티오페녹시 또는 아닐리노일 경우 B는 CH2또는 CHOH이거나 A는 수소이고,R3는 저급알킬, 저급알케닐, ((알콕시)알콕시)알킬, 카복시알킬, (티오알콕시)알킬, 아지도알킬, 아미노알킬, (알킬)아미노알킬, 디알킬아미노알킬, (알콕시)(알킬)아미노알킬, (알콕시)아미노알킬, 벤질 또는 메틸 치환된 헤테로사이클릭환이며,R4는 저급알킬, 사이클로알킬메틸 또는 벤질이고,R5는 OH 또는 NH2DLAU,Z는[여기에서, M은 O,S 또는 NH이고, T는 C=O, C=S, S, S(O), S(O)2또는 CH2이며,E는 O, S, NR6(여기서, R6은 수소, 저급알킬, 하이드록시알킬, 하이드록시알콕시, 아미노 또는 알킬아미노이다), CR6R42(여기서, R6은 상기 정의한 바와 같고, R42는 수소 또는 저급알킬이다), 또는 C=CR43R44(여기서, R43및 R44는 수소 및 저급알킬중에서 독립적으로 선택된다)이고,G는 생략되거나, CH2또는 NR11(여기서, R11은 수소 또는 저급알킬이다)이며, 단, G가 NR11일 경우 R6은 저급알킬 또는 하이드록시알킬이고,Q는 CR45R46(여기서, R45및 R46은 수소 및 저급알킬 중에서 독립적으로 선택된다) 또는 C=CR47R48(여기서, R47및 R48은 수소 및 저급알킬 중에서 독립적으로 선택된다)이며,R49는 -CH2OH, 카복시, 알콕시카보닐 또는 -CONR50R51(여기서, R50은 수소 또는 저급알킬이고, R51은 수소, 저급알킬, 아미노알킬, 알킬아미노알킬, 디알킬아미노알킬 또는 알콕시알킬이다)]이다.
- 제1항에 있어서, 헤테로사이클이 하기 구조식 또는 일반식의 화합물.상기식에서,n은 1 또는 2이고,X는 N, NH, O, S이며, 단, X가 N일 경우에만 X는 결합점이고,Y는 NH, N-저급알킬, O,S 또는 SO2이며,Z1은 N, O 또는 S이고, 결합점은 아니며,Z2은 결합점일 경우 N이고, 결합점이 아닐 경우 NH, O 또는 S이다.
- 제1항에 있어서, R1이 벤질이고, R3가 (4-이미다졸릴)메틸이며, R4가 사이클로헥실메틸이고, R5가 OH이며, Z가[여기에서, M은 O이고, T는 C=O이며, E는 NR6(여기서, R6은 수소, 저급알킬, 하이드록시알킬, 하이드록시, 알콕시, 아미노 또는 알킬아미노이다)이거나, M은 O이고, T는 CH2이며, G는 생략되고, E는 CH(CH3)이다] 또는[여기에서, Q는 CR45R46(여기서, R45및 R46은 수소 및 저급알킬 중에서 독립적으로 선택된다) 또는 C=CR47R48(여기서, R47및 R48은 수소 및 저급 알킬 중에서 독립적으로 선택된다)이고, R49는 -CH2OH, 카복시, 알콕시카보닐 또는 -CONR50R51(여기서, R50또는 저급알킬이고, R51은 수소, 저급알킬, 아미노알킬, 알킬아미노알킬, 디알킬아미노알킬 또는 알콕시알킬이다)인 화합물.
- (2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-모르폴린-4-일카보닐프로피오닐-L-(4-티아졸릴)-AIa아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-(4-트리플루오로에틸-피페라진-4-일카보닐)-프로피오닐-L-(4-티아졸릴)-AIa아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-티아졸-4-일프로필오닐-L-(4-티아졸릴)-AIa아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-3급-부틸설포닐-프로피오닐-His 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-((2-이미디졸-1-일에틸)-메틸아미노카보닐)-프로필오닐)-L-4-티아졸릴-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-((2-디에틸아미노에틸)메틸아미노카보닐)프로피오닐-L-(4-티아졸릴)-AIa아미드 및(2'S,4S,1'R,2'S)-2-(2-아미노-3-사이클로헥실-1-하이드록시)-4-메틸테트라하이드로푸란의 (2R)-2-벤질-3-(모르폴리노카보닐)-프로피오닐-L-(4-티아졸릴)-AIa 아미드로 구성된 그룹중에서 선택된 화합물 또는 이의 약제학적으로 허용되는 염 또는 에스테르.
- 약제학적 담체 및 치료유효량의 제1항에 따른 화합물을 함유함을 특징으로 하는, 고혈압 치료용 약제 조성물.
- 약제학적 담체 및(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-모르폴린-4-일카보닐프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-(4-트리플루오로에틸-피페라진-4-일카보닐)-프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-티아졸-4-일프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-3급-부틸설포닐-프로피오닐-His 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 (2R)-2-벤질-3-((2-이미다졸-1-일에틸)-메틸아미노카보닐)-프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 (2R)-2-벤질-3-((2-디에틸아미노에틸)메틸아미노카보닐)프로피오닐-L-(4-티아졸릴)-AIa 아미드 및(2'S,4S,1'R,2'S)-2-(2-아미노-3-사이클로헥실-1-하이드록시)-4-메틸테트라하이드로푸란의 (2R)-2-벤질-3-(모르폴리노카보닐)-프로피오닐-L-(4-티아졸릴)-AIa 아미드로 구성된 그룹중에서 선택된 치료 유효량의 화합물 또는 이의 약제학적으로 허용되는 염 또는 에스테르를 함유함을 특징으로 하는, 고혈압 치료용 약제 조성물.
- 고혈압 치료가 필요한 숙주에게 치료유효량의 제1항에 따른 화합물을 투여함을 특징으로 하여, 고혈압을 치료하는 방법.
- (2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-모르폴린-4-일카보닐프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-(4-트리플루오로에틸-피페라진-4-일카보닐)-프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-티아졸-4-일프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 2(R)-2-벤질-3-3급-부틸설포닐-프로피오닐-His 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 (2R)-2-벤질-3-((2-이미다졸-1-일에틸)-메틸아미노카보닐)-프로피오닐)-L-(4-티아졸릴)-AIa 아미드,(2'S,1'R,5S)-3-에틸-5-(1'-하이드록시-2'-아미노-3'-사이클로헥실프로필)-옥사졸리딘-2-온의 (2R)-2-벤질-3-((2-디에틸아미노에틸)메틸아미노카보닐)프로피오닐-L-(4-티아졸릴)-AIa 아미드,(2'S,4S,1'R,2'S)-2-(2-아미노-3-사이클로헥실-1-하이드록시)-4-메틸테트라하이드로푸란의 (2R)-2-벤질-3-(모르폴리노카보닐)-프로피오닐-L-(4-티아졸릴)-AIa 아미드로 구성된 그룹중에서 선택된 치료 유효량의 화합물 또는 이의 약제학적으로 허용되는 염 또는 이의 약제학적으로 허용되는 염 또는 에스테르를 고혈압 치료가 필요한 숙주에게 투여함을 특징으로 하여, 고혈압을 치료하는 방법.
- 일반식(II)의 화합물.상기식에서,R4은 저급알킬, 사이클로알킬메틸 또는 벤질이고,R88은 수소 또는 N-보호그룹이며,R89은 -OR90또는 -NHR91(여기에서, R90은 수소 또는 O-보호그룹이고, R91은 수소 또는 N-보호그룹이다)이고,Z는[여기에서, M은 O, S 또는 NH이고, T는 C=O, C=S, S, S(O), S(O)2또는 CH2이며,E는 O, S, NR6(여기서, R6은 수소, 저급알킬, 하이드록시, 알킬, 하이드록시알콕시, 아미노 또는 알킬아미노이다), CR6R42(여기서, R6은 상기 정의한 바와 같고, R42는 수소 또는 저급알킬이다), 또는 C=CR43R44(여기서, R43및 R44는 수소 및 저급알킬중에서 독립적으로 선택된다)이고,G는 생략되거나, CH2또는 NR11(여기서, R11은 수소 또는 저급알킬이다)이며, 단, G가 NR11일 경우 R6은 저급알킬 또는 하이드록시알킬이고,Q는 CR45R46(여기서, R45및 R46은 수소 및 저급알킬 중에서 독립적으로 선택된다) 또는 C=CR47R48(여기서, R47및 R48은 수소 및 저급알킬 중에서 독립적으로 선택된다)이며,R49는 -CH2OH, 카복시, 알콕시카보닐 또는 -CONR50R51(여기서, R50은 수소 또는 저급알킬이고, R51은 수소, 저급알킬, 아미노알킬, 알킬아미노알킬, 디알킬아미노알킬 또는 알콕시알킬이다)]이다.
- 일반식(Ia)의 화합물 또는 이의 산할라이드 또는 활성화된 에스테르 유도체를 일반식(Ib)의 화합물과 커플링 시킴을 특징으로하여, 제1항의 화합물을 제조하는 방법.상기식에서,A는 수소, 저급알킬, 아미노알킬, (알킬)아미노알킬, 디알킬아미노알킬, (알콕시)아미노알킬, (알콕시)(알킬)아미노알킬, 페닐알킬, (치환된 페닐) 알킬[여기에서, 페닐 환은 저급알콕시, 저급알킬, 아미노, 알킬아미노, 디알킬아미노, 하이드록시, 할로, 머캅토, 니트로, 티오알콕시, 카복스알데히드, 카복시, 알콕시 카보닐 및 카복스아미드 중에서 독립적으로 선택된 하나, 두개 또는 세개의 치환제로 치환된다], 나프틸 알킬, (치환된 나프틸)알킬[여기에서, 나프틸 환은 저급알콕시, 저급알킬, 아미노, 알킬아미노, 디알킬아미노, 하이드록시, 할로, 머캅토, 니트로, 티오알콕시, 카복스알데히드, 카복시, 알콕시카보닐 및 카복스아미드 중에서 독립적으로 선택된 하나, 두개 또는 세개의 치환체로 치환된다], 치환되거나 비치환된 헤테로사이클[여기에서, 포화된 헤테로사이클은 비치환되거나, 하이드록시, 옥소, 아미노, 알킬아미노, 디알킬아미노, 알콕시, 폴리알콕시, 저급알킬, 할로알킬 또는 폴리할로알킬로 일치환되거나 이치환될 수 있고, 불포화된 헤테로사이클은 비치환되거나 하이드록시, 아미노, 알킬아미노, 디알킬아미노, 알콕시, 폴리알콕시, 저급알킬, 할로알킬 또는 폴리할로알킬로 일치환될 수 있다]이거나; (비치환된 헤테로사이클릭)알킬 또는 (치환된 헤테로사이클릭) 알킬[여기에서, 비치환되거나 치환된 헤테로사이클은 상기 정의한 바와 같다]이거나; OR7또는 -SR7[여기에서, R7은 수소, 저급알킬, 아미노알킬, (알킬)아미노알킬, 디알킬아미노알킬, (알콕시)아미노알킬, (알콕시)(알킬)아미노알킬, 페닐알킬, (치환된 페닐) 알킬(여기에서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알킬, (치환된 나프틸) 알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 치환되거나 비치환된 헤테로사이클(상기 정의한 바와 같다), (비치환된 헤테로사이클릭) 알킬 또는 (치환된 헤테로사이클릭) 알킬(여기서, 비치환되거나 치환된 헤테로사이클은 상기 정의한 바와 같다), (비치환된 헤테로사이클릭) C(O)- 또는 (치환된 헤테로사이클릭) C(O)- (여기서, 비치환되거나 치환된 헤테로사이클릭) C(O)- 또는 (치환된 헤테로사이클릭) C(O)- (여기서, 비치환거나 치환된 헤테로사이클은 상기 정의한 바와 같다)]이거나; NR8R9[여기에서, R8및 R9는 수소, 하이드록시, 알콕시, 저급알킬, 아미노알킬, 시아노알킬 및 하이드록시 알킬 중에서 독립적으로 선택된다]이거나;[여기에서, B는 NH, 알킬아미노, S,O,CH2NHCH2또는 CH(OR52))(여기서, R52는 수소, 저급알킬 또는 저급알킬카보닐이다)이고, R10은 수소, 저급알킬, 사이클로알킬, 페닐, 치환된 페닐(상기 정의한 바와 같다), 나프틸, 치환된 나프틸(상기 정의한 바와 같다), 알콕시, 알케닐옥시, 하이드록시알콕시, 디하이드록시알콕시, 페닐알콕시, (치환된 페닐) 알콕시(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알콕시(치환된 나프틸) 알콕시(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 페닐설포닐알킬, (치환된 페닐), 알콕시알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알콕시알킬(치환된 페닐)알콕시알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 티오알콕시알킬, 저급알킬설피닐알킬, 저급알킬설포닐알킬, 페닐티오알킬, (치환된 페닐) 티오알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸티오알킬, (치환된 나프틸) 티오알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 페닐설포닐알킬, (치화된 페닐) 설포닐알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸설포닐(치환된 나프틸)설포닐 알킬, (여기서, 치환된 나프틸은 상기 정의한 바와 같다), 아미노 알킬아미노 디알킬아미노(하이드록시 알킬)(알킬)아미노, (디하이드록시알킬)(알킬) 아미노, 아미노알킬, 알콕시카보닐알킬, 카복시알킬, (N-보호된)아미노알킬, 알킬아미노알킬, (N-보호된)(알킬)아미노알킬, 디알킬아미노알킬, (헤테로사이클릭)알킬, 치환되거나 비치환된 헤테로사이클(상기 정의한 바와 같다), 아미노사이클로알킬, 아미노알킬아미노, (디알킬아미노알킬)(알킬)아미노, 페닐알킬아미노, (치환된 페닐)알킬아미노(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알킬아미노, (치환된 나프틸) 알킬아미노(여기서, 치환된 나프틸은 상기 정의한 바와 같다), (페닐알킬)(알킬)아미노, ((치환된 페닐)알킬)(알킬), 아미노(여기서, 치환된 페닐은 상기 정의한 바와 같다), (나프틸알킬)(알킬)아미노, ((치환된 나프틸)알킬(알킬) 아미노(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 알콕시알킬(알킬)아미노, (폴리알콕시)알킬(알킬)아미노, 디-(알콕시알킬)아미노, 디-(하이드록시알킬)아미노, 디-((폴리알콕시)알킬)아미노, ((헤테로사이클릭)알킬)(알킬)아미노, ((헤테로사이클릭알킬)(알킬) 아미노, ((알콕시)(알킬)아미노알킬)(알킬)아미노, ((알콕시)아미노알킬)(알킬)아미노, 폴리알콕시 또는 (폴리알콕시)알킬 이다]이거나 ;R41CH(OH)CH2- 또는R41CH(OH)CH(OH)-[여기서, R41은 저급알킬, 사이클로알킬, 페닐, 치환된 페닐(상기 정의한 바와 같다), 나프틸, 치환된 나프틸(상기 정의한 바와 같다), 페닐알킬, (치환된 페닐) 알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알킬, (치환된 나프틸) 알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 페닐 알콕시알킬, (치환된 페닐) 알콕시알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸알콕시알킬, (치환된 나프틸)알콕시알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 티오알콕시알킬, 저급알킬설피닐알킬, 저급알킬설포닐알킬, 페닐티오알킬, (치환된 페닐) 티오알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다)). 나프틸티오알킬, (치환된 나프틸) 티오알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 페닐설포닐알킬, (치환된 페닐) 설포닐알킬(여기서, 치환된 페닐은 상기 정의한 바와 같다), 나프틸설포닐알킬, (치환된 나프틸) 설포닐알킬(여기서, 치환된 나프틸은 상기 정의한 바와 같다), 아미노알킬, 알콕시카보닐알킬, 카복시알킬, (N-보호된)아미노알킬, 알킬아미노알킬, (N-보호된)(알킬)아미노알킬, 디알킬아미노알킬, 헤테로사이클릭알킬, 치환되거나 비치환된 헤테로사이클(상기 정의한 바와 같다), 아미노사이클로알킬 또는(폴리알콕시)알킬 이다]이고,W는 C=O,CHOH 또는 NR2[여기서, R2는 수소 또는 저급알킬이다]이며,u는 C=O, CH2또는 NR2[여기서, R2는 수소 또는 저급알킬이다]이고, 단 W가 CHOH일 경우 u는 CH2이며, W가 NR2일 경우 u는 C=O 또는 CH2이고,V는 CH, C(OH) 또는 C(할로겐)이며, 단 u가 NR2일 경우 V는 CH다.R1은 저급알킬, 사이클로알킬알킬, 벤질, (알파, 알파)-디메틸벤질, 4-메톡시벤질, 할로벤질, 4-하이드록시벤질, (1-나프틸)메틸, (2-나프틸)메틸, (비치환된 헤테로사이클릭)메틸, (치환된 헤테로사이클릭) 메틸(여기에서, 비치환되거나 치환된 헤테로사이클은 상기 정의한 바와 같다), 펜에틸, 1-벤질옥시에틸, 페녹시, 티오페녹시 또는 아닐리노이며, 단,R1이 페녹시, 티오페녹시 또는 아닐리노일 경우 B는 CH2또는 CHOH이거나 A는 수소이고,R3는 저급알킬, 저급알케닐, ((알콕시)알콕시)알킬, 카복시알킬, (티오알콕시)알킬, 아지도알킬, 아미노알킬, (알킬)아미노알킬, 디알킬아미노알킬, (알콕시)(알킬)아미노알킬, (알콕시)아미노알킬, 벤질 또는 메틸 치환된 헤테로사이클릭환이며,R4는 저급알킬, 사이클로알킬메틸 또는 벤질이고,R89는 -OR90또는 -NHR91(여기에서, R90은 수소 또는 O-보호그룹이고, R91은 수소 또는 N-보호그룹이다)이며,Z는[여기에서, M은 O,S 또는 NH이고, T는 C=O, C=S-, S, S(O), S(O)2또는 CH2이며,E는 O, S, NR6(여기서, R6은 수소, 저급알킬, 하이드록시알킬, 하이드록시, 알콕시, 아미노 또는 알킬아미노이다), CR6R42(여기서, R6은 상기 정의한 바와 같고, R42는 수소 또는 저급알킬이다), 또는 C=CR43R44(여기서, R43및 R44는 수소 및 저급알킬중에서 독립적으로 선택된다)이고,G는 생략되거나, CH2또는 NR11(여기서, R11은 수소 또는 저급알킬이다)이며, 단, G가 NR11일 경우 R6은 저급알킬 또는 하이드록시알킬이고,Q는 CR45R46(여기서, R45및 R46은 수소 및 저급알킬 중에서 독립적으로 선택된다) 또는 C=CR47R48(여기서, R47및 R48은 수소 및 저급알킬 중에서 독립적으로 선택된다)이며,R49는 -CH2OH, 카복시, 알콕시카보닐 또는 -CONR50R51(여기서, R50은 수소 또는 저급알킬이고, R51은 수소, 저급알킬, 아미노알킬, 알킬아미노알킬, 디알킬아미노알킬 또는 알콕시알킬이다)]이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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US23186988A | 1988-08-16 | 1988-08-16 | |
US231.869 | 1988-08-16 |
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EP (1) | EP0307837A3 (ko) |
JP (1) | JPH01221357A (ko) |
KR (1) | KR890005147A (ko) |
AU (1) | AU613956B2 (ko) |
DK (1) | DK514688A (ko) |
IL (1) | IL87614A0 (ko) |
NZ (1) | NZ226002A (ko) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA1329680C (en) * | 1987-11-23 | 1994-05-17 | Harold Norris Weller, Iii | N-heterocyclic alcohol derivatives |
US4981843A (en) * | 1988-04-07 | 1991-01-01 | E. R. Squibb & Sons, Inc. | N-heterocyclic alcohol derivatives |
US5246959A (en) * | 1988-07-01 | 1993-09-21 | G. D. Searle & Co. | Poly(aminoalkyl)aminocarbonyl aminoacyl aminodiol amino acid derivatives as anti-hypertensive agents |
US4900746A (en) * | 1988-07-01 | 1990-02-13 | G. D. Searle & Co. | Ethereal N-terminal aminodiol amino acid derivatives as anti-hypertensive agents |
NZ229791A (en) * | 1988-07-01 | 1991-08-27 | Searle & Co | Ether derivatives of amino acid amides containing hydroxy groups, and pharmaceutical compositions |
US4902706A (en) * | 1988-07-01 | 1990-02-20 | G. D. Searle & Co. | Aminoalkylaminocarbonyl aminodiol amino acid derivatives as antihypertensive agents |
US4900745A (en) * | 1988-07-01 | 1990-02-13 | G. D. Searle & Co. | Poly(aminoalkyl)aminocarbonyl aminodiol amino acid derivatives as anti-hypertensive agents |
EP0355331A3 (en) * | 1988-07-01 | 1991-08-14 | G.D. Searle & Co. | Poly(aminoalkyl)aminocarbonyl aminoacyl aminodiol amino acid derivatives as anti-hypertensive agents |
US5229420A (en) * | 1988-07-01 | 1993-07-20 | G. D. Searle & Co. | Ethereal N-terminal aminodiol amino acid derivatives as anti-hypertensive agents |
US5059589A (en) * | 1988-09-08 | 1991-10-22 | Abbott Laboratories | Glaucoma treatment |
WO1990006914A1 (en) * | 1988-12-22 | 1990-06-28 | The Upjohn Company | N-alkylation of n-alpha-boc-protected amino acids |
IE902446A1 (en) * | 1989-07-26 | 1991-02-13 | Abbott Lab | Peptidyl aminodiol renin inhibitors |
US5147888A (en) * | 1989-12-04 | 1992-09-15 | G. D. Searle & Co. | N-terminal indolyy indolylalkylaminodiol β-amino acid derivatives |
US5223512A (en) * | 1989-12-04 | 1993-06-29 | G. D. Searle & Co. | Quinolonyl/quinolonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino acid derivatives |
US5223534A (en) * | 1989-12-04 | 1993-06-29 | G. D. Searle & Co. | Benzofuuranyl/benofuranylaklyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino acid derivatives |
US5223532A (en) * | 1989-12-04 | 1993-06-29 | G. D. Searle & Co. | Chromonyl/chromonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino derivatives |
US5223514A (en) * | 1989-12-04 | 1993-06-29 | G. D. Searle & Co. | Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino acid derivatives |
US5182266A (en) * | 1990-01-31 | 1993-01-26 | Abbott Laboratories | Method for treating renal disease |
IL96942A (en) * | 1990-01-31 | 1995-01-24 | Abbott Lab | A pharmaceutical mixture containing a history of amide prevents renin |
US5258362A (en) * | 1991-06-11 | 1993-11-02 | Abbott Laboratories | Renin inhibiting compounds |
PL294870A1 (ko) * | 1991-06-21 | 1993-02-08 | Hoechst Ag | |
US5422349A (en) * | 1992-08-14 | 1995-06-06 | G. D. Seale & Co. | Morpholino-oxazinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension |
GB9402500D0 (en) * | 1994-02-09 | 1994-03-30 | Mccracken James | Security system |
US6329372B1 (en) * | 1998-01-27 | 2001-12-11 | Celltech Therapeutics Limited | Phenylalanine derivatives |
FR2832152A1 (fr) * | 2001-11-09 | 2003-05-16 | Aventis Pharma Sa | Utilisation de derives de 2-amino-thiazoline comme inhibiteurs de no-synthase inductible |
WO2003040115A1 (fr) | 2001-11-09 | 2003-05-15 | Aventis Pharma S.A. | Derives de 2-amino-thiazoline et leur utilisation comme inhibiteurs de no-synthase inductible |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK34086A (da) * | 1985-01-23 | 1986-07-24 | Abbott Lab | Peptidylaminodioler |
ZA87563B (en) * | 1986-02-03 | 1987-09-30 | Squibb & Sons Inc | N-heterocyclic alcohol renin inhibitors |
DE3627877A1 (de) * | 1986-07-30 | 1988-02-04 | Hoechst Ag | Renin-hemmende di- und tripeptide, verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung |
DE3732971A1 (de) * | 1987-09-30 | 1989-04-20 | Hoechst Ag | Renin-hemmende dipeptide, verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung |
-
1988
- 1988-08-30 IL IL87614A patent/IL87614A0/xx unknown
- 1988-08-31 NZ NZ226002A patent/NZ226002A/xx unknown
- 1988-09-12 EP EP19880114867 patent/EP0307837A3/en not_active Withdrawn
- 1988-09-14 AU AU22223/88A patent/AU613956B2/en not_active Ceased
- 1988-09-14 JP JP63231430A patent/JPH01221357A/ja active Pending
- 1988-09-15 DK DK514688A patent/DK514688A/da not_active Application Discontinuation
- 1988-09-16 KR KR1019880011966A patent/KR890005147A/ko not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
EP0307837A3 (en) | 1991-12-11 |
NZ226002A (en) | 1990-06-26 |
AU613956B2 (en) | 1991-08-15 |
AU2222388A (en) | 1989-04-20 |
DK514688A (da) | 1989-03-17 |
JPH01221357A (ja) | 1989-09-04 |
EP0307837A2 (en) | 1989-03-22 |
IL87614A0 (en) | 1989-01-31 |
DK514688D0 (da) | 1988-09-15 |
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WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |