Use of ethynyl alanine amino diol compounds to inhibit enzymatic conversion of angiotensinogen to angiotensin I
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/165
A61K-031/18
출원번호
US-0729534
(2000-12-04)
발명자
/ 주소
Hanson, Gunnar J.
Baran, John S.
출원인 / 주소
Pharmacia Corporation
대리인 / 주소
Keane, J. Timothy
인용정보
피인용 횟수 :
1인용 특허 :
4
초록▼
Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to inhibit enzymatic conversion of angiotensinogen to angiotensin I. Such enzymatic inhibition is useful to treat disorders mediated by plasma renin activity. An example of such disorders is hypertension. Compound
Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to inhibit enzymatic conversion of angiotensinogen to angiotensin I. Such enzymatic inhibition is useful to treat disorders mediated by plasma renin activity. An example of such disorders is hypertension. Compounds of particular interest are those of Formula I. wherein A is selected from CO and SO2wherein X is selected from oxygen atom and methylene; wherein each of R1and R9is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1and R9are attached may be combined with oxygen to form an N-oxide; wherein R2is selected from hydrido, methyl, ethyl and isopropyl; wherein R3is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R5is propargyl or a propargyl-containing moiety; wherein R7is cyclohexylmethyl; wherein each of R4and R6is independently selected from hydrido and methyl; wherein R8is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R11and R12is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.
대표청구항▼
Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to inhibit enzymatic conversion of angiotensinogen to angiotensin I. Such enzymatic inhibition is useful to treat disorders mediated by plasma renin activity. An example of such disorders is hypertension. Compound
Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to inhibit enzymatic conversion of angiotensinogen to angiotensin I. Such enzymatic inhibition is useful to treat disorders mediated by plasma renin activity. An example of such disorders is hypertension. Compounds of particular interest are those of Formula I. wherein A is selected from CO and SO2wherein X is selected from oxygen atom and methylene; wherein each of R1and R9is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1and R9are attached may be combined with oxygen to form an N-oxide; wherein R2is selected from hydrido, methyl, ethyl and isopropyl; wherein R3is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R5is propargyl or a propargyl-containing moiety; wherein R7is cyclohexylmethyl; wherein each of R4and R6is independently selected from hydrido and methyl; wherein R8is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R11and R12is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.
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이 특허에 인용된 특허 (4)
Hanson Gunnar J. (Skokie IL) Baran John S. (Winnetka IL), Ethynyl alanine amino diol compounds for treatment of hypertension.
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