KR900701748A - 심장혈관 장애의 치료 및 진통제로서 유용한 머캅토-아실 아미노산 - Google Patents
심장혈관 장애의 치료 및 진통제로서 유용한 머캅토-아실 아미노산Info
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- KR900701748A KR900701748A KR1019900701086A KR900701086A KR900701748A KR 900701748 A KR900701748 A KR 900701748A KR 1019900701086 A KR1019900701086 A KR 1019900701086A KR 900701086 A KR900701086 A KR 900701086A KR 900701748 A KR900701748 A KR 900701748A
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- Prior art keywords
- lower alkyl
- compound
- alkyl
- pharmaceutical composition
- formula
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- 238000011282 treatment Methods 0.000 title claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 title 1
- 229940035676 analgesics Drugs 0.000 title 1
- 239000000730 antalgic agent Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 6
- -1 α-naphthyl Chemical group 0.000 claims 6
- 206010020772 Hypertension Diseases 0.000 claims 5
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 5
- 230000001746 atrial effect Effects 0.000 claims 5
- 239000002934 diuretic Substances 0.000 claims 5
- 230000001882 diuretic effect Effects 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052708 sodium Inorganic materials 0.000 claims 5
- 239000011734 sodium Substances 0.000 claims 5
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 4
- 206010019280 Heart failures Diseases 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 239000005541 ACE inhibitor Substances 0.000 claims 3
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims 3
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims 3
- 230000000202 analgesic effect Effects 0.000 claims 3
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 230000009467 reduction Effects 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 238000006482 condensation reaction Methods 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 150000002829 nitrogen Chemical class 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- NVXFXLSOGLFXKQ-JMSVASOKSA-N (2s)-1-[(2r,4r)-5-ethoxy-2,4-dimethyl-5-oxopentanoyl]-2,3-dihydroindole-2-carboxylic acid Chemical compound C1=CC=C2N(C(=O)[C@H](C)C[C@@H](C)C(=O)OCC)[C@H](C(O)=O)CC2=C1 NVXFXLSOGLFXKQ-JMSVASOKSA-N 0.000 claims 1
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 claims 1
- XRKXJJYSKUIIEN-UHFFFAOYSA-N 2-[cyclopentyl-[3-(2,2-dimethylpropanoylsulfanyl)-2-methylpropanoyl]amino]acetic acid Chemical compound CC(C)(C)C(=O)SCC(C)C(=O)N(CC(O)=O)C1CCCC1 XRKXJJYSKUIIEN-UHFFFAOYSA-N 0.000 claims 1
- DKIDEFUBRARXTE-UHFFFAOYSA-N 3-mercaptopropanoic acid Chemical compound OC(=O)CCS DKIDEFUBRARXTE-UHFFFAOYSA-N 0.000 claims 1
- 108010061435 Enalapril Proteins 0.000 claims 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 102000003729 Neprilysin Human genes 0.000 claims 1
- 108090000028 Neprilysin Proteins 0.000 claims 1
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 1
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 1
- VXFJYXUZANRPDJ-WTNASJBWSA-N Trandopril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@H]2CCCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 VXFJYXUZANRPDJ-WTNASJBWSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 1
- 229940024606 amino acid Drugs 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 108010082685 antiarrhythmic peptide Proteins 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 230000000740 bleeding effect Effects 0.000 claims 1
- 229960000830 captopril Drugs 0.000 claims 1
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 claims 1
- 125000005242 carbamoyl alkyl group Chemical group 0.000 claims 1
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 1
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229960000873 enalapril Drugs 0.000 claims 1
- GBXSMTUPTTWBMN-XIRDDKMYSA-N enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 229950009810 indolapril Drugs 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229960000310 isoleucine Drugs 0.000 claims 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 1
- 125000000741 isoleucyl group Chemical group [H]N([H])C(C(C([H])([H])[H])C([H])([H])C([H])([H])[H])C(=O)O* 0.000 claims 1
- 125000005358 mercaptoalkyl group Chemical group 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 229950008492 pentopril Drugs 0.000 claims 1
- 229960002582 perindopril Drugs 0.000 claims 1
- IPVQLZZIHOAWMC-QXKUPLGCSA-N perindopril Chemical compound C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H]21 IPVQLZZIHOAWMC-QXKUPLGCSA-N 0.000 claims 1
- 125000003884 phenylalkyl group Chemical group 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 229960003401 ramipril Drugs 0.000 claims 1
- HDACQVRGBOVJII-JBDAPHQKSA-N ramipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@@H]2CCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 HDACQVRGBOVJII-JBDAPHQKSA-N 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229960002909 spirapril Drugs 0.000 claims 1
- 108700035424 spirapril Proteins 0.000 claims 1
- HRWCVUIFMSZDJS-SZMVWBNQSA-N spirapril Chemical group C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2(C1)SCCS2)C(O)=O)CC1=CC=CC=C1 HRWCVUIFMSZDJS-SZMVWBNQSA-N 0.000 claims 1
- 229960002769 zofenopril Drugs 0.000 claims 1
- IAIDUHCBNLFXEF-MNEFBYGVSA-N zofenopril Chemical compound C([C@@H](C)C(=O)N1[C@@H](C[C@@H](C1)SC=1C=CC=CC=1)C(O)=O)SC(=O)C1=CC=CC=C1 IAIDUHCBNLFXEF-MNEFBYGVSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C327/00—Thiocarboxylic acids
- C07C327/20—Esters of monothiocarboxylic acids
- C07C327/32—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—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 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—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
- 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
- C07C323/60—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 with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C327/00—Thiocarboxylic acids
- C07C327/20—Esters of monothiocarboxylic acids
- C07C327/22—Esters of monothiocarboxylic acids having carbon atoms of esterified thiocarboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C327/00—Thiocarboxylic acids
- C07C327/20—Esters of monothiocarboxylic acids
- C07C327/26—Esters of monothiocarboxylic acids having carbon atoms of esterified thiocarboxyl groups bound to carbon atoms of six-membered aromatic rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (20)
- 일반식(Ⅰ)의 화합물 및 이의 약제학적으로 허용되는 산부가염.상기식에서, R1은 H또는 R5CO-이고, R2는 Y-C6H4-, Y-C6H4S-, Y-C6H4O-, Y-C6H4CH26-, Y-C6H4CH2O-, α-나프틸, β-나프틸, 푸릴, 티에닐, 벤조푸릴, 벤조티에닐, 디페닐메틸 또는 이며, -R3는 -OR6, -NR6R7또는이고, R4는 수소, 저급 알킬 또는 아릴 저급 알킬이며, R5는 저급알킬, 하이드록시 저급알킬, 저급 알콕시 저급알킬, (디-저급 알킬)아미노 저급알킬, Y1-C6H4- 저급알킬, 저급알콕시, Y1-C6H4-, 나프틸, 푸릴, 티에닐 또는 피리딜이고, R6및 R7은 독립적으로 수소, 저급 알킬 또는 치환된 저급 알킬[여기에서, 치환체는 1또는 2개의 하이드록시 그룹, 1또는 2개의 저급알콕시 그룹, 저급 알콕시 저급 알콕시, 할로게노, 할로게노 저급 알콕시, 아미노, 모노-또는 디-저급 알킬아미노, 헤테로사이클로 알킬, 저급알킬 헤테로사이클로 알킬, 아릴, 치환된 아릴(여기에서, 아릴상의 치환체는 저급알킬, 하이드록시, 할로게노, 저급 알콕시 및 아미노로 이루어진 그룹중에서 선택되는 1 내지 3개의 치환체이 선택된다), 및 환원으로서 1 내지 2개이 산소원자를 함유하는 5내지 6원의 포화된 환(여기에서, 환 탄소원자는 0내지 2개의 저급 알킬 치환체로 치환된다)으로 이루어진 그룹중에서 선택된다]이거나, R6및 R7은 이들이 결합된 질소원자와 함께 5내지 7원환(여기서, R6및 R7을 포함한 4내지 6개의 환원중 0내지 1개는 질소원자, 알킬-치환된 질소원자 또는 산소원자이고, 환은 환탄소 원자상에서 알킬 및 하이드록시로 이루어진 그룹중에서 선택된 0내지 3개의 치환체로 치환된다)을 완성하며, R28은 수소, 알킬, 카복시알킬, 머캅토알킬, 알킬티오알킬, 아미노알킬, 하이드록시알킬, 페닐알킬, 하이드록시페닐알킬, 구아니디노알킬, 이미다졸릴알킬, 인돌릴알킬 또는 카바모일알킬이고, n은 0내지 3이며,A는또는이고,Y2및 X1은 독립적으로 결합, -O-, -S-, 또는 -CH2-이며, Y, Y1및 Y2는 독립적으로 수소, 저급알킬, 사이클로저급알킬, 저급알콕시, OH, F, Cl, Br, I, -CN-, -CO2H, -CO2-저급알킬, -CH2NH2, -CONH2및 아릴로 이루어진 그룹중에서 선택된 1내지 3개의 치환체이다.
- 제1항에 있어서, R4가 수소인 화합물.
- 제1항 또는 2항에 있어서, n이 1임을 특징으로 하는 화합물.
- 제1항 내지 3항중 어느 한항에 있어서, R2가 Y-C6H4임을 특징으로 하는 화합물.
- 제1항 내지 4항중 어느 한항에 있어서, R1이 수소 아세틸 또는 벤조일임을 특징으로 하는 화합물.
- 제1항 내지 5항중 어느 한항에 있어서, A가임을 특징으로 하는 화합물.
- 제1항 내지 6항중 어느 한항에 있어서, R3가 OH, 아미노 또는 -NR6R7[여기에서, R6및 R7중 하나는 수소이고 다튼 하나는 아릴 저급 알킬 헤테로사이클로알킬 또는 저급 알킬 헤테로사이클로알킬이거나 R6및 R7의 이들과 결합된 질소와 함께 5내지 7원환(여기에서, R6및 R7을 포함한 4내지 6개의 환원중 0내지 1개는 질소원자, 알킬-치환된 질소원자 또는 산소원자이고, 환은 환 탄소원자상에서 알킬 및 하이드록시 그룹으로 이루어진 그룹중에서 선택된 0내지 3개의 치환체로 치환된다)을 완성한다]임을 특징으로 하는 화합물.
- 제1내지 7항중 어느 한항에 있어서, R3가 OH, 아미노, 2-(4-모르폴리닐)에틸아미노, 2-(4-피리디닐)에틸아미노, 또는 4-메틸-1-피페라지닐임을 특징으로 하는 화합물.
- 제1항에 있어서, 일반식(Ⅱ)로 나타내는 화합물.상기식에서 R1, A 및 R3는 하기와 같다.
- 포유 동물에게 제1항 내지 9항중 어느 한항에 따른 화합물을 단독으로 또는 심방성 나트륨 이뇨성 인자 또는 안지오텐신 전환 효소 억제제와 혼합하여 교혈압또는 울혈성 심장마비 치료 유효량으로 투여함을 특징으로 하여, 포유 동물에서 고혈압 또는 울혈성 심장마비를 치료하는 방법.
- 약제학적으로 허용되는 담체중에 제1항 내지 9항중 어느 한항에 따른 화합물을 단독으로 또는 심방성나트륨 이뇨성 인자 또는 안지오텐신 전환 효소 억제제와 혼합하여 고혈압 또는 울혈성 심장마비 치료 유효량으로 함유하는 약제학적 조성물.
- 제10항에 있어서, 심방성 나트륨 이뇨성 인자가 α사람 AP 21, α사람 AP 28, α사람 AP 23, α사람 AP 24, α사람 AP 25, α사람 AP 26, α사람 AP 33 및 위치 12에 있는 메티오닌이 이소로이신으로 대체된 상응하는 심방 펩타이드중에서 선택되는 방법.
- 제10항에 있어서, 안지오텐신 전환 효소가 스피라프릴, 에날라프릴, 라미프릴, 페린도프릴, 인돌라프릴 리시노프릴, [3S-[2R, (R′),3R]]-2-[2-[1-(에톡시 카보닐)-3-페닐프로필]아미노-1-옥소프로필]-1,2,3,4-테트라하이드로-6,7-디메톡시-3-이소퀴놀린-카복실산, 펜토프릴, 실라자프릴, 카프토프릴, 조페노프릴, 피발로프릴 및 포시노프릴 중에서 선택되는 방법.
- 포유 동물에게 진통-유효량의 제1항 내지 9항중 어느 한 항에 따른 화합물을 투여함을 특징으로 하여, 포유 동물에서 엔케팔리나제의 작용을 억제함으로써 진통 효과를 유도하는 방법.
- 약제학적으로 허용되는 담체중에 진통 유효량의 제1항 내지 9항중 어느 한 항에 따튼 화합물을 함유하는 약제학적 조성물.
- (A)일반식(Ⅱ)의 3-티오프로피온산 또는 이의 반응성 유도체를 일반식(Ⅳ)의 아민과 축합반응시켜 일반식(Ⅰ)의 화합물을 제조하거나, (B) 일반식 (Ⅰa)의 화합물을 일반식(Ⅴ)의 아민과 축합반응시켜 R3가 -NR6R7인 일반식(Ⅰ)의 화합물을 제조한 후, 필료한 경우 목적하는 이성체를 분리하고, 필요한 경우 보호 그룹을 제거시켜 목적하는 생성물을 수득하며, 필요한 경우 이의 염을 제조함을 특징으로 하여, 제1항에 따른 일반식(Ⅰ)의 화합물을 제조하는 방법.상기식에서, R1,R2,R3,R4,A 및 n은 제1항에서 정의한 바와같다.
- 제1용기에는 머캅토-아실 아미노산을 함유하는 약제학적 조성물이 함유되고 제2용기에는 심방성 나트륨 이뇨성 인자를 함유하는 약제학적 조성물이 함유됨을 특징으로 하는, 포유 동물의 고혈압 또는 울혈성 심장 마비를 치료하기 위해 배합하여 사용하기 위한 단일 포장내 분리 용기내에 약제학적 조성물을 함유하는 키트.
- 제1용기에는 머캅토-아실 아미노산을 함유하는 약제학적 조성물이 함유되고 제2용기에는 안지오텐신전환 효소 억제제를 함윰하는 약제학적 조성물이 함유됨을 특징으로 하는, 포유 동물의 고혈압 또는 울혈성 심장 마비를 치료하기 위해 배합하여 사용하기 위한 단일 포장내 분리 용기내에 약제학적 조성물을 함유하는 키트
- 제1항에 따른 화합물과 약제학적으로 허용되는 담체를 혼합함을 특징으로 하여 약제학적 조성물을 제조하는 방법.
- 고혈압, 울혈성 심장마비 또는 통증 상태 치료용 약제 제조를 위한 제1항에 따른 화합물의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25003588A | 1988-09-27 | 1988-09-27 | |
| US250035 | 1988-09-27 | ||
| US07/304,881 US4879309A (en) | 1988-09-27 | 1989-01-30 | Mercapto-acylamino acids as antihypertensives |
| US304881 | 1989-01-30 | ||
| PCT/US1989/004068 WO1990003364A1 (en) | 1988-09-27 | 1989-09-25 | Mercapto-acylamino acids useful in the treatment of cardiovascular disorders and as analgesics |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR900701748A true KR900701748A (ko) | 1990-12-04 |
Family
ID=26940546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019900701086A KR900701748A (ko) | 1988-09-27 | 1989-09-25 | 심장혈관 장애의 치료 및 진통제로서 유용한 머캅토-아실 아미노산 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US4879309A (ko) |
| EP (1) | EP0364767A1 (ko) |
| KR (1) | KR900701748A (ko) |
| AU (1) | AU4342989A (ko) |
| WO (1) | WO1990003364A1 (ko) |
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|---|---|---|---|---|
| FR2540495B1 (fr) * | 1983-02-07 | 1986-02-14 | Roussel Uclaf | Nouveaux derives de o-mercaptopropanamide et de ses homologues, leur procede de preparation, leur application comme medicaments, les compositions les renfermant et les nouveaux intermediaires obtenus |
| US5179125A (en) * | 1987-12-03 | 1993-01-12 | Dainippon Pharmaceutical Co., Ltd. | N-substituted mercaptopropanamide derivatives |
| WO1989005796A1 (en) * | 1987-12-16 | 1989-06-29 | Schering Corporation | Mercapto-acylamino acid antihypertensives |
| ZA902661B (en) * | 1989-04-10 | 1991-01-30 | Schering Corp | Mercapto-acyl amino acids |
| US5223516A (en) * | 1990-03-22 | 1993-06-29 | E. R. Squibb & Sons, Inc. | 3,3,3-trifluoro-2-mercaptomethyl-N-tetrazolyl substituted propanamides and method of using same |
| US5173506A (en) * | 1990-08-16 | 1992-12-22 | Schering Corporation | N-(mercaptoalkyl)ureas and carbamates |
| FR2679564A1 (fr) * | 1991-07-23 | 1993-01-29 | Inst Nat Sante Rech Med | Nouveaux acylmercaptoalcanoldipeptides, leur preparation et les compositions qui les contiennent. |
| US5340828A (en) * | 1991-09-30 | 1994-08-23 | Merck & Co., Inc. | Inhibitors of farnesyl protein transferase |
| FR2682952B1 (fr) * | 1991-10-25 | 1993-12-03 | Institut Nal Sante Recherc Medic | Nouveaux n-(mercaptoacyl) amino-acides, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| AU679452B2 (en) * | 1992-08-24 | 1997-07-03 | Merrell Dow Pharmaceuticals Inc. | Novel 2-substituted indane-2-mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase |
| US5508272A (en) * | 1993-06-15 | 1996-04-16 | Bristol-Myers Squibb Company | Compounds containing a fused bicycle ring and processes therefor |
| US5362727A (en) * | 1993-07-26 | 1994-11-08 | Bristol-Myers Squibb | Substituted azepino[2,1-a]isoquinoline compounds |
| IT1266571B1 (it) * | 1993-07-30 | 1997-01-09 | Zambon Spa | Derivati della beta-mercapto-propanammide utili nel trattamento delle malattie cardiovascolari |
| US5525723A (en) * | 1993-11-18 | 1996-06-11 | Bristol-Myers Squibb Co. | Compounds containing a fused multiple ring lactam |
| WO1995021857A1 (en) * | 1994-02-14 | 1995-08-17 | Merrell Pharmaceuticals Inc. | Novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and ace |
| HUT74584A (en) * | 1994-02-14 | 1997-01-28 | Merrell Pharma Inc | Novel heterocycle fused benzazepine-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase, process for producing them and pharmaceutical compositions containing them |
| JPH09508906A (ja) * | 1994-02-14 | 1997-09-09 | メレル ファーマスーティカルズ インコーポレーテッド | エンケファリナーゼ及びａｃｅの阻害剤として有用な新規なメルカプトアセチルアミド１，３，４，５−テトラヒドロベンゾ［ｃ］アゼピン−３−オンジスルフィド誘導体類 |
| US5616775A (en) * | 1994-05-05 | 1997-04-01 | Bristol-Myers Squibb Co. | Process for preparing homocystein analogs useful as intermediates for compounds containing a fused bicyclic ring |
| US5587375A (en) * | 1995-02-17 | 1996-12-24 | Bristol-Myers Squibb Company | Azepinone compounds useful in the inhibition of ACE and NEP |
| US5877313A (en) | 1995-05-17 | 1999-03-02 | Bristol-Myers Squibb | Benzo-fused azepinone and piperidinone compounds useful in the inhibition of ACE and NEP |
| US5650408A (en) * | 1995-06-07 | 1997-07-22 | Karanewsky; Donald S. | Thiazolo benzazepine containing dual action inhibitors |
| US5635504A (en) * | 1995-06-07 | 1997-06-03 | Bristol-Myers Squibb Co. | Diazepine containing dual action inhibitors |
| EA006153B1 (ru) * | 2000-06-26 | 2005-10-27 | Пфайзер Продактс Инк. | СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ |
| EP1401840A4 (en) * | 2001-04-30 | 2007-05-16 | Bayer Corp | NEW 4-AMINO-5,6-SUBSTITUTED THIOPHENO 2,3 D | PYRIMIDINE |
| ME01269B (me) | 2008-08-20 | 2013-06-20 | Zoetis Services Llc | Jedinjenja pirolo (2,3-d) pirimidina |
| NL2022471B1 (en) | 2019-01-29 | 2020-08-18 | Vationpharma B V | Solid state forms of oclacitinib |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4005222A (en) * | 1975-05-21 | 1977-01-25 | Mead Johnson & Company | Mucolytic mercaptoacylamidobenzoic and benzenesulfonic acid compounds and process |
| US4053651A (en) * | 1976-05-10 | 1977-10-11 | E. R. Squibb & Sons, Inc. | Compounds and method for alleviating angiotensin related hypertension |
| US4132802A (en) * | 1976-10-18 | 1979-01-02 | Mead Johnson & Company | Benzoic acid derivative and benzenesulfonic acid mucolytic process |
| US4329363A (en) * | 1978-09-08 | 1982-05-11 | Merck & Co., Inc. | Substituted mercapto acid amides and their use |
| EP0038046B1 (en) * | 1980-04-11 | 1984-02-29 | The Wellcome Foundation Limited | Pharmaceutical amides, and preparation, formulations and use thereof |
| FR2480747A1 (fr) * | 1980-04-17 | 1981-10-23 | Roques Bernard | Derives d'acides amines et leur application therapeutique |
| JPS5732260A (en) * | 1980-08-07 | 1982-02-20 | Meito Sangyo Kk | Mercaptofatty acid derivative and its preparation |
| US4329495A (en) * | 1981-05-18 | 1982-05-11 | Pfizer Inc. | Enkephalinase enzyme inhibiting compounds |
| US4401677A (en) * | 1981-10-09 | 1983-08-30 | E. R. Squibb & Sons, Inc. | Enkephalinase inhibitors |
| BE890948A (fr) * | 1981-10-30 | 1982-02-15 | Luitpold Werk Chem Pharm | Derives de l'acide anthranilique |
| FR2540495B1 (fr) * | 1983-02-07 | 1986-02-14 | Roussel Uclaf | Nouveaux derives de o-mercaptopropanamide et de ses homologues, leur procede de preparation, leur application comme medicaments, les compositions les renfermant et les nouveaux intermediaires obtenus |
| US4774256A (en) * | 1983-10-03 | 1988-09-27 | E. R. Squibb & Sons, Inc. | Use of enkephalinase inhibitors as analgesic agents |
| DE3467754D1 (de) * | 1983-10-03 | 1988-01-07 | Squibb & Sons Inc | Enkephalinase inhibitors |
| JPS62270555A (ja) * | 1986-05-19 | 1987-11-24 | Dainippon Pharmaceut Co Ltd | スルホン酸誘導体およびその塩 |
| US4801609B1 (en) * | 1987-03-27 | 1993-11-09 | Mercapto-acylamino acid antihypertensives | |
| US4740499A (en) * | 1986-07-28 | 1988-04-26 | Monsanto Company | Method of enhancing the bioactivity of atrial peptides |
-
1989
- 1989-01-30 US US07/304,881 patent/US4879309A/en not_active Expired - Fee Related
- 1989-09-25 WO PCT/US1989/004068 patent/WO1990003364A1/en unknown
- 1989-09-25 EP EP89117684A patent/EP0364767A1/en not_active Withdrawn
- 1989-09-25 KR KR1019900701086A patent/KR900701748A/ko not_active Application Discontinuation
- 1989-09-25 AU AU43429/89A patent/AU4342989A/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO1990003364A1 (en) | 1990-04-05 |
| AU4342989A (en) | 1990-04-18 |
| US4879309A (en) | 1989-11-07 |
| US4879309B1 (ko) | 1992-07-14 |
| EP0364767A1 (en) | 1990-04-25 |
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| PA0109 | Patent application |
Patent event code: PA01091R01D Comment text: Patent Application Patent event date: 19900525 |
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| PC1203 | Withdrawal of no request for examination | ||
| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |