JPH11507662A - 抗虚血性ヒドロキシルアミン誘導体および医薬組成物 - Google Patents
抗虚血性ヒドロキシルアミン誘導体および医薬組成物Info
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- JPH11507662A JPH11507662A JP9502829A JP50282997A JPH11507662A JP H11507662 A JPH11507662 A JP H11507662A JP 9502829 A JP9502829 A JP 9502829A JP 50282997 A JP50282997 A JP 50282997A JP H11507662 A JPH11507662 A JP H11507662A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—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
- C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/092—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
-
- 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C275/64—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 singly-bound to oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—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
- C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.一般式(I): (式中、XはO、−NHまたは式:−NR’−により表される基であり、ここで RおよびR’は互いに独立にアルキル、シクロアルキル、フェニルアルキル;ハ ロ、ハロアルキル、アルキル、アルコキシまたはニトロにより任意に置換された フェニル基;または窒素含有ヘテロ環であり、R1はHまたはアルカノイルであ り、R2はHまたはアルカノイルにより任意にアシル化されたヒドロキシであり 、R3は式:−N(R4)R5により表される基であり、ここでR4およびR5は互 いに独立にH、アルキルまたは式:−C(O)−NH−Rにより表される基であ って、Rが上記定義の通りのものであるか、またはR4およびR5はそれらに結合 している隣接する窒素と共に窒素、酸素および硫黄から選ばれる1個の追加のヘ テロ原子を含んでいてもよい5〜7員複素環であって、フェニルアルキルのアル キルにより任意に置換された複素環を形成する。) により表されるヒドロキシルアミン誘導体および医薬として許容可能なそれらの 酸付加塩。 2.XがOであり、R、R’、R1、R2およびR3が請求項1に定義される通 りのものである請求項1記載の一般式(I)により 表される化合物。 3.XがNHまたは−NR’であり、R、R’、R1、R2およびR3が請求項 1に定義される通りのものである請求項1記載の一般式(I)により表される化 合物。 4.R3を表す−N(R4)R5基がピペリジノ、ピペラジノまたはモルホリノ により任意に置き換えられた請求項1〜3のいずれか1項に記載の一般式(I) により表される化合物。 5.R3を表す−N(R4)R5基がジアルキルアミノである請求項1〜3のい ずれか1項に記載の一般式(I)により表される化合物。 6.R3が−N(R4)R5であり、R4がアルキルであり、R5が−C(=O) −NH−Rである請求項1〜3のいずれか1項に記載の一般式(I)により表さ れる化合物。 7.活性成分として請求項1〜6のいずれか1項に定義される一般式(I)に より表される化合物または医薬的に活性なそれらの酸付加塩を含む医薬組成物。 8.一般式(I): (式中、XはO、−NHまたは式:−NR’−により表される基であり、ここで RおよびR’は互いに独立にアルキル、シクロアルキル、フェニルアルキル;ハ ロ、ハロアルキル、アルキル、アルコキ シまたはニトロにより任意に置換されたフェニル基;または窒素含有ヘテロ環で あり、R1はHまたはアルカノイルであり、R2はHまたはアルカノイルにより任 意にアシル化されたヒドロキシであり、R3は式:−N(R4)R5により表され る基であり、ここでR4およびR5は互いに独立にH、アルキルまたは式:−C( O)−NH−Rにより表される基であって、Rが上記定義の通りのものであるか 、またはR4およびR5はそれらに結合している隣接する窒素と共に窒素、酸素お よび硫黄から選ばれる1個の追加のヘテロ原子を含んでいてもよい5〜7員複素 環であって、フェニルアルキルのアルキルにより任意に置換された複素環を形成 する。) により表されるヒドロキシルアミン誘導体および医薬として許容可能なそれらの 酸付加塩の調製方法であって、 a)XがOである一般式(I)により表される化合物を調製するために、 i)一般式(II): (式中、R2およびR3は上記定義の通りのものである。) により表される化合物を一般式(III): (式中、Rは上記定義の通りのものであり、Yはハロまたはアジドである。) により表される化合物と反応させるか、もしくは、 ii)一般式(VI): により表される化合物を一般式(VII): により表される化合物と反応させるか、もしくは、 iii)一般式(VI)により表される化合物を一般式(VIII): により表される化合物と反応させるか、または、 iv)一般式(VI)により表される化合物を一般式(IX): により表される化合物と反応させ、その後、式:R3Hにより表される化合物と 反応させること、ただし式(VI)、(VII)、(VIII)および(IX)においてR 、R2およびR3は上記定義の通りのものであり、Yはハロである; b)Xが−NH−である一般式(I)により表される化合物を調製するために 、R2およびR3が上記定義の通りのものである一般式(II)により表される化合 物を式(IV)または(IVa): (式中、Rは上記定義の通りのものであり、Yはハロである。) により表される化合物と反応させること: c)Xが−NH−または−NR’−である一般式(I)により表される化合物 を調製するために、一般式(X): (式中、R1、R2およびR3は上記定義の通りのものであり、Zはアルキル、ア ラルキルまたは任意に置換アリールである。) により表される化合物を一般式:RNH2またはRR’NH(式中、RおよびR ’は上記定義の通りのものである。)により表される化合物と反応させること; もしくは d)Xが−NH−であり、R3が−N(R4)R5であり、R4がアルキルであり 、R5が−C(O)−NH−Rである一般式(I)により表される化合物を調製 するために、 i)R3が−N(R4)R5であり、R4がアルキルであり、R5がHであり、R2 が上記定義の通りのものである式(II)により表される化合物を、Rが上記定義 の通りのものであり、かつ、Yがハロである過剰の式(IV)または(IVa)によ り表される化合物と反応させること;もしくは ii)R3が−N(R4)R5であり、R4がアルキルであり、R5がHであり、R1 、R2およびR3が上記定義の通りのものである一般式(I)により表される化合 物をRが上記定義の通りのものであり、かつ、Yがハロである一般式(IV)また は(IVa)により表される化合物と反応させること;または e)Xが−NR’−である一般式(I)により表される化合物を調製するため に、一般式(II)により表される化合物を一般式(V): (式中、R、R’、R2およびR3は上記定義の通りのものであり、Yはハロであ る。) により表される化合物と反応させること; を含み、所望であれば、一般式(I)により表される化合物をその酸付加塩に転 化させるか、または所望であれば、R1がHであり、かつ、R2がヒドロキシであ る一般式(I)により表される化合物を、R2がアシロキシであるか、もしくは R1がアシルであり、かつ、R2がアシロキシである一般式(I)により表される 化合物に転化させ、続いて塩形成させることを特徴とする方法。 9.医薬組成物の調製における請求項1〜6のいずれか1項に定義される一般 式(I)により表される化合物および医薬的に活性なそれらの酸付加塩の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
HU9501756 | 1995-06-15 | ||
HU9501756A HU218480B (hu) | 1995-06-15 | 1995-06-15 | Hidroxilaminszármazékok, eljárás előállításukra és a vegyületeket tartalmazó gyógyszerkészítmények |
PCT/HU1996/000033 WO1997000251A1 (en) | 1995-06-15 | 1996-06-14 | Anti-ischaemic hydroxylamine derivatives and pharmaceutical compositions |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH11507662A true JPH11507662A (ja) | 1999-07-06 |
JP4083800B2 JP4083800B2 (ja) | 2008-04-30 |
Family
ID=10986948
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50282997A Expired - Fee Related JP4083800B2 (ja) | 1995-06-15 | 1996-06-14 | 抗虚血性ヒドロキシルアミン誘導体および医薬組成物 |
Country Status (23)
Country | Link |
---|---|
US (1) | US6002002A (ja) |
EP (1) | EP0832079B1 (ja) |
JP (1) | JP4083800B2 (ja) |
KR (1) | KR100444780B1 (ja) |
AT (1) | ATE215075T1 (ja) |
AU (1) | AU703163B2 (ja) |
BR (1) | BR9608929A (ja) |
CA (1) | CA2221689C (ja) |
CZ (1) | CZ295547B6 (ja) |
DE (1) | DE69620175T2 (ja) |
DK (1) | DK0832079T3 (ja) |
ES (1) | ES2174077T3 (ja) |
HR (1) | HRP960279B1 (ja) |
HU (1) | HU218480B (ja) |
IL (1) | IL122141A (ja) |
IN (1) | IN185781B (ja) |
PL (1) | PL185592B1 (ja) |
PT (1) | PT832079E (ja) |
SI (1) | SI0832079T1 (ja) |
SK (1) | SK282953B6 (ja) |
WO (1) | WO1997000251A1 (ja) |
YU (1) | YU49419B (ja) |
ZA (1) | ZA964978B (ja) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA64716C2 (en) * | 1996-08-09 | 2004-03-15 | Pharmaceuticals for therapy or prevention of illnesses connected with dysfunction of vascular endothelial cells | |
CN1615296A (zh) | 2002-01-11 | 2005-05-11 | 拜奥列克斯研究发展公司 | 甲脒衍生物及其在治疗血管疾病中的用途 |
WO2005074594A2 (en) | 2004-01-30 | 2005-08-18 | Great Lakes Chemical Corporation | Production processes and systems, compositions, surfactants, monomer units, metal complexes, phosphate esters, glycols, aqueous film forming foams, and foam stabilizers |
US8318656B2 (en) | 2007-07-03 | 2012-11-27 | E. I. Du Pont De Nemours And Company | Production processes and systems, compositions, surfactants, monomer units, metal complexes, phosphate esters, glycols, aqueous film forming foams, and foam stabilizers |
KR101405103B1 (ko) * | 2014-03-25 | 2014-06-10 | 재 남 우 | 레버식 수동개방기구를 구비하는 초고압 압축가스 개폐장치 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE369944C (de) * | 1918-03-07 | 1923-02-24 | Anilin Fabrikation Ag | Verfahren zur Darstellung von Tetrahydronaphthalin |
DE2651083A1 (de) * | 1976-11-09 | 1978-05-18 | Hoechst Ag | Neue o-alkylierte hydroxylamine, verfahren zu ihrer herstellung und ihre verwendung |
EP0369944A1 (de) * | 1988-11-18 | 1990-05-23 | Ciba-Geigy Ag | Substituierte Oxadiaminobutane |
EP0495750A3 (en) * | 1991-01-14 | 1992-09-16 | Ciba-Geigy Ag | Heterocyclic hydroxylamine |
-
1995
- 1995-06-15 HU HU9501756A patent/HU218480B/hu not_active IP Right Cessation
-
1996
- 1996-06-12 IN IN1286DE1996 patent/IN185781B/en unknown
- 1996-06-12 ZA ZA9604978A patent/ZA964978B/xx unknown
- 1996-06-12 HR HR960279A patent/HRP960279B1/xx not_active IP Right Cessation
- 1996-06-14 YU YU36996A patent/YU49419B/sh unknown
- 1996-06-14 DE DE69620175T patent/DE69620175T2/de not_active Expired - Fee Related
- 1996-06-14 BR BR9608929A patent/BR9608929A/pt active Search and Examination
- 1996-06-14 CA CA002221689A patent/CA2221689C/en not_active Expired - Fee Related
- 1996-06-14 ES ES96921009T patent/ES2174077T3/es not_active Expired - Lifetime
- 1996-06-14 KR KR1019970709431A patent/KR100444780B1/ko not_active IP Right Cessation
- 1996-06-14 SK SK1713-97A patent/SK282953B6/sk not_active IP Right Cessation
- 1996-06-14 SI SI9630462T patent/SI0832079T1/xx unknown
- 1996-06-14 WO PCT/HU1996/000033 patent/WO1997000251A1/en active IP Right Grant
- 1996-06-14 AT AT96921009T patent/ATE215075T1/de not_active IP Right Cessation
- 1996-06-14 PL PL96324197A patent/PL185592B1/pl not_active IP Right Cessation
- 1996-06-14 AU AU62376/96A patent/AU703163B2/en not_active Ceased
- 1996-06-14 IL IL12214196A patent/IL122141A/xx not_active IP Right Cessation
- 1996-06-14 US US08/914,115 patent/US6002002A/en not_active Expired - Fee Related
- 1996-06-14 PT PT96921009T patent/PT832079E/pt unknown
- 1996-06-14 EP EP96921009A patent/EP0832079B1/en not_active Expired - Lifetime
- 1996-06-14 CZ CZ19974015A patent/CZ295547B6/cs not_active IP Right Cessation
- 1996-06-14 DK DK96921009T patent/DK0832079T3/da active
- 1996-06-14 JP JP50282997A patent/JP4083800B2/ja not_active Expired - Fee Related
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