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1. 发明授权

US5278161A Amino acid derivatives useful as renin inhibitors 失效
标题翻译：用作肾素抑制剂的氨基酸衍生物
公开(公告)号：US5278161A
公开(公告)日：1994-01-11
申请号：US971787
申请日：1992-11-05
申请人： Quirico Branca , Marie-Paule Heitz , Marcel Muller , Werner Neidhart , Stadler Heinz , Eric Vieira , Wolfgang Wostl
发明人： Quirico Branca , Marie-Paule Heitz , Marcel Muller , Werner Neidhart , Stadler Heinz , Eric Vieira , Wolfgang Wostl
IPC分类号： C07D263/06 , C07D471/04 , C07D487/04 , A61K31/495
CPC分类号： C07D471/04 , C07D263/06 , C07D487/04
摘要： Compounds of the formula ##STR1## wherein A, B, X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as set forth in the specification, in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diasteromeric racemates as well as pharmaceutically acceptable salts thereof which inhibit the activity of the natural enzyme renin and are useful in the control or prevention of high blood pressure and cardiac insufficiency are described.
摘要翻译：其中A，B，X，Y，R 1，R 2，R 3，R 4和R 5如说明书中所述的光学纯非对映异构体的形式，非对映异构体的混合物，非对映体外消旋体或混合物的非对映异构体外消旋物及其药学上可接受的盐，其抑制天然酶肾素的活性并且可用于控制或预防高血压和心脏功能不全。

2. 发明授权

US5278148A Amino acid derivatives useful for treating high blood pressure 失效
标题翻译：用于治疗高血压的氨基酸衍生物
公开(公告)号：US5278148A
公开(公告)日：1994-01-11
申请号：US499852
申请日：1990-03-27
申请人： Quirico Branca , Hans P. Marki , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
发明人： Quirico Branca , Hans P. Marki , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
IPC分类号： A61K31/16 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/4427 , A61K31/445 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , C07C237/06 , C07C271/16 , C07C271/18 , C07C271/20 , C07D231/12 , C07D233/54 , C07D233/64 , C07D277/20 , C07D277/30 , C07D333/24 , C07D401/12 , C07D403/12 , C07K5/02 , C07K5/065 , A61K37/02 , A61K37/43 , C07C233/08 , C07C235/02 , C07C237/02 , C07K5/06 , C07K5/08
CPC分类号： C07D231/12 , C07D233/64 , C07D277/30 , C07D333/24 , C07D401/12 , C07D403/12 , C07K5/0207 , C07K5/06078 , A61K38/00
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.-naphthyl, Y is a bivalent residue in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译：丙基，异丙基，咪唑-2-基，咪唑-4-基，吡唑-3-基，噻唑-4-基，噻吩-2-基，噻吩-2-基，噻吩-2-基，噻吩-2-基，叔丁基羰基甲基，苄氧基羰基甲基或叔丁氧基，R 3是异丁基，环己基甲基或苄基，R 4是硝基，氨基或式-N（R 5）（R 6）的基团，其中R5和R6是烷基或烷氧基烷基; 或任选取代的苯基，苯基烷基或苯基磺酰基烷基等，条件是当R6为烷酰基，烷氧基羰基或芳基烷氧基羰基时，A不为（b）组，虚线可为附加键，R7为苯基或取代苯基，R8为氢或有机羰基烷基，条件是当R 7是苯基，苄基或α-萘基时，R 8不是烷氧基羰基氨基或芳基烷氧基羰基氨基，Y是光学纯非对映异构体形式的二价残基，非对映异构体的混合物，非对映体外消旋物或非对映体外消旋物的混合物，以及其药学上可用的盐抑制天然酶肾素的活性，因此可用于控制或预防高血压和心脏功能不全。

3. 发明授权

US4513002A Cycloheptene derivatives 失效
标题翻译：环庚烯衍生物
公开(公告)号：US4513002A
公开(公告)日：1985-04-23
申请号：US330733
申请日：1981-12-14
申请人： Werner Aschwanden , Quirico Branca , Emilio Kyburz , Rudolf Pfister
发明人： Werner Aschwanden , Quirico Branca , Emilio Kyburz , Rudolf Pfister
IPC分类号： C07D295/02 , A61K31/00 , A61P37/08 , C07C1/00 , C07C13/547 , C07C17/00 , C07C17/16 , C07C17/26 , C07C22/04 , C07C27/00 , C07C33/34 , C07C35/37 , C07C67/00 , C07C301/00 , C07C303/22 , C07C303/32 , C07C309/63 , C07D207/04 , C07D295/03 , A61K31/40
CPC分类号： C07D295/03 , C07C2103/32
摘要： 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidine of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions, such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.
摘要翻译：具有式I的1- [2-（4,5,10,11-四氢-1H-二苯并[a，d]环庚烯-5-基）乙基]吡咯并且其药学上可接受的酸加成盐，制备通过各种中间体进行描述。这些化合物具有有价值的组胺H1拮抗性质，适用于控制或预防过敏反应，如荨麻疹，花粉热，过敏反应和过度敏感的药物。

4. 发明授权

US06297375B1 4-phenyl-pyridine derivatives 有权
标题翻译： 4-苯基 - 吡啶衍生物
公开(公告)号：US06297375B1
公开(公告)日：2001-10-02
申请号：US09507456
申请日：2000-02-22
申请人： Michael Bös , Quirico Branca , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Quirico Branca , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07D21382
CPC分类号： C07D213/30 , C07D213/38 , C07D213/40 , C07D213/74 , C07D213/75 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14
摘要： The compounds of the related invention are related to 4-phenyl-pyridine derivatives connected by a bridge containing oxygen or nitrogen to a phenyl derivative.
摘要翻译：相关发明的化合物涉及通过含有氧或氮的桥与苯基衍生物连接的4-苯基 - 吡啶衍生物。

5. 发明授权

US4374773A Triazolo-benzodiazepine derivatives 失效
标题翻译：三唑并苯并二氮杂衍生物
公开(公告)号：US4374773A
公开(公告)日：1983-02-22
申请号：US225747
申请日：1981-01-16
申请人： Quirico Branca , Albert E. Fischli , Andre Szente
发明人： Quirico Branca , Albert E. Fischli , Andre Szente
IPC分类号： A61K31/55 , A61P1/16 , A61P9/04 , A61P9/12 , C07D243/24 , C07D487/04
CPC分类号： C07D487/04 , C07D243/24 , Y10S514/893
摘要： There are presented compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 and R.sup.3 each are a hydrogen atom or a lower alkyl group, R.sup.4 is a halogen atom and either R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 is a lower alkyl or lower hydroxyalkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached are a 3-membered to 7-membered heterocycle,and pharmaceutically acceptable acid addition salts thereof.The compounds and their salts are novel and possess valuable pharmacodynamic properties.
摘要翻译：提供式Ⅰ的化合物，其中R 1是氢原子或低级烷基，R 2和R 3各自是氢原子或低级烷基，R 4是卤素原子，R 5是氢原子或低级烷基，R 6为低级烷基或低级羟基烷基或R 5和R 6与它们所连接的氮原子一起为3-元至7-元杂环，及其药学上可接受的酸加成盐。化合物及其盐是新颖的，具有有价值的药效学性质。

6. 发明授权

US5393875A Amino acid derivatives having renin inhibiting activity 失效
标题翻译：具有肾素抑制活性的氨基酸衍生物
公开(公告)号：US5393875A
公开(公告)日：1995-02-28
申请号：US100959
申请日：1993-08-03
申请人： Quirico Branca , Marie-Paule Heitz , Werner Neidhart , Heinz Stadler , Eric Vieira , Wolfgang Wostl
发明人： Quirico Branca , Marie-Paule Heitz , Werner Neidhart , Heinz Stadler , Eric Vieira , Wolfgang Wostl
IPC分类号： A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/535 , A61P9/00 , A61P9/04 , A61P9/12 , C07C317/44 , C07C317/50 , C07C323/51 , C07D207/08 , C07D207/12 , C07D211/22 , C07D213/40 , C07D213/53 , C07D213/56 , C07D231/12 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D233/64 , C07D277/20 , C07D277/30 , C07D295/088 , C07D295/185 , C07D295/205 , C07D307/54 , C07D317/24 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00 , C07H15/12 , C07D295/12 , A61K37/00
CPC分类号： C07D207/08 , C07C317/44 , C07C317/50 , C07D207/12 , C07D211/22 , C07D213/40 , C07D213/53 , C07D213/56 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D277/30 , C07D295/088 , C07D295/185 , C07D295/205 , C07D307/54 , C07D317/24 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the significance given in claim 1,in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharamaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency. They can be manufactured according to various methods which are known per se.
摘要翻译：其中A，R 1，R 2，R 3，R 4和R 5具有权利要求1中给出的含义的化合物，其为光学纯非对映异构体，非对映异构体的混合物，非对映体外消旋物或非对映异构体外消旋物的混合物作为其药学上可用的盐抑制天然酶肾素的活性，因此可以以药物制剂的形式用于控制或预防高血压和心脏功能不全。它们可以根据本身已知的各种方法制造。

7. 发明授权

US5256645A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5256645A
公开(公告)日：1993-10-26
申请号：US872736
申请日：1992-04-22
申请人： Quirico Branca , Werner Neidhart , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
发明人： Quirico Branca , Werner Neidhart , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
IPC分类号： C07C215/26 , C07C237/00 , C07C317/44 , C07D233/54 , C07D263/04 , C07D263/24 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12 , A61K37/00
CPC分类号： C07D233/64 , C07C215/26 , C07C237/00 , C07C317/44 , C07D263/04 , C07D263/24 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要： The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译：其中A，R 1，R 2，R 3，R 4，R 5和R 6如上所述的式Ⅺ化合物被描述。式I的化合物对天然酶肾素具有抑制活性，因此可以以用于控制或预防高血压和心功能不全的药物制剂的形式使用。

8. 发明授权

US5140011A Amino acid derivatives which have renin inhibiting activity 失效
标题翻译：具有疝抑制活性的氨基酸衍生物
公开(公告)号：US5140011A
公开(公告)日：1992-08-18
申请号：US501694
申请日：1990-03-29
申请人： Quirico Branca , Hans P. Marki , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
发明人： Quirico Branca , Hans P. Marki , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
IPC分类号： A61K31/16 , A61K38/00 , A61P9/04 , A61P9/12 , C07C237/06 , C07C271/20 , C07C279/12 , C07D231/12 , C07D233/54 , C07D233/58 , C07D233/64 , C07D277/22 , C07D333/10 , C07D401/12 , C07K5/02 , C07K5/065 , C07K5/097
CPC分类号： C07D233/54 , C07D401/12 , C07K5/021 , C07K5/06078 , C07K5/0823 , A61K38/00
摘要： The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in claim 1, in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译：其中A，R 1，R 2，R 3和R 4具有权利要求1给出的含义的化合物，其形式为光学纯非对映异构体，非对映异构体的混合物，非对映体外消旋体或非对映体外消旋体的混合物，以及药学上其可用的盐抑制天然酶肾素的活性，因此可以以药物制剂的形式用于控制或预防高血压和心脏功能不全。

9. 发明授权

US4808605A Tetrahydronaphthalene derivatives as calcium antagonists 失效
标题翻译：四氢萘衍生物作为钙拮抗剂
公开(公告)号：US4808605A
公开(公告)日：1989-02-28
申请号：US119114
申请日：1987-11-10
申请人： Quirico Branca , Roland Jaunin , Hans P. Maki , Franzi Marti , Henri Ramuz
发明人： Quirico Branca , Roland Jaunin , Hans P. Maki , Franzi Marti , Henri Ramuz
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/55 , A61K31/551 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D233/54 , C07D233/64 , C07D235/14 , C07D235/26 , C07D243/14 , C07D277/62 , C07D277/64 , C07D401/06 , C07D471/04 , C07D487/04 , C07D521/00 , C07D413/06
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D235/14 , C07D235/26 , C07D243/14 , C07D249/08 , C07D277/64 , C07D401/06 , C07D471/04 , C07D487/04
摘要： Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof. The compounds of formual I have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias, high blood pressure and cardiac insufficiency.
摘要翻译：其中R为低级烷基，R 1为卤素，R 2为C 1 -C 12 - 烷基，R 3为羟基，低级烷氧基，低级烷基 - 羰基氧基，低级烷氧基 - 低级 - 烷基羰基氧基，低级烷基氨基羰基氧基，芳基氨基羰基氧基或芳基 - 低级烷基氨基羰基氧基，X是C1-C18-亚烷基，其任选可以被1,4-亚苯基中断或被1,4-亚环己基中断或延长，A是二或三取代的2-咪唑基经由亚乙基或取代或未取代的选自苯并咪唑基，苯并咪唑啉酮，咪唑并[4,5-c]吡啶基，咪唑并[4,5-c]吡啶基，苯并噻唑基，苯并二氮杂-2,5-二 -1-基和吡咯并[2,1-c] - [1,4]苯并二氮杂-5,11-二酮-10-基，n为0或1，以外消旋体和光学对映体的形式，以及作为N-氧化物及其可药用的酸加成盐。形式I的化合物具有显着的钙拮抗和抗心律不齐活性，因此可以用作药物，特别是用于控制或预防心绞痛，局部缺血，心律失常，高血压和心脏功能不全。

10. 发明授权

US4327026A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US4327026A
公开(公告)日：1982-04-27
申请号：US283711
申请日：1981-07-16
申请人： Quirico Branca , Albert E. Fischli , Andre' Szente
发明人： Quirico Branca , Albert E. Fischli , Andre' Szente
IPC分类号： A61K31/55 , A61K31/551 , A61P5/38 , C07D243/16 , C07D243/18 , C07D243/24 , C07D243/26 , C07D243/28
CPC分类号： C07D243/24
摘要： There is presented benzodiazepine derivatives of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is lower alkyl, R.sup.2 and R.sup.3 each are hydrogen or lower alkyl, R.sup.4 is the group ##STR3## R.sup.5 is hydrogen or halogen, R.sup.8 is hydrogen or lower alkyl, R.sup.9 is lower alkyl or lower alkoxyalkyl, R.sup.10 is lower alkyl, R.sup.11 is hydrogen, lower alkyl or lower hydroxyalkyl, R.sup.12 is hydrogen or lower alkyl and R.sup.14 is lower alkyl or aryl, and either R.sup.6 is hydrogen or lower alkyl and R.sup.7 is lower alkyl or lower hydroxyalkyl or R.sup.6 and R.sup.7 together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N-R.sup.13, in which R.sup.13 is hydrogen or lower alkyl, and either R.sup.6 ' is hydrogen or lower alkyl and R.sup.7 ' is lower alkyl or R.sup.6 ' and R.sup.7 ' together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula > N-R.sup.13 ', in which R.sup.13 ' is lower alkyl, with the proviso that R.sup.4 is the group R.sup.6 ' R.sup.7 ' N--CO--NH--CH(R.sup.8)-- when A is the group (c),and pharmaceutically acceptable acid addition salts thereof.The compounds exhibit aldosterone-antagonistic properties and are suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.
摘要翻译：呈现下式的苯并二氮杂衍生物其中A是下列基团：R 1是低级烷基，R 2和R 3各自是氢或低级烷基，R 4是基团 + TR R5是氢或卤素，R8是氢或低级烷基，R9是低级烷基或低级烷氧基烷基，R10是低级烷基，R11是氢，低级烷基或低级羟烷基，R12是氢或低级烷基，R14是低级烷基或芳基，并且R 6是氢或低级烷基，且R 7是低级烷基或低级羟基烷基，或者R 6和R 7与氮原子一起是3-至7-元杂环，当它至少为5元时，它可以含有一个环成员为氧或硫原子或式> N-R13的基团，其中R13为氢或低级烷基，R6'为氢或低级烷基，R7'为低级烷基或R6'和R7'以及氮原子是3-至7-元杂环，当其为至少5元时，其可以含有作为环成员的氧或硫原子或式“N-R13”的基团，其中R13'为低级烷基，条件是R4为R6'R7'N-CO-NH-CH（R8） - 当A为（c）组及其药学上可接受的酸加成盐。该化合物显示醛固酮拮抗性质，适用于控制或预防心力衰竭，肝腹水，原发性醛固酮增多症和特发性高血压。

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