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1. 发明授权

US07674825B2 Dicarboxylic acid derivatives with pharmaceutical properties 失效
标题翻译：具有药物性质的二羧酸衍生物
公开(公告)号：US07674825B2
公开(公告)日：2010-03-09
申请号：US11823462
申请日：2007-06-27
申请人： Cristina Alonso-Alija , Markus Heil , Dietmar Flubacher , Paul Naab , Johannes-Peter Stasch , Frank Wunder , Klaus Dembowsky , Elisabeth Perzborn , Elke Stahl
发明人： Cristina Alonso-Alija , Markus Heil , Dietmar Flubacher , Paul Naab , Johannes-Peter Stasch , Frank Wunder , Klaus Dembowsky , Elisabeth Perzborn , Elke Stahl
IPC分类号： C07C65/28 , C07C69/76
CPC分类号： C07D213/64 , C07C63/33 , C07C63/72 , C07C65/24 , C07C65/28 , C07C69/76 , C07C69/92 , C07C69/94 , C07C217/22 , C07C229/38 , C07C229/52 , C07C233/25 , C07C235/42 , C07C275/42 , C07C323/56 , C07C323/62 , C07D211/60 , C07D213/65 , C07D231/12 , C07D233/90 , C07D261/08 , C07D263/57 , C07D271/06 , C07D277/24 , C07D295/088 , C07D295/185 , C07D295/21 , C07D307/42 , C07D333/54
摘要： The present invention relates to the use of compounds of the formula (I) and to their salts and stereoisomers, for the preparation of medicaments for the treatment of cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物及其盐和立体异构体用于制备用于治疗心血管疾病的药物的用途。

2. 发明申请

US20060004015A1 Substituted 2-phenyl-3(2h)-pyridazinones 失效
标题翻译：取代的2-苯基-3（2h） - 哒嗪酮
公开(公告)号：US20060004015A1
公开(公告)日：2006-01-05
申请号：US10511225
申请日：2003-04-08
申请人： Rudolf Schohe-Loop , Elmar Burchardt , Christiane Faeste , Claudia Hirth-Dietrich , Jorg Keldenich , Andreas Knorr , Thomas Lampe , Paul Naab , Delf Schmidt
发明人： Rudolf Schohe-Loop , Elmar Burchardt , Christiane Faeste , Claudia Hirth-Dietrich , Jorg Keldenich , Andreas Knorr , Thomas Lampe , Paul Naab , Delf Schmidt
IPC分类号： A61K31/501 , C07D43/02
CPC分类号： C07D231/12 , C07D233/56 , C07D237/22 , C07D249/08 , C07D401/04 , C07D401/12
摘要： The invention relates to substituted 2-phenyl-3(2h)-pyridazinones, to a method for the production thereof, and to their use as medicaments used in the prophylaxis and/or treatment of diseases in humans and/or animals.
摘要翻译：本发明涉及取代的2-苯基-3（2h） - 哒嗪酮，其制备方法及其用作预防和/或治疗人和/或动物疾病的药物。

3. 发明授权

US5132419A Process for the preparation of 7-amino-3-((Z)-1-propen-1yl)-3-cephem-4-carboxylic acid 失效
标题翻译：制备7-氨基-3-（（Z）-1-丙烯-1-基）-3-辛基-4-羧酸的方法
公开(公告)号：US5132419A
公开(公告)日：1992-07-21
申请号：US589304
申请日：1990-09-27
申请人： Joachim Lanz , Paul Naab , Ulrich Rosentreter
发明人： Joachim Lanz , Paul Naab , Ulrich Rosentreter
IPC分类号： C07D205/095 , C07D501/00 , C07D501/04 , C07D501/08 , C07D501/18 , C07D501/22
CPC分类号： C07D205/095 , C07D501/00
摘要： (7-APCA) having the formula (I) ##STR1## which is an important synthesis intermediate in the preparation of cephalosporin-like antibiotics, is prepared by treating a compound of the formula (II) ##STR2## in which R.sub.1 and R.sub.2 represent alkyl, aryl and aralkyl radicals, with a strong protonic acid or with a Lewis acid. Compound (II) is prepared by adding triphenylphosphine and alkali metal iodide to a compound of the formula (VI) ##STR3## then reacting with acetaldehyde in base. Compound (VI) is prepared by treating a compound of the formula (VII) ##STR4## with a base in a polar solvent at -70.degree. C. to 0.degree. C. Compound (VII) is prepared by treating a compound of the formula (VIII) ##STR5## with a chlorinating agent in an organic solvent.
摘要翻译：通过将式（II）化合物（II）化合物制备，其具有式（I）的化合物（I）作为制备头孢菌素样抗生素的重要的合成中间体，其中R 1和R 2表示烷基，芳基和芳烷基，具有强质子酸或路易斯酸。通过将三苯基膦和碱金属碘化物加入到式（VI）化合物（VI）中，然后与乙醛在碱中反应来制备化合物（II）。通过在极性溶剂中在-70℃至0℃下用碱处理式（VII）的化合物（VII）制备化合物（VI）。化合物（VII）通过将化合物（VIII）的化合物（VIII）与有机溶剂中的氯化剂反应。

4. 发明授权

US4782162A Novel intermediates for the synthesis of cephalosporins 失效
标题翻译：用于合成头孢菌素的新型中间体
公开(公告)号：US4782162A
公开(公告)日：1988-11-01
申请号：US872304
申请日：1986-06-09
申请人： Michael Boberg , Paul Naab , Samir Samaan
发明人： Michael Boberg , Paul Naab , Samir Samaan
IPC分类号： C07D277/20 , C07D277/44 , C07D277/46 , C07D501/20
CPC分类号： C07D277/20
摘要： The new compounds of the formula ##STR1## in which Acyl is alkylcarbonyl optionally substituted by halogen or aryl, or arylcarbonyl, which is substituted by lower alkoxy, halogen or nitro,R.sup.1 is an alkyl or alkenyl radical, andR.sup.4 is an optionally substituted branched or straight-chain C.sub.1 -C.sub.6 -alkyl radical or a cycloalkyl radical,are produced by reacting a 2-halogenoacetylacrylic acid ester of the formula ##STR2## with an acylthiourea of the formula ##STR3## The reaction can be conducted in aqueous DMF, substantially pure Z-isomer selectively crystallizing out.
摘要翻译：酰基为任选被卤素或芳基取代的烷基羰基或被低级烷氧基，卤素或硝基取代的芳基羰基的新化合物“IMAGE”，R1为烷基或烯基，R4为任选取代的支链或直链C 1 -C 6 - 烷基或环烷基是通过使下式得到的式I的2-卤代乙酰基丙烯酸酯与下式的酰基硫脲反应制备的。反应可以在DMF水溶液中进行，基本上纯Z-异构体选择性结晶出来。

5. 发明授权

US4438114A .beta.-Lactam antibiotics 失效
标题翻译： β-内酰胺抗生素
公开(公告)号：US4438114A
公开(公告)日：1984-03-20
申请号：US415632
申请日：1982-09-07
申请人： Michael Boberg , Dieter Habich , Karl G. Metzger , Paul Naab
发明人： Michael Boberg , Dieter Habich , Karl G. Metzger , Paul Naab
IPC分类号： A23L29/00 , A23L2/44 , A61K31/535 , A61P31/04 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00 , Y02P20/55
摘要： A .beta.-lactam of the formula ##STR1## or a hydrate thereof, in whichR represents a hydrogen atom or a methoxy group,n is 1 or 2,Z represents a group of the formula ##STR2## wherein R.sup.1 denotes an optionally substituted aryl group or an optionally substituted heterocyclyl group;or, when n is 1,Z can also represent an optionally substituted cycloalkyl group or an optionally substituted pseudoaromatic heterocyclic 5-membered or 6-membered ring,B represents an optionally substituted phenyl or cyclohexadienyl group, or an unsaturated optionally subtituted heterocyclic ring,T denotes an alkyl--CO--O--, pyridinium, aminopyridinium, carbamoylpyridinium or carbamoyloxy group, an --S--phenyl group which can be substituted, or an --S--Het group in which Het represents an optionally substituted heterocyclic 5-membered or 6-membered ring; andE represents a hydrogen atom, a pharmaceutically acceptable ester grouping a salt-forming cation or a protective group, or represents a negative charge when T contains a quaternary nitrogen,which possesses antibacterial activity rendering it useful as an antibiotic and animal feed supplement.
摘要翻译：其中R表示氢原子或甲氧基，其中n表示1或2，Z表示下式的基团：其中R 1，R 2，R 3，表示任选取代的芳基或任选取代的杂环基; 或者当n为1时，Z还可以表示任选取代的环烷基或任选取代的假芳香杂环5元或6元环，B表示任选取代的苯基或环己二烯基，或不饱和任选取代的杂环，T 表示烷基-CO-O-，吡啶鎓，氨基吡啶鎓，氨基甲酰基吡啶鎓或氨基甲酰氧基，可被取代的-S-苯基或其中Het表示任选取代的杂环5元或6-元烷基的-S-Het基团，元环并且E表示氢原子，成盐阳离子或保护基的药学上可接受的酯基，或当T含有季氮时具有负电荷，其具有抗菌活性，使其可用作抗生素和动物饲料添加剂。

6. 发明申请

US20080058314A1 Novel dicarboxylic acid derivatives with pharmaceutical properties 失效
标题翻译：具有药物性质的新型二羧酸衍生物
公开(公告)号：US20080058314A1
公开(公告)日：2008-03-06
申请号：US11823462
申请日：2007-06-27
申请人： Cristina Alonso-Alija , Markus Heil , Dietmar Flubacher , Paul Naab , Johannes-Peter Stasch , Frank Wunder , Klaus Dembowsky , Elisabeth Perzborn , Elke Stahl
发明人： Cristina Alonso-Alija , Markus Heil , Dietmar Flubacher , Paul Naab , Johannes-Peter Stasch , Frank Wunder , Klaus Dembowsky , Elisabeth Perzborn , Elke Stahl
IPC分类号： A61K31/192 , A61K31/4412 , A61K31/495 , A61K31/5375 , A61K31/54 , A61K31/55
CPC分类号： C07D213/64 , C07C63/33 , C07C63/72 , C07C65/24 , C07C65/28 , C07C69/76 , C07C69/92 , C07C69/94 , C07C217/22 , C07C229/38 , C07C229/52 , C07C233/25 , C07C235/42 , C07C275/42 , C07C323/56 , C07C323/62 , C07D211/60 , C07D213/65 , C07D231/12 , C07D233/90 , C07D261/08 , C07D263/57 , C07D271/06 , C07D277/24 , C07D295/088 , C07D295/185 , C07D295/21 , C07D307/42 , C07D333/54
摘要： The present invention relates to the use of compounds of the formula (I) and to their salts and stereoisomers, for the preparation of medicaments for the treatment of cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物及其盐和立体异构体用于制备用于治疗心血管疾病的药物的用途。

7. 发明授权

US07320977B2 Substituted 2-phenyl-3(2h)-pyridazinones 失效
标题翻译：取代的2-苯基-3（2h） - 哒嗪酮
公开(公告)号：US07320977B2
公开(公告)日：2008-01-22
申请号：US10511225
申请日：2003-04-08
申请人： Rudolf Schohe-Loop , Elmar Burchardt , Christiane Faeste , Claudia Hirth-Dietrich , Jörg Keldenich , Andreas Knorr , Thomas Lampe , Paul Naab , Delf Schmidt , Gunter Schmidt
发明人： Rudolf Schohe-Loop , Elmar Burchardt , Christiane Faeste , Claudia Hirth-Dietrich , Jörg Keldenich , Andreas Knorr , Thomas Lampe , Paul Naab , Delf Schmidt , Gunter Schmidt
IPC分类号： C07D403/04 , A61K31/501
CPC分类号： C07D231/12 , C07D233/56 , C07D237/22 , C07D249/08 , C07D401/04 , C07D401/12
摘要： The invention relates to substituted 2-Phenyl-3(2H)-Pyridazinones, to a method for the production thereof, and to their use as medicaments for the prophylaxis and/or treatment of diseases in humans and/or animals.
摘要翻译：本发明涉及取代的2-苯基-3（2H） - 哒嗪酮，其制备方法及其用作预防和/或治疗人和/或动物疾病的药物。

8. 发明授权

US07087644B1 Derivatives of dicarboxylic acid having pharmaceutical properties 失效
标题翻译：具有药物性质的二羧酸的衍生物
公开(公告)号：US07087644B1
公开(公告)日：2006-08-08
申请号：US10088060
申请日：2000-08-31
申请人： Cristina Alonso-Alija , Markus Heil , Dietmar Flubacher , Paul Naab , Josef Pernerstorfer , Johannes-Peter Stasch , Frank Wunder , Klaus Dembowsky , Elisabeth Perzborn , Elke Stahl
发明人： Cristina Alonso-Alija , Markus Heil , Dietmar Flubacher , Paul Naab , Josef Pernerstorfer , Johannes-Peter Stasch , Frank Wunder , Klaus Dembowsky , Elisabeth Perzborn , Elke Stahl
IPC分类号： C07C229/00 , A61K31/20
CPC分类号： C07D239/30 , C07C229/38 , C07C233/25 , C07C235/56 , C07C237/12 , C07C255/54 , C07C275/24 , C07C317/18 , C07C323/19 , C07C2601/14 , C07C2602/10 , C07D239/38 , C07D271/06 , C07D277/24 , C07D285/06 , C07D295/088 , C07D333/16
摘要： The invention relates to compounds of formula (I) as well as the salts and stereoisomers thereof wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, pharmaceutical compositions containing them, and methods for using them for treatment of cardiovascular disorders are also disclosed and claimed.
摘要翻译：本发明涉及式（I）化合物及其盐和立体异构体，其中若干可变基团如说明书和权利要求中所定义。还公开并要求保护制备这些材料的方法，含有它们的药物组合物及其用于治疗心血管疾病的方法。

9. 发明授权

US5639886A One-pot process for the preparation of 3-quinolonecarboxylic acid derivatives 失效
标题翻译：一锅法制备3-喹诺酮羧酸衍生物
公开(公告)号：US5639886A
公开(公告)日：1997-06-17
申请号：US348400
申请日：1994-12-02
申请人： Rudolf Zerbes , Paul Naab , Gerhard Franckowiak , Herbert Diehl
发明人： Rudolf Zerbes , Paul Naab , Gerhard Franckowiak , Herbert Diehl
IPC分类号： C07D215/233 , A61K31/4709 , C07D215/56 , C07D401/04 , C07D471/04 , C07D498/04 , C07D519/00 , C07D215/227 , C07D215/38
CPC分类号： C07D215/56 , C07D471/04
摘要： The present invention relates to a one-pot process for the preparation of 7-heterocyclyl-substituted 3-quinolonecarboxylic acid derivatives. They possess a strong anti-microbial effect. They include active compounds such as, for example, ofloxacin, ciprofloxacin or enrofloxacin.
摘要翻译：本发明涉及一种制备7-杂环基取代的3-喹诺酮羧酸衍生物的一锅法。它们具有很强的抗菌作用。它们包括活性化合物，例如氧氟沙星，环丙沙星或恩氟沙星。

10. 发明授权

US4600778A Process for the preparation of 1,4-dihydropyridinedicarboxylic esters 失效
标题翻译： 1,4-二氢吡啶二羧酸酯的制备方法
公开(公告)号：US4600778A
公开(公告)日：1986-07-15
申请号：US591614
申请日：1984-03-20
申请人： Werner Teller , Wolfgang Koebernick , Arthur Haaf , Paul Naab , Michael Preiss
发明人： Werner Teller , Wolfgang Koebernick , Arthur Haaf , Paul Naab , Michael Preiss
IPC分类号： C07C205/56 , C07D211/90 , C07B53/00
CPC分类号： C07C201/12 , C07D211/90
摘要： In the preparation of a 1,4-dihydropyridine of the formula ##STR1## in which R is a phenyl radical which is optionally substituted once or twice by nitro and/or chlorine,R.sub.1 is a C.sub.1 -C.sub.4 -alkyl radical which is optionally substituted by a C.sub.1 -C.sub.4 -alkoxy group, andR.sub.2 is a C.sub.1 -C.sub.12 -alkyl radical which is optionally substituted by a C.sub.1 -C.sub.4 -alkoxy group, a trifluoromethyl group or the radical (C.sub.6 H.sub.5 CH.sub.2) (CH.sub.3)N,by preparing an ylidene compound of the formula ##STR2## and reacting such ylidene compound with an enamine compound of the formula ##STR3## the improvement which comprises preparing the ylidene compound by reaction of a ketocarboxylic ester of the formula ##STR4## with an aldehyde of the formula RCHO, in a solvent in the presence of a catalytic amount of any acetate salt of an amine, at a temperature from about -10.degree. C. up to 100.degree. C. The products symmetrical or unsymmetrical, are produced in high yield and purity.
摘要翻译：在制备式“IMAGE”的1,4-二氢吡啶的制备中，其中R是任选被硝基和/或氯取代一次或两次的苯基，R 1是任选取代的C 1 -C 4 - 烷基通过C 1 -C 4 - 烷氧基，并且R 2是任选地被C 1 -C 4 - 烷氧基，三氟甲基或基团（C 6 H 5 CH 2）（CH 3）N）取代的C 1 -C 12 - 烷基，并且使该亚基化合物与式“IMAGE”或“IMAGE”的烯胺化合物反应，该改进包括通过下式的酮羧酸酯反应制备亚基化合物：或“IMAGE”与式RCHO的醛在溶剂中，在催化量的任何乙酸盐的存在下，在约-10℃至100℃的温度下进行。产物对称或不对称，以高产率和纯度生产。

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