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1. 发明授权

US5149717A Alkanophenones useful for treating allergies 失效
标题翻译：用于治疗过敏的苯胺酮
公开(公告)号：US5149717A
公开(公告)日：1992-09-22
申请号：US795227
申请日：1991-11-15
申请人： Andreas von Sprecher , Andreas Beck , Bruno Schaub , Robert W. Lang
发明人： Andreas von Sprecher , Andreas Beck , Bruno Schaub , Robert W. Lang
IPC分类号： C07D311/24 , C07D405/04
CPC分类号： C07D405/04 , C07D311/24
摘要： Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.
摘要翻译：其中R 1为未取代或氟化的低级烷基，R 2为氢或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键的通式为（Ⅰ）的取代的烷基苯醌，低级亚烷基，n是1或2，R3是未取代的或被未取代或氟化的低级烷基取代的苯基，被醚化或酯化的羟基，被未取代或低级烷基化的氨基和/或被游离的，酯化的或酰胺化的羧基取代，或者是未取代的低级烷基，被氟和氯取代或被游离的酯化或酰胺化的羧基取代，R4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性质，并且可以使用作为药物中的抗过敏活性成分。

2. 发明授权

US4808572A .alpha.-Hydroxy thioethers 失效
标题翻译： α-羟基硫醚
公开(公告)号：US4808572A
公开(公告)日：1989-02-28
申请号：US936671
申请日：1986-12-01
申请人： Andreas Beck , Werner Breitenstein , Andreas von Sprecher , Robert W. Lang , Konrad Oertle
发明人： Andreas Beck , Werner Breitenstein , Andreas von Sprecher , Robert W. Lang , Konrad Oertle
IPC分类号： A61K31/16 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/23 , A61K38/00 , A61K45/00 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C313/00 , C07C321/18 , C07C323/00 , C07C323/52 , C07C323/58 , C07C323/59 , C07C323/60 , C07K1/113 , C07K5/02 , C07K5/06 , C07C149/243
CPC分类号： C07K5/0606 , A61K31/19 , A61K31/215 , C07C323/00 , A61K38/00
摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.1-7 -alkoxy or an optionally substituted amino group, and--X-- represents a single bond, a methylene group of an optionally N-acylated primary aminomethylene group,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
摘要翻译：式（I）的新型不对称硫醚，其中通式具有以下含义：a为1至7的整数，R 4表示氢或C 1-7 - 烷酰基，R 1表示C 1-3 - 烷基，可以在末端碳原子上被游离或酰化的羟基，原子数至多为17的卤素原子或甲氧基取代，或表示C1-3-全氟烷基，R2表示任选不饱和的脂肪族基，其具有 5至15个碳原子，A代表乙烯，或者，如果R1代表卤代基，和/或B代表亚苯基或亚乙基，则单键或亚乙烯基，B代表单键，亚乙炔基或亚苯基，R3代表羟基，C1-7 - 烷氧基或任选取代的氨基，-X-表示单键，任选N-酰化的伯氨基亚甲基的亚甲基，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除平滑肌的收缩b 由白细胞三烯生成，因此适用于治疗过敏性疾病，特别是哮喘病症。

3. 发明授权

US5145868A Alkanophenones useful for treating allergies 失效
标题翻译：用于治疗过敏的苯胺酮
公开(公告)号：US5145868A
公开(公告)日：1992-09-08
申请号：US794608
申请日：1991-11-15
申请人： Andreas von Sprecher , Andreas Beck
发明人： Andreas von Sprecher , Andreas Beck
IPC分类号： C07D333/16 , A61K8/00 , A61K8/49 , A61K31/38 , A61K31/381 , A61K31/40 , A61P7/02 , A61P11/00 , A61P17/00 , A61P37/08 , A61Q17/04 , C07D311/24 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14
CPC分类号： C07D405/04 , C07D311/24 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14
摘要： Substituted alkanophenones of the general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is a 5-membered heteroaryl radical that contains 1N, O or S atom as hetero atom and is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterfied or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties can e used as antiallergic active ingredients in medicaments.
摘要翻译：其中R 1为未取代或氟化的低级烷基，R 2为氢，或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键合的取代的烷基苯甲酮键，alk是低级亚烷基，n是1或2，R3是含有1N，O或S原子作为杂原子的5元杂芳基，未被取代或被未取代或氟化的低级烷基取代，通过醚化或酯化的羟基通过未取代或低级烷基化的氨基和/或游离的酯化或酰胺化的羧基，R 4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性能可以用作抗过敏活性药物成分。

4. 发明授权

US5508408A Quinoline compound 失效
标题翻译：喹啉化合物
公开(公告)号：US5508408A
公开(公告)日：1996-04-16
申请号：US288537
申请日：1994-08-10
申请人： Andreas von Sprecher , Andreas Beck , Marc Gerspacher
发明人： Andreas von Sprecher , Andreas Beck , Marc Gerspacher
IPC分类号： C07D215/12 , A61K31/47 , A61K31/473 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/14 , C07D215/16 , C07D215/18 , C07D215/20 , C07D221/06 , C07D221/16 , C07D215/06 , C07D221/08
CPC分类号： C07D215/14 , C07D215/18 , C07D215/20 , C07D221/16
摘要： Compounds of formula I ##STR1## wherein R.sub.1 -R.sub.5, X, Ar and Y are as defined in the description, have valuable pharmaceutical properties and are especially effective as leukotriene antagonists. They are prepared in a manner known per se.
摘要翻译：式I的化合物其中R1-R5，X，Ar和Y如说明书中所定义，其具有有价值的药物性质，并且作为白三烯拮抗剂是特别有效的。它们是以本身已知的方式准备的。

5. 发明授权

US4649215A Aliphatic thioethers 失效
标题翻译：脂族硫醚
公开(公告)号：US4649215A
公开(公告)日：1987-03-10
申请号：US748656
申请日：1985-06-25
申请人： Andreas von Sprecher , Ivan Ernest , Alan J. Main , Andreas Beck
发明人： Andreas von Sprecher , Ivan Ernest , Alan J. Main , Andreas Beck
IPC分类号： A61K38/00 , C07D309/12 , C07K5/06 , C07C149/20 , C07C147/02
CPC分类号： C07K5/06191 , C07C323/00 , C07D309/12 , C07K5/0606 , A61K38/00
摘要： Novel asymmetric thioethers of the formula ##STR1## in which R.sup.1 represents a C.sub.1-3 -alkyl radical or a C.sub.1-3 -hydroxyalkyl radical of which the hydroxy group may be in esterified form,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,R.sup.3 represents hydroxy, alkoxy or an optionally substituted amino group, and-X- represents a single bond, a methylene group or an optionally N-acylated primary aminomethylene groupwherein the O-atom of the hydroxy group is in the transconfiguration relative to the S-atom, are effective as leucotriene-antagonists since they eliminate the contractions of smooth muscles caused by leucotrienes and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
摘要翻译：式（I）的新型不对称硫醚，其中R 1表示C 1-3 - 烷基或羟基可以被酯化形成的C 1-3 - 羟基烷基，R 2表示具有 5至15个碳原子，R 3表示羟基，烷氧基或任选取代的氨基，-X-表示单键，亚甲基或任选N-酰化的伯氨基亚甲基，其中羟基的O-原子是在相对于S原子的反式构型中，作为白三烯拮抗剂是有效的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于治疗变态反应，特别是哮喘病症。

6. 发明授权

US06319917B1 Acylaminoalkenylene-amide derivatives as NK1 and NK2 antagonists 失效
标题翻译：作为NK1和NK2拮抗剂的酰氨基亚烯基酰胺衍生物
公开(公告)号：US06319917B1
公开(公告)日：2001-11-20
申请号：US09655170
申请日：2000-09-05
申请人： Marc Gerspacher , Andreas von Sprecher , Robert Mah , Silvio Roggo , Stefan Stutz
发明人： Marc Gerspacher , Andreas von Sprecher , Robert Mah , Silvio Roggo , Stefan Stutz
IPC分类号： A61K3155
CPC分类号： C07D403/12 , C07C237/22 , C07D209/20 , C07D209/24 , C07D223/12
摘要： Compounds of formula I wherein R1, R1-R3, R4′, R4″ and R5 are as defined in the description, have valuable pharmaceutical properties and are effective especially as NK1 and NK2 antagonists. They are prepared in a manner known per se.
摘要翻译：在R1，R1-R3，R4'，R4“和R5中的式I化合物如说明书中所定义，具有有价值的药物性质，特别是作为NK1和NK2拮抗剂是有效的。它们是以本身已知的方式准备的。

7. 发明授权

US4523030A Benzophenones 失效
标题翻译：二苯甲酮
公开(公告)号：US4523030A
公开(公告)日：1985-06-11
申请号：US618152
申请日：1984-06-07
申请人： Georges Haas , Andreas von Sprecher , Pier G. Ferrini
发明人： Georges Haas , Andreas von Sprecher , Pier G. Ferrini
IPC分类号： C07C69/035 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61P29/00 , C07C33/34 , C07C45/67 , C07C51/00 , C07C59/90 , C07C62/38 , C07C65/40 , C07C67/00 , C07C69/753 , C07C69/757 , C07C69/76 , C07C69/94 , C07C201/00 , C07C205/55 , C07C231/00 , C07C231/12 , C07C231/14 , C07C233/00 , C07C235/82 , C07C253/00 , C07C255/40 , C07C255/57 , C07C313/00 , C07C323/62 , C07C65/32
CPC分类号： C07C255/00 , C07C323/00 , C07C33/34 , C07C45/673 , C07C62/38 , Y02P20/55
摘要： Substituted benzophenones of the formula ##STR1## in which Ph represents unsubstituted or substituted phenyl and R represents free, esterified or amidated carboxy, have anti-inflammatory and/or analgesic properties and can be used as active ingredients in medicaments. They are manufactured, for example, as follows:a compound or a mixture of compounds of the formula ##STR2## in which X.sub.1 and X.sub.2 together represent a group of the formula --C(.dbd.O)--O that is bonded via the carbonyl group to the radical Ph and X.sub.3 represents hydrogen, or one of the radicals X.sub.1 and X.sub.3 represents a group of the formula --C(.dbd.O)--Z, the other represents hydrogen and X.sub.2 represents a group R'O-- in which R' represents hydrogen or a hydroxy-protecting group, is subjected to acid treatment and the primary product is decomposed solvolytically.
摘要翻译： Ph取代的二苯甲酮，其中Ph代表未取代或取代的苯基，R代表游离的，酯化的或酰胺化的羧基，具有抗炎和/或止痛特性，可用作药物中的活性成分。它们例如如下制备：式（II）的化合物或化合物的混合物，其中X 1和X 2一起表示式-C（= O）-O的基团，其通过对于基团Ph和X 3的羰基表示氢，或者基团X 1和X 3中的一个表示式-C（= O）-Z的基团，另一个表示氢，X 2表示基团R 10 - ，其中 R'表示氢或羟基保护基，进行酸处理，初级产物在溶剂中分解。

8. 发明授权

US5177257A Benzocycloalkenecarboxylic acid and process for its preparation 失效
标题翻译：苯并二恶唑酸及其制备方法
公开(公告)号：US5177257A
公开(公告)日：1993-01-05
申请号：US776385
申请日：1991-11-20
申请人： Andreas von Sprecher , Hansjurg Wetter
发明人： Andreas von Sprecher , Hansjurg Wetter
IPC分类号： A61K31/19 , A61P29/00 , A61P43/00 , C07B57/00 , C07C51/487 , C07C62/38
CPC分类号： C07C62/38 , C07C51/487
摘要： The novel (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic i.e. the compound of the formula ##STR1## in free form or in salt form, can be used as active ingredient in pharmaceutical preparations and can be prepared by a novel process, which is characterized in that racemic 4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is reacted at elevated temperature with at least the equimolar amount of quinine in an alcoholic solvent for from approximately 6 to approximately 48 hours, the quinine salt of the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid, precipitated in crystalline form as the direct reaction product, is separated from the reaction mixture, and the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is set free from this salt by acid treatment in a customary manner, and, if desired, this free acid is converted into a salt.
摘要翻译： PCT No.PCT / CH91 / 00064 Sec。 371日期1991年11月20日 102（e）1991年11月20日日期PCT 1991年3月19日PCT公布。 WO91 / 14671 PCT出版物日期为1991年10月3日。新型（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸，即游离形式或盐形式的式（I）化合物，可以用作药物制剂中的活性成分，并且可以通过一种新的方法制备，其特征在于外消旋的4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸在升高的温度下至少与在酒精溶剂中等摩尔量的奎宁约6至约48小时，（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸的奎宁盐以晶体形式沉淀作为直接反应产物，与反应混合物分离，并以常规方式通过酸处理使（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸不含该盐，如果需要，将该游离酸转化成盐。

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