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1. 发明授权

US06403577B1 Hexamethyleneiminyl tachykinin receptor antagonists 失效
标题翻译：六亚甲基亚胺基速激肽受体拮抗剂
公开(公告)号：US06403577B1
公开(公告)日：2002-06-11
申请号：US08153847
申请日：1993-11-17
申请人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
发明人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
IPC分类号： A61K3155
CPC分类号： C07D401/12 , C07C233/44 , C07C233/78 , C07C271/20 , C07D209/14 , C07D209/16 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14
摘要： This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.
摘要翻译：本发明提供了一系列非肽基化合物，其可用于治疗或预防与超速激肽相关的生理障碍。本发明还提供了治疗这些生理障碍的方法以及使用这些新化合物的药物制剂。

2. 发明授权

US5371275A Methods for preparing ethylidene diacetate 失效
标题翻译：亚乙基二乙酸酯的制备方法
公开(公告)号：US5371275A
公开(公告)日：1994-12-06
申请号：US097370
申请日：1993-07-23
申请人： Dae C. Park , Sung Y. Cho
发明人： Dae C. Park , Sung Y. Cho
IPC分类号： B01J31/04 , B01J29/00 , B01J31/24 , C07C67/29 , C07C67/36 , C07C69/16 , C07C69/34
CPC分类号： C07C67/29 , Y02P20/582
摘要： The present invention relates to a process for preparing a catalyst useful in producing ethylidene diacetate and to a process for producing ethylidene diacetate by a continuous process using the catalyst prepared. In the preparation of ethylidene diacetate from carbon monoxide and hydrogen, the conventional preparation method using a homogeneous catalyst system comprising a transition metal catalyst is hampered by difficulty in separating the catalyst from the reaction product after completion of the reaction. The catalyst of the present invention is separated easily from the reaction product. The heterogeneous catalyst of the present invention is prepared by adding a compound of a group VIII metal, preferably rhodium or palladium, to a carrier, preferably .alpha.-alumina, kieselguhr or silica, together with an accelerator containing phosphorus or nitrogen, preferably triphenylphosphine. Using the improved catalyst of the present invention also resulted in increased yield of product over conventional methods. The ethylidene diacetate produced using the present method is useful as a starting material for the production of vinyl acetate monomer.
摘要翻译：本发明涉及一种制备可用于生产亚乙基二乙酸酯的催化剂的方法和使用所制备的催化剂通过连续方法生产亚乙基双乙酸酯的方法。在从一氧化碳和氢气制备亚乙基二乙酸酯时，使用包含过渡金属催化剂的均相催化剂体系的常规制备方法在反应完成后难以从反应产物中分离催化剂受到阻碍。本发明的催化剂容易与反应产物分离。通过将第Ⅷ族金属，优选铑或钯的化合物与含有磷或氮的促进剂，优选三苯基膦一起加入到载体，优选α-氧化铝，硅藻土或二氧化硅中来制备本发明的非均相催化剂。使用本发明的改进的催化剂还导致产物的产率比常规方法提高。使用本方法制备的亚乙基二乙酸酯可用作制备乙酸乙烯酯单体的原料。

3. 发明授权

US5371274A Methods for producing ethylidene diacetate using catalysts supported on an organic carrier 失效
标题翻译：使用负载在有机载体上的催化剂生产亚乙基二乙酸酯的方法
公开(公告)号：US5371274A
公开(公告)日：1994-12-06
申请号：US94485
申请日：1993-07-19
申请人： Dae C. Park , Sung Y. Cho , Woo S. Chang
发明人： Dae C. Park , Sung Y. Cho , Woo S. Chang
IPC分类号： B01J31/04 , B01J31/06 , B01J31/24 , C07C55/00 , C07C67/29 , C07C67/36 , C07C69/16
CPC分类号： C07C67/29
摘要： The present invention relates to the field of catalyst technology, and more particularly to the preparation of a supported catalyst and a method of producing ethylidene diacetate using that supported catalyst. The catalyst is represented by the formula M.sub.a X. Compound M includes a group VIII transition metal which catalyzes the formation of ethylidene diacetate, preferably a compound of rhodium or palladium. Carrier X is an organic carrier, preferably selected from the divinylbenzene-polystyrene copolymers, most preferably copolymers having about 1-20% crosslinking. The weight percent of metal M contained in the catalyst is represented by the latter a. The supported heterogenized catalyst results from covalent bonding of the transition metal compound to the organic polymer carrier. Ethylidene diacetate was produced by reacting methyl acetate, iodomethane, carbon monoxide and hydrogen in the presence of this supported catalyst and an accelerator at elevated temperature and pressure. According to the present invention, the reaction product, ethylidene diacetate, is easily separated from the catalyst. The produced ethylidene diacetate may be used as a starting material for preparing vinyl acetate monomer.
摘要翻译：本发明涉及催化剂技术领域，更具体地涉及负载型催化剂的制备和使用负载型催化剂生产亚乙基双乙酸酯的方法。催化剂由式MaX表示。化合物M包括催化亚乙基二乙酸酯，优选铑或钯化合物的VIII族过渡金属。载体X是优选选自二乙烯基苯 - 聚苯乙烯共聚物的有机载体，最优选具有约1-20％交联的共聚物。催化剂中所含金属M的重量百分数由后者a表示。负载的异质化催化剂是由过渡金属化合物与有机聚合物载体的共价键合而产生的。通过使乙酸甲酯，碘甲烷，一氧化碳和氢气在该负载型催化剂和促进剂的存在下，在升高的温度和压力下反应制备亚乙基二乙酸酯。根据本发明，反应产物亚乙基二乙酸酯容易与催化剂分离。所生产的亚乙基二乙酸酯可以用作制备乙酸乙烯酯单体的起始原料。

4. 发明授权

US5354886A Catalysts on inorganic carriers for producing ethylidene diacetate 失效
标题翻译：用于生产亚乙基二乙酸酯的无机载体上的催化剂
公开(公告)号：US5354886A
公开(公告)日：1994-10-11
申请号：US97647
申请日：1993-07-26
申请人： Dae C. Park , Sung Y. Cho
发明人： Dae C. Park , Sung Y. Cho
IPC分类号： B01J27/13 , B01J27/10 , B01J31/20 , B01J31/24 , C07C67/28 , C07C67/29 , C07C69/16 , C07C69/34 , B01J31/18
CPC分类号： B01J27/10 , B01J27/13 , B01J31/0244 , B01J31/1616 , B01J31/20 , B01J31/2404 , C07C67/29 , B01J2231/34 , B01J2231/341 , B01J2231/641 , B01J2531/80 , B01J2531/822
摘要： The present invention relates to a catalyst, a process for preparing the catalyst and a process for using the catalyst to produce ethylidene diacetate. The conventional preparation methods of ethylidene diacetate suffer from difficulty in separating the catalyst from the product after completion of the reaction. The catalyst of the present invention is simply separated from the product by mere filtration following the completion of reaction. This is a result of using a heterogenized catalyst which is obtained by supporting a homogeneous catalyst in an inorganic carder. The catalyst of the present invention is of the general formula M.sub.a X where M is a compound of a group VIII transition metal, most preferably RhCl.sub.3 .multidot.xH.sub.2 O, and X is an inorganic carrier, preferably selected from the group consisting of kieselguhr, .gamma.-alumina, silica, TiO.sub.2, MgO, ZnO and activated charcoal. Ethylidene diacetate produced using the present method is useful as an intermediate for producing precision chemical articles or as a starting material for the production of vinyl acetate monomer.
摘要翻译：本发明涉及一种催化剂，一种制备该催化剂的方法和一种使用该催化剂生产亚乙基二乙酸酯的方法。乙酰亚乙基二乙酸酯的常规制备方法难以在反应完成后将催化剂与产物分离。本发明的催化剂在反应完成后仅通过过滤简单地与产物分离。这是使用通过在无机梳理器中负载均相催化剂获得的异质催化剂的结果。本发明的催化剂具有通式MaX，其中M为第VIII族过渡金属化合物，最优选为RhCl 3·xH 2 O，X为无机载体，优选选自由硅藻土，γ-氧化铝，二氧化硅， TiO2，MgO，ZnO和活性炭。使用本方法制备的二乙酸亚乙酯可用作制备精密化学制品的中间体或用作生产乙酸乙烯酯单体的原料。

5. 发明授权

US06869957B1 Non-peptide tachykinin receptor antagonists 失效
标题翻译：非肽速激肽受体拮抗剂
公开(公告)号：US06869957B1
公开(公告)日：2005-03-22
申请号：US10668565
申请日：2003-09-23
申请人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
发明人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
IPC分类号： C07C233/44 , C07C233/78 , C07C271/20 , C07D209/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , A61K31/4045 , C07D209/20
CPC分类号： C07D401/12 , C07C233/44 , C07C233/78 , C07C271/20 , C07D209/16 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14
摘要： This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.
摘要翻译：本发明提供了一系列非肽基化合物，其可用于治疗或预防与超速激肽相关的生理障碍。本发明还提供了治疗这种生理疾病的方法以及采用这些新化合物的药物制剂。

6. 发明授权

US06727255B1 Piperidinyl and piperazinyl tachykinin receptor antagonists 失效
标题翻译：哌啶基和哌嗪基速激肽受体拮抗剂
公开(公告)号：US06727255B1
公开(公告)日：2004-04-27
申请号：US08463951
申请日：1995-06-05
申请人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
发明人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
IPC分类号： A61K31454
CPC分类号： C07D401/12 , C07C233/44 , C07C233/78 , C07C271/20 , C07D209/14 , C07D209/16 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14
摘要： This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.
摘要翻译：本发明提供了一系列非肽基化合物，其可用于治疗或预防与超速激肽相关的生理障碍。本发明还提供了治疗这种生理疾病的方法以及采用这些新化合物的药物制剂。

7. 发明授权

US5684033A Non-peptide tachykinin receptor antagonists 失效
标题翻译：非肽速激肽受体拮抗剂
公开(公告)号：US5684033A
公开(公告)日：1997-11-04
申请号：US463874
申请日：1995-06-05
申请人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
发明人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
IPC分类号： C07D295/12 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4725 , A61K31/475 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P13/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P43/00 , C07C211/10 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/53 , C07C211/58 , C07C211/59 , C07C217/58 , C07C233/36 , C07C233/44 , C07C233/76 , C07C233/78 , C07C271/20 , C07D209/12 , C07D209/14 , C07D209/16 , C07D209/20 , C07D211/58 , C07D223/04 , C07D233/76 , C07D233/78 , C07D295/14 , C07D295/15 , C07D333/58 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12
CPC分类号： C07D401/12 , C07C233/44 , C07C233/78 , C07C271/20 , C07D209/14 , C07D209/16 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14
摘要： This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.
摘要翻译：本发明提供了一系列非肽基化合物，其可用于治疗或预防与超速激肽相关的生理障碍。本发明还提供了治疗这种生理疾病的方法以及采用这些新化合物的药物制剂。

8. 发明授权

US5670499A Non-peptide tachykinin receptor antagonists 失效
公开(公告)号：US5670499A
公开(公告)日：1997-09-23
申请号：US462415
申请日：1995-06-05
申请人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
发明人： Sung Y. Cho , Thomas A. Crowell , Bruce D. Gitter , Philip A. Hipskind , J. Jeffry Howbert , Joseph H. Krushinski, Jr. , Karen L. Lobb , Brian S. Muehl , James A. Nixon
IPC分类号： C07D295/12 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4725 , A61K31/475 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P13/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P43/00 , C07C211/10 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/53 , C07C211/58 , C07C211/59 , C07C217/58 , C07C233/36 , C07C233/44 , C07C233/76 , C07C233/78 , C07C271/20 , C07D209/12 , C07D209/14 , C07D209/16 , C07D209/20 , C07D211/58 , C07D223/04 , C07D233/76 , C07D233/78 , C07D295/14 , C07D295/15 , C07D333/58 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D295/108
CPC分类号： C07D401/12 , C07C233/44 , C07C233/78 , C07C271/20 , C07D209/14 , C07D209/16 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14
摘要： This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

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