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1. 发明授权

US07767705B2 Compounds that inhibit TRPV1 and uses thereof 有权
标题翻译：抑制TRPV1的化合物及其用途
公开(公告)号：US07767705B2
公开(公告)日：2010-08-03
申请号：US11844712
申请日：2007-08-24
申请人： Chih-hung Lee , Richard J Perner , Brian S. Brown , John Darbyshire
发明人： Chih-hung Lee , Richard J Perner , Brian S. Brown , John Darbyshire
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： A61K31/416 , C07D231/56
摘要： Compounds of formula (I) wherein R3, R7, R9 and L are defined in the description are TRPV1 antagonists that exhibit low inhibitory activity against CYP3A4. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
摘要翻译：在描述中定义R3，R7，R9和L的式（I）化合物是对CYP3A4表现出低抑制活性的TRPV1拮抗剂。还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

2. 发明申请

US20100249203A1 COMPOUNDS THAT INHIBIT TRPV1 AND USES THEREOF 有权
标题翻译：禁止TRPV1的化合物及其用途
公开(公告)号：US20100249203A1
公开(公告)日：2010-09-30
申请号：US12815259
申请日：2010-06-14
申请人： Chih-hung Lee , Richard J. Perner , Brian S. Brown , John Darbyshire
发明人： Chih-hung Lee , Richard J. Perner , Brian S. Brown , John Darbyshire
IPC分类号： A61K31/415 , C07D231/56 , A61P25/00 , A61P19/02 , A61P35/04 , A61P15/00 , A61P1/00 , A61P29/00
CPC分类号： A61K31/416 , C07D231/56
摘要： Compounds of formula (I) wherein R3, R7, R9 and L are defined in the description are TRPV1 antagonists that exhibit low inhibitory activity against CYP3A4. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
摘要翻译：在描述中定义R3，R7，R9和L的式（I）化合物是对CYP3A4表现出低抑制活性的TRPV1拮抗剂。还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

3. 发明申请

US20080058401A1 COMPOUNDS THAT INHIBIT TRPV1 AND USES THEREOF 有权
标题翻译：禁止TRPV1的化合物及其用途
公开(公告)号：US20080058401A1
公开(公告)日：2008-03-06
申请号：US11844712
申请日：2007-08-24
申请人： Chih-hung Lee , Richard Perner , Brian Brown , John Darbyshire
发明人： Chih-hung Lee , Richard Perner , Brian Brown , John Darbyshire
IPC分类号： A61K31/416 , A61P29/00 , C07D231/56
CPC分类号： A61K31/416 , C07D231/56
摘要： Compounds of formula (I) wherein R3, R7, R9 and L are defined in the description are TRPV1 antagonists that exhibit low inhibitory activity against CYP3A4. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
摘要翻译：在描述中定义的其中R 3，R 7，R 9和L的式（I）的化合物是表现出低抑制性的TRPV1拮抗剂对CYP3A4的活性。还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

4. 发明申请

US20080171751A1 Triazole Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor 失效
标题翻译：适用于治疗多巴胺D3受体调节反应的三唑化合物
公开(公告)号：US20080171751A1
公开(公告)日：2008-07-17
申请号：US11792596
申请日：2005-12-01
申请人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
发明人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
IPC分类号： A61K31/496 , C07D403/14 , A61P25/00
CPC分类号： C07D403/12
摘要： The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
摘要翻译：本发明涉及式I化合物：其中n是1或2，Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基，和其中一个氮原子上的基团R 1a， R 1是氢，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，氟化C 1 -C 6烷基，氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基，杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，氟化C 1 -C 6烷基或氟化C 3 -C 6环烷基; 以及这些化合物的生理上耐受的酸加成盐。本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D 3的病症的方法受体拮抗剂或多巴胺D 3激动剂，所述方法包括向有需要的受试者施用有效量的至少一种式III的三唑化合物或生理耐受的酸加成盐。

5. 发明授权

US06953592B2 Water soluble powders and tablets 有权
标题翻译：水溶性粉末和片剂
公开(公告)号：US06953592B2
公开(公告)日：2005-10-11
申请号：US10235671
申请日：2002-09-04
申请人： John Darbyshire , Oliver Chmiel , Johan Bernard Ubbink , Annemarie Schoonman
发明人： John Darbyshire , Oliver Chmiel , Johan Bernard Ubbink , Annemarie Schoonman
IPC分类号： A61K9/36 , A23F5/38 , A23G3/00 , A23G3/02 , A23G3/10 , A23G3/34 , A23G3/36 , A23G3/44 , A23G3/52 , A23K1/00 , A23K1/18 , A23L1/00 , A23L2/395 , A23P1/02 , A61K9/00 , A61K9/20 , C11D3/22 , C11D17/00 , A61K9/14
CPC分类号： A23G3/36 , A23F5/385 , A23G3/0221 , A23G3/10 , A23G3/346 , A23G3/44 , A23G3/52 , A23G2200/00 , A23G2200/10 , A23G2220/02 , A23K40/10 , A23K40/20 , A23K40/25 , A23K50/40 , A23L2/395 , A23L5/55 , A23P10/28 , A23V2002/00 , A61K9/0056 , A61K9/2009 , A61K9/2018 , A61K9/2059 , C11D3/221 , C11D3/222 , C11D17/0073 , A23V2200/226 , A23V2250/5114 , A23V2250/54246 , A23V2250/10 , A23V2250/124 , A23V2200/224
摘要： The invention relates to water soluble or water dispersible powders, tablets, or precursors therefor based on a carbohydrate matrix with improved dissolution properties in water. These components are subjected to treatment with a gas so that gas is entrapped therein, and sufficient closed porosity is provided so that gas entrapped therein promotes dissolution or dispersion upon contact with water. The powders or tablets may be pharmaceuticals or foods that optionally contain an active ingredient therein.
摘要翻译：本发明涉及基于具有改善的在水中的溶解性质的碳水化合物基质的水溶性或水分散性粉末，片剂或其前体。将这些组分用气体进行处理，使得气体被截留在其中，并且提供足够的闭孔，使得截留在其中的气体促进与水接触时的溶解或分散。粉末或片剂可以是任选地含有活性成分的药物或食品。

6. 发明授权

US4579739A Process for the manufacture of a naturally carbonated beverage 失效
标题翻译：用于制造天然碳酸饮料的方法
公开(公告)号：US4579739A
公开(公告)日：1986-04-01
申请号：US561044
申请日：1983-12-13
申请人： John Darbyshire , Jaroslav Dasek , Hugh Hose
发明人： John Darbyshire , Jaroslav Dasek , Hugh Hose
IPC分类号： C12G3/02 , A23L2/00 , A23L2/02 , A23L2/38 , A23L2/84 , C12G3/08 , C12N1/20 , C12G1/00 , A23L2/26 , C12G3/00
CPC分类号： C12G3/08 , A23L2/84 , Y10S435/853 , Y10S435/856 , Y10S435/942 , Y10S435/943
摘要： A must is fermented with a combination of at least one yeast and at least one lactobacillus, the former being selected from the group of Saccharomyces cerevisiae and Kluyveromyces lactis and the latter being selected from the group of Lactobacillus casei and Lactobacillus hilgardii for their symbiotic ability and capability to produce a synergistic organoleptic effect which eliminates all after-taste of yeast. The must is inoculated such that the respective numbers of yeast germs and lactobacilli germs per ml have a ratio of from 1:10 to 1:500.
摘要翻译：必须用至少一种酵母和至少一种乳杆菌的组合发酵，前者选自酿酒酵母和乳酸克鲁维酵母，后者选自干酪乳杆菌和黑麦草乳杆菌的共生能力，能够产生消除酵母的所有后味的协同感官作用。必须接种，使得每毫升的酵母菌和乳杆菌菌的相应数目的比例为1:10至1:500。

7. 发明授权

US08263146B2 Consumable product containing probiotics 有权
标题翻译：含有益生菌的消耗品
公开(公告)号：US08263146B2
公开(公告)日：2012-09-11
申请号：US10468645
申请日：2002-02-12
申请人： Annmarie Bengtsson-Riveros , Johannes De Reu , Robert Dustan Wood , John Darbyshire , Hermann Knauf , Christoph Cavadini
发明人： Annmarie Bengtsson-Riveros , Johannes De Reu , Robert Dustan Wood , John Darbyshire , Hermann Knauf , Christoph Cavadini
IPC分类号： A23L1/00
CPC分类号： A23L7/104 , A23L29/065
摘要： The present invention relates to any kinds of consumable products enriched with probiotics and a method for obtaining them. After production of probiotic biomass, the probiotics are applied to the product. Also metabolites obtained from a fermentation product may be directly applied to a consumable product.
摘要翻译：本发明涉及富含益生菌的任何种类的消费品及其获得方法。生产益生菌后，将益生菌用于产品。还可以将从发酵产物获得的代谢物直接施用于消耗品。

8. 发明授权

US08101754B2 Triazole compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的三唑化合物
公开(公告)号：US08101754B2
公开(公告)日：2012-01-24
申请号：US11792596
申请日：2005-12-01
申请人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
发明人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
IPC分类号： C07D403/14 , C07D403/12 , A61K31/506 , A61P25/18
CPC分类号： C07D403/12
摘要： The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionially substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
摘要翻译：本发明涉及式I化合物：其中n为1或2，Ar为在其余碳原子上携带基团R 1的C结合的1,2,4-三唑基团，其中一个氮气上具有基团R 1a 原子 R 1是氢，C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 4烷氧基甲基，氟化C 1 -C 6烷基，氟化C 3 -C 6环烷基，氟化C 1 -C 4烷氧基甲基或选择性取代的苯基或5或6元杂芳基; R 1a是氢或C 1 -C 4烷基; 和R2是C1-C6烷基，C3-C6环烷基，氟化C1-C6烷基或氟化C3-C6环烷基; 以及这些化合物的生理上耐受的酸加成盐。本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D3受体拮抗剂或多巴胺的病症的方法 D3激动剂，所述方法包括向有需要的受试者施用有效量的至少一种式III的三唑化合物或生理耐受的酸加成盐。

9. 发明申请

US20120095015A1 TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
标题翻译：适用于治疗多巴胺D3受体调节症状的三唑化合物
公开(公告)号：US20120095015A1
公开(公告)日：2012-04-19
申请号：US13333702
申请日：2011-12-21
申请人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
发明人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
IPC分类号： A61K31/506 , A61P25/00 , A61P25/18 , C07D403/14
CPC分类号： C07D403/12
摘要： The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of there compounds. The invention also relates to a pharmaceutically composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.
摘要翻译：本发明涉及式（I）化合物，其中n为1或2，Ar为在其余碳原子上携带基团R1的C结合的1,2,4-三唑基团，氮原子; R 1是氢，C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 4烷氧基甲基，氟化C 1 -C 6烷基，氟化C 3 -C 6环烷基，氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6-元杂芳基; R 1a是氢或C 1 -C 4烷基; 和R2是C1-C6烷基，C3-C6环烷基，氟化C1-C6烷基或氟化C3-C6环烷基; 以及该化合物的生理耐受酸加成盐。本发明还涉及包含至少一种式（I）的三唑化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D3受体拮抗剂的病症的方法或多巴胺D3激动剂，所述方法包括向有需要的受试者施用有效量的至少一种式（I）的三唑化合物或生理上耐受的酸加成盐。

10. 发明授权

US4815958A Apparatus for agglomeration 失效
标题翻译：用于凝聚的装置
公开(公告)号：US4815958A
公开(公告)日：1989-03-28
申请号：US224818
申请日：1988-07-27
申请人： Marcel Buhler , John Darbyshire , Michel Jaccard
发明人： Marcel Buhler , John Darbyshire , Michel Jaccard
IPC分类号： A23C9/16 , A23G1/00 , A23G1/04 , A23G1/30 , A23G3/26 , A23L1/00 , A23L1/164 , A23L1/18 , A23P1/02 , A23P1/08 , B01J2/12 , B29C67/06
CPC分类号： B01J2/12 , A23L7/122 , A23P10/20 , Y10S425/02
摘要： Apparatus particularly for agglomerating particles of different products. A rotatable drum, which has a wall which defines a cylinder and a cylinder void, is mounted on a frame in a horizontal or inclined position. The apparatus includes provision for rotating the cylinder in one direction thereby defining ascending and descending halves of the cylinder. A first part of the cylinder receives particles of a product and has means, such as projecting elements, to rotate the particles for forming a vortex of particles about an axis within the ascending half of the cylinder void such that the axis of the vortex is displaced from and substantially parallel to a central longitudinal axis of the cylinder. The apparatus also includes provision for introducing a product into a second part of the cylinder in the ascending half of the cylinder void, the second part being displaced from the first end of the cylinder and abutting the first part of the cylinder, for distributing secondary product into the vortex of particles within a zone about which the vortex rotates. A spraying device is positioned in the second part of the cylinder void in the descending half of the cylinder for spraying an agglomerating agent onto the particles of the vortex from outside of the vortex.
摘要翻译：特别是用于聚集不同产品的颗粒的装置。具有限定气缸和气缸空隙的壁的可旋转滚筒以水平或倾斜的位置安装在框架上。该装置包括用于在一个方向上旋转气缸的装置，从而限定气缸的上升和下降两半。气缸的第一部分接收产品的颗粒并且具有诸如突出元件的装置以使颗粒旋转以形成围绕汽缸空隙的上升半部内的轴线的颗粒涡旋，使得涡流的轴线被移位从并且基本上平行于圆柱体的中心纵向轴线。该设备还包括用于将产品引入汽缸的上半部分中的第二部分中的第二部分，第二部分从气缸的第一端移动并邻接气缸的第一部分，用于分配二次产品进入涡旋旋转的区域内的颗粒涡流。喷射装置位于气缸的第二部分中，在气缸的下半部分中具有空隙，用于从涡流外部将附聚剂喷射到涡流颗粒上。

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