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1. 发明授权

US08791162B2 Cathepsin cysteine protease inhibitors 有权
标题翻译：组织蛋白酶半胱氨酸蛋白酶抑制剂
公开(公告)号：US08791162B2
公开(公告)日：2014-07-29
申请号：US13984877
申请日：2012-02-09
申请人： Kelem Kassahun , Christine Fandozzi , Donald R. Gauthier, Jr. , Lisa A. Shipley
发明人： Kelem Kassahun , Christine Fandozzi , Donald R. Gauthier, Jr. , Lisa A. Shipley
IPC分类号： A61K31/277 , C07C255/46
CPC分类号： C07C255/46 , A61K31/277 , A61K45/06 , C07B59/001 , C07C317/32 , C07C317/50 , C07C2601/02
摘要： This invention relates to deuterated compounds which are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译：本发明涉及祛痰化合物，其可用于治疗其中指示骨吸收抑制的疾病，例如骨质疏松症。

2. 发明授权

US07923459B2 Process for the synthesis of 4-(3-methanesulfonylphenyl)-1-N-propyl-piperidine 有权
标题翻译：合成4-（3-甲磺酰基苯基）-1-丙基 - 哌啶的方法
公开(公告)号：US07923459B2
公开(公告)日：2011-04-12
申请号：US11733512
申请日：2007-04-10
申请人： Donald R. Gauthier , Richard Desmond , Paul N. Devine
发明人： Donald R. Gauthier , Richard Desmond , Paul N. Devine
IPC分类号： A61K31/445
CPC分类号： C07D211/24
摘要： The present invention is directed to processes for the preparation of 4-(3-methanesulfonyl-phenyl)-1-N-propylpiperidine (I) or a pharmaceutically acceptable salt thereof, which comprises: oxidizing a sulfide of the formula (II): with a catalytic oxidizing agent and an oxidant; to give a compound of the formula (III): followed by catalytic reduction of the compound of formula (III).
摘要翻译：本发明涉及制备4-（3-甲磺酰基 - 苯基）-1-N-丙基哌啶（I）或其药学上可接受的盐的方法，其包括：将式（II）的硫化物氧化：用催化氧化剂和氧化剂; 得到式（III）化合物：然后催化还原式（III）化合物。

3. 发明申请

US20150329521A1 PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS 有权
标题翻译：制备逆转录酶抑制剂的方法
公开(公告)号：US20150329521A1
公开(公告)日：2015-11-19
申请号：US14649837
申请日：2013-12-04
申请人： Tetsuji ITOH , Ingyu JEON , Ian MANGION , Gang QIAN , Benjamin D. SHERRY , Donald R. GAUTHIER , Yang CAO , MERCK SHARP & DOHME CORP.
发明人： Tetsuji Itoh , Ingyu Jeon , Ian Mangion , Gang QIAN , Benjamin D. Sherry , Donald R. Gauthier , Yang CAO
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans.
摘要翻译：本发明涉及一种合成3-（取代的苯氧基）-1 - [（5-氧代-4,5-二氢-1H-1,2,4-三唑-3-基）甲基]] - 吡啶-2（1H） - 酮衍生物。通过本发明的方法合成的化合物是可用于抑制逆转录酶，HIV复制和人类免疫缺陷病毒感染治疗的HIV逆转录酶抑制剂。

4. 发明授权

US4230618A Azo dyestuffs containing an amino or acylated amino naphthol di-sulfonic acid radical and at least one reactive phosphoric or phosphonic acid group 失效
标题翻译：含有氨基或酰化氨基萘酚二磺酸基团的偶氮染料和至少一种反应性磷酸或膦酸基团
公开(公告)号：US4230618A
公开(公告)日：1980-10-28
申请号：US837625
申请日：1977-09-27
申请人： Donald R. Gauthier
发明人： Donald R. Gauthier
IPC分类号： C09B69/00 , D06P1/384 , C09B62/82 , D06P3/66
CPC分类号： C09B69/007 , D06P1/384
摘要： Azo dyestuffs of the formula: ##STR1## wherein A is a phenylene or naphthalene nucleus containing at least one phosphoric or phosphonic acid group; R.sub.1 and R.sub.2 are hydrogen or --SO.sub.3 H; and R.sub.3 -R.sub.6 are hydrogen, --SO.sub.3 H, or NR.sub.7 Q wherein R.sub.7 is hydrogen or lower alkyl and Q is hydrogen or an acyl group of 2 to 8 carbon atoms, at least two of R.sub.1 -R.sub.6 being --SO.sub.3 H and at least one being --NHQ, provided that when the dyestuff is monoazo, then Q is an acyl group of 3 to 8 carbons and when the dyestuff is disazo, Q is hydrogen or an acyl group of 2 to 8 carbon atoms. The dyestuff may be used to reactively dye cellulosic materials, e.g., cotton or cotton/polyester blends. The dyestuffs are particularly useful in dyeing mixed fabrics of cellulose and synthetics together with disperse dyes from a single bath.
摘要翻译：下式的偶氮染料：其中A是含有至少一个磷酸或膦酸基团的亚苯基或萘核; R1和R2是氢或-SO3H; 和R 3 -R 6是氢，-SO 3 H或NR 7 Q，其中R 7是氢或低级烷基，Q是氢或2至8个碳原子的酰基，R 1 -R 6中的至少两个是-SO 3 H，至少一个是 - NHQ，条件是当染料为单偶氮时，Q为3至8个碳的酰基，当染料为双偶氮时，Q为氢或2至8个碳原子的酰基。染料可用于反应性地染色纤维素材料，例如棉或棉/聚酯混合物。该染料特别适用于将纤维素和合成纤维的混合织物与来自单一浴液的分散染料一起染色。

5. 发明授权

US4225491A Azo pyridone dyestuffs containing at least one reactive phosphoric or phosphonic acid group 失效
标题翻译：含有至少一个反应性磷酸或膦酸基的偶氮吡啶酮染料
公开(公告)号：US4225491A
公开(公告)日：1980-09-30
申请号：US832374
申请日：1977-09-12
申请人： Donald R. Gauthier
发明人： Donald R. Gauthier
IPC分类号： C09B29/42 , C09B69/00 , D06P1/384 , C09B29/36 , C09B62/82 , D06P3/66
CPC分类号： D06P1/384 , C09B29/363 , C09B69/007
摘要： Azo pyridone dyestuffs containing at least one reactive phosphoric or phosphonic acid group. The dyestuffs are characterized by the formula:A -- N .dbd. N -- Rwherein A is an aromatic radical containing at least one phosphoric or phosphonic acid group and R is a monovalent radical derived from a pyridone coupling component by removing a hydrogen atom attached to a ring carbon atom of the pyridone ring. The aromatic radical A is preferably a phenyl or naphthyl group. In addition to its phosphonic or phosphoric acid group or groups, radical A may be substituted with one or more halogen, alkyl, alkoxy, nitro, sulfonic acid or carboxylic acid groups. Cellulosic textiles, e.g., cotton or cotton/polyester blends, may be reactively dyed with these dyestuffs in an acid, neutral or alkaline bath using dicyandiamide or the equivalent. The phosphoric or phosphonic acid groups and the cellulosic material react to fix the dye through an ester linkage.Examples of suitable dyestuffs include those having the formula: ##STR1## and ##STR2##
摘要翻译：含有至少一个反应性磷酸或膦酸基的偶氮吡啶酮染料。染料的特征在于下式：A-N = N-R其中A是含有至少一个磷酸或膦酸基团的芳族基团，R是衍生自吡啶酮偶联组分的一价基团，通过除去附着于吡啶酮环的环碳原子。芳基A优选为苯基或萘基。除了其膦酸基或磷酸基团之外，基团A可以被一个或多个卤素，烷基，烷氧基，硝基，磺酸或羧酸基团取代。纤维素纺织品，例如棉或棉/聚酯共混物，可以在酸，中性或碱性浴中用这些染料用双氰胺或其等同物反应染色。磷酸或膦酸基团和纤维素材料通过酯键反应固定染料。合适的染料的实例包括具有下式的那些：和

6. 发明申请

US20130324610A1 CATHEPSIN CYSTEINE PROTEASE INHIBITORS 有权
公开(公告)号：US20130324610A1
公开(公告)日：2013-12-05
申请号：US13984877
申请日：2012-02-09
申请人： Kelem Kassahun , Christne Fandozzi , Donald R. Gauthier , Lisa A. Shipley
发明人： Kelem Kassahun , Christne Fandozzi , Donald R. Gauthier , Lisa A. Shipley
IPC分类号： C07C317/50 , A61K45/06 , A61K31/277
CPC分类号： C07C255/46 , A61K31/277 , A61K45/06 , C07B59/001 , C07C317/32 , C07C317/50 , C07C2601/02
摘要： This invention relates to deuterated compounds which are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译：本发明涉及祛痰化合物，其可用于治疗其中指示骨吸收抑制的疾病，例如骨质疏松症。

7. 发明授权

US4472168A Aqueous lithium salt solutions of fiber reactive dyestuff stabilized with arylamino sulfonic acid/salt mixtures 失效
标题翻译：用芳基氨基磺酸/盐混合物稳定的纤维活性染料的锂盐水溶液
公开(公告)号：US4472168A
公开(公告)日：1984-09-18
申请号：US510829
申请日：1983-07-05
申请人： Donald R. Gauthier
发明人： Donald R. Gauthier
IPC分类号： C09B67/26
CPC分类号： C09B67/0073
摘要： Lithium salts of fiber reactive dyestuffs are stabilized in aqueous solution with N,N dialkylamine benzene sulfonic acid salt/acid buffers.
摘要翻译：纤维活性染料的锂盐在N，N二烷基胺苯磺酸盐/酸缓冲液的水溶液中稳定。

8. 发明授权

US11634511B2 Processes for the preparation of sugammadex 有权
公开(公告)号：US11634511B2
公开(公告)日：2023-04-25
申请号：US17059925
申请日：2019-06-03
申请人： Merck Sharp & Dohme Corp. , Jamie M. McCabe Dunn , Nadine Kuhl , Wenyong Chen , Yang Cao , Donald R. Gauthier, Jr. , Alan Michael Hyde , Susan L. Zultanski
发明人： Jamie M. McCabe Dunn , Nadine Kuhl , Wenyong Chen , Yang Cao , Donald R. Gauthier, Jr. , Alan Michael Hyde , Susan L. Zultanski
IPC分类号： C08B37/16
摘要： The present invention provides processes for the preparation of sugammadex: (I) In one aspect, there is provided a process for the preparation of sugammadex from 8-per-deoxy-8-bromo-γ-cyclodextrin and 3-mercaptopropionic acid. In another aspect, there is provided an alternative process for the preparation of sugammadex from 8-per-deoxy-8-bromo-γ-cyclodextrin and disodium 3 -mercaptopropionate. In another aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-γ-cyclod extrin, which may be used in the production of sugammadex. In one such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-y-cyclodextrin from γ-cyclodextrin and a brominating agent. In another such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-γ-cyclodextrin comprising, inter alia, reacting γ-cyclodextrin with an electrophilic brominating agent, a deoxygenating agent, and an acid in the presence of an organic solvent.

9. 发明授权

US4472308A Azo dyestuffs containing an amino or acylated amino naphthol monosulfonic acid radical and at least one reactive phosphoric or phosphonic acid group 失效
标题翻译：含有氨基或酰化氨基萘酚单磺酸基团和至少一种反应性磷酸或膦酸基团的偶氮染料
公开(公告)号：US4472308A
公开(公告)日：1984-09-18
申请号：US160427
申请日：1980-06-17
申请人： Donald R. Gauthier
发明人： Donald R. Gauthier
IPC分类号： C09B69/00 , D06P1/384 , C09B62/82 , C09B62/825 , C09B62/83 , D06P3/66
CPC分类号： C09B69/007 , D06P1/384
摘要： Azo dyestuffs of the formulae: ##STR1## which are useful for reactively dyeing such cellulosic materials as cotton or cotton/polyester blends.
摘要翻译：具有下式的偶氮染料：，其可用于反应性染色诸如棉或棉/聚酯混合物的纤维素材料。

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