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1. 发明授权

US5763631A Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof 失效
标题翻译：不可逆的HIV蛋白酶抑制剂，中间体，组合物及其制备方法
公开(公告)号：US5763631A
公开(公告)日：1998-06-09
申请号：US667133
申请日：1996-06-20
申请人： Sung Chun Kim , Nakyen Choy , Chang Sun Lee , Ho I. Choi , Jong Sung Koh , Heungsik Yoon , Chi Hyo Park , Sang Soo Kim , Young Chan Son
发明人： Sung Chun Kim , Nakyen Choy , Chang Sun Lee , Ho I. Choi , Jong Sung Koh , Heungsik Yoon , Chi Hyo Park , Sang Soo Kim , Young Chan Son
IPC分类号： A61K31/335 , A61K31/00 , A61K31/336 , A61K38/00 , A61P31/00 , A61P31/12 , A61P31/18 , C07C213/02 , C07C217/08 , C07C269/04 , C07C271/20 , C07C271/22 , C07D301/02 , C07D303/36 , C07D303/38 , C07D303/40 , C07D303/46 , C07D405/12 , C07D405/14 , C07D493/08 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K7/02 , C07D303/08 , C07D215/38 , C07D235/04 , C07D413/00
CPC分类号： C07D303/38 , C07C217/08 , C07C271/20 , C07C271/22 , C07D303/36 , C07D303/46 , C07D405/12 , C07D405/14 , C07D493/08 , C07K5/0207 , C07K5/06026 , C07K5/06078 , C07K5/06139 , C07K7/02 , A61K38/00 , C07C2101/14
摘要： Cis-epoxide compounds of formula (I-3) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or arly-substituted lower alkyl group; K and J are independently a group having the formula of ##STR2## wherein R.sup.18 is a lower alkyl group optionally substituted with an aryl radical; X is O, NH, or N--CH.sub.3 ; and R.sup.19 is an aromatic hetercyclic sysstem containing a nitrogen atom in its ring, or a lower alkyl group optionally substituted with an aryl radical, or a hydrogen; G is an amino acid which is linked to K-- and ##STR3## by peptide bonds in formula (I-3); Q is an amino acid which is linked to by peptide bonds in formula (I-3), or a group having the formula of wherein R.sup.20 is a lower alkyl group optionally substituted with an aromatic radical; and Y is CH.sub.2, O or NH; and r is 0 or 1, except that Q is a group having the formula of r is 0.
摘要翻译：式（I-3）的顺式环氧化合物及其药学上可接受的盐，水合物和溶剂化物：其中：R1是环烷基或芳取代的低级烷基; K和J独立地是具有下式的基团：其中R18是任选被芳基取代的低级烷基; X是O，NH或N-CH 3; R19是在其环中含有氮原子的芳族杂环体系，或任选被芳基取代的低级烷基或氢; G是通过式（I-3）中的肽键与K-和连接的氨基酸; Q是通过式（I-3）中的肽键连接的氨基酸或具有下式的基团：其中R 20是任选被芳族基团取代的低级烷基; 并且Y是CH 2，O或NH; 并且r为0或1，除了Q是具有式r的基团为0。

2. 发明授权

US5744621A Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof 失效
标题翻译：不可逆的HIV蛋白酶抑制剂，中间体，组合物及其制备方法
公开(公告)号：US5744621A
公开(公告)日：1998-04-28
申请号：US667888
申请日：1996-06-20
申请人： Sung Chun Kim , Nakyen Choy , Chang Sun Lee , Young Chan Son , Ho Il Choi , Jong Sung Koh , Heungsik Yoon , Chi Hyo Park , Sang Soo Kim
发明人： Sung Chun Kim , Nakyen Choy , Chang Sun Lee , Young Chan Son , Ho Il Choi , Jong Sung Koh , Heungsik Yoon , Chi Hyo Park , Sang Soo Kim
IPC分类号： A61K31/335 , A61K31/00 , A61K31/336 , A61K38/00 , A61P31/00 , A61P31/12 , A61P31/18 , C07C213/02 , C07C217/08 , C07C269/04 , C07C271/20 , C07C271/22 , C07D301/02 , C07D303/36 , C07D303/38 , C07D303/40 , C07D303/46 , C07D405/12 , C07D405/14 , C07D493/08 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K7/02 , C07D303/08 , C07D215/38 , C07D265/30
CPC分类号： C07D303/38 , C07C217/08 , C07C271/20 , C07C271/22 , C07D303/36 , C07D303/46 , C07D405/12 , C07D405/14 , C07D493/08 , C07K5/0207 , C07K5/06026 , C07K5/06078 , C07K5/06139 , C07K7/02 , A61K38/00 , C07C2101/14
摘要： Cis-epoxide compounds of formula (I-1) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or aryl-substituted lower alkyl group; A is a functionalized acyl group of the formula ##STR2## wherein R.sup.2 is a C.sub.1-4 alkyl, or amide-substituted C.sub.1-2 alkyl group; R.sup.3 is a C.sub.1-4 alkoxy, aryloxyalkyl or arylalkoxy, or a nitrogen-containing aromatic radical, or a lower alkoxy group substituted with a nitrogen-containing aromatic radical, or a radical having the formula of ##STR3## wherein R.sup.4 is a hydrogen or a methyl group and R.sup.5 is an alkyl group substituted with a nitrogen-containing aromatic radical; and m is 0 or 1; and B is a functionalized amino group of the formula ##STR4## wherein R.sup.8 and R.sup.9 are independently a C.sub.1-4 alkyl group optionally substituted with an aromatic radical, or an aromatic group.
摘要翻译：式（I-1）的顺式环氧化合物及其药学上可接受的盐，水合物和溶剂合物：其中：R1是环烷基或芳基取代的低级烷基; A是下式的官能化酰基：其中R 2是C 1-4烷基或酰胺取代的C 1-2烷基; R 3是C 1-4烷氧基，芳氧基烷基或芳基烷氧基或含氮芳族基团，或被含氮芳族基团取代的低级烷氧基或具有下式的基团：其中R 4是氢或甲基，R 5为被含氮芳族基团取代的烷基; m为0或1; 并且B是式“IMAGE”的官能化氨基，其中R 8和R 9独立地是任选被芳族基团或芳族基团取代的C 1-4烷基。

3. 发明授权

US5696134A Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof 失效
标题翻译：不可逆的HIV蛋白酶抑制剂，中间体，组合物及其制备方法
公开(公告)号：US5696134A
公开(公告)日：1997-12-09
申请号：US473877
申请日：1995-06-07
申请人： Heungsik Yoon , Nakyen Choy , Sung Chun Kim , Ho Il Choi , Young Chan Son , Chi Hyo Park , Kwang-Yul Moon , Wonhee Jung , Chung Ryeol Kim , Chang Sun Lee , Jong Sung Koh , Sang Soo Kim
发明人： Heungsik Yoon , Nakyen Choy , Sung Chun Kim , Ho Il Choi , Young Chan Son , Chi Hyo Park , Kwang-Yul Moon , Wonhee Jung , Chung Ryeol Kim , Chang Sun Lee , Jong Sung Koh , Sang Soo Kim
IPC分类号： A61K38/00 , C07K5/02 , A61K31/44 , A61K31/47
CPC分类号： C07K5/0207 , A61K38/00
摘要： Novel cis-epoxide compounds of formula (I) are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein A, B, R.sub.1 to R.sub.4 and n have the same meanings as defined in the specification. The novel HIV protease inhibitor of the formula (I) has a specific structure to form a stable bonding with the enzyme active site, which entails a highly enhanced irreversible inhibition against HIV protease.
摘要翻译：式（I）的新型顺式环氧化合物可用于治疗或预防由HIV感染引起的疾病：其中A，B，R 1至R 4和n具有与说明书中所定义相同的含义。式（I）的新型HIV蛋白酶抑制剂具有与酶活性位点形成稳定结合的特定结构，这对HIV蛋白酶具有高度的不可逆抑制作用。

4. 发明授权

US5670517A Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof 失效
标题翻译：不可逆的HIV蛋白酶抑制剂，含有它们的组合物及其制备方法
公开(公告)号：US5670517A
公开(公告)日：1997-09-23
申请号：US659791
申请日：1996-06-06
申请人： Nakyen Choy , Hoil Choi , Chi-Hyo Park , Young-Chan Son , Chang-Sun Lee , Heungsik Yoon , Sung-Chun Kim , Jong-Sung Koh , Chung-Ryeol Kim
发明人： Nakyen Choy , Hoil Choi , Chi-Hyo Park , Young-Chan Son , Chang-Sun Lee , Heungsik Yoon , Sung-Chun Kim , Jong-Sung Koh , Chung-Ryeol Kim
IPC分类号： A61K38/00 , C07D303/36 , C07D405/12 , C07K5/02 , A61K31/47 , A61K31/335 , C07D215/14 , C07D217/15
CPC分类号： C07D405/12 , C07D303/36 , C07K5/021 , A61K38/00
摘要： The present invention relates to novel compounds of formula (I) which has inhibitory activities against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group; R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group; R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group; R.sup.4 is hydrogen or a C.sub.1-2 alkyl group; R.sup.5 is a C.sub.1-10 alkyl group optionally substituted with an aromatic group; and n is 1 or 2.
摘要翻译：本发明涉及对人体免疫缺陷病毒（“HIV”）蛋白酶具有抑制活性的新型式（I）化合物，其制备方法，以及用于通过HIV感染预防或治疗AIDS的组合物，其包含上述化合物作为有效成分。（I）其中：R1是芳基，含氮芳香基，任选被芳基或含氮芳基取代的C1-4烷基，任选被芳族取代的C 1-4烷氧基基团或含氮芳族基团; R2是被C1-4烷基磺酰基取代的氨基酸残基或C1-8烷基; R3是任选被芳基取代的C 1-4烷基; R4是氢或C1-2烷基; R5是任选被芳基取代的C 1-10烷基; n为1或2。

5. 发明授权

US5773468A Irreversible HIV protease inhibitor having an anti-aids activity and process for the preparation thereof 失效
标题翻译：具有抗艾滋病活性的不可逆的HIV蛋白酶抑制剂及其制备方法
公开(公告)号：US5773468A
公开(公告)日：1998-06-30
申请号：US572402
申请日：1995-12-14
申请人： Sung Chun Kim , Young Chan Son , Ho Il Choi , Heungsik Yoon , Chi Hyo Park , Nakyen Choy , Chang Sun Lee , Jong Sung Koh , Kwang Yul Moon , Won Hee Jung , Chung Ryeol Kim
发明人： Sung Chun Kim , Young Chan Son , Ho Il Choi , Heungsik Yoon , Chi Hyo Park , Nakyen Choy , Chang Sun Lee , Jong Sung Koh , Kwang Yul Moon , Won Hee Jung , Chung Ryeol Kim
IPC分类号： A61K38/00 , C07D303/46 , A01N43/20 , A01N31/34
CPC分类号： C07D303/46 , A61K38/00
摘要： The present invention relates to a novel compound of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof which is an irreversible HIV protease inhibitor; a process for the preparation thereof; and a pharmaceutical composition containing the compound as an active ingredient which is useful for treating or preventing diseases caused by HIV infection. ##STR1##
摘要翻译：本发明涉及新的式（I）化合物及其药学上可接受的盐，水合物和溶剂化物，其是不可逆的HIV蛋白酶抑制剂; 其制备方法; 以及含有该化合物作为活性成分的药物组合物，其可用于治疗或预防由HIV感染引起的疾病。（一）

6. 发明授权

US5679687A Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof 失效
标题翻译：不可逆的HIV蛋白酶抑制剂，含有它们的组合物及其制备方法
公开(公告)号：US5679687A
公开(公告)日：1997-10-21
申请号：US659794
申请日：1996-06-06
申请人： Nakyen Choy , Hoil Choi , Chi-Hyo Park , Young-Chan Son , Chang-Sun Lee , Heungsik Yoon , Sung-Chun Kim , Jong-Sung Koh , Chung-Ryeol Kim
发明人： Nakyen Choy , Hoil Choi , Chi-Hyo Park , Young-Chan Son , Chang-Sun Lee , Heungsik Yoon , Sung-Chun Kim , Jong-Sung Koh , Chung-Ryeol Kim
IPC分类号： A61K38/00 , C07K5/078 , A61K31/47 , A61K31/335 , C07D217/14 , C07D217/16
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention relates to novel compounds of formula (I) which have inhibitory activity against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group; R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group; R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group; R.sup.4 is hydrogen or a C.sub.1-4 alkyl group; R.sup.5 is an aromatic group, a C.sub.1-10 alkyl group or a C.sub.1-4 alkyl groups optionally substituted with an aromatic group; and n is 1 or 2.
摘要翻译：本发明涉及对人体免疫缺陷病毒（“HIV”）蛋白酶具有抑制活性的新型式（I）化合物，其制备方法，以及用于通过HIV感染预防或治疗AIDS的组合物，其包含上述化合物作为有效成分。（I）其中：R1是芳基，含氮芳香基，任选被芳基或含氮芳基取代的C1-4烷基，任选被芳族取代的C 1-4烷氧基基团或含氮芳族基团; R2是被C1-4烷基磺酰基取代的氨基酸残基或C1-8烷基; R3是任选被芳基取代的C 1-4烷基; R4是氢或C1-4烷基; R5是芳基，C1-10烷基或任选被芳基取代的C 1-4烷基; n为1或2。

7. 发明授权

US5587388A Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof 失效
标题翻译：不可逆的HIV蛋白酶抑制剂，中间体，组合物及其制备方法
公开(公告)号：US5587388A
公开(公告)日：1996-12-24
申请号：US159382
申请日：1993-11-30
申请人： Sung C. Kim , Nakyen Choy , Chang S. Lee , Young C. Son , Ho I. Choi , Jong S. Koh , Heungsik Yoon , Chi H. Park , Sang S. Kim
发明人： Sung C. Kim , Nakyen Choy , Chang S. Lee , Young C. Son , Ho I. Choi , Jong S. Koh , Heungsik Yoon , Chi H. Park , Sang S. Kim
IPC分类号： A61K31/335 , A61K31/00 , A61K31/336 , A61K38/00 , A61P31/00 , A61P31/12 , A61P31/18 , C07C213/02 , C07C217/08 , C07C269/04 , C07C271/20 , C07C271/22 , C07D301/02 , C07D303/36 , C07D303/38 , C07D303/40 , C07D303/46 , C07D405/12 , C07D405/14 , C07D493/08 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K7/02 , C07D215/38 , A61K31/47
CPC分类号： C07D303/38 , C07C217/08 , C07C271/20 , C07C271/22 , C07D303/36 , C07D303/46 , C07D405/12 , C07D405/14 , C07D493/08 , C07K5/0207 , C07K5/06026 , C07K5/06078 , C07K5/06139 , C07K7/02 , A61K38/00 , C07C2101/14
摘要： The present invention provides cis-epoxide compounds represented by formula (I-1), (I-2) or (I-3) which are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein: A, B, D, E, R.sup.1, R.sup.10, R.sup.11, K, G, Q, r and J have the meanings as defined in the specification.
摘要翻译：本发明提供可用于治疗或预防由HIV感染引起的疾病的由式（I-1），（I-2）或（I-3）表示的顺式环氧化合物：（I-1）（I-2）（I-3）其中：A，B，D，E，R1，R10，R11，K，G，Q，r和J具有说明书中定义的含义。

8. 发明授权

US08497379B2 Method and intermediates for the preparation of 2,2,2-trifluoro-N-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride 有权
标题翻译：用于制备2,2,2-三氟-N-（4-氟-3-吡啶-4-基 - 苄基） - 乙酰胺盐酸盐的方法和中间体
公开(公告)号：US08497379B2
公开(公告)日：2013-07-30
申请号：US13534580
申请日：2012-06-27
申请人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory B. Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
发明人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory B. Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
IPC分类号： A61K31/44 , C07D401/00
CPC分类号： C07D401/06
摘要： The present invention is directed to a method for the preparation of 2,2,2-trifluoro-n-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride of the formula: and reaction intermediates used in the method.
摘要翻译：本发明涉及制备下式的2,2,2-三氟正（4-氟-3-吡啶-4-基 - 苄基） - 乙酰胺盐酸盐的方法：和方法。

9. 发明授权

US08217178B2 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-flouro-1-(2-methoxy-ethyl)-4-trifluorom as an inhibitor of mast cell tryptase 有权
标题翻译： [4-（5-氨基甲基-2-氟 - 苯基） - 哌啶-1-基] - [7-氟-1-（2-甲氧基 - 乙基）-4-三氟甲磺隆作为肥大细胞类胰蛋白酶抑制剂
公开(公告)号：US08217178B2
公开(公告)日：2012-07-10
申请号：US13028745
申请日：2011-02-16
申请人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory Bernard Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
发明人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory Bernard Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
IPC分类号： C07D401/00 , A61K31/445
CPC分类号： C07D401/06
摘要： The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及式I的吲哚苄胺化合物，其可用作类胰蛋白酶抑制剂。此外，本发明涉及该化合物用于治疗患有或受制于需要通过抑制类胰蛋白酶而改善的生理条件的患者，其包括向患者施用治疗有效量的化合物以及包含药学有效量的式I化合物和药学上可接受的载体的药物组合物。

10. 发明授权

US08633321B2 Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof 有权
标题翻译：（4-氟-3-哌啶-4-基 - 苄基） - 氨基甲酸叔丁酯的合成及其中间体
公开(公告)号：US08633321B2
公开(公告)日：2014-01-21
申请号：US13426721
申请日：2012-03-22
申请人： Nakyen Choy , John J. Shay, Jr. , Adam W. Sledeski
发明人： Nakyen Choy , John J. Shay, Jr. , Adam W. Sledeski
IPC分类号： C07D211/02
CPC分类号： C07D211/18 , C07D213/16 , C07F5/025
摘要： The present invention is an improved method for the preparation of (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).
摘要翻译：本发明是制备（4-氟-3-吡啶-4-基 - 苄基） - 氨基甲酸叔丁酯，式I化合物的改进方法。本发明涉及一种合成方法包括形成5 - （（叔丁氧基羰基）氨基甲基）-2-氟苯硼酸（化合物11），化合物11在Suzuki偶联条件下的反应，得到（4-氟-2-吡啶-2-基）苄基） - 氨基甲酸叔丁酯，并在氢化条件下对上述产物进行选择性氢化，得到化合物I.本发明还涉及中间体5 - （（叔丁氧基羰基）氨基 - 甲基）-2- 氟化硼酸（化合物11）和（4-氟-3-吡啶-4-基 - 苄基） - 氨基甲酸叔丁酯（化合物13）。

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