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1. 发明授权

US5658880A Sialic acid/fucose based medicaments 失效
标题翻译：唾液酸/岩藻糖基药物
公开(公告)号：US5658880A
公开(公告)日：1997-08-19
申请号：US289715
申请日：1994-08-12
申请人： Falguni Dasgupta , John H. Musser , Daniel E. Levy , Peng Cho Tang
发明人： Falguni Dasgupta , John H. Musser , Daniel E. Levy , Peng Cho Tang
IPC分类号： G01N33/566 , A61K31/70 , A61K31/7028 , A61K49/00 , A61K51/00 , A61P29/00 , A61P31/04 , C07D309/10 , C07H3/06 , C07H11/00 , C07H15/04 , C07H15/18 , A61K31/715 , A61K38/14 , C07K2/00
CPC分类号： A61K31/7012 , C07D309/10 , C07H11/00 , C07H15/04 , C07H15/18 , C07H3/06
摘要： Compounds that exhibit selectin binding activity are described and have the following structural formula: ##STR1## where W is selected from a group including structures a-d below ##STR2## wherein p is an integer of from 0-2, q is an integer of from 0-3, and r is an integer of from 0-5;A is selected from the group consisting of .alpha. and .beta. forms of sialic acid, Kemp's acid, quinic acid, R and S forms of mandelic acid, R and S forms of glyceric acid, R and S forms of lactic acid, propionic and acetic acid, and esters and amides thereof, --SO.sub.3, sulfonate, --PO.sub.3, phosphonate, trifluoromethyl, diazine and triazine;B is selected from a group consisting of .alpha. and .beta. forms of fucose, arabinose and esters and substituted forms thereof wherein one or more of the OH groups is independently substituted with F, N.sub.3, NHAc, NHCOCF.sub.3. The remaining variable are described in the specification.
摘要翻译：描述具有选择素结合活性的化合物，并具有以下结构式：其中W选自包含以下结构的组（a）（b）（c）（d）其中p是0-2的整数，q是0-3的整数，r是0-5的整数; A选自唾液酸的α和β形式，肯普酸，奎尼酸，R和S形扁桃酸，R和S形式的甘油酸，R和S形式的乳酸，丙酸和乙酸，及其酯和酰胺，-SO 3，磺酸盐，-PO 3，膦酸盐，三氟甲基，二嗪和三嗪; B选自由岩藻糖，阿拉伯糖和酯及其取代形式的α和β形式组成的组，其中一个或多个OH基团独立地被F，N 3，NHAc，NHCOCF 3取代。剩余变量在说明书中描述。

2. 发明授权

US5789385A Sialyl Lewis.sup.x mimetics containing phenyl backbones 失效
标题翻译：含有苯基主链的唾液酸Lewisx模拟物
公开(公告)号：US5789385A
公开(公告)日：1998-08-04
申请号：US604162
申请日：1996-02-21
申请人： Mark B. Anderson , Daniel E. Levy , Peng Cho Tang , John H. Musser , Narasinga Rao , Jing Rong Cui
发明人： Mark B. Anderson , Daniel E. Levy , Peng Cho Tang , John H. Musser , Narasinga Rao , Jing Rong Cui
IPC分类号： C07D309/10 , C07D405/12 , C07D407/12 , C07D493/04 , C07D499/00 , C07H3/06 , C07H11/00 , C07H15/04 , C07H15/18 , A61K31/70 , C07H15/00
CPC分类号： C07D493/04 , A61K31/7012 , C07D309/10 , C07D405/12 , C07D407/12 , C07D499/00 , C07H11/00 , C07H15/04 , C07H15/18 , C07H3/06
摘要： Compounds that possess selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs, derivatives, or mimics of these groups, such that sialic acid and fucose or their mimics are separated by a linker that permits binding between those groups and the selecting, such compounds being represented by the following general structural formula I: ##STR1##
摘要翻译：描述了具有选择蛋白结合活性的化合物，其具有唾液酸和岩藻糖的三维稳定构型，或这些基团的类似物，衍生物或模拟物，使得唾液酸和岩藻糖或其模拟物通过允许结合的接头分离在这些基团和选择之间，这些化合物由以下通式结构式I表示：（I）

3. 发明授权

US5837689A Sialyl lewis-x mimetics containing naphthyl backbones 失效
标题翻译：含有萘基骨架的唾液酸lewis-x模拟物
公开(公告)号：US5837689A
公开(公告)日：1998-11-17
申请号：US604160
申请日：1996-02-21
申请人： Mark B. Anderson , Daniel E. Levy , Peng Cho Tang , John H. Musser , Narasinga Rao
发明人： Mark B. Anderson , Daniel E. Levy , Peng Cho Tang , John H. Musser , Narasinga Rao
IPC分类号： C07D309/10 , C07D405/12 , C07D407/12 , C07D493/04 , C07D499/00 , C07H3/06 , C07H11/00 , C07H15/04 , C07H15/18 , A61K31/70 , C07H15/00
CPC分类号： C07D493/04 , A61K31/7012 , C07D309/10 , C07D405/12 , C07D407/12 , C07D499/00 , C07H11/00 , C07H15/04 , C07H15/18 , C07H3/06
摘要： Compounds that possess selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs, derivatives, or mimics of these groups, such that sialic acid and fucose or their mimics are separated by a linker that permits binding between those groups and the selecting, such compounds being represented by the following general structural formula I: ##STR1##
摘要翻译：描述了具有选择蛋白结合活性的化合物，其具有唾液酸和岩藻糖的三维稳定构型，或这些基团的类似物，衍生物或模拟物，使得唾液酸和岩藻糖或其模拟物通过允许结合的接头分离在这些基团和选择之间，这些化合物由以下通式结构式I表示：（I）

4. 发明授权

US5728685A Methods of treating inflammation using cell adhesion inhibitors 失效
标题翻译：使用细胞粘附抑制剂治疗炎症的方法
公开(公告)号：US5728685A
公开(公告)日：1998-03-17
申请号：US466667
申请日：1995-06-06
申请人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
发明人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
IPC分类号： C07H15/04 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61P9/08 , A61P9/10 , A61P29/00 , A61P35/00 , A61P37/06 , C07H3/04 , C07H3/06 , C07H11/00 , C07H15/18 , C07H17/04 , C07H23/00 , A61K31/715
CPC分类号： C07H11/00 , C07H15/18 , C07H23/00 , C07H3/04 , C07H3/06 , Y10S514/825 , Y10S514/885 , Y10S514/886 , Y10S514/921
摘要： Compounds and methods of making them having the following formula are described which bind to selectin receptors and thus modulate the course of inflammation, cancer and related diseases by modulating cell-cell adhesion events: ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, OH or lower alkyl (1-4C), or a lipophilic group such as a higher alkyl group (5-15C), alkylaryl or one or more additional saccharide residues; R.sup.3 is a negatively charged moiety including SO.sub.4.sup.2-, PO.sub.4.sup.2-, or related group; Y is H or lower alkyl (1-4C); and X is H or --CHR.sup.4 (CHOR.sup.1).sub.2 CHR.sup.5 OR.sup.1 wherein R.sup.4 and R.sup.5 are each independently H, lower alkyl (1-4C), or taken together result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ; said five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 with the proviso that if X represents a hexose substituent R.sup.3 and R.sup.4, taken together, cannot provide a hexose substituent.
摘要翻译：描述了使其具有下式的化合物和方法，它们结合选择素受体，从而通过调节细胞粘附事件来调节炎症，癌症和相关疾病的过程：其中每个R1独立地是H或低级烷基（ 1-4C）; R2是H，OH或低级烷基（1-4C），或亲脂基团如高级烷基（5-15C），烷基芳基或一个或多个另外的糖残基; R3是包含SO42-，PO42-或相关基团的带负电荷的部分; Y为H或低级烷基（1-4C）; 并且X是H或-CHR 4（CHOR 1）2 CHR 5 OR 1，其中R 4和R 5各自独立地为H，低级烷基（1-4C）或一起形成任选含有选自以下的杂原子的五元或六元环：的O，S和NR1; 所述五元或六元环任选被一个选自R 1，CH 2 OR 1，OR 1，OOCR 1，NR 12，NHCOR 1和SR 1的取代基取代，条件是如果X表示己糖取代基R 3和R 4，不能提供己糖取代基。

5. 发明授权

US5591835A Substituted lactose derivatives 失效
标题翻译：取代的乳糖衍生物
公开(公告)号：US5591835A
公开(公告)日：1997-01-07
申请号：US189630
申请日：1994-02-01
申请人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
发明人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
IPC分类号： C07H15/04 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61P9/08 , A61P9/10 , A61P29/00 , A61P35/00 , A61P37/06 , C07H3/04 , C07H3/06 , C07H11/00 , C07H15/18 , C07H17/04 , C07H23/00
CPC分类号： C07H11/00 , C07H15/18 , C07H23/00 , C07H3/04 , C07H3/06 , Y10S514/825 , Y10S514/885 , Y10S514/886 , Y10S514/921
摘要： Compounds and methods of making them having the following formula are described which bind to selectin receptors and thus modulate the course of inflammation, cancer and related diseases by modulating cell-cell adhesion events: ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, OH or lower alkyl (1-4C), or a lipophilic group such as a higher alkyl group (5-15C), alkylaryl or one or more additional saccharide residues;R.sup.3 is a negatively charged moiety including SO.sub.4.sup.2-, PO.sub.4.sup.2-, or related group;Y is H or lower alkyl (1-4C); andX is H or --CHR.sub.4 (CHOR.sup.1).sub.2 CHR.sup.5 OR.sup.1 wherein R.sup.4 and R.sup.5 are each independently H, lower alkyl (1-4C), or taken together result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;the five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 with the proviso that if X represents a hexose substituent R.sup.3 and R.sup.4, taken together, cannot provide a hexose substituent.
摘要翻译：描述了使其具有下式的化合物和方法，它们结合选择素受体，从而通过调节细胞粘附事件来调节炎症，癌症和相关疾病的过程：其中每个R1独立地是H或低级烷基（ 1-4C）; R2是H，OH或低级烷基（1-4C），或亲脂基团如高级烷基（5-15C），烷基芳基或一个或多个另外的糖残基; R3是包含SO42-，PO42-或相关基团的带负电荷的部分; Y为H或低级烷基（1-4C）; 并且X是H或-CHR 4（CHOR 1）2 CHR 5 OR 1，其中R 4和R 5各自独立地为H，低级烷基（1-4C）或一起形成任选含有选自以下的杂原子的五元或六元环：的O，S和NR1; 任选被一个选自R1，CH2OR1，OR1，OOCR1，NR12，NHCOR1和SR1的取代基取代的五元或六元环，条件是如果X表示己糖取代基R 3和R 4，不能提供己糖取代基。

6. 发明授权

US5567683A Substituted lactose and lactosamine derivatives as cell adhesion inhibitors 失效
标题翻译：取代的乳糖和乳糖胺衍生物作为细胞粘附抑制剂
公开(公告)号：US5567683A
公开(公告)日：1996-10-22
申请号：US270874
申请日：1994-07-01
申请人： Mina A. Nashed , Falguni Dasgupta , Saeed A. Abbas , John H. Musser , Darwin S. Asa
发明人： Mina A. Nashed , Falguni Dasgupta , Saeed A. Abbas , John H. Musser , Darwin S. Asa
IPC分类号： C07H5/04 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/7042 , A61K31/715 , A61P29/00 , A61P37/06 , A61P37/08 , C07H3/06 , C07H5/10 , C07H13/04 , C07H15/20 , C07H17/00 , A61K31/70 , A61K38/00 , A61K38/16
CPC分类号： C07H3/06
摘要： Simple lactose or lactosamine related compounds which behave as ligands for the ELAM-1 and related receptors are described. These compounds are useful in the treatment of conditions characterized by excess inflammation. These compounds are of the formula ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, lower alkyl (1-4C), alkylaryl or one or more additional saccharide residues;R.sup.3 and R.sup.4 are each independently H, alkyl(1-6C), aryl or R.sup.3 and R.sup.4, taken together, form a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;wherein said five- or six-membered ring may further be substituted by one or more substituents selected from the group consisting of (CHOR.sup.1).sub.m H wherein m is 1-4, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 ;Y is H, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NCOR.sup.1 or SR.sup.1 ; andX is --CHR.sup.5 (CHOR.sup.1).sub.2 CHR.sup.6 OR.sup.1 wherein R.sup.5 and R.sup.6 are each independently H, lower alkyl(1-4C) optionally substituted with one or more F, or result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;said five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, SR.sup.1 and F;or X is benzoyl or naphthoyl having 1-3 hydroxyl substituents,with the proviso that if X represents a hexose substituent R.sup.3 and R.sup.4, taken together, cannot provide a hexose substituent.
摘要翻译：描述了作为ELAM-1和相关受体的配体的简单的乳糖或乳糖胺相关化合物。这些化合物可用于治疗以过量炎症为特征的病症。这些化合物具有式“IMAGE”，其中每个R 1独立地是H或低级烷基（1-4C）; R2是H，低级烷基（1-4C），烷基芳基或一个或多个另外的糖残基; R 3和R 4各自独立地为H，烷基（1-6C），芳基或R 3和R 4一起形成任选含有选自O，S和NR 1的杂原子的五元或六元环; 其中所述五元或六元环可以进一步被一个或多个选自（CHOR1）mH的取代基取代，其中m是1-4，OR1，OOCR1，NR12，NHCOR1和SR1; Y是H，OR1，OOCR1，NR12，NCOR1或SR1; 并且X是-CHR 5（CHOR 1）2 CHR 6OR 1，其中R 5和R 6各自独立地为H，任选地被一个或多个F取代的低级烷基（1-4C），或者产生任选含有选自以下的杂原子的五元或六元环由O，S和NR1组成的组; 所述五元或六元环任选被一个选自由R 1，CH 2 OR 1，OR 1，OOCR 1，NR 12，NHCOR 1，SR 1和F的取代基取代; 或X是具有1-3个羟基取代基的苯甲酰基或萘甲酰基，条件是如果X表示己糖取代基R 3和R 4一起不能提供己糖取代基。

7. 发明授权

US5773438A Synthetic matrix metalloprotease inhibitors and use thereof 失效
标题翻译：合成基质金属蛋白酶抑制剂及其用途
公开(公告)号：US5773438A
公开(公告)日：1998-06-30
申请号：US464927
申请日：1994-06-05
申请人： Daniel E. Levy , Damian Grobelny , Cho Tang , Kevin R. Holme , Richard E. Galardy , Gregory S. Schultz , Asaad Nematalia , John H. Musser
发明人： Daniel E. Levy , Damian Grobelny , Cho Tang , Kevin R. Holme , Richard E. Galardy , Gregory S. Schultz , Asaad Nematalia , John H. Musser
IPC分类号： A61K45/00 , A61K31/00 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/535 , A61K38/00 , A61K38/04 , A61K38/55 , A61P29/00 , A61P35/00 , C07C259/06 , C07C271/02 , C07D209/20 , C07D209/26 , C07D401/12 , C07K5/072 , C07K5/078 , C07D207/32 , C07D265/28
CPC分类号： C07D401/12 , A61K31/00 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/535 , A61K38/005 , A61K38/04 , A61K38/55 , C07C259/06 , C07C271/02 , C07D209/20 , C07D209/26 , C07K5/06104 , C07K5/06113 , C07K5/06156 , C07C2101/16
摘要： Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.
摘要翻译：合成的哺乳动物基质金属蛋白酶抑制剂可用于治疗或预防所述疾病由不想要的哺乳动物基质金属蛋白酶活性引起的疾病，并且包括皮肤病，圆锥角膜，再狭窄，类风湿性关节炎，伤口，癌症，血管生成和休克。

8. 发明授权

US5892112A Process for preparing synthetic matrix metalloprotease inhibitors 失效
标题翻译：制备合成基质金属蛋白酶抑制剂的方法
公开(公告)号：US5892112A
公开(公告)日：1999-04-06
申请号：US184727
申请日：1994-01-21
申请人： Daniel E. Levy , Damian Grobelny , Cho Tang , Kevin R. Holme , Richard E. Galardy , Gregory S. Schultz , Asaad Nematalia , John H. Musser
发明人： Daniel E. Levy , Damian Grobelny , Cho Tang , Kevin R. Holme , Richard E. Galardy , Gregory S. Schultz , Asaad Nematalia , John H. Musser
IPC分类号： A61K45/00 , A61K31/00 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/535 , A61K38/00 , A61K38/04 , A61K38/55 , A61P29/00 , A61P35/00 , C07C259/06 , C07C271/02 , C07D209/20 , C07D209/26 , C07D401/12 , C07K5/072 , C07K5/078 , C07B57/00 , C07C227/18 , C07C235/16
CPC分类号： C07D401/12 , A61K31/00 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/535 , A61K38/005 , A61K38/04 , A61K38/55 , C07C259/06 , C07C271/02 , C07D209/20 , C07D209/26 , C07K5/06104 , C07K5/06113 , C07K5/06156 , C07C2101/16
摘要： Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.
摘要翻译：合成的哺乳动物基质金属蛋白酶抑制剂可用于治疗或预防所述疾病由不想要的哺乳动物基质金属蛋白酶活性引起的疾病，并且包括皮肤病，圆锥角膜，再狭窄，类风湿性关节炎，伤口，癌症，血管生成和休克。

9. 发明申请

US20120101025A1 Compounds For Enzyme Inhibition 审中-公开
标题翻译：化合物用于酶抑制
公开(公告)号：US20120101025A1
公开(公告)日：2012-04-26
申请号：US13341022
申请日：2011-12-30
申请人： Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
发明人： Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
IPC分类号： A61K38/06 , A61P17/06 , A61P11/08 , A61P11/00 , A61P31/18 , A61P25/28 , A61P25/00 , A61P9/10 , A61P25/02 , A61P25/16 , A61P31/04 , A61P33/00 , A61P31/12 , A61P21/00 , A61P35/00 , A61P27/02 , A61P9/04 , A61P17/00 , A61P37/00 , A61P37/06 , A61P19/02 , A61P1/00 , A61P31/00 , A61P13/12 , A61P1/16 , A61P11/06 , A61P37/08 , A61P1/18 , A61P29/00
CPC分类号： C07K5/0812 , C07K5/06034 , C07K5/0827 , Y02A50/412
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的糜蛋白酶样活性。肽类化合物包括环氧化物或氮丙啶，并且在N-末端官能化。除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

10. 发明申请

US20100331554A1 TRIPTOLIDE LACTONE RING DERIVATIVES AS IMMUNOMODULATORS AND ANTICANCER AGENTS 有权
公开(公告)号：US20100331554A1
公开(公告)日：2010-12-30
申请号：US12874434
申请日：2010-09-02
申请人： Hongwei Yuan , John H. Musser , Dongcheng Dai
发明人： Hongwei Yuan , John H. Musser , Dongcheng Dai
IPC分类号： C07D407/14
CPC分类号： C07D493/22
摘要： Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
摘要翻译：公开了基于雷公藤内酯和羟基化的雷公藤内酯的内酯环修饰的化合物，用于治疗，如抗增殖，抗癌和免疫抑制治疗。

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