专利检索 ap:("Amos B. Smith, III" OR "Stephen M. Condon" OR "Johnnie L. Leazer, Jr." OR "Robert E. Maleczka" OR "John A. McCauley" OR "James W. Leahy") AND inv:"Amos B. Smith, III" 第 3 页

21.

发明授权
Synthetic techniques and intermediates for polyhydroxy, dienyl lactones and mimics thereof 失效

公开(公告)号：US5789605A

公开(公告)日：1998-08-04

申请号：US759817

申请日：1996-12-03

申请人： Amos B. Smith, III , Yuping Qiu , Michael Kaufman , Hirokaza Arimoto , David R. Jones , Kaoru Kobayashi

发明人： Amos B. Smith, III , Yuping Qiu , Michael Kaufman , Hirokaza Arimoto , David R. Jones , Kaoru Kobayashi

IPC分类号： C07D303/16 , A61K31/047 , A61K31/12 , A61K31/27 , A61K31/336 , A61K31/351 , A61K31/366 , A61K31/422 , A61K31/427 , A61K31/5355 , A61K31/7028 , A61P35/00 , A61P37/06 , C07C239/06 , C07D263/22 , C07D309/10 , C07D309/30 , C07D309/32 , C07D319/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07F7/18 , C07H23/00 , C07D407/06

CPC分类号： C07D413/12 , C07C239/06 , C07D263/22 , C07D309/30 , C07D319/06 , C07F7/1892

摘要： Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.

22.

发明授权
2-Hydroxy-3-aminopropylsulfonamides 失效
标题翻译： 2-羟基-3-氨基丙基磺酰胺

公开(公告)号：US5612339A

公开(公告)日：1997-03-18

申请号：US373651

申请日：1995-01-17

申请人： Paul Sprengeler , Amos B. Smith, III , Ralph F. Hirschmann , Akihisa Yokoyama

发明人： Paul Sprengeler , Amos B. Smith, III , Ralph F. Hirschmann , Akihisa Yokoyama

IPC分类号： C07D213/38 , C07D303/36 , A61K31/50

CPC分类号： C07D303/36 , C07D213/38

摘要： 2-Hydroxy-3-aminopropylsulfonamides are provided along with methods for synthesizing and using such compounds, and chemical intermediates employed in the synthetic methods.

摘要翻译： 提供2-羟基-3-氨基丙基磺酰胺以及用于合成和使用这些化合物的方法以及在合成方法中使用的化学中间体。

23.

发明授权
Pyrrolinone-based compounds 失效
标题翻译：吡咯烷酮类化合物

公开(公告)号：US5489692A

公开(公告)日：1996-02-06

申请号：US18696

申请日：1993-02-17

申请人： Ralph Hirschmann , Amos B. Smith, III , Paul Sprengeler , Ryan C. Holcomb , Terence Keenan , John L. Wood , Mark Guzman

发明人： Ralph Hirschmann , Amos B. Smith, III , Paul Sprengeler , Ryan C. Holcomb , Terence Keenan , John L. Wood , Mark Guzman

IPC分类号： C07D207/36 , C07D207/38 , C07D207/00 , C07D413/00

CPC分类号： C07D207/38 , C07D207/36

摘要： Novel pyrrolinone-based compounds mimic or inhibit the biological and/or chemical activity of peptides, including peptide .beta.-strand conformations. Certain compounds contain functionalized pyrrolinone units in place of one or more amino acids of a target peptide.

摘要翻译： 新的基于吡咯啉酮的化合物模拟或抑制肽的生物和/或化学活性，包括肽β-链构象。某些化合物含有官能化的吡咯啉酮单元代替目标肽的一个或多个氨基酸。

24.

发明授权
Spiroketals useful as intermediates in the synthesis of milbemycin and avermectin macrolides 失效
标题翻译：螺旋酮可用作合成米尔倍霉素和阿维菌素大环内酯的中间体

公开(公告)号：US4408059A

公开(公告)日：1983-10-04

申请号：US327641

申请日：1981-12-04

申请人： Amos B. Smith, III , Steven R. Schow

发明人： Amos B. Smith, III , Steven R. Schow

IPC分类号： C07H19/01 , C07D309/06 , C07C65/00 , C07D493/22 , C07H17/08

CPC分类号： C07H19/01

摘要： Milbemycin and avermectin macrolides are synthesized by the cyclized linking of separately synthesized northern and southern hemisphere intermediates. The northern hemisphere intermediate is a spiroketal alkenyl aldehyde, and the southern hemisphere intermediate is an aryl alkenyl phosphine oxide anion.

摘要翻译： 通过单独合成的北半球和南半球中间体的环化连接合成米尔贝霉素和除虫菌素大环内酯类。北半球中间体是螺缩酮链烯基醛，南半球中间体是芳基烯基氧化膦阴离子。

25.

发明授权
Small molecule CD4 mimetics and uses thereof 有权

公开(公告)号：US09776963B2

公开(公告)日：2017-10-03

申请号：US13128549

申请日：2009-11-10

申请人： Joseph G. Sodroski , Navid Madani , Arne Schön , Judith M. LaLonde , Joel R. Courter , Takahiro Soeta , Danny Ng , Ernesto Freire , Amos B. Smith, III , Amy M. Princiotto , Matthew Le-Khac , Wayne A. Hendrickson

发明人： Joseph G. Sodroski , Navid Madani , Arne Schön , Judith M. LaLonde , Joel R. Courter , Takahiro Soeta , Danny Ng , Ernesto Freire , Amos B. Smith, III , Amy M. Princiotto , Matthew Le-Khac , Wayne A. Hendrickson

IPC分类号： A61K31/397 , C07D211/58 , C07D205/04 , C07D207/09 , C07D207/16 , C07D207/22 , C07D211/26 , C07D211/44 , C07D211/56 , C07D217/14 , C07D223/04 , C07D231/56 , C07D233/64 , C07D235/02 , C07D235/14 , C07D237/32 , C07D239/42 , C07D239/47 , C07D239/90 , C07D249/08 , C07D265/36 , C07D295/13 , C07D307/52 , C07D317/28 , C07D333/20 , C07D333/48 , C07D401/04 , C07D401/06 , C07D405/06 , C07D409/14 , C07D455/02 , C07D471/08 , C07D473/18 , C07D487/04 , C07D495/04

CPC分类号： C07D211/58 , C07D205/04 , C07D207/09 , C07D207/16 , C07D207/22 , C07D211/26 , C07D211/44 , C07D211/56 , C07D217/14 , C07D223/04 , C07D231/56 , C07D233/64 , C07D235/02 , C07D235/14 , C07D237/32 , C07D239/42 , C07D239/47 , C07D239/90 , C07D249/08 , C07D265/36 , C07D295/13 , C07D307/52 , C07D317/28 , C07D333/20 , C07D333/48 , C07D401/04 , C07D401/06 , C07D405/06 , C07D409/14 , C07D455/02 , C07D471/08 , C07D473/18 , C07D487/04 , C07D495/04

摘要： The invention provides for compounds of formula I: wherein Z is absent or (CRARB)nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHRc, NRcRc, SH, S(O)mRc; or (iii) RA and RB together form C(O); W is absent, C(O), C(O)O, C(O)NRcRc, O, S(O)m, or NRcRc; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NRXRY; wherein Rx and Ry are each independently H, alkyl or aryl; X1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each Rc is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof.

26.

发明授权
Hemi-phorboxazole A derivatives and methods of their use 有权
标题翻译： Hemi-phorboxazole一种衍生物及其使用方法

公开(公告)号：US08957097B2

公开(公告)日：2015-02-17

申请号：US13386783

申请日：2010-07-23

申请人： Amos B. Smith, III , Zhuqing Liu , Anne-Marie L. Hogan , Doralyn S. Dalisay , Tadeusz F. Molinski

发明人： Amos B. Smith, III , Zhuqing Liu , Anne-Marie L. Hogan , Doralyn S. Dalisay , Tadeusz F. Molinski

IPC分类号： A01N43/76 , A61K31/42 , C07D487/00 , C07D513/00 , C07D309/00 , A01N43/90 , C07D498/22

CPC分类号： A01N43/90 , C07D498/22

摘要： The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.

摘要翻译： 本发明涉及半柔霉唑A及其立体异构体，以及式I的半菲唑唑A的衍生物：其中环A为芳基或任选被一个或多个卤素取代的5-或6-元杂芳基， OH或-C 1-6烷基; 和R为-CN，5-或6-元杂芳基或卤素; 和其药学上可接受的盐形式，以及使用这些化合物的方法。

27.

发明授权
Cycloalkyl-dione derivatives and methods of their use 有权
标题翻译：环烷基二酮衍生物及其使用方法

公开(公告)号：US08530520B2

公开(公告)日：2013-09-10

申请号：US13489745

申请日：2012-06-06

申请人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchuan Huang , Donna M. Huryn , Michael James , Virginia M. Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski

发明人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchuan Huang , Donna M. Huryn , Michael James , Virginia M. Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski

IPC分类号： A61K31/18

CPC分类号： C07C311/17 , A61K31/18 , C07C2601/02 , C07C2601/04 , C07C2601/10 , C07C2601/14 , C07D257/04

摘要： The present invention is directed to carboxylic acid-containing pharmaceutical compounds where the carboxylic acid moieties have been substituted with cycloalkyl-dione derivatives, as well as tautomers and pharmaceutically acceptable salt forms thereof. These bioisosteric replacements improve the compound's ability to effectively cross the blood brain barrier and result in improved pharmacokinetic, toxicological, and/or safety profiles.

摘要翻译： 本发明涉及羧酸部分已被环烷基二酮衍生物取代的含羧酸的药物化合物，以及其互变异构体及其药学上可接受的盐形式。这些生物电泳替代物可以改善化合物有效跨越血脑屏障的能力，并改善药代动力学，毒理学和/或安全性。

28.

发明申请
Cycloalkyl-dione Derivatives And Methods Of Their Use 有权
标题翻译：环烷基 - 二酮衍生物及其使用方法

公开(公告)号：US20120329877A1

公开(公告)日：2012-12-27

申请号：US13489745

申请日：2012-06-06

申请人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchun Huang , Donna M. Huryn , Michael James , Virginia M.Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski

发明人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchun Huang , Donna M. Huryn , Michael James , Virginia M.Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski

IPC分类号： C07C311/19 , A61P11/00 , A61P3/10 , A61P11/06 , A61K31/18 , A61P25/28

CPC分类号： C07C311/17 , A61K31/18 , C07C2601/02 , C07C2601/04 , C07C2601/10 , C07C2601/14 , C07D257/04

摘要： The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R1 is H or C1-6alkyl and R2 is H, C1-6 alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and X is O or N; as well as tautomers and pharmaceutically acceptable salt forms thereof. Uses of these compounds are also described.

摘要翻译： 本发明涉及式I化合物：其中A是n是0,1或2; m为0或1; R 1是H或C 1-6烷基，R 2是H，C 1-6烷基，取代或未取代的芳基或取代或未取代的杂芳基; X为O或N; 以及互变异构体及其药学上可接受的盐形式。还描述了这些化合物的用途。