公开(公告)号：US07956185B2

公开(公告)日：2011-06-07

申请号：US11753279

申请日：2007-05-24

Applicant: Robert B. Diebold ,  Stevan W. Djuric ,  Vincent L. Giranda ,  Laura A. Hexamer ,  Nan-Horng Lin ,  Julie M. Miyashiro ,  Thomas D. Penning ,  Magdalena Przytulinska ,  Thomas J. Sowin ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Yunsong Tong ,  Anil Vasudevan ,  Le Wang ,  Keith W. Woods ,  Zhiren Xia ,  Henry Q. Zhang

Inventor： Robert B. Diebold ,  Stevan W. Djuric ,  Vincent L. Giranda ,  Laura A. Hexamer ,  Nan-Horng Lin ,  Julie M. Miyashiro ,  Thomas D. Penning ,  Magdalena Przytulinska ,  Thomas J. Sowin ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Yunsong Tong ,  Anil Vasudevan ,  Le Wang ,  Keith W. Woods ,  Zhiren Xia ,  Henry Q. Zhang

IPC: C07D239/02

CPC classification number: C07D249/14 ,  C07C225/20 ,  C07C2601/02 ,  C07C2601/04 ,  C07D277/64 ,  C07D285/06 ,  C07D333/20

Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.

Abstract translation: 其中X1，C1和D1在本文中定义的式（I）化合物是polo样激酶的抑制剂。 式（I）化合物可用于治疗细胞增殖疾病，例如癌症。

公开(公告)号：US07456169B2

公开(公告)日：2008-11-25

申请号：US11466638

申请日：2006-08-23

Applicant: Lisa A. Hasvold ,  Laura Hexamer ,  Gaoquan Li ,  Nan-Horng Lin ,  Hing Sham ,  Thomas J. Sowin ,  Gerard M. Sullivan ,  Le Wang ,  Ping Xia

Inventor： Lisa A. Hasvold ,  Laura Hexamer ,  Gaoquan Li ,  Nan-Horng Lin ,  Hing Sham ,  Thomas J. Sowin ,  Gerard M. Sullivan ,  Le Wang ,  Ping Xia

IPC: C07D413/00 ,  A61K31/5513

CPC classification number: C07D243/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D491/10

Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract translation: 具有该式的化合物可用于抑制蛋白激酶。 还公开了制备化合物，含有化合物的组合物和使用该化合物的处理方法的方法。

公开(公告)号：US20070254867A1

公开(公告)日：2007-11-01

申请号：US11466638

申请日：2006-08-23

Applicant: Lisa Hasvold ,  Laura Hexamer ,  Gaoquan Li ,  Nan-Horng Lin ,  Hing Sham ,  Thomas Sowin ,  Gerard Sullivan ,  Le Wang ,  Ping Xia

Inventor： Lisa Hasvold ,  Laura Hexamer ,  Gaoquan Li ,  Nan-Horng Lin ,  Hing Sham ,  Thomas Sowin ,  Gerard Sullivan ,  Le Wang ,  Ping Xia

IPC: A61K31/55 ,  A61K31/551 ,  A61P43/00 ,  C07D471/04 ,  C07D471/14 ,  C07D487/00

CPC classification number: C07D243/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D491/10

Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract translation: 具有该式的化合物可用于抑制蛋白激酶。 还公开了制备化合物，含有化合物的组合物和使用该化合物的处理方法的方法。

公开(公告)号：US06437138B1

公开(公告)日：2002-08-20

申请号：US09472399

申请日：2000-03-01

Applicant: Nan-Horng Lin ,  Yun He ,  Mark W. Holladay ,  Keith Ryther ,  Yihong Li ,  Hao Bai

Inventor： Nan-Horng Lin ,  Yun He ,  Mark W. Holladay ,  Keith Ryther ,  Yihong Li ,  Hao Bai

IPC: C07D40100

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

Abstract: Novel 3-pyridyloxymethyl heterocyclic ether compounds of the formula: or the pharmaceutically-acceptable salts or prodrugs thereof are selective and potent ligands at neuronal nicotinic cholinergic channel receptors, and are effective in controlling synaptic transmission. Key intermediates and processes using this key intermediates to produce compounds of formula I with the variables defined in the specification are also described.

Abstract translation: 下式的新型3-吡啶氧基甲基杂环醚化合物或其药学上可接受的盐或前药是神经元烟碱胆碱能通道受体的选择性和有效配体，并且有效地控制突触传递。 还描述了使用该关键中间体产生具有本说明书中定义的变量的式I化合物的关键中间体和方法。

公开(公告)号：US6133253A

公开(公告)日：2000-10-17

申请号：US987581

申请日：1997-12-09

Applicant: Mark W. Holladay ,  Stephen P. Arneric ,  Hao Bai ,  Michael J. Dart ,  Nan-Horng Lin ,  John K. Lynch ,  Yat Sun Or ,  Keith B. Ryther ,  James P. Sullivan ,  James T. Wasicak ,  Paul P. Ehrlich

Inventor： Mark W. Holladay ,  Stephen P. Arneric ,  Hao Bai ,  Michael J. Dart ,  Nan-Horng Lin ,  John K. Lynch ,  Yat Sun Or ,  Keith B. Ryther ,  James P. Sullivan ,  James T. Wasicak ,  Paul P. Ehrlich

IPC: A61K31/4427 ,  A61K31/485 ,  C07D205/04 ,  C07D401/12 ,  A61K31/44

CPC classification number: A61K31/485 ,  A61K31/4427 ,  C07D205/04 ,  C07D401/12

Abstract: The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula I: ##STR1## or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula I above which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.

Abstract translation: 本发明涉及一种控制包括人在内的哺乳动物疼痛的方法，包括向需要治疗的哺乳动物或患者施用选择的式I化合物或其药学上可接受的盐。 本发明还涉及上述式（I）的选择的（R）和（S）化合物，其可用作止痛剂以及神经元细胞死亡预防剂和抗炎剂。

公开(公告)号：US6001849A

公开(公告)日：1999-12-14

申请号：US834053

申请日：1997-04-11

Applicant: Richard L. Elliott ,  Keith B. Ryther ,  Mark W. Holladay ,  James T. Wasicak ,  Jerome F. Daanen ,  Nan-Horng Lin ,  Michael J. Dart ,  Yun He ,  Yihong Li

Inventor： Richard L. Elliott ,  Keith B. Ryther ,  Mark W. Holladay ,  James T. Wasicak ,  Jerome F. Daanen ,  Nan-Horng Lin ,  Michael J. Dart ,  Yun He ,  Yihong Li

IPC: A61K31/00 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/4355 ,  A61P9/00 ,  A61P25/00 ,  A61P25/30 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/4355 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: Novel heterocyclic ether compounds having the formula: ##STR1## wherein A, m, R, X, Y.sup.1, Y.sup.2 and Y.sup.3 are specifically defined, which are useful in selectively controlling chemical synaptic transmission; therapeutically-effective pharmaceutical compositions thereof; and use of said compositions to selectively control synaptic transmission in mammals.

Abstract translation: 具有下式的新型杂环醚化合物：其中A，m，R，X，Y 1，Y 2和Y 3具体定义，其可用于选择性地控制化学突触传递; 其治疗有效的药物组合物; 以及使用所述组合物来选择性地控制哺乳动物中的突触传递。

公开(公告)号：US5948793A

公开(公告)日：1999-09-07

申请号：US474873

申请日：1995-06-07

Applicant: Melwyn A. Abreo ,  David E. Gunn ,  Nan-Horng Lin ,  David S. Garvey ,  Mark W. Holladay ,  Keith B. Ryther

Inventor： Melwyn A. Abreo ,  David E. Gunn ,  Nan-Horng Lin ,  David S. Garvey ,  Mark W. Holladay ,  Keith B. Ryther

IPC: C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  A61K31/55

CPC classification number: C07D401/12 ,  C07D403/12 ,  C07D417/12

Abstract: Novel heterocyclic ether compounds of the formula: ##STR1## wherein n, *, R.sup.1, R.sup.2, R.sup.3 and y are specifically defined, or pharmaceutically acceptable salts or prodrugs thereof, which are useful in selectively controlling neurotransmitter release; therapeutically-effective pharmaceutical compositions of these compounds; and use of said compositions to selectively control neurotransmitter release in mammals.

Abstract translation: 具有下式的新型杂环醚化合物：其中n，*，R1，R2，R3和y被具体定义，或其药学上可接受的盐或前药，其可用于选择性控制神经递质释放; 这些化合物的治疗有效的药物组合物; 以及使用所述组合物选择性地控制哺乳动物中的神经递质释放。

公开(公告)号：US5508418A

公开(公告)日：1996-04-16

申请号：US477057

申请日：1995-06-07

Applicant: Nan-Horng Lin ,  Yun He ,  William H. Bunnelle

Inventor： Nan-Horng Lin ,  Yun He ,  William H. Bunnelle

IPC: C07D413/04 ,  C07D207/06 ,  C07D261/04 ,  C07D261/06

CPC classification number: C07D413/04

Abstract: Novel compounds useful in the preparation of enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, namely 5(S)-(3-methyl-5-isoxazolyl)-2-pyrrolidinone, 3-methyl-5-(1-methyl-2-pyrrolidinyl)-5-hydroxy-4,5-dihydro-isoxazole, and 1-(1-methyl-2(S)-pyrrolidinyl)-1,3-butanedione-3-oxime.

Abstract translation: 用于以高产率制备对映异构纯的3-甲基-5-（1-（C 1 -C 3 - 烷基）-2-吡咯烷基）异恶唑的新型化合物，即5（S） - （3-甲基-5-异恶唑基 ）-2-吡咯烷酮，3-甲基-5-（1-甲基-2-吡咯烷基）-5-羟基-4,5-二氢异恶唑和1-（1-甲基-2（S） - 吡咯烷基） - 1,3-丁二酮-3-肟。

公开(公告)号：US20190328895A1

公开(公告)日：2019-10-31

申请号：US16349975

申请日：2017-11-14

Applicant: Nan-Horng LIN ,  CHO PHARMA INC.

Inventor： Nan-Horng LIN ,  Charng-Sheng TSAI ,  Ting-Chun HUNG ,  Hong-Yang CHUANG

IPC: A61K47/68 ,  A61K31/40 ,  C07K16/32 ,  A61P35/00 ,  A61K47/61 ,  A61K47/54

Abstract: An antibody-drug conjugate (ADC) has a structure represented by Formula (I): a pharmaceutically acceptable salt thereof wherein Ab is an antibody without glycans (i.e., the protein portion an antibody); G1 and G2 are glycan moieties, which may be the same or different; Cn1 and Cn2 are conjugation moieties, which may be the same or different; L1 and L2 are linker moieties, which may be the same or different; D1 and D2; are drug units which may be the same or different; and x and y are independently an integer from 0 to 8, provided that x+y≠0.

公开(公告)号：US08580808B2

公开(公告)日：2013-11-12

申请号：US12609518

申请日：2009-10-30

Applicant: Lindsay Burns Barbier ,  Hoau-Yan Wang ,  Nan-Horng Lin ,  Andrei Blasko

Inventor： Lindsay Burns Barbier ,  Hoau-Yan Wang ,  Nan-Horng Lin ,  Andrei Blasko

IPC: A61K31/44 ,  C07D471/10

CPC classification number: C07D471/10 ,  C07D498/10

Abstract: A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within.

Abstract translation: 公开了化合物，其药学上可接受的盐，含有其的组合物和可以提供镇痛和/或减轻炎症的治疗方法。 考虑的化合物具有对应于式A的结构，其中G，W，Q，Z，D，E，F，K，Y，d，e，f，k，n，m和圆B和全部R基团 被定义在