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1. 发明授权

US09522876B2 Cytotoxic and anti-mitotic compounds, and methods of using the same 有权
标题翻译：细胞毒性和抗有丝分裂的化合物及其使用方法
公开(公告)号：US09522876B2
公开(公告)日：2016-12-20
申请号：US14213504
申请日：2014-03-14
申请人： ZYMEWORKS INC.
发明人： Geoffrey C. Winters , Alexander L. Mandel , Bradley J. Hedberg , John Babcook , James R. Rich , Tom Han Hsiao Hsieh , Elyse Marie Josée Bourque
IPC分类号： C07C311/51 , C07C323/67 , C07C381/08 , C07C327/06 , C07C323/12 , C07D207/452 , C07D211/34 , C07D207/08 , C07D333/34 , C07D213/56 , C07D211/60 , C07D213/71 , C07K5/027 , C07K5/065 , A61K38/05 , A61K38/06 , A61K31/445 , A61K39/395 , A61K47/48 , C07K5/02 , C07C317/28 , C07C317/32 , C07C317/50
CPC分类号： C07C311/51 , A61K31/445 , A61K38/05 , A61K38/06 , A61K39/3955 , A61K47/48261 , A61K47/48415 , A61K47/6415 , C07C317/28 , C07C317/32 , C07C317/50 , C07C323/12 , C07C323/67 , C07C327/06 , C07C381/08 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/452 , C07D211/34 , C07D211/60 , C07D213/56 , C07D213/71 , C07D333/34 , C07K5/0205 , C07K5/06078 , Y02A50/385 , Y02A50/414 , Y02A50/423
摘要： Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).

2. 发明授权

US6034067A Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂
公开(公告)号：US6034067A
公开(公告)日：2000-03-07
申请号：US125169
申请日：1998-08-12
申请人： Peter Diederik Jan Grootenhuis , Adrianus Petrus Antonius de Man , Anton Egbert Peter Adang
发明人： Peter Diederik Jan Grootenhuis , Adrianus Petrus Antonius de Man , Anton Egbert Peter Adang
IPC分类号： A61K38/00 , A61K31/00 , A61K38/04 , A61P7/00 , A61P7/02 , C07K5/00 , C07K5/02 , C07K5/023 , C07K5/027 , C07K5/06 , C07K5/078 , C07K5/08 , A61K38/05 , A61K38/06 , A61K38/07
CPC分类号： C07K5/0222 , C07K5/0202 , C07K5/0205 , C07K5/022 , A61K38/00 , Y02P20/55
摘要： The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases. ##STR1##
摘要翻译： PCT No.PCT / EP97 / 00625 Sec。 371日期1998年8月12日 102（e）日期1998年8月12日PCT提交1997年2月11日PCT公布。公开号WO97 / 30073 日期：1997年8月21日本发明涉及具有式（I）的化合物，其中A，B，X，N，Z和Q如说明书所述定义。本发明化合物具有抗凝血活性，可用于治疗或预防凝血酶相关疾病。

3. 发明授权

US5521284A Human cancer inhibitory pentapeptide amides and esters 失效
标题翻译：人类癌抑制五肽酰胺和酯
公开(公告)号：US5521284A
公开(公告)日：1996-05-28
申请号：US283806
申请日：1994-08-01
申请人： George R. Pettit , Jayaram K. Srirangam
发明人： George R. Pettit , Jayaram K. Srirangam
IPC分类号： A61K38/00 , A61P35/00 , C07K5/02 , C07K5/027 , C07K7/02 , A61K38/04 , C07K5/00 , C07K14/00
CPC分类号： C07K5/0205 , C07K7/02 , A61K38/00
摘要： The isolation, elucidation and synthetic replication of novel pentapeptidemides and esters are described. The compounds have the general structure ##STR1## in which R.sub.1 and R.sub.2 are selected as shown below: ##STR2##R.sub.1 =CH.sub.3 ; R.sub.2 =--O--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 16a)R.sub.1 =CH.sub.3 ; R.sub.2 =--O--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 16b)R.sub.1 =CH.sub.3 ; R.sub.2 =--NH--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 16c)
摘要翻译：描述了新型五肽酰胺和酯的分离，阐明和合成复制。该化合物具有以下一般结构： R1 = CH3; R2 = -O-CH2CH2CH2CH2CH316a）R1 = CH3; R2 = -O-CH2CH2CH2CH2CH2CH2CH2CH316b）R1 = CH3; R2 = -NH-CH2CH2CH2CH2CH2CH316c）

4. 发明申请

US20050197299A1 Peptidomimetic protease inhibitors 有权
标题翻译：拟肽蛋白酶抑制剂
公开(公告)号：US20050197299A1
公开(公告)日：2005-09-08
申请号：US10344112
申请日：2001-08-31
申请人： Robert Babine , Shu-Hul Chen , Jason Lamar , Nancy Snyder , Xicheng Sun , Mark Tebbe , Frantz Victor , Q. Wang , Yvonne Yip , Ivan Collado , Cristina Garcia-Paredes , Raymond Parker , Ling Jing , Deqi Guo , John Glass
发明人： Robert Babine , Shu-Hul Chen , Jason Lamar , Nancy Snyder , Xicheng Sun , Mark Tebbe , Frantz Victor , Q. Wang , Yvonne Yip , Ivan Collado , Cristina Garcia-Paredes , Raymond Parker , Ling Jing , Deqi Guo , John Glass
IPC分类号： C12N9/99 , A61K20060101 , A61K31/13 , A61K31/437 , A61K31/7052 , A61K31/713 , A61K38/00 , A61K38/04 , A61K38/05 , A61K38/21 , A61K38/55 , A61K45/00 , A61P20060101 , A61P1/16 , A61P31/14 , A61P43/00 , C07D209/02 , C07D209/52 , C07K20060101 , C07K5/02 , C07K5/023 , C07K5/027 , C07K5/03 , C07K5/04 , C07K5/06 , C07K7/02 , C07K7/06 , C07K14/18 , C12N7/06
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及可用作蛋白酶抑制剂的肽模拟化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理病症的患者的方法。还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法使用该组合物的患者中的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

5. 发明授权

US6153590A Biologically active peptides and compositions, their use 失效
标题翻译：生物活性肽和组合物，其用途
公开(公告)号：US6153590A
公开(公告)日：2000-11-28
申请号：US930584
申请日：1998-02-02
申请人： Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Teresa Allen
发明人： Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Teresa Allen
IPC分类号： A61K38/00 , A61P35/00 , C07K5/02 , C07K5/027 , C07K5/078 , C07K5/08 , C07K5/083
CPC分类号： C07K5/0205 , C07K5/0827 , A61K38/00
摘要： Compounds of general formula I ##STR1## wherein: R.sub.1 and R.sub.70 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group; R.sub.2 represents a hydrogen atom or an optionally substituted alkyl or acyl group or is absent when R.sub.6 represents a group --CH.dbd. as hereinafter described; R.sub.73 represents a hydrogen atom or an optional substituent or is absent when R.sub.6 represents a methylene group or a group --CH.dbd. as hereinafter described; Y represents an optional substituent; n represents 0, 1, 2, 3, or 4; R.sub.3 represents a hydrogen atom, or an optionally substituted alkyl group; R.sub.74 represents a hydrogen atom, a hydroxy group or an optionally substituted alkyl or acyl group; R.sub.7 represents a hydrogen atom or an alkyl group; R.sub.75 represents an optionally substituted alkyl group; and i) R.sub.6 and R.sub.71 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group; and R.sub.72 represents a hydrogen atom; or ii) R.sub.71 represents a hydrogen atom or an optionally susbtituted alkyl or acyl group and R.sub.72 represents a hydrogen atom or R.sub.71 and R.sub.72 are joined together such that a double bond is formed between the carbon atoms to which they are attached; and R.sub.6 represents an optionally substituted methylene group bonded to the indole moiety thereby forming a tricyclic moiety; or R.sub.6 represents an optionally substituted group --CH.dbd. bonded to the indole moiety thereby to form an aromatic tricyclic moiety; for use in therapy and as antimitotic reagents are described.
摘要翻译： PCT No.PCT / GB96 / 00942 Sec。 371日期1998年2月2日 102（e）1998年2月2日PCT 1996年4月22日PCT PCT。出版物WO96 / 33211 日期：1996年10月24日通式I化合物其中：R 1和R 70独立地表示氢原子或任选取代的烷基或酰基; R2表示氢原子或任选取代的烷基或酰基，或当R6表示基团-CH =时不存在，如下所述; 当R 6表示亚甲基或-CH =如下所述时，R 73表示氢原子或任选的取代基或不存在; Y表示任选的取代基; n表示0,1,2,3或4; R3表示氢原子或任选取代的烷基; R 74表示氢原子，羟基或任选取代的烷基或酰基; R7表示氢原子或烷基; R75表示任选取代的烷基; 和i）R 6和R 71独立地表示氢原子或任选取代的烷基或酰基; R 72表示氢原子; 或ii）R 71表示氢原子或任选取代的烷基或酰基，R 72表示氢原子或R 71和R 72连接在一起，使得在它们所连接的碳原子之间形成双键; 并且R 6表示与吲哚部分键合的任选取代的亚甲基，从而形成三环部分; 或R6表示与吲哚部分键合的任选取代的基团-CH =，从而形成芳族三环部分; 用于治疗和用作抗有益剂的试剂。

6. 发明授权

US5635483A Tumor inhibiting tetrapeptide bearing modified phenethyl amides 失效
标题翻译：具有改性苯乙基酰胺的肿瘤抑制四肽
公开(公告)号：US5635483A
公开(公告)日：1997-06-03
申请号：US985827
申请日：1992-12-03
申请人： George R. Pettit , Jozsef Barkoczy
发明人： George R. Pettit , Jozsef Barkoczy
IPC分类号： A61K38/00 , A61P35/00 , A61P35/02 , C07K5/02 , C07K5/027 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/0205 , A61K38/00
摘要： New tetrapeptides bearing modified phenethyl amides are elucidated and syesized and found to exhibit tumor inhibiting effects when measured against the NCI screen for six major types of human cancer and against the murine P388 lymphocytic cell line. The new modified tetrapeptides phenethyl amides are 6(a-k).
摘要翻译：当对六种主要类型的人类癌症和针对小鼠P388淋巴细胞细胞系的NCI筛选进行测量时，阐明并合成具有改性的苯乙基酰胺的新四肽，显示出肿瘤抑制作用。新修饰的四肽苯乙酰胺为6（a-k）。

7. 发明授权

US5599902A Cancer inhibitory peptides 失效
标题翻译：癌抑制肽
公开(公告)号：US5599902A
公开(公告)日：1997-02-04
申请号：US338004
申请日：1994-11-10
申请人： George R. Pettit , Jayaram K. Srirangam
发明人： George R. Pettit , Jayaram K. Srirangam
IPC分类号： A61K38/00 , A61P35/02 , C07D207/08 , C07K5/02 , C07K5/027 , C07K5/03 , C07K7/02 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07D207/08 , C07K5/0205 , C07K7/02 , A61K38/00
摘要： The sea hare Dolabella auricularia has yielded many structurally distinct ptides which possess antineoplastic activity. Presently the compound denominated "dolastatin 10" represents the most important of such peptides because of its demonstrated potential as an anticancer drug.The present invention relates to the systematic creation of seven unique pentapeptides by selectively coupling a tripeptide-trifluoroacetate salt with a preselected dipeptide trifluoroacetate salt which provide active molecules capable of emulating the measured therapeutic effect of dolastatin 10.
摘要翻译：海豚Dolabella auricularia已经产生了许多具有抗肿瘤活性的结构不同的肽。目前，称为“多拉司他汀10”的化合物代表了这些肽中最重要的化合物，因为其作为抗癌药具有潜力。本发明涉及通过选择性地将三肽 - 三氟乙酸盐与预选的二肽三氟乙酸盐偶联来系统地产生七种独特的五肽，其提供能够模拟测定的多拉司他汀10的治疗效果的活性分子。

8. 发明申请

US20130045930A1 CRYSTALLINE FORMS OF THE MONO-SODIUM SALT OF D-ISOGLUTAMYL-D-TRYPTOPHAN 失效
标题翻译： D-GlyGLUTAMYL-D-TRYPTOPHAN单钠盐的晶体形态
公开(公告)号：US20130045930A1
公开(公告)日：2013-02-21
申请号：US13491177
申请日：2012-06-07
申请人： Tim Fat TAM , Blaise N'ZEMBA , Regis LEUNG-TOUNG , Yingsheng WANG , Yanqing ZHAO , Lily YU
发明人： Tim Fat TAM , Blaise N'ZEMBA , Regis LEUNG-TOUNG , Yingsheng WANG , Yanqing ZHAO , Lily YU
IPC分类号： C07D209/20 , A61P17/06 , C07K5/027 , A61P29/00 , A61P19/02 , A61K31/405 , A61P17/00
CPC分类号： C07D209/20 , A61K38/00 , C30B7/00
摘要： The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 2 (polymorphic form I) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.
摘要翻译：本发明涉及D-异谷氨酰-D-色氨酸的单钠盐的结晶形式，包含它们的药物组合物，它们在各种疾病和病症的治疗中的用途及其制备方法。特别地，本发明涉及D-异谷氨酰-D-色氨酸的单钠盐的晶体改性2（多晶型I）。

9. 发明申请

US20050090449A1 Novel statine derivatives for the treatment of Alzheimer's disease 审中-公开
标题翻译：用于治疗阿尔茨海默病的新型statine衍生物
公开(公告)号：US20050090449A1
公开(公告)日：2005-04-28
申请号：US10840037
申请日：2004-05-06
申请人： Klaus Fuchs , Stefan Peters , Comelia Dorner-Ciossek , Marcus Kostka , Sandra Handschuh , Christian Haass
发明人： Klaus Fuchs , Stefan Peters , Comelia Dorner-Ciossek , Marcus Kostka , Sandra Handschuh , Christian Haass
IPC分类号： A61K38/00 , A61K38/04 , A61K38/05 , A61K38/06 , A61K38/08 , A61P25/28 , C07K5/02 , C07K5/027 , C07K5/06 , C07K7/06
CPC分类号： C07K5/0207 , A61K38/00 , C07K5/0205
摘要： The invention relates to a compound of the formula wherein R1, R2, X, Y, n, t and m are defined as in the specification and claims and to its use for treating or preventing Alzheimer's disease and other similar diseases.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2，X，Y，n，t和m如说明书和权利要求中所定义，用于治疗或预防阿尔茨海默病和其他类似疾病。

10. 发明授权

US6034216A Low molecular weight peptidomimetic growth hormone secretagogues 失效
公开(公告)号：US6034216A
公开(公告)日：2000-03-07
申请号：US57074
申请日：1998-04-08
申请人： Todd C. Somers , Kathleen A. Elias , Ross G. Clark , Robert S. McDowell , Mark S. Stanley , John P. Burnier , Thomas E. Rawson
发明人： Todd C. Somers , Kathleen A. Elias , Ross G. Clark , Robert S. McDowell , Mark S. Stanley , John P. Burnier , Thomas E. Rawson
IPC分类号： C07D295/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K38/00 , A61K38/04 , A61K38/27 , A61P3/08 , A61P5/00 , C07D209/16 , C07D209/20 , C07D211/62 , C07D401/12 , C07D403/12 , C07K5/02 , C07K5/023 , C07K5/027 , C07K5/03 , C07K5/065 , C07K5/078 , C07K5/087 , C07K5/097 , C07K5/107 , C07K5/117 , C07K7/06 , C07K14/60 , A61K38/06
CPC分类号： C07D401/12 , C07D209/20 , C07D211/62 , C07D403/12 , C07K14/60 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06078 , C07K5/0812 , C07K5/1016 , C07K5/1024 , C07K7/06 , A61K38/00
摘要： The present invention comprises growth hormone releasing peptides/peptidomimetics (GHRP) capable of causing release of growth hormone from the pituitary. Compositions containing the GHRP's of this invention are used to promote growth in mammals either alone or in combination with other growth promoting compounds, especially IGF-1. In a method of this invention GHRP's in combination with IGF-1 are used to treat Type II diabetes. An exemplary compound of this invention is provided below. ##STR1##

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