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1. 发明授权

US06602883B1 Inhibitors of farnesyl protein transferase 失效
公开(公告)号：US06602883B1
公开(公告)日：2003-08-05
申请号：US09566396
申请日：2000-05-05
申请人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
发明人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
IPC分类号： A61K3147
CPC分类号： C07D401/06 , C07D403/06 , C07D403/12 , C07D409/14
摘要： Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.

2. 发明授权

US06387926B1 Inhibitors of farnesyl protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US06387926B1
公开(公告)日：2002-05-14
申请号：US09087179
申请日：1998-05-29
申请人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
发明人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
IPC分类号： A61K3147
CPC分类号： C07D401/06 , C07D403/06 , C07D403/12 , C07D409/14
摘要： Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.
摘要翻译：公开了抑制法尼基蛋白转移酶（FTase）和致癌蛋白Ras的法呢基化的喹啉和苯并氮杂衍生物。因此，这些化合物可用作抗癌剂。所述化合物还可用于治疗除癌症以外的疾病。

3. 发明授权

US06458783B1 Non-imidazole benzodiazepine inhibitors of farnesyl protein transferase 失效
标题翻译：法尼基蛋白转移酶的非咪唑苯并二氮类抑制剂
公开(公告)号：US06458783B1
公开(公告)日：2002-10-01
申请号：US09556740
申请日：2000-04-21
申请人： Charles Z. Ding , John T. Hunt , Katerina Leftheris , Rajeev S. Bhide
发明人： Charles Z. Ding , John T. Hunt , Katerina Leftheris , Rajeev S. Bhide
IPC分类号： A61K31675
CPC分类号： C07D401/06 , C07D243/14 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/12 , C07D413/06
摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof.
摘要翻译：对参与ras癌基因表达的酶的法呢基转移酶的抑制是由formulastheir对映异构体，非对映异构体及其药学上可接受的盐，前药和溶剂化物的化合物进行的。

4. 发明授权

US06455523B1 Inhibitors of farnesyl protein transferase 失效
公开(公告)号：US06455523B1
公开(公告)日：2002-09-24
申请号：US09374210
申请日：1999-08-13
申请人： Charles Z. Ding , Soong-Hoon Kim , John T. Hunt , Toomas Mitt , Rajeev Bhide , Katerina Leftheris
发明人： Charles Z. Ding , Soong-Hoon Kim , John T. Hunt , Toomas Mitt , Rajeev Bhide , Katerina Leftheris
IPC分类号： A61K3155
CPC分类号： C07D243/14 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D495/04
摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras ocogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof inhibit farnesyl protein transferase which is an enzyme involved in ras oncogene expression. In formulas I-IV and throughout their specification, the above symbols are defined as follows: m, n, r, s and t are 0 or 1; p is 0, 1 or 2; V, W and X are selected from the group consisting of oxygen, hydrogen, R1, R2 or R3; Z and Y are selected from the group consisting of CHR9, SO2, SO3, CO, CO2, O, NR10, So2NR11, CONR12, or Z may be absent; R6, R7, R9, R10, R11, R12 R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R24, R25, R26, R27, R28, R29, R30, R31, R32,R33, R34, R35, R36, R37, and R38 are selected from the group consisting of hydrogen, lower alkyl, substituted alkyl, aryl or substituted aryl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R23; U is selected from the group consisting of sulfur, oxygen, NR24, CO, SO, SO2, CO2, NR25CO2, NR26CONR27, NR28SO2, NR29SO2NR30, SO2NR31, NR32CO, CONR33, PO2R34 and PO3R35 or U is absent; R1, R2, and R3 are selected from the group consisting of hydrogen, alkyl, alkoxycarbonyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo, cyano, carboxy, carbamyl (e.g. CONH2) or substituted carbamyl further selected from CONH alkyl, CONH aryl, CONH aralkyl or cases where there are two substituents on the nitrogen selected from alkyl, aryl or aralkyl; R8 and R23 are selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo; Any two of R1, R2, and R3 can be joined to form a cycloalkyl group; R, S and T are selected from the group consisting of CH2, CO and CH(CH2)pQ wherein Q is NR36R37, OR38, or CN; and A, B, C and D are carbon, oxygen, sulfur or nitrogen. with the provisos that 1. When m is zero then V and W are not both oxygen or 2 W and X together can be oxygen only if Z is either absent, O, NR10, in formulas I and II, and V and X together can be oxygen only if Y is O, NR10, in formulas III and IV or 3. R23 may be hydrogen except when U is SO, SO2, NR25CO2 or NR28SO2, or 4. R8 may be hydrogen except when Z is SO2, CO2, or

5. 发明授权

US6011029A Inhibitors of farnesyl protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US6011029A
公开(公告)日：2000-01-04
申请号：US802329
申请日：1997-02-20
申请人： Charles Z. Ding , Soong-Hoon Kim , John T. Hunt , Toomas Mitt , Rajeev Bhide , Katerina Leftheris
发明人： Charles Z. Ding , Soong-Hoon Kim , John T. Hunt , Toomas Mitt , Rajeev Bhide , Katerina Leftheris
IPC分类号： C07D401/14 , A61K31/00 , A61K31/35 , A61K31/4178 , A61K31/495 , A61K31/498 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/675 , A61P35/00 , A61P43/00 , C07D20060101 , C07D243/14 , C07D245/06 , C07D401/04 , C07D401/10 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/044 , C07D491/048 , C07D495/04 , C07D497/04 , C07D513/04 , C07F9/645 , C07D243/24
CPC分类号： C07D243/14 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D495/04
摘要： The present invention comprises benzodiazepine compounds having farnesyl transferase inhibitory activity.
摘要翻译：本发明包括具有法呢基转移酶抑制活性的苯并二氮杂类化合物。

6. 发明授权

US6156746A 1,2,5-benzothiadiazepine-1,1-dioxides with n-2 imidazolylalkyl substituents 有权
标题翻译：具有n-2个咪唑基烷基取代基的1,2,5-苯并噻二氮杂-1,1-二氧化物
公开(公告)号：US6156746A
公开(公告)日：2000-12-05
申请号：US354038
申请日：1999-07-15
申请人： Katerina Leftheris , John T. Hunt , Charles Z. Ding
发明人： Katerina Leftheris , John T. Hunt , Charles Z. Ding
IPC分类号： C07D417/06 , A61K31/551 , C07D419/14
CPC分类号： C07D417/06
摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.
摘要翻译：抑制参与ras癌基因表达的酶的法呢基转移酶由下式的化合物及其对映异构体，非对映异构体及其药学上可接受的盐包括其前体药物和溶剂化物来实现。式I化合物可用于治疗各种癌症。此外，式I化合物还可用于治疗除癌症以外的疾病。

7. 发明授权

US07244733B2 Pyrrolotriazine inhibitors of kinases 有权
标题翻译：吡咯并三嗪激酶抑制剂
公开(公告)号：US07244733B2
公开(公告)日：2007-07-17
申请号：US11345845
申请日：2006-02-02
申请人： John T. Hunt , Rajeev S. Bhide , Robert Michael Borzilleri , Ligang Qian
发明人： John T. Hunt , Rajeev S. Bhide , Robert Michael Borzilleri , Ligang Qian
IPC分类号： A61K31/53 , A61P35/00 , A61P19/02 , C07D487/04
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制生长因子受体如VEGFR-2，FGFR-1，PDGFR，HER-1，HER-2的酪氨酸激酶活性，从而使其成为抗癌剂。式I化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。

8. 发明授权

US06982265B1 Pyrrolotriazine inhibitors of kinases 有权
标题翻译：吡咯并三嗪激酶抑制剂
公开(公告)号：US06982265B1
公开(公告)日：2006-01-03
申请号：US09573829
申请日：2000-05-18
申请人： John T. Hunt , Rajeev S. Bhide , Robert Michael Borzilleri , Ligang Qian
发明人： John T. Hunt , Rajeev S. Bhide , Robert Michael Borzilleri , Ligang Qian
IPC分类号： C07D487/04 , A61K31/153 , A61P35/00 , A61P27/02 , A61P29/00
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制生长因子受体如VEGFR-2，FGFR-1，PDGFR，HER-1，HER-2的酪氨酸激酶活性，从而使其成为抗癌剂。式I化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。

9. 发明授权

US07112675B2 Pyrrolotriazine inhibitors of kinases 有权
公开(公告)号：US07112675B2
公开(公告)日：2006-09-26
申请号：US11190412
申请日：2005-07-27
申请人： John T. Hunt , Rajeev S. Bhide , Robert Michael Borzilleri , Ligang Qian
发明人： John T. Hunt , Rajeev S. Bhide , Robert Michael Borzilleri , Ligang Qian
IPC分类号： C07D487/04 , A61K31/53 , A61P19/02
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

10. 发明授权

US4574916A Step to safety 失效
标题翻译：踏踏实实
公开(公告)号：US4574916A
公开(公告)日：1986-03-11
申请号：US748162
申请日：1985-06-24
申请人： John T. Hunt , George Spector
发明人： John T. Hunt , George Spector
IPC分类号： E06C9/00 , E06C5/34
CPC分类号： E06C7/081 , E06C9/00
摘要： A safety step fire escape is provided and consists of a plurality of steps mounted in a vertical spaced relationship to an outside wall of a building adjacent windows of the building. The last step is elevated high enough from ground level so that a person can only climb down the fire escape. A descent cable extends through the steps to guide the person down the fire escape. A signaling device is operable by movement of the descent cable from its normal position.
摘要翻译：提供安全步骤防火逃生，并且由与建筑物的建筑物的窗户的建筑物的外壁的垂直隔开的关系安装的多个台阶构成。最后一步从地面升高到足够高的地方，以至于一个人只能爬起火来逃跑。下降的电缆延伸穿过台阶，以引导人员逃离逃生。信号装置可通过下降电缆从其正常位置的移动来操作。

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