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41. 发明申请

US20100286192A1 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：US20100286192A1
公开(公告)日：2010-11-11
申请号：US12839807
申请日：2010-07-20
申请人： Neville J. Anthony , Robert Gomez
发明人： Neville J. Anthony , Robert Gomez
IPC分类号： A61K31/437 , A61K31/4709 , A61P31/18
CPC分类号： C07D471/04 , C07D231/54 , C07D249/18
摘要： Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R1, R2, R4, R5, R6, ring A, ring B, j and k are defined herein. The compounds of Formula I, and the pharmaceutically acceptable salts and prodrugs thereof, are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物是HIV逆转录酶抑制剂，其中V，W，X，Y，Z，R 1，R 2，R 4，R 5，R 6，环A，环B，j和k如本文所定义。式I化合物及其药学上可接受的盐和前药可用于抑制HIV逆转录酶，预防和治疗HIV感染以及预防，延缓发病或进展以及AIDS治疗。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

42. 发明授权

US07790754B2 Alpha-hydroxy amides as bradykinin antagonists or inverse agonists 有权
标题翻译： α-羟基酰胺作为缓激肽拮抗剂或反向激动剂
公开(公告)号：US07790754B2
公开(公告)日：2010-09-07
申请号：US10583675
申请日：2004-12-17
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
IPC分类号： A61K31/4439 , C07D413/10
CPC分类号： C07D239/26 , C07C235/06 , C07C235/08 , C07C235/12 , C07C235/26 , C07C235/34 , C07C235/40 , C07C2601/02 , C07C2601/04 , C07C2601/18 , C07D209/12 , C07D213/56 , C07D213/61 , C07D257/04 , C07D271/06 , C07D275/06 , C07D401/10 , C07D413/10
摘要： α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3) (CH2)nNRbSO2Rd. (4) (CH2)nNRbCO2Ra. (5) (CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6) (CH2)kCO2Ra. and (7) (CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl.
摘要翻译：通式（I）的α-羟基酰胺衍生物是可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状的缓激肽B1拮抗剂或反向激动剂。 R2a选自（1）选自Ra的基团。（2）（CH2）nNRbC（O）Ra。（3）（CH2）nNRbSO2Rd。（4）（CH2）nNRbCO2Ra。（5）（CH2）k-杂环，其任选被1至3个独立地选自卤素，硝基，氰基，硫代C 1-4烷基和C 1-3卤代烷基的基团取代，其中所述杂环是（a）5元杂芳族环，其具有选自NO和S的环杂原子，并且任选地具有至多3个另外的环氮原子，其中所述环任选地被苯并稠合; 或（b）含有1至3个环氮原子的6-元杂环和其N-氧化物。其中所述环任选地被苯并稠合。（6）（CH2）kCO2Ra。和（7）（CH 2）C（O）NR b R c。 R2b是OH或选自R2a的基团; 或R 2a和R 2b与它们所连接的碳原子一起形成任选被1至4个独立地选自卤素的基团取代的3至7元碳环。 ORa。 C 1-4烷基和C 1-4卤代烷基。

43. 发明授权

US07781454B2 Non-nucleoside reverse transcriptase inhibitors 有权
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US07781454B2
公开(公告)日：2010-08-24
申请号：US11999686
申请日：2007-12-06
申请人： Neville J. Anthony , Robert Gomez
发明人： Neville J. Anthony , Robert Gomez
IPC分类号： A01N43/42 , A61K31/44 , A61K31/415 , C07D471/02 , C07D491/02 , C07D498/02 , C07D213/56
CPC分类号： C07D471/04 , C07D231/54 , C07D249/18
摘要： Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R1, R2, R4, R5, R6, ring A, ring B, j and k are defined herein. The compounds of Formula I, and the pharmaceutically acceptable salts and prodrugs thereof, are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物是HIV逆转录酶抑制剂，其中V，W，X，Y，Z，R 1，R 2，R 4，R 5，R 6，环A，环B，j和k如本文所定义。式I化合物及其药学上可接受的盐和前药可用于抑制HIV逆转录酶，预防和治疗HIV感染以及预防，延缓发病或进展以及AIDS治疗。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

44. 发明授权

US07332499B2 Sulfonyl substituted n-(biarylmethyl) aminocyclopropanecarboxamides 失效
标题翻译：磺酰基取代的正（联芳基甲基）氨基环丙烷甲酰胺
公开(公告)号：US07332499B2
公开(公告)日：2008-02-19
申请号：US10565040
申请日：2004-08-03
申请人： Neville J. Anthony , Robert Gomez , Samson M. Jolly , John Jin Lim , Dai-shi Su
发明人： Neville J. Anthony , Robert Gomez , Samson M. Jolly , John Jin Lim , Dai-shi Su
IPC分类号： A61K31/505 , A61K31/12 , C07D417/00 , C07D239/00 , C07C233/00
CPC分类号： C07D213/82 , C07C307/02 , C07C309/65 , C07C309/66 , C07C309/67 , C07C309/76 , C07C311/09 , C07C311/46 , C07C2601/02 , C07D215/58 , C07D239/28 , C07D417/12
摘要： N-(Sulfonyloxybiarylmethyl) aminocyclopropanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-（磺酰氧基联芳基甲基）氨基环丙烷甲酰胺衍生物是缓激肽B1拮抗剂或反激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

45. 发明授权

US06358985B1 Inhibitors of prenyl-protein transferase 失效
公开(公告)号：US06358985B1
公开(公告)日：2002-03-19
申请号：US09342577
申请日：1999-06-29
申请人： Neville J. Anthony , Ian M. Bell , Douglas C. Beshore , Terrence M. Ciccarone , S. Jane de Solms , Christopher J. Dinsmore , Gerald E. Stokker
发明人： Neville J. Anthony , Ian M. Bell , Douglas C. Beshore , Terrence M. Ciccarone , S. Jane de Solms , Christopher J. Dinsmore , Gerald E. Stokker
IPC分类号： A61K314164
CPC分类号： A61K31/4174 , A61K31/00
摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

46. 发明授权

US06248756B1 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：US06248756B1
公开(公告)日：2001-06-19
申请号：US09248883
申请日：1999-02-11
申请人： Neville J. Anthony , Christopher Dinsmore , Robert P. Gomez , John H. Hutchinson , John S. Wai , Theresa M. Williams , Ian M. Bell , Mark W. Embrey , Thorsten E. Fisher
发明人： Neville J. Anthony , Christopher Dinsmore , Robert P. Gomez , John H. Hutchinson , John S. Wai , Theresa M. Williams , Ian M. Bell , Mark W. Embrey , Thorsten E. Fisher
IPC分类号： A61K314468
CPC分类号： C07D401/06 , C07D211/62 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferas (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译：本发明涉及抑制法尼基蛋白转移（Fatease-protein transferas，FTase）和致癌基因蛋白Ras的法呢基化的化合物。本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。

47. 发明授权

US5972984A 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：US5972984A
公开(公告)日：1999-10-26
申请号：US960248
申请日：1997-10-29
申请人： Neville J. Anthony , Jeffrey M. Bergman , S. Jane deSolms , Chrisopher J. Dinsmore , Robert P. Gomez , Suzanne C. MacTough , Kelly M. Solinsky , Theresa M. Williams
发明人： Neville J. Anthony , Jeffrey M. Bergman , S. Jane deSolms , Chrisopher J. Dinsmore , Robert P. Gomez , Suzanne C. MacTough , Kelly M. Solinsky , Theresa M. Williams
IPC分类号： C07D233/54 , C07D401/14 , C07D403/06 , C07D403/02 , A61K31/40 , A61K31/415
CPC分类号： C07D233/64 , C07D401/14 , C07D403/06
摘要： The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
摘要翻译：本发明包括抑制法呢基蛋白转移酶的低分子量肽基化合物。此外，这些化合物不同于先前描述为法呢基 - 蛋白转移酶抑制剂的单或二肽类似物，因为它们不具有硫醇部分。缺乏硫醇在改善动物药代动力学行为方面提供独特的优势，防止硫醇依赖的化学反应，如快速自身氧化和内源性硫醇形成二硫键，并减少全身毒性。本发明还包含含有这些法呢基转移酶抑制剂的化疗组合物及其生产方法。

48. 发明授权

US5891889A Inhibitors of farnesyl-protein transferase 失效
公开(公告)号：US5891889A
公开(公告)日：1999-04-06
申请号：US831308
申请日：1997-04-01
申请人： Neville J. Anthony , Robert P. Gomez , John S. Wai , Mark W. Embrey , Thorsten E. Fisher
发明人： Neville J. Anthony , Robert P. Gomez , John S. Wai , Mark W. Embrey , Thorsten E. Fisher
IPC分类号： C07D211/62 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/14 , C07D401/08 , A61K31/445
CPC分类号： C07D401/06 , C07D211/62 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

49. 发明授权

US5686472A 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：US5686472A
公开(公告)日：1997-11-11
申请号：US143943
申请日：1993-10-27
申请人： Neville J. Anthony , S. Jane deSolms , Ta Jyh Lee, deceased
发明人： Neville J. Anthony , S. Jane deSolms , Ta Jyh Lee, deceased
IPC分类号： A61K31/195 , A61K31/215 , A61K31/365 , A61P35/00 , A61P35/02 , A61P43/00 , C07C323/25 , C07C323/52 , C07C323/56 , C07C323/57 , C07C323/58 , C07C323/59 , C07D307/33 , C07D213/28 , A61K31/41 , C07C381/00 , C07C729/00
CPC分类号： C07D307/33 , C07C323/25 , C07C323/56 , C07C323/59
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译：本发明涉及抑制法呢基蛋白转移酶（FTase）和致癌基因蛋白Ras的法呢基化的化合物。本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。

50. 发明授权

US5661161A 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：US5661161A
公开(公告)日：1997-08-26
申请号：US527972
申请日：1995-09-14
申请人： Neville J. Anthony , Terrence M. Ciccarone , S. Jane deSolms , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
发明人： Neville J. Anthony , Terrence M. Ciccarone , S. Jane deSolms , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
IPC分类号： A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K38/00 , A61P9/00 , A61P9/10 , A61P31/00 , A61P43/00 , C07D207/28 , C07D401/06 , C07D403/06 , C07K5/02 , C07K5/06 , C07K5/08 , C07D207/16
CPC分类号： C07D401/06 , C07D207/28 , C07D403/06 , C07K5/0207 , C07K5/06026 , A61K38/00
摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid antoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
摘要翻译：本发明包括通过体内法尼基化修饰的蛋白Ras的CAAX基序的类似物。这些CAAX类似物抑制法呢基蛋白转移酶。此外，这些CAAX类似物与先前描述为法呢基 - 蛋白转移酶抑制剂的不同之处在于它们不具有硫醇部分。缺乏硫醇在改善动物体内的药代动力学行为方面提供独特的优势，预防硫醇依赖的化学反应，如用内源性硫醇快速无毒化和二硫化物形成，并减少全身毒性。本发明还包含含有这些法呢基转移酶抑制剂的化疗组合物及其生产方法。

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