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1. 发明专利

CA2124396A1 CHEMICAL COMPOUNDS 未知
公开(公告)号：CA2124396A1
公开(公告)日：1995-11-27
申请号：CA2124396
申请日：1994-05-26
申请人： BONDINELL WILLIAM E , CALLAHAN JAMES F , HUFFMAN WILLIAM F , KEENAN RICHARD M , METCALF BRIAN W , SAMANEN JAMES , YELLIN TOBIAS O
发明人： BONDINELL WILLIAM E , CALLAHAN JAMES F , HUFFMAN WILLIAM F , KEENAN RICHARD M , METCALF BRIAN W , SAMANEN JAMES , YELLIN TOBIAS O
IPC分类号： A61K31/41 , A61K31/44 , A61K45/06 , C07D235/30 , C07D277/64 , C07D277/82 , C07D403/12 , C07K5/00 , A61K38/04 , C07D213/73
摘要： This invention relates to compounds of the formula: W-(CR'2)q-Z-(CR'R10)r-U-(CR'2)s-V-(Gly)n-(Asp)m-A which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.

2. 发明申请

WO0234760A3 COMPOUNDS AND METHODS 审中-公开
标题翻译：化合物和方法
公开(公告)号：WO0234760A3
公开(公告)日：2003-01-23
申请号：PCT/US0151175
申请日：2001-10-23
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , NEEB MICHAEL J
发明人： BONDINELL WILLIAM E , NEEB MICHAEL J
IPC分类号： C07D209/44 , C07D209/62 , C07D215/08 , C07D217/06 , C07D223/16 , C07D223/32 , C07D401/12 , C07D413/04 , C07D491/10 , A61K31/55 , A61K31/34 , C07D217/00 , C07D453/04
CPC分类号： C07D401/12 , C07D209/44 , C07D209/62 , C07D215/08 , C07D217/06 , C07D223/16 , C07D223/32 , C07D413/04 , C07D491/10
摘要： The invention relates to substituted urea compounds which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis, or idiopathic pulmonary fibrosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, treating and/or preventing rejection of transplanted organs, and inflammatory bowel disease, all in mammals, by the use of substituted urea compounds which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators maybe useful in the treatment of HIV infection.
摘要翻译：本发明涉及作为CCR5受体的调节剂，激动剂或拮抗剂的取代的脲化合物。此外，本发明涉及治疗和预防CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如特应性皮炎和过敏），类风湿性关节炎，结节病或特发性肺纤维化等纤维化疾病，动脉粥样硬化，牛皮癣，自身免疫性疾病如多发性硬化，治疗和/或预防移植器官的排斥，以及哺乳动物的炎症性肠病，都是通过使用作为CCR5受体拮抗剂的取代脲化合物。此外，由于CD8 + T细胞与COPD有牵连，因此CCR5可能在其募集中发挥作用，因此CCR5拮抗剂可为COPD治疗提供潜在的治疗方法。此外，由于CCR5是HIV进入细胞的共同受体，选择性受体调节剂也可用于治疗HIV感染。

3. 发明申请

WO2004011427A3 SUBSTITUTED BENZANILIDES AS MODULATORS OF THE CCR5 RECEPTOR 审中-公开
标题翻译：作为CCR5受体的调节剂的替代苯扎林
公开(公告)号：WO2004011427A3
公开(公告)日：2005-02-03
申请号：PCT/US0323343
申请日：2003-07-28
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , NEEB MICHAEL J
发明人： BONDINELL WILLIAM E , NEEB MICHAEL J
IPC分类号： C07D211/26 , C07D211/64 , C07D405/04 , C07D413/10 , C07C233/65 , A61K31/165
CPC分类号： C07D405/04 , C07D211/26 , C07D211/64 , C07D413/10
摘要： This invention relates to substituted benzanilides which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.
摘要翻译：本发明涉及作为CCR5受体的调节剂，激动剂或拮抗剂的取代的苯甲酰苯胺。此外，本发明涉及治疗和预防由CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如特应性皮炎和过敏），类风湿性关节炎，结节病和其他纤维化疾病，动脉粥样硬化，牛皮癣，自身免疫性疾病如多发性硬化和炎症性肠病，全部在哺乳动物中，通过使用作为CCR5受体拮抗剂的取代的苯甲酰苯胺。此外，由于CD8 + T细胞与COPD有牵连，因此CCR5可能在其募集中发挥作用，因此CCR5拮抗剂可为COPD治疗提供潜在的治疗方法。此外，由于CCR5是HIV进入细胞的共同受体，因此选择性受体调节剂可用于治疗HIV感染。

4. 发明申请

WO2004017911A3 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2004017911A3
公开(公告)日：2004-07-01
申请号：PCT/US0326358
申请日：2003-08-22
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , HALL RALPH F , JIN QI , KERNS JEFFREY K , NIE HONG , WIDDOWSON KATHERINE L
发明人： BONDINELL WILLIAM E , HALL RALPH F , JIN QI , KERNS JEFFREY K , NIE HONG , WIDDOWSON KATHERINE L
IPC分类号： A61P31/00 , C07D223/08 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , H04B3/54 , H04L5/14 , H04L27/26 , A61K31/55 , C07D401/00 , C07D403/00 , C07D405/00 , C07D413/00 , C07D415/00 , C07D417/00 , C07D419/00
CPC分类号： H04L27/2601 , C07D223/08 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： This invention relates 4-amino-azepan-3-ones of formula (1) which are useful as protease inhibitors, particularly of cathepsin S, and as such are useful for preventing a number of diseases amongst which are atherosclerotic lesions and pulmonary diseases such as asthma and allergic reactions.
摘要翻译：本发明涉及可用作蛋白酶抑制剂，特别是组织蛋白酶S的式（1）的4-氨基 - 氮杂环庚烷-3-酮，因此可用于预防许多疾病，其中包括动脉粥样硬化病变和肺部疾病如哮喘和过敏反应。

5. 发明申请

WO9850032A9 BETA-LACTAM INHIBITORS OF CoA-IT 审中-公开
标题翻译： CoA-IT的BETA-LACTAM抑制剂
公开(公告)号：WO9850032A9
公开(公告)日：1999-03-25
申请号：PCT/US9809483
申请日：1998-05-08
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , WINKLER JAMES DAVID
发明人： BONDINELL WILLIAM E , WINKLER JAMES DAVID
IPC分类号： A61K31/397 , A61K31/4436 , A61P1/00 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P37/08 , A61P43/00 , C07D205/085 , C07D205/095 , C07D405/12 , C07D409/14 , A61K31/395
CPC分类号： C07D405/12 , A61K31/397 , A61K31/4436 , C07D205/085 , C07D205/095 , C07D409/14
摘要： This invention relates to a novel method for treating disease or disorders mediated by the lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprising administering to a mammal in need thereof an effective Coenzyme A independent transacylase (CoA-IT) inhibiting amount of a compound of formula (I). This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of formula (I).
摘要翻译：本发明涉及一种用于治疗由脂质炎症介质，花生四烯酸，其代谢物和/或血小板活化因子（PAF）介导的疾病或病症的新方法，该方法包括向有需要的哺乳动物施用有效的辅酶A独立的转酰胺酶（CoA-IT）抑制量的式（I）化合物。本发明还涉及在有需要的哺乳动物中治疗或减轻炎症的方法，其包括给予所述哺乳动物有效量的式（I）化合物或组合物。

6. 发明专利

MX9700235A ANTAGONISTAS DE RECEPTOR DE INTEGRINO. 未知
公开(公告)号：MX9700235A
公开(公告)日：1998-06-30
申请号：MX9700235
申请日：1996-12-19
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , WILLIAM H MILLER
发明人： BONDINELL WILLIAM E , MILLER WILLIAM H
IPC分类号： C07D223/14
摘要： Los compuestos de la formula (I): (Ver Formula); en donde A1 es C o N; E es un anillo heteroaromático de cinco o seis miembros o un anillo aromático de seis miembros substituido opcionalmente por R3 o R4; X1-X2 es CHR1-CH, CR1=CH, NR1-CH, S(O)u-CH o O-CH; X3 es CR5R6', NR6, S(O)u-CH o O; R2 es -OR', -NR'R", -NR'SO2R''', -NR'OR', -OCR'2C(O)OR', -OCR'2OC()-R', -OCR'2C(O)NR'2, CF3 O -COCR'2R2'; R3, R4, y R7 son independientemente H, halogeno, -OR12, -SR12, -CN, -NR'R12, -NO2, -CF3, CF3S(O)r-, CO2R', -CONR'2, R14-alquilo de Co-6, R14-oxoalquilo de C1-6, R14-alquenilo de C2-6, R14-alquinilo de C2-6, R14-alquiloxi de Co-6, R14-alquilamino de Co-6, o R14-alquilo de Co-6-S(O)r-; R6 es W-(CR'2)q-Z-(CR'R10)R- -U-(CR'2)s-V- o W-(CR'2)q-U- (CR'2)s -V- U Y V están ausentes o CO, CR'2, C(=CR'R15S), S(O)n, O, NR15, CR15'OR15, CR'(OR")CR'2, CR'2CR'(OR"), C(O)CR'2, CR152C(O), CONR15, NR15CO, OC(O) C(O)O, C(5)O, OC(5), C(5)NR15, NR15C(5), 52NR15, R15SO2, N=N, NR15NR15, NR15CR15S, NR15CR15S, CR152O, OCR152, C=C, CR15-CR15, Het, o Ar, siempre que U y V no estén ausentes simultáneamente; y W y W' son un sustituyente que contiene nitrogeno, son antagonistas de receptor de integrador.

7. 发明申请

WO2004010943A3 SUBSTITUTED BENZANILIDES AS MODULATORS OF THE CCR5 RECEPTOR 审中-公开
标题翻译：取代的苯甲酰胺作为CCR5受体的调节剂
公开(公告)号：WO2004010943A3
公开(公告)日：2004-09-16
申请号：PCT/US0323524
申请日：2003-07-28
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , NEEB MICHAEL J
发明人： BONDINELL WILLIAM E , NEEB MICHAEL J
IPC分类号： C07D207/08 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/58 , C07D211/72 , C07D401/12 , C07D413/12 , C07C233/75 , A61K31/165 , A61K31/275 , C07C233/05 , C07C233/84
CPC分类号： C07D413/12 , C07D207/08 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/58 , C07D211/72 , C07D401/12
摘要： This invention relates to substituted benzanilides which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.
摘要翻译：本发明涉及取代的苯甲酰苯胺类化合物，它们是CCR5受体的调节剂，激动剂或拮抗剂。此外，本发明涉及治疗和预防由CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如特应性皮炎和变态反应），类风湿性关节炎，结节病和其他纤维化疾病，动脉粥样硬化，牛皮癣，自身免疫性疾病如多发性硬化症和炎症性肠病，都是在哺乳动物中，通过使用取代的苯甲酰苯胺类（它们是CCR5受体拮抗剂）。此外，由于CD8 + T细胞与COPD有关，CCR5可能在其募集中发挥作用，因此CCR5的拮抗剂可为COPD的治疗提供潜在治疗。而且，因为CCR5是HIV进入细胞的辅助受体，所以选择性受体调节剂可用于治疗HIV感染。

8. 发明申请

WO2004010942A3 SUBSTITUTED HETEROCYCLIC COMPOUNDS AS MODULATORS OF THE CCR5 RECEPTOR 审中-公开
标题翻译：取代的杂环化合物作为CCR5受体的调节剂
公开(公告)号：WO2004010942A3
公开(公告)日：2004-07-08
申请号：PCT/US0323523
申请日：2003-07-28
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , NEEB MICHAEL J
发明人： BONDINELL WILLIAM E , NEEB MICHAEL J
IPC分类号： A61K31/435 , A61K31/495 , A61K31/497 , C07D295/215 , C07D211/56
CPC分类号： C07D295/215 , A61K31/435 , A61K31/495 , A61K31/497
摘要： This invention relates to substituted heterocyclic compounds which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis, or idiopathic pulmonary fibrosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, treating and/or preventing rejection of transplanted organs, and inflammatory bowel disease, all in mammals, by the use of substituted heterocyclic compounds which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.
摘要翻译：本发明涉及取代的杂环化合物，它们是CCR5受体的调节剂，激动剂或拮抗剂。此外，本发明涉及治疗和预防由CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如，特应性皮炎和变态反应），类风湿性关节炎，结节病或特发性肺纤维化和其他纤维化疾病，动脉粥样硬化，牛皮癣，自身免疫性疾病如多发性硬化症，治疗和/或预防移植器官的排斥反应，以及炎症性肠病，所有这些在哺乳动物中都是通过使用取代的杂环化合物，即CCR5受体拮抗剂。此外，由于CD8 + T细胞与COPD有关，CCR5可能在其募集中发挥作用，因此CCR5的拮抗剂可为COPD的治疗提供潜在治疗。而且，因为CCR5是HIV进入细胞的辅助受体，所以选择性受体调节剂可用于治疗HIV感染。

9. 发明申请

WO02076396A2 COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES 审中-公开
公开(公告)号：WO02076396A2
公开(公告)日：2002-10-03
申请号：PCT/US0208968
申请日：2002-03-22
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM E , HOLT DENNIS A , LAGO MARIA AMPARO , NEEB MICHAEL J , SEMONES MARCUS A
发明人： BONDINELL WILLIAM E , HOLT DENNIS A , LAGO MARIA AMPARO , NEEB MICHAEL J , SEMONES MARCUS A
IPC分类号： A61P35/00 , C07D471/04 , A61K
CPC分类号： C07D471/04
摘要： Novel kinase inhibitors and methods of using them are provided.

10. 发明申请

WO0006146A9 SUBSTITUTED ANILIDE COMPOUNDS AND METHODS 审中-公开
标题翻译：取代的苯胺化合物和方法
公开(公告)号：WO0006146A9
公开(公告)日：2000-08-03
申请号：PCT/US9917121
申请日：1999-07-28
申请人： SMITHKLINE BEECHAM CORP , KU THOMAS W , BONDINELL WILLIAM E , NEEB MICHAEL J
发明人： KU THOMAS W , BONDINELL WILLIAM E , NEEB MICHAEL J
IPC分类号： C07D215/38 , A61K31/00 , A61K31/167 , A61K31/18 , A61K31/426 , A61K31/438 , A61K31/4427 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/498 , A61K31/538 , A61P1/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P29/00 , A61P37/00 , A61P37/06 , A61P37/08 , C07C233/75 , C07C235/42 , C07C235/56 , C07C235/84 , C07C237/40 , C07C251/48 , C07C311/39 , C07C317/44 , C07D211/14 , C07D215/06 , C07D241/54 , C07D265/36 , C07D277/20 , C07D277/46 , C07D277/56 , C07D295/092 , C07D401/12 , C07D491/10 , C07D491/107 , A61K31/165 , C07D235/56
CPC分类号： C07D295/088 , A61K31/00 , A61K31/167 , A61K31/18 , A61K31/426 , A61K31/438 , A61K31/445 , A61K31/47 , A61K31/498 , A61K31/538 , A61K31/5383 , C07C233/75 , C07C235/42 , C07C235/56 , C07C235/84 , C07C237/40 , C07C251/48 , C07C311/39 , C07C317/44 , C07D215/06 , C07D241/54 , C07D265/36 , C07D277/56 , C07D491/10
摘要： This invention relates to substituted anilide compounds which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5.
摘要翻译：本发明涉及作为CCR5受体的调节剂，激动剂或拮抗剂的取代的酰苯胺化合物。此外，本发明涉及治疗和预防由CCR5介导的疾病状态。

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