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1. 发明申请

WO2013130962A1 BENZOFURAN- 2 - SULFONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：苯佐芬2 - 磺酰胺衍生物作为化学受体调节剂
公开(公告)号：WO2013130962A1
公开(公告)日：2013-09-06
申请号：PCT/US2013/028607
申请日：2013-03-01
申请人： ALLERGAN, INC. , YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
发明人： YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
IPC分类号： C07D405/12 , C07D405/14 , A61K31/443 , A61P29/00
CPC分类号： C07D307/78 , A61P29/00 , C07D307/82 , C07D405/12 , C07D405/14
摘要： The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives of formula (1), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
摘要翻译：本发明涉及式（1）的新型苯并呋喃-2-磺酰胺吡啶衍生物，其制备方法，含有它们的药物组合物及其作为药物作为趋化因子受体调节剂的用途。

2. 发明申请

WO2012082633A1 NOVEL 1,2- BIS-SULFONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：新型1,2-二磺酰胺衍生物作为化学受体调节剂
公开(公告)号：WO2012082633A1
公开(公告)日：2012-06-21
申请号：PCT/US2011/064441
申请日：2011-12-12
申请人： ALLERGAN, INC. , YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
发明人： YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
IPC分类号： C07D231/18 , C07D307/82 , C07D333/34 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07D513/04 , C07C311/44 , A61K31/381 , A61K31/427 , A61K31/422
CPC分类号： A61K31/381 , A61K31/343 , A61K31/37 , A61K31/404 , A61K31/4155 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/429 , A61K31/4436 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/55 , A61K31/635 , C07C311/21 , C07C311/44 , C07D231/18 , C07D307/82 , C07D333/34 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07D513/04
摘要： The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
摘要翻译：本发明涉及新的双磺酰胺衍生物，其制备方法，含有它们的药物组合物及其作为药物作为趋化因子受体调节剂的用途。

3. 发明申请

WO2013090227A1 BENZISOTHIAZOL-3(1H)-ONE-5-SULFONYL DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：苯并噻唑-3（1H） - 酮-5-磺酰基衍生物作为化合物受体调节剂
公开(公告)号：WO2013090227A1
公开(公告)日：2013-06-20
申请号：PCT/US2012/068873
申请日：2012-12-11
申请人： ALLERGAN, INC. , YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena
发明人： YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena
IPC分类号： C07D275/04 , C07D417/12 , C07D417/14 , A61K31/425 , A61P27/02
CPC分类号： C07D417/12 , C07D275/04 , C07D417/14
摘要： The present invention relates to novel benzisothiazol-3(1 H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
摘要翻译：本发明涉及新的苯并异噻唑-3（1H） - 酮-5-磺酰基衍生物，其制备方法，含有它们的药物组合物及其作为药物作为趋化因子受体调节剂的用途。

4. 发明申请

WO2012082566A1 SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：硫磺衍生物作为化学受体调节剂
公开(公告)号：WO2012082566A1
公开(公告)日：2012-06-21
申请号：PCT/US2011/064233
申请日：2011-12-09
申请人： ALLERGAN, INC. , YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
发明人： YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
IPC分类号： C07D213/34 , C07D213/62 , C07D233/64 , C07D307/18 , C07D307/82 , C07D333/34 , C07D407/12 , C07D417/12 , A61K31/343 , A61P31/00 , C07C311/00
CPC分类号： C07C311/21 , C07C317/34 , C07C317/36 , C07C317/42 , C07C317/44 , C07C317/50 , C07C321/30 , C07C323/49 , C07C323/52 , C07C323/56 , C07C323/60 , C07C323/67 , C07C2601/08 , C07D207/09 , C07D207/46 , C07D213/32 , C07D213/52 , C07D233/64 , C07D277/40 , C07D295/13 , C07D295/185 , C07D295/24 , C07D307/64 , C07D307/82 , C07D333/34 , C07D405/12 , C07D413/12 , C07D417/12 , C07F9/304 , C07F9/3229 , C07F9/4021 , C07F9/5325 , C07F9/591 , C07F9/6533
摘要： The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
摘要翻译：本发明涉及新的硫衍生物，其制备方法，含有它们的药物组合物及其作为药物作为趋化因子受体调节剂的用途。

5. 发明申请

WO2013130958A1 BENZOFURAN-2-SULFONAMIDES DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：苯唑呋喃-2-磺酰胺衍生物作为化学受体调节剂
公开(公告)号：WO2013130958A1
公开(公告)日：2013-09-06
申请号：PCT/US2013/028599
申请日：2013-03-01
申请人： ALLERGAN, INC. , YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
发明人： YUAN, Haiqing , BEARD, Richard L. , LIU, Xiaoxia , DONELLO, John E. , VISWANATH, Veena , GARST, Michael E.
IPC分类号： C07D401/12 , C07D307/82 , A61K31/343 , A61P29/00
CPC分类号： C07D307/78 , A61P29/00 , C07D307/82 , C07D405/12 , C07D405/14
摘要： The present invention relates to novel benzofuran-2-sulfonamide derivatives formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
摘要翻译：本发明涉及式（I）的新型苯并呋喃-2-磺酰胺衍生物，其制备方法，含有它们的药物组合物及其作为药物作为趋化因子受体调节剂的用途。

6. 发明申请

WO2012082568A1 PHOSPHOROUS DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：作为化学受体调节剂的磷酸衍生物
公开(公告)号：WO2012082568A1
公开(公告)日：2012-06-21
申请号：PCT/US2011/064242
申请日：2011-12-09
申请人： ALLERGAN, INC. , YUAN, Haiqing , BEARD, Richard, L. , LIU, Xiaoxia , DONELLO, John, E. , VISWANATH, Veena , GARST, Michael, E.
发明人： YUAN, Haiqing , BEARD, Richard, L. , LIU, Xiaoxia , DONELLO, John, E. , VISWANATH, Veena , GARST, Michael, E.
IPC分类号： C07F9/32 , A61K31/662 , C07F9/36
CPC分类号： C07C311/21 , C07C317/34 , C07C317/36 , C07C317/42 , C07C317/44 , C07C317/50 , C07C321/30 , C07C323/49 , C07C323/52 , C07C323/56 , C07C323/60 , C07C323/67 , C07C2601/08 , C07D207/09 , C07D207/46 , C07D213/32 , C07D213/52 , C07D233/64 , C07D277/40 , C07D295/13 , C07D295/185 , C07D295/24 , C07D307/64 , C07D307/82 , C07D333/34 , C07D405/12 , C07D413/12 , C07D417/12 , C07F9/304 , C07F9/3229 , C07F9/4021 , C07F9/5325 , C07F9/591 , C07F9/6533
摘要： The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
摘要翻译：本发明涉及新型磷衍生物，其制备方法，含有它们的药物组合物及其作为药物作为趋化因子受体调节剂的用途。

7. 发明申请

WO2008030843A1 HETEROAROMATIC COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR AGONIST AND/OR ANTAGONIST BIOLOGICAL ACTIVITY 审中-公开
标题翻译：具有丝氨酸1-磷酸（S1P）受体激动剂和/或拮抗剂生物活性的异构体化合物
公开(公告)号：WO2008030843A1
公开(公告)日：2008-03-13
申请号：PCT/US2007/077588
申请日：2007-09-05
申请人： ALLERGAN, INC. , BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , LIU, Xiaoxia
发明人： BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , LIU, Xiaoxia
IPC分类号： C07D213/79 , C07D241/24 , C07D253/07 , C07F9/40 , A61K31/4418 , A61P37/00
CPC分类号： C07D253/07 , C07D213/79 , C07D241/24
摘要： A novel compound having antagonist activity at the S1P3 receptor represented by the formula (I); [C(R 3 ) 2 ] a (W) b [C(R 3 ) 2 ] c [P(O)(OR 3 ) 2 ] d [C(V) x (OR4)y(R 4 ) z ] e wherein X is selected from the group consisting of CR 3 and N; Y is selected from the group consisting of CR 3 and N; Z is selected from the group consisting of CR 3 and N; and at least one of X, Y and Z is N; W is NR 3 or O; V is oxo or represents two H atoms; provided that when V is two H atoms, z is 0; R 1 is an aryl group; R 2 is an aryl group; R 3 is selected from the group consisting of H and alkyl and lower alkyl; R 4 is selected from the group consisting of H and alkyl; and 2 of said R 3 or R 4 may together form a cyclic alkyl ring having from 3 to 6 carbon atoms; a is 0 or an integer of from 1 to 6; b is 0 or 1; c is O or an integer of from 1 to 6; d is 0 or 1; e is 0 or 1; x is 1; y is 0 or an integer of from 1 to 3; z is 0 or an integer of from 1 to 3; provided however that when d is 0, e is 1, and when e is 0, d is 1, and when y is 0, z is 1 and when z is 0, y is 1.
摘要翻译：由式（I）表示的S1P3受体具有拮抗活性的新化合物; [C（R ^{3 ）_{2 ] _{一（W）_{B'/ SUB> [C（R ^{3 < / SUP>）_{2 ] _{C [P（O）（OR ^{3 ）_{2 ] _{ð （OR 4）y（R 4）其中C（V）x（OR 4）y（R 4） X选自CR 3和N; Y选自CR 3和N; Z选自CR 3和N 3; X，Y和Z中的至少一个为N; W是NR 3或O; V是氧代或代表两个H原子; 条件是当V是两个H原子时，z是0; R 1是芳基; R 2是芳基; R 3选自H和烷基和低级烷基; R 4选自H和烷基; 并且所述R 3或R 4的2个可以一起形成具有3至6个碳原子的环状烷基; a为0或1〜6的整数; b为0或1; c为0或1〜6的整数; d为0或1; e为0或1; x为1; y为0或1〜3的整数; z为0或1〜3的整数; 但是当d为0时，e为1，当e为0时，d为1，当y为0时，z为1，z为0时，y为1。}}}}}}}}}}

8. 发明申请

WO2007095561A2 INDOLE-3-CARBOXYLIC ACID AMIDE, ESTER, THIOAMIDE AND THIOL ESTER COMPOUNDS BEARING ARYL OR HETEROARYL GROUPS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY 审中-公开
标题翻译：含有磷脂酰肌醇（S1P）受体拮抗剂生物活性的叶绿体酰胺，酯，硫代酰胺和硫醇酯化合物
公开(公告)号：WO2007095561A2
公开(公告)日：2007-08-23
申请号：PCT/US2007/062106
申请日：2007-02-14
申请人： ALLERGAN, INC. , BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , LIU, Xiaoxia , DUONG, Tien , COLON, Diana, F. , HU, Yihui
发明人： BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , LIU, Xiaoxia , DUONG, Tien , COLON, Diana, F. , HU, Yihui
IPC分类号： C07D209/42 , C07D401/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04
CPC分类号： C07D209/42 , C07D401/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06
摘要： The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1 -phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R 4 , n, A, X, Z, R 1 , o, R 3 , R 2 and p are as defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, and wound healing.
摘要翻译：本发明提供了由式I表示的化合物，其中每一种化合物可具有鞘氨醇-1-磷酸受体激动剂和/或拮抗剂生物活性：并且其中变量Y，R 4，n，A，X ，Z，R 1，O，R 3，R 2和p如说明书中所定义。这些化合物可用于治疗选自青光眼，干眼症，血管发生，心血管疾病和疾病以及伤口愈合的疾病或病症。

9. 发明申请

WO2008030838A3 HETEROAROMATIC COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR AGONIST BIOLOGICAL ACTIVITY 审中-公开
公开(公告)号：WO2008030838A3
公开(公告)日：2008-03-13
申请号：PCT/US2007/077581
申请日：2007-09-05
申请人： ALLERGAN, INC. , BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , LIU, Xiaoxia
发明人： BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , LIU, Xiaoxia
IPC分类号： C07D213/30 , C07D213/50 , C07D213/53 , C07D213/74 , C07D213/79 , C07D213/89 , C07D239/28 , C07D241/12 , C07D241/24 , C07D253/07
摘要： A novel compound having agonist activity at the S 1 P 3 receptor which is represented by the formula (I) wherein X is selected from the group consisting of CR 3 , N and NO; Y is selected from the group consisting of CR 3 , N and NO; Z is selected from the group consisting of CR 3 , N and NO; and at least one of X, Y and Z is N or NO; V is O or NOR 4 R 1 is an aryl group; R 2 is an aryl group; R 3 is selected from the group consisting of H and alkyl; and 2 of said R 3 groups may together form a cyclic alkyl ring having from 3 to 6 carbon atoms; R 4 is selected from the group consisting of H and alkyl; a is 0 or an integer of from 1 to 6; b is 0 or 1; c is 0 or 1; f is 0 or an integer of 1 or 2; x is 0 or 1; y is 0 or an integer of from 1 to 3; and z is 0 or an integer of from 1 to 3.

10. 发明申请

WO2007112322A2 INDOLE COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR AGONIST AND/OR ANTAGONIST BIOLOGICAL ACTIVITY 审中-公开
标题翻译：具有丝氨酸1-磷酸（S1P）受体激动剂和/或拮抗剂生物活性的吲哚化合物
公开(公告)号：WO2007112322A2
公开(公告)日：2007-10-04
申请号：PCT/US2007/064841
申请日：2007-03-23
申请人： ALLERGAN, INC. , BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , VULIGONDA, Vidyasagar , DUONG, Tien, T.
发明人： BEARD, Richard, L. , DONELLO, John, E. , YUAN, Haiqing , VULIGONDA, Vidyasagar , DUONG, Tien, T.
IPC分类号： C07D209/42 , C07D209/12 , C07D209/14 , C07D209/08 , C07D209/30 , C07D209/40 , C07D413/04 , A61K31/404 , A61P27/06
CPC分类号： C07D209/14 , C07D209/12 , C07D209/30 , C07D209/40 , C07D209/42 , C07D405/12 , C07D409/06 , C07D413/04 , C07F9/5728
摘要： The present invention provides novel compounds having the following general formula (I) wherein: A, B, X, Y, R 1 , R 2 , R 3 , R 4 , n, o and p are as defined in the specification. Such compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions or diseases and wound healing.
摘要翻译：本发明提供具有以下通式（I）的新化合物，其中：A，B，X，Y，R 1，R 2，R 3， / SUP>，R 4，n，o和p如说明书中所定义。这样的化合物可用于治疗选自青光眼，干眼症，血管生成，心血管疾病或疾病和伤口愈合的疾病或病症。

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