公开(公告)号：US08889670B2

公开(公告)日：2014-11-18

申请号：US13147432

申请日：2010-02-16

Applicant: Alessandra Bartolozzi ,  Angela Berry ,  Pier Francesco Cirillo ,  Eugene Richard Hickey ,  Doris Riether ,  Lifen Wu ,  Renee M. Zindell

Inventor： Alessandra Bartolozzi ,  Angela Berry ,  Pier Francesco Cirillo ,  Eugene Richard Hickey ,  Doris Riether ,  Lifen Wu ,  Renee M. Zindell

IPC: A61K31/4545 ,  C07D211/60 ,  C07D401/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D413/12 ,  C07D211/60 ,  C07D401/12 ,  C07D405/04 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract translation: 公开了调节CB2受体的化合物。 根据本发明的化合物与CB2受体结合并且是激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。

公开(公告)号：US08299111B2

公开(公告)日：2012-10-30

申请号：US12956322

申请日：2010-11-30

Applicant: Angela Berry ,  Pier Francesco Cirillo ,  Eugene Richard Hickey ,  Doris Riether ,  David S. Thomson ,  Monika Ermann ,  James Edward Jenkins ,  Innocent Mushi ,  Christopher Francis Palmer ,  Nigel Blumire

Inventor： Angela Berry ,  Pier Francesco Cirillo ,  Eugene Richard Hickey ,  Doris Riether ,  David S. Thomson ,  Monika Ermann ,  James Edward Jenkins ,  Innocent Mushi ,  Christopher Francis Palmer ,  Nigel Blumire

IPC: A61K31/415 ,  C07D231/10

CPC classification number: C07D261/14 ,  C07C317/44 ,  C07D213/75 ,  C07D215/38 ,  C07D217/22 ,  C07D231/40 ,  C07D233/88 ,  C07D235/30 ,  C07D249/14 ,  C07D261/20 ,  C07D263/28 ,  C07D263/58 ,  C07D271/07 ,  C07D271/113 ,  C07D277/46 ,  C07D277/56 ,  C07D277/60 ,  C07D277/82 ,  C07D285/08 ,  C07D285/135 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract translation: 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。

公开(公告)号：US20110071127A1

公开(公告)日：2011-03-24

申请号：US12956322

申请日：2010-11-30

Applicant: Angela BERRY ,  Pier Francesco CIRILLO ,  Eugene Richard HICKEY ,  Doris RIETHER ,  David THOMSON ,  Monika ERMANN ,  James Edward JENKINS ,  Innocent MUSHI ,  Malcolm TAYLOR ,  Chandana CHOWDHURY ,  Christopher Francis PALMER ,  Nigel BLUMIRE

Inventor： Angela BERRY ,  Pier Francesco CIRILLO ,  Eugene Richard HICKEY ,  Doris RIETHER ,  David THOMSON ,  Monika ERMANN ,  James Edward JENKINS ,  Innocent MUSHI ,  Malcolm TAYLOR ,  Chandana CHOWDHURY ,  Christopher Francis PALMER ,  Nigel BLUMIRE

IPC: A61K31/5377 ,  C07D261/14 ,  A61K31/42 ,  C07D213/70 ,  A61K31/4402 ,  C07C321/28 ,  A61K31/216 ,  C07D277/36 ,  A61K31/426 ,  C07D413/12 ,  A61K31/4439 ,  C07D309/08 ,  A61K31/351 ,  C07D417/14 ,  C07D413/14 ,  A61P29/00 ,  A61P1/00 ,  A61P25/28 ,  A61P35/00 ,  A61P37/06

CPC classification number: C07D261/14 ,  C07C317/44 ,  C07D213/75 ,  C07D215/38 ,  C07D217/22 ,  C07D231/40 ,  C07D233/88 ,  C07D235/30 ,  C07D249/14 ,  C07D261/20 ,  C07D263/28 ,  C07D263/58 ,  C07D271/07 ,  C07D271/113 ,  C07D277/46 ,  C07D277/56 ,  C07D277/60 ,  C07D277/82 ,  C07D285/08 ,  C07D285/135 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract translation: 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。

公开(公告)号：US07279475B2

公开(公告)日：2007-10-09

申请号：US10940898

申请日：2004-09-14

Applicant: Pier Francesco Cirillo ,  Abdelhakim Hammach ,  Victor Kamhi ,  Neil Moss ,  Paul S Riska ,  Christopher Pargellis

Inventor： Pier Francesco Cirillo ,  Abdelhakim Hammach ,  Victor Kamhi ,  Neil Moss ,  Paul S Riska ,  Christopher Pargellis

IPC: A61K31/5377 ,  A61K31/496 ,  C07D413/06 ,  C07D403/06

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D239/34 ,  C07D239/47 ,  C07D239/52 ,  C07D401/12 ,  C07D405/12

Abstract: Disclosed are compounds of formula(I): wherein R1, R2, W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.

Abstract translation: 公开了式（I）的化合物：其中式（I）的R 1，R 2，W和X如本文所定义。 该化合物抑制涉及炎症过程的细胞因子的产生，因此可用于治疗涉及诸如慢性炎性疾病的炎症的疾病和病理状况。 还公开了制备这些化合物的方法和包含这些化合物的药物组合物。

公开(公告)号：US06720321B2

公开(公告)日：2004-04-13

申请号：US10154535

申请日：2002-05-24

Applicant: Pier Francesco Cirillo ,  Eugene R. Hickey

Inventor： Pier Francesco Cirillo ,  Eugene R. Hickey

IPC: A61K315355

CPC classification number: C07D213/64 ,  C07D213/36 ,  C07D213/68 ,  C07D213/70 ,  C07D213/81 ,  C07D239/34 ,  C07D239/47 ,  C07D239/52 ,  C07D251/46 ,  C07D295/088 ,  C07D295/13 ,  C07D309/38 ,  C07D401/06

Abstract: Disclosed are compounds of the formula (I) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein n, X, A, L, J, p, Q, Y and z are described herein.

Abstract translation: 公开了下述式（I）的化合物，其作为抗炎剂是有活性的。 还公开了使用和制备这种化合物的方法。其中n，X，A，L，J，p，Q，Y和z在本文中描述。

公开(公告)号：US20080312185A1

公开(公告)日：2008-12-18

申请号：US12191561

申请日：2008-08-14

Applicant: Zhidong Chen ,  Pier Francesco Cirillo ,  Darren DiSalvo ,  Weimin Liu ,  Daniel Richard Marshall ,  Lifen Wu ,  Erick Richard Roush Young

Inventor： Zhidong Chen ,  Pier Francesco Cirillo ,  Darren DiSalvo ,  Weimin Liu ,  Daniel Richard Marshall ,  Lifen Wu ,  Erick Richard Roush Young

IPC: A61K31/695 ,  A61K31/4365 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D495/04

Abstract: Disclosed are methods of treating cancer by administration of compounds according to formula (I): wherein the variables R1, R2, R3 and Z are described herein.

Abstract translation: 公开了通过给予根据式（I）的化合物治疗癌症的方法：其中本文描述了变量R1，R2，R3和Z。

公开(公告)号：US07335657B2

公开(公告)日：2008-02-26

申请号：US11426603

申请日：2006-06-27

Applicant: Pier Francesco Cirillo ,  Donghong Amy Gao ,  Daniel R. Goldberg ,  Abdelhakim Hammach ,  Ming-Hong Hao ,  Victor Marc Kamhi ,  Neil Moss ,  Matthew Russell Netherton ,  Kevin Chungeng Qian ,  Mark Stephen Ralph ,  Lifen Wu ,  Zhaoming Xiong ,  Ronald A. Aungst, Jr.

Inventor： Pier Francesco Cirillo ,  Donghong Amy Gao ,  Daniel R. Goldberg ,  Abdelhakim Hammach ,  Ming-Hong Hao ,  Victor Marc Kamhi ,  Neil Moss ,  Matthew Russell Netherton ,  Kevin Chungeng Qian ,  Mark Stephen Ralph ,  Lifen Wu ,  Zhaoming Xiong ,  Ronald A. Aungst, Jr.

IPC: A61K31/50 ,  A61K43/54 ,  C07D239/02

CPC classification number: C07D401/12 ,  C07D403/12

Abstract: Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.

Abstract translation: 公开了式（I）的化合物，其中Ar 1，X，Y，Q，W，R 3，R 4，R SUP > 5，R 6和R y在本文中定义。 本发明的化合物抑制涉及炎症过程的细胞因子的产生，因此可用于治疗涉及诸如慢性炎性疾病的炎症的疾病和病理状况。 该化合物也可用于治疗与肿瘤学和抗凝血剂或纤维蛋白溶解疗法有关的疾病或病症。 还公开了制备这些化合物的方法和包含这些化合物的药物组合物。

公开(公告)号：US06872726B2

公开(公告)日：2005-03-29

申请号：US10632998

申请日：2003-08-01

Applicant: Pier Francesco Cirillo ,  Abdelhakim Hammach ,  Victor Kamhi ,  Neil Moss ,  Paul S. Riska ,  Christopher Pargellis

Inventor： Pier Francesco Cirillo ,  Abdelhakim Hammach ,  Victor Kamhi ,  Neil Moss ,  Paul S. Riska ,  Christopher Pargellis

IPC: C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D401/12 ,  C07D405/12 ,  C07D521/00 ,  A61K31/505 ,  C07D239/24

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D239/34 ,  C07D239/47 ,  C07D239/52 ,  C07D401/12 ,  C07D405/12

Abstract: Disclosed are compounds of formula (I): wherein R1, R2, W and X of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.

Abstract translation: 公开了式（I）的化合物：其中式（I）的R 1，R 2，W和X在本文中定义。 该化合物抑制涉及炎症过程的细胞因子的产生，因此可用于治疗涉及诸如慢性炎性疾病的炎症的疾病和病理状况。 还公开了制备这些化合物的方法和包含这些化合物的药物组合物。

公开(公告)号：US06743788B2

公开(公告)日：2004-06-01

申请号：US10147675

申请日：2002-05-17

Applicant: Pier Francesco Cirillo ,  Victor Kamhi ,  John Robinson Regan ,  Michele Tsang

Inventor： Pier Francesco Cirillo ,  Victor Kamhi ,  John Robinson Regan ,  Michele Tsang

IPC: C07D41314

CPC classification number: C07D207/08 ,  C07C275/40 ,  C07D213/38 ,  C07D239/26 ,  C07D239/28 ,  C07D241/24 ,  C07D295/135 ,  C07D295/185 ,  C07D295/192 ,  C07D307/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract translation: 公开了本文所述的式（I）的新型芳族化合物，其中G，E，W，Ar，X，Y和Z在本文中公开。 该化合物可用于治疗细胞因子介导的疾病或病症如慢性炎性疾病。 还公开了含有制备这些化合物的药物组合物。

公开(公告)号：US06525046B1

公开(公告)日：2003-02-25

申请号：US10165372

申请日：2002-06-07

Applicant: Pier Francesco Cirillo ,  Roger Dinallo ,  John Robinson Regan ,  Paul S. Riska ,  Alan David Swinamer ,  Zhulin Tan ,  Brian Andrew Walter

Inventor： Pier Francesco Cirillo ,  Roger Dinallo ,  John Robinson Regan ,  Paul S. Riska ,  Alan David Swinamer ,  Zhulin Tan ,  Brian Andrew Walter

IPC: A61K315377

CPC classification number: C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.