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1. 发明专利

ES2318009T3 ARIL OXIMA-PIPERAZINAS UTILES COMO ANTAGONISTAS DE CCR5. 未知
公开(公告)号：ES2318009T3
公开(公告)日：2009-05-01
申请号：ES02731174
申请日：2002-03-27
申请人： SCHERING CORP
发明人： CLADER JOHN W , LIN SUE-ING Y , MCCOMBIE STUART W , PUSHPAVANAM PRADEEP B , VICE SUSAN
IPC分类号： C07D211/58 , A61K31/496 , A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/04 , C07D401/06 , C07D401/14
摘要： Un compuesto que incluye enantiómeros, estereoisómeros, rotámeros, tautómeros y racematos del citado compuesto y sales o solvatos farmacéuticamente aceptables del citado compuesto que tiene la estructura general mostrada en la fórmula I:** ver fórmula** donde: donde: X se selecciona del grupo que consiste en H; F; Cl; Br; I; -CF 3; -CF 3O; -CN; CH 3SO 2-; y CF 3SO 2-; R 1 es H; alquilo de cadena lineal o alquilo ramificado; un fluoro-alquilo (C1-C6); un alquileno de C1-C6 que lleva un cicloalquilo de C3-C7 (por ejemplo ciclopropilmetilo); -CH2CH2OH; -CH2CH2-O-alquilo(C1-C6), -CH2C(O)- O-alquilo(C1-C6); -CH2C(O)NH2; CH2C(O)-NH-alquilo(C1-C6) ó CH2C(O)-NH(alquilo C1-C6))2; R 2 es H; un alquilo de cadena lineal de C 1-C 6 o un alquilo ramificado; o un alquenilo de C 2-C 6 R 3 es un alquilo de cadena lineal o alquilo ramificado; fenilo sustituido con R 4 , R 5 , R 6 ; heteroarilo de 6 eslabones sustituido con R 4 , R 5 , R 6 , heteroarilo de 6 eslabones sustituido con R 4 , R 5 , R 6 ; N-óxido de heteroarilo de 6 eslabones sustituido con R 4 , R 5 , R 6, heteroarilo de 5 eslabones sustituido con R 7 , R 8 ; naftilo; fluorenilo; difenilmetilo R 4 y R 5 pueden ser iguales o diferentes y se seleccionan independientemente del grupo que consiste en alquilo (C1-C6), halógeno, NR 12 R 13 , -OH, -CF3, -OCH3, -O-acilo, -OCF3 y -Si(CH3)3; R 6 es R 4 ; hidrógeno; fenilo; -NO 2; -CN; -CH 2F; CHF 2; -CHO; -CH=NOR 12 , piridilo, N-óxido de piridilo;N-óxido de piridilo; pirimidinilo; pirazinilo; -N(R 12 )CONR 13 R 14 ; -NHCONH(cloro-alquilo(C1-C6); -NHCONH-cicloalquil (C3-C10)alquilo(C1-C6); -NH-COalquilo(C1-C6), -NHCOCF3, -NHSO2N(alquilo(C1-C6))2, NH-(SO2-alquilo(C1- C6), -N(SO2CF3)2; NHCO2alquilo(C1-C6), cicloalquiloC3-C10, -SR 15 , -SOR 15 , -SO2R 15 ,-SO2NH(alquilo(C1-C6); -OSO 2alquilo(C 1-C 6); -OSO 2CF 3; hidroxi-alquilo(C 1-C 6); -CONR 12 R 13 ; -CON(CH 2CH 2-O-CH 3) 2, -OCONH-alquilo(C 1-C 6); -CO 2R 2 ; -Si(CH 3) 3 ó B (OC(CH 3) 2) 2 R 7 es alquilo (C1-C6), -NH2 ó R 9 -fenilo: R 9 corresponde a 1 a 3 sustituyentes que pueden ser iguales o diferentes y se seleccionan independientemente del grupo que consiste en hidrógeno, alquilo de C1-C6, -CF3, CO2R 12 , -CN, alcoxi de C1-C6 y halógeno; R 10 y R 11 pueden ser iguales o diferentes y se seleccionan, independientemente, del grupo consistente en hidrógeno y alquilo de C 1-C 6, ó R 10 y R 11 juntos son grupo alquileno de C 2-C 5 y con el carbono al que se unen forman un espiro-anillo de 3 a 6 átomos de carbono. R 12 R 13 y R 14 pueden ser iguales o diferentes y se seleccionan independientemente del grupo que consiste en H y alquilo de C1-C6.; y R 15 es alquilo de C1-C6 o fenilo.

2. 发明专利

HK1057211A1 ARYL OXIME-PIPERAZINES USEFUL AS CCR5 ANTAGONISTS 未知
公开(公告)号：HK1057211A1
公开(公告)日：2004-03-19
申请号：HK04100067
申请日：2004-01-06
申请人： SCHERING CORP
发明人： CLADER JOHN W , LIN SUE-ING Y , MCCOMBIE STUART W , PUSHPAVANAM PRADEEP B , VICE SUSAN
IPC分类号： A61K20090101 , A61K31/506 , A61K45/00 , A61P20090101 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D20090101 , C07D401/06 , C07D401/14
摘要： In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor. An illustrative inventive compound is shown below:

3. 发明专利

AU2002303168B2 Aryl oxime-piperazines useful as ccr5 antagonists 未知
公开(公告)号：AU2002303168B2
公开(公告)日：2005-10-06
申请号：AU2002303168
申请日：2002-03-27
申请人： SCHERING CORP
发明人： LIN SUE-ING Y , CLADER JOHN W , MCCOMBIE STUART W , PUSHPAVANAM PRADEEP B , VICE SUSAN
IPC分类号： A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/06 , C07D401/14 , C07D211/58 , A61K031/506 , A61P031/18 , A61K031/496 , C07D401/04
摘要： In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor. An illustrative inventive compound is shown below:

4. 发明专利

CA2526725A1 MCH ANTAGONISTS FOR THE TREATMENT OF OBESITY 未知
公开(公告)号：CA2526725A1
公开(公告)日：2005-01-20
申请号：CA2526725
申请日：2004-06-28
申请人： SCHERING CORP
发明人： PUSHPAVANAM PRADEEP B , CLADER JOHN W , BARA THOMAS A , PALANI ANANDAN , SHAPIRO SHERRY A , JOSIEN HUBERT B , MCBRIAR MARK , LI SHENGJIAN
IPC分类号： C07D409/14 , A61K31/496 , C07D409/06
摘要： The present invention discloses methods of using antagonists for melanin- concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as well as novel compounds whic h are antagonists for melanin-concentrating hormone (MCH). In other aspects, t he invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods for preparing such compounds. Compounds of th e invention generally have the structure of formula (I) where the substituents are as defined herein.

5. 发明专利

DE60230491D1 未知
公开(公告)号：DE60230491D1
公开(公告)日：2009-02-05
申请号：DE60230491
申请日：2002-03-27
申请人： SCHERING CORP
发明人： CLADER JOHN W , LIN SUE-ING Y , MCCOMBIE STUART W , PUSHPAVANAM PRADEEP B , VICE SUSAN
IPC分类号： C07D211/58 , A61K31/496 , A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/04 , C07D401/06 , C07D401/14
摘要： In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor. An illustrative inventive compound is shown below:

6. 发明专利

HU0400389A2 ARYL OXIME-PIPERAZINES USEFUL AS CCR5 ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：HU0400389A2
公开(公告)日：2004-08-30
申请号：HU0400389
申请日：2002-03-27
申请人： SCHERING CORP
发明人： CLADER JOHN W , LIN SUE-ING Y , MCCOMBIE STUART W , PUSHPAVANAM PRADEEP B , VICE SUSAN
IPC分类号： A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/06 , C07D401/14 , C07D211/58
摘要： In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor. An illustrative inventive compound is shown below:

7. 发明专利

CA2442210C ARYL OXIME-PIPERAZINES USEFUL AS CCR5 ANTAGONISTS 未知
公开(公告)号：CA2442210C
公开(公告)日：2009-09-08
申请号：CA2442210
申请日：2002-03-27
申请人： SCHERING CORP
发明人： CLADER JOHN W , LIN SUE-ING Y , VICE SUSAN , PUSHPAVANAM PRADEEP B , MCCOMBIE STUART W
IPC分类号： C07D211/58 , A61K31/496 , A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/04 , C07D401/06 , C07D401/14
摘要： In one embodiment, this invention provides a novel class of aryl oxime- piperazine compounds as antagonists of the CCR5 receptor, methods of prepari ng such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one o r more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor. An illustrative inventive compound is shown below: (Formula I).

8. 发明专利

MY134019A ARYL OXIME-PIPERAZINES USEFUL AS CCR5 ANTAGONISTS 未知
公开(公告)号：MY134019A
公开(公告)日：2007-11-30
申请号：MYPI20021141
申请日：2002-03-28
申请人： SCHERING CORP
发明人： CLADER JOHN W , MCCOMBIE STUART W , LIN SUE-ING Y , PUSHPAVANAM PRADEEP B , VICE SUSAN
IPC分类号： C07D401/04 , A61K31/496 , A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/06 , C07D401/14
摘要： IN ONE EMBODIMENT, THIS INVENTION PROVIDES A NOVEL CLASS OF ARYL OXIME-PIPERAZINE COMPOUNDS AS ANTAGONISTS OF THE CCR5 RECEPTOR, METHODS OF PREPARING SUCH COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING ONE OR MORE OF THE COMPOUNDS. METHODS OF PREPARING PHARMACEUTICAL FORMULATIONS COMPRISING ONE OR MORE SUCH COMPOUNDS, AND METHODS OF TREATMENT, PREVENTION OR AMELIORATION OF ONE OR MORE OF DISEASES ASSOCIATED WITH THE CCR5 RECEPTOR. AN ILLUSTRATIVE INVENTIVE COMPOUNDS IS SHOWN BELOW.

9. 发明专利

ZA200307171B Aryl oxime-piperazines useful as CCR5 antagonists. 未知
公开(公告)号：ZA200307171B
公开(公告)日：2004-12-13
申请号：ZA200307171
申请日：2003-09-12
申请人： SCHERING CORP
发明人： CLADER JOHN W , MCCOMBIE STUART W , VICE SUSAN , LIN SUE-ING Y , PUSHPAVANAM PRADEEP B
IPC分类号： A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/06 , C07D401/14 , C07D , A61K , A61P
摘要： In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor. An illustrative inventive compound is shown below:

10. 发明专利

NZ528011A Aryl oxime-piperazines useful as CCR5 antagonists 未知
公开(公告)号：NZ528011A
公开(公告)日：2004-08-27
申请号：NZ52801102
申请日：2002-03-27
申请人： SCHERING CORP
发明人： CLADER JOHN W , LIN SUE-ING Y , MCCOMBIE STUART W , PUSHPAVANAM PRADEEP B , VICE SUSAN
IPC分类号： A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/06 , C07D401/14 , C07D211/58 , C07D401/04 , A61K31/496
摘要： Aryl oxime-piperazine compounds of formula (I) useful as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds and methods of preparing pharmaceutical formulations comprising one or more such compounds.

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