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1. 发明专利

JP2011079857A Gonadotropin-releasing hormone receptor antagonist and method relating thereto 审中-公开
标题翻译：促性腺激素释放激素受体拮抗剂及其相关方法
公开(公告)号：JP2011079857A
公开(公告)日：2011-04-21
申请号：JP2010274139
申请日：2010-12-08
申请人： Neurocrine Biosciences Inc , ニューロクラインバイオサイエンシーズ,インコーポレイテッド
发明人： HUANG CHARLES Q , CHEN CHEN , CHEN YONGSHENG , GUO ZHIQIANG , WADE WARREN , ROWBOTTOM MARTIN , RUETER JAIMIE K
IPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P5/06 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/08 , A61P17/14 , A61P25/20 , A61P35/00 , A61P43/00 , C07D239/54 , C07D403/06 , C07D403/12
CPC分类号： C07D239/54 , C07D403/12
摘要： PROBLEM TO BE SOLVED: To provide GnRH (gonadotropin-releasing hormone) receptor antagonists that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. SOLUTION: There are provided pharmaceutical compositions containing a compound having a structure of formula (I), stereoisomers, prodrugs or pharmaceutically acceptable salts thereof. In formula (I), n is 0 or 1; and R 1a , R 1b , R 1c , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 and X represent substituents. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供可用于治疗男性和女性各种性激素相关病症的GnRH（促性腺激素释放激素）受体拮抗剂。提供了含有具有式（I）结构的化合物，立体异构体，前药或其药学上可接受的盐的药物组合物。在式（I）中，n为0或1; R＆lt; SB＆gt; 1a＆lt; /＆gt;，R＆lt; SB＆gt; 1b＆lt; / SB＆gt;，R＆lt; SB＆lt; 1＆lt; SB＆gt; R SB 3，R SB 3，R SB 5，SB SB 6，X代表取代基。版权所有（C）2011，JPO＆INPIT

2. 发明专利

JP2011088903A Pyrimidine-2,4-dione derivative as gonadotropin releasing hormone receptor antagonist 审中-公开
标题翻译：哌嗪-2,4-二酮衍生物作为甘油磷酸盐释放激素受体拮抗剂
公开(公告)号：JP2011088903A
公开(公告)日：2011-05-06
申请号：JP2010265832
申请日：2010-11-29
申请人： Neurocrine Biosciences Inc , ニューロクラインバイオサイエンシーズ,インコーポレイテッド
发明人： ZHU YUN-FEI , REGAN COLLIN , RUETER JAIMIE K , GUO ZHIQIANG , CHEN YONGSHENG , HUANG CHARLES Q
IPC分类号： C07D239/54 , A61K31/513 , A61P5/02 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/08 , A61P25/20 , A61P35/00 , A61P37/02 , A61P43/00 , C07D401/06
CPC分类号： C07D239/54 , C07D401/06
摘要： PROBLEM TO BE SOLVED: To provide a gonadotropin releasing hormone (GnRH) receptor antagonist, a method for preparing the same, a method for using the same, and a pharmaceutical composition containing the compound. SOLUTION: The GnRH receptor antagonist has utility in the treatment of a variety of sex-hormone related conditions in both men and women, and is a compound represented by structural formula (I), or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供促性腺激素释放激素（GnRH）受体拮抗剂，其制备方法，其使用方法和含有该化合物的药物组合物。解决方案：GnRH受体拮抗剂可用于治疗男性和女性各种性激素相关病症，并且是由结构式（I）表示的化合物，或立体异构体，前药或药学上可接受的盐它们。版权所有（C）2011，JPO＆INPIT

3. 发明申请

WO2007084914A3 PHENOXY-SUBSTITUTED PYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为腺苷受体拮抗剂的苯氧基取代的吡咯烷
公开(公告)号：WO2007084914A3
公开(公告)日：2007-10-04
申请号：PCT/US2007060632
申请日：2007-01-17
申请人： NEUROCRINE BIOSCIENCES INC , ALMIRALL LAB , SLEE DEBORAH , ZHANG XIAOHU , RUETER JAIMIE K , LIN EMILY , CRESPO CRESPO MARIA ISABEL , CASTRO PALOMINO LARIA JULIO CE
发明人： SLEE DEBORAH , ZHANG XIAOHU , RUETER JAIMIE K , LIN EMILY , CRESPO CRESPO MARIA ISABEL , CASTRO PALOMINO LARIA JULIO CE
IPC分类号： C07D407/14 , A61K31/506 , A61P25/16 , C07D417/14
CPC分类号： C07D405/14 , C07D417/14
摘要： Compounds of formula (I), including pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, m and n are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
摘要翻译：其中R 1，R 2，R 3，R 3，R 3，R 3， R 4，R 4，R 5，X，m和n如本文所定义。还公开了含有结构（I）化合物的药物组合物，以及与其使用有关的方法。

4. 发明专利

ES2387495T3 Arilpirimidinas útiles en el tratamiento de trastornos relacionados con las hormonas sexuales, tales como endometriosis, cáncer de próstata y similares 未知
公开(公告)号：ES2387495T3
公开(公告)日：2012-09-25
申请号：ES04756667
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： HUANG CHARLES Q , CHEN CHEN , CHEN YONGSHENG , GUO ZHIQIANG , WADE WARREN , ROWBOTTOM MARTIN , RUETER JAIMIE K
IPC分类号： C07D239/54 , A61K31/513 , A61P5/06 , C07D207/00 , C07D239/00 , C07D241/00 , C07D403/12
摘要： Compuesto que tiene la estructura siguiente:**Fórmula**o un estereoisómero, profármaco o sal farmacéuticamente aceptable del mismo, en el que:n es 0 o 1;R1a, R1b, R1c son iguales o diferentes y significan, independientemente, hidrógeno, halógeno, alquilo o alcoxi C1-4, oR1a y R1b, juntos, forman -OCH2O- o -OCH2CH2-;R2a y R2b son iguales o diferentes y significan, independientemente, hidrógeno, halógeno, trifluorometilo, ciano o -SO2CH3-;R3 es hidrógeno o metilo;R4 es fenilo o alquilo C3-7;R5 es hidrógeno o alquilo C1-4;R6 es -NR7R8;R7 y R8 son iguales o diferentes y significan, independientemente, hidrógeno o alquilo C1-4, opcionalmente sustituidocon 1-2 hidroxi o alcoxi;o R7 y R8 y el átomo de nitrógeno al que están unidos forman heterociclos o heterociclo sustituido;o R7 y el átomo de nitrógeno al que está unido, conjuntamente con R5 y el átomo de nitrógeno al que está unidoforman piperazina, homopiperazina u homopiperazina sustituida;o R7 y el átomo de nitrógeno al que está unido, conjuntamente con 1 o más átomos de carbono de alcanodiilo C1-6 deX forma heterociclo o heterociclo sustituido; yX es alcanodiilo C1-6, opcionalmente sustituido con 1 hasta 3 grupos alquilo C1-4,en donde "heterociclo" significa un anillo heterocíclico monocíclico de 4 a 7 miembros, o bicíclico de 7 a 10 miembros,que es saturado, insaturado o aromático, y que contiene de 1 a 4 heteroátomos seleccionados independientementede nitrógeno, oxígeno y azufre, y en donde los heteroátomos de nitrógeno y azufre pueden estar opcionalmenteoxidados, y el heteroátomo de nitrógeno puede estar opcionalmente cuaternizado, incluyendo anillos bicíclicos en losque cualquiera de los heterociclos anteriores está fusionado con un anillo de benceno, y el término "sustituido", comose usa en este documento, significa cualquiera de los grupos anteriores (es decir, alquilo, heterociclo y/o piperazina),en donde al menos un átomo de hidrógeno está sustituido con un sustituyente, en donde en el caso de unsustituyente ceto ("-C(>=O)-") los átomos de hidrógeno sustituidos son dos, en donde los "sustituyentes" dentro delcontexto de esta invención se seleccionan entre halógeno, hidroxi, ciano, nitro, amino, alquilamino, dialquilamino,alquilo, alcoxi, alquiltio, haloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclo y heterociclo-alquilo, asícomo -NRaRb, -NRaC(>=O)Rb, -NRaC(>=O)ORb, -NRaSO2Rb, -C(>=O)Ra, -C(>=O)NRaRb, -ORa, -SRa, -S(>=O)2Ra, -OS(>=O)2Ra y -S(>=O)2ORa, en donde los sustituyentes anteriores pueden estar sustituidos adicionalmentecon uno o más de los sustituyentes anteriores, y en donde Ra y Rb pueden ser iguales o diferentes, y representan independientemente hidrógeno, alquilo, haloalquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilosustituido, heterociclo, heterociclo sustituido, heterociclo-alquilo o heterociclo-alquilo sustituido.

5. 发明专利

CA2531507C PYRIMIDINE-2,4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2531507C
公开(公告)日：2013-10-01
申请号：CA2531507
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , REGAN COLLIN , RUETER JAIMIE K , GUO ZHIQIANG , CHEN YONGSHENG , HUANG CHARLES Q
IPC分类号： C07D239/54 , A61K31/506 , A61K31/513 , A61P5/02 , A61P5/04 , C07D401/06
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure formula (I) wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

6. 发明专利

DE602004020638D1 未知
公开(公告)号：DE602004020638D1
公开(公告)日：2009-05-28
申请号：DE602004020638
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , REGAN COLLIN , RUETER JAIMIE K , GUO ZHIQIANG , CHEN YONGSHENG , HUANG CHARLES Q
IPC分类号： A61K31/513 , A61P5/02 , C07D239/54 , C07D401/06
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R 1a , R 1b , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 , R 7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

7. 发明专利

CA2531507A1 PYRIMIDINE-2,4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2531507A1
公开(公告)日：2005-01-27
申请号：CA2531507
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： HUANG CHARLES Q , ZHU YUN-FEI , REGAN COLLIN , RUETER JAIMIE K , GUO ZHIQIANG , CHEN YONGSHENG
IPC分类号： A61K31/513 , A61P5/02 , C07D239/54 , C07D401/06
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment o f a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure formula (I) wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

8. 发明专利

AU2004257636A1 Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists 未知
公开(公告)号：AU2004257636A1
公开(公告)日：2005-01-27
申请号：AU2004257636
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： HUANG CHARLES Q , RUETER JAIMIE K , CHEN YONGSHENG , REGAN COLLIN , ZHU YUN-FEI , GUO ZHIQIANG
IPC分类号： A61K31/513 , A61P5/02 , C07D239/54 , C07D401/06
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R 1a , R 1b , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 , R 7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

9. 发明专利

AU2004257636B2 Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists 未知
公开(公告)号：AU2004257636B2
公开(公告)日：2011-01-06
申请号：AU2004257636
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： HUANG CHARLES Q , RUETER JAIMIE K , CHEN YONGSHENG , REGAN COLLIN , ZHU YUN-FEI , GUO ZHIQIANG
IPC分类号： C07D239/54 , A61K31/495 , A61P5/02 , C07D401/06
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R 1a , R 1b , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 , R 7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

10. 发明专利

MXPA06000300A DERIVADOS DE PIRIMIDINA-2,4-DIONA COMO ANTAGONISTAS DEL RECEPTOR DE LA HORMONA DE LIBERACION DE GONADOTROPINA. 未知
公开(公告)号：MXPA06000300A
公开(公告)日：2006-03-28
申请号：MXPA06000300
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： RUETER JAIMIE K
IPC分类号： A61P5/02 , C07D239/54 , C07D401/06 , A61K31/513
摘要： Se describen antagonistas del receptor de GnRH que tienen utilidad en el tratamiento de una variedad de condiciones que se relacionan con la hormona sexual tanto en hombres como en mujeres; los compuestos de esta invencion tienen la formula estructural (I): en donde R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 y X son como se definen en la presente, incluyendo estereoisomeros, profarmacos y sales farmaceuticamente aceptables de los mismos; tambien se describen composiciones que contienen un compuesto de esta invencion en combinacion con un portador farmaceuticamente aceptable, asi como metodos que se relacionan con el uso del mismo para antagonizar la hormona de liberacion de gonadotropina en un sujeto en necesidad de esto.

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