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1. 发明专利

PL369742A1 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 未知
公开(公告)号：PL369742A1
公开(公告)日：2005-05-02
申请号：PL36974202
申请日：2002-10-15
申请人： GPC BIOTECH INC , GPC BIOTECH AG
发明人： BOCKOVICH NICHOLAS , KLUGE ARTHUR F , RAM SIYA , WANG ZHONGHUO , OALMANN CHRIS , MURTHI KRISHNA K , BECKER FRANK
IPC分类号： A61K31/496 , A61K31/522 , A61K31/5377 , A61K31/675 , A61P17/14 , A61P31/12 , A61P31/18 , A61P35/00 , A61P43/00 , C07D231/54 , C07D403/12 , C07D487/04 , C07F9/6558 , C07F9/6561 , C40B30/04 , G01N33/68 , A61K31/519
摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

2. 发明专利

CA2463571A1 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 未知
公开(公告)号：CA2463571A1
公开(公告)日：2003-04-24
申请号：CA2463571
申请日：2002-10-15
申请人： GPC BIOTECH INC , GPC BIOTECH AG , BECKER FRANK
发明人： KLUGE ARTHUR F , OALMANN CHRIS , RAM SIYA , WANG ZHONGHUO , BOCKOVICH NICHOLAS , MURTHI KRISHNA K , BECKER FRANK
IPC分类号： A61K31/496 , A61K31/522 , A61K31/5377 , A61K31/675 , A61P17/14 , A61P31/12 , A61P31/18 , A61P35/00 , A61P43/00 , C07D231/54 , C07D403/12 , C07D487/04 , C07F9/6558 , C07F9/6561 , C40B30/04 , G01N33/68 , C07D231/00 , C07D239/00 , A61K31/416 , A61K31/519 , C07F9/6503
摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) an d specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell- cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

3. 发明专利

BRPI0715566A2 未知
公开(公告)号：BRPI0715566A2
公开(公告)日：2013-07-02
申请号：BRPI0715566
申请日：2007-10-16
申请人： GPC BIOTECH INC , GPC BIOTECH AG
发明人： MURTHI KRISHNA K , CASAUBON REBECCA , KLUGE ARTHUR F , SMITH CHASE C
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00

4. 发明申请

WO2006002119A3 KINASE INHIBITORS FOR TREATING CANCERS 审中-公开
标题翻译：用于治疗癌症的激酶抑制剂
公开(公告)号：WO2006002119A3
公开(公告)日：2007-02-22
申请号：PCT/US2005021843
申请日：2005-06-17
申请人： GPC BIOTECH INC , CALIGIURI MAUREEN G , KLEY NIKOLAI A , MURTHI KRISHNA K
发明人： CALIGIURI MAUREEN G , KLEY NIKOLAI A , MURTHI KRISHNA K
IPC分类号： A61K31/416 , A61K31/00 , A61P9/10 , A61P25/16 , A61P25/28 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00
CPC分类号： A61K31/00 , A61K31/416 , A61K2300/00
摘要： The invention pertains to inhibitors of various kinases (e.g. S/T kinases, Tyr kinases, etc.), which inhibitors are previously known as cyclin dependent kinase inhibitors (CDKs). As described herein, the inhibitors of this invention are capable of inhibiting various wild-type and mutant form kinases, including drug resistant forms of mutant kinases. Thus the subject kinase inhibitors are useful in treating a wide range of diseases / conditions associated with abnormal functions / excessive activities of the target kinases, including mutant kinases. The invention further provides methods for treating cancers, tumors and patients which are resistant or refractory to other therapeutic agents. Pharmaceutical compositions and packaged pharmaceuticals with instructions of these inhibitors, and methods of using these inhibitors are also provided.
摘要翻译：本发明涉及各种激酶（例如S / T激酶，Tyr激酶等）的抑制剂，该抑制剂先前称为细胞周期蛋白依赖性激酶抑制剂（CDK）。如本文所述，本发明的抑制剂能够抑制各种野生型和突变体形式的激酶，包括耐药形式的突变型激酶。因此，受试激酶抑制剂可用于治疗与靶激酶（包括突变型激酶）的异常功能/过度活性相关的广泛范围的疾病/病症。本发明还提供了治疗对其它治疗剂具有抗性或难治性的癌症，肿瘤和患者的方法。还提供了具有这些抑制剂的说明书的药物组合物和包装药物以及使用这些抑制剂的方法。

5. 发明申请

WO03033499A3 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 审中-公开
标题翻译：环孢素依赖性激酶的抑制剂，组合物和与之相关的用途
公开(公告)号：WO03033499A3
公开(公告)日：2003-08-14
申请号：PCT/US0233052
申请日：2002-10-15
申请人： GPC BIOTECH INC , BOCKOVICH NICHOLAS , KLUGE ARTHUR F , RAM SIYA , WANG ZHONGHUO , OALMANN CHRIS , MURTHI KRISHNA K
发明人： BOCKOVICH NICHOLAS , KLUGE ARTHUR F , RAM SIYA , WANG ZHONGHUO , OALMANN CHRIS , MURTHI KRISHNA K
IPC分类号： A61K31/496 , A61K31/522 , A61K31/5377 , A61K31/675 , A61P17/14 , A61P31/12 , A61P31/18 , A61P35/00 , A61P43/00 , C07D231/54 , C07D403/12 , C07D487/04 , C07F9/6558 , C07F9/6561 , C40B30/04 , G01N33/68 , A61K31/416 , A61K31/519 , C07F9/6503
CPC分类号： C07F9/6561 , C07D231/54 , C07D403/12 , C07D487/04 , C07F9/65583 , C40B30/04 , G01N2500/10
摘要： The invention pertains to novel cyclin dependent kinase inhibitors cdks and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.
摘要翻译：本发明涉及新的细胞周期蛋白依赖性激酶抑制剂cdks，具体而非排他地作为cdk /细胞周期蛋白复合物的抑制剂。如本文所述，本发明的抑制剂能够抑制细胞周期机制，因此可用于调节细胞周期进程，最终控制细胞生长和分化。这样的化合物可用于治疗患有与过度细胞增殖相关的疾病的受试者。

6. 发明申请

WO2004092139A3 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 审中-公开
标题翻译：环孢素依赖性激酶的抑制剂，组合物和与之相关的用途
公开(公告)号：WO2004092139A3
公开(公告)日：2005-03-31
申请号：PCT/US2004010381
申请日：2004-04-06
申请人： GPC BIOTECH INC , BOCKOVICH NICHOLAS , KLUGE ARTHUR , OALMANN CHRIS , MURTHI KRISHNA K , RAM SIYA , WANG ZHONGGUO , HUANG JIANXING
发明人： BOCKOVICH NICHOLAS , KLUGE ARTHUR , OALMANN CHRIS , MURTHI KRISHNA K , RAM SIYA , WANG ZHONGGUO , HUANG JIANXING
IPC分类号： A61P31/12 , A61P35/00 , C07D231/00 , C07F9/6558 , C07F9/6561 , C07D487/04 , A61K31/416 , A61K31/519 , A61K31/675 , C07D231/54 , C07D403/12 , C07D413/12 , C07D519/00
CPC分类号： C07F9/65583 , C07F9/6561
摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) of formulae (II) and (I) wherein the substituents are as defined in the claims and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.
摘要翻译：本发明涉及式（II）和（I）的新型细胞周期蛋白依赖性激酶抑制剂（cdks），其中取代基如权利要求中所定义，具体而非排他地作为cdk /细胞周期蛋白复合物的抑制剂。如本文所述，本发明的抑制剂能够抑制细胞周期机制，因此可用于调节细胞周期进程，最终控制细胞生长和分化。这样的化合物可用于治疗患有与过度细胞增殖相关的疾病的受试者。

7. 发明专利

CA2521854C INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 未知
公开(公告)号：CA2521854C
公开(公告)日：2011-11-01
申请号：CA2521854
申请日：2004-04-06
申请人： GPC BIOTECH INC
发明人： BOCKOVICH NICHOLAS , KLUGE ARTHUR F , OALMANN CHRIS , MURTHI KRISHNA K , RAM SIYA , WANG ZHONGGUO , HUANG JIANXING
IPC分类号： C07D487/04 , A61K31/416 , A61K31/519 , A61K31/675 , A61P31/12 , A61P35/00 , C07D231/00 , C07D231/54 , C07D403/12 , C07D413/12 , C07D519/00 , C07F9/6558 , C07F9/6561
摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) of formulae (II) and (I) wherein the substituents are as defined in the claims and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

8. 发明专利

CA2521854A1 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 未知
公开(公告)号：CA2521854A1
公开(公告)日：2004-10-28
申请号：CA2521854
申请日：2004-04-06
申请人： GPC BIOTECH INC
发明人： MURTHI KRISHNA K , RAM SIYA , OALMANN CHRIS , BOCKOVICH NICHOLAS , KLUGE ARTHUR F , HUANG JIANXING , WANG ZHONGGUO
IPC分类号： A61P31/12 , A61P35/00 , C07D231/00 , C07F9/6558 , C07F9/6561 , C07D487/04 , C07D519/00 , C07D403/12 , C07D413/12 , A61K31/416 , A61K31/519 , C07D231/54 , A61K31/675
摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) of formulae (II) and (I) wherein the substituents are as defined in the claims and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes . As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

9. 发明专利

ES2327840T3 DERIVADOS DE ACIDO ESCUARICO CON ACTIVIDAD ANTIPROLIFERATIVA. 未知
公开(公告)号：ES2327840T3
公开(公告)日：2009-11-04
申请号：ES04030696
申请日：2004-12-23
申请人： GPC BIOTECH AG
发明人： MURTHI KRISHNA K , KOSTLER ROLAND , SMITH CHASE , BRANDSTETTER TILMAN , KLUGE ARTHUR F
IPC分类号： C07D213/74 , A61K31/4406 , A61K31/4409 , A61P35/00 , C07D401/12
摘要： Un compuesto de fórmula general (Ia):** ver fórmula** en la que R1 es 3-piridilo o 4-piridilo; R5 es un resto enlazador seleccionado entre el grupo que consiste en alquileno C2-C10, alquenileno C2-C10, alquinileno C2-C10, -[alquileno C0-C5-(carbociclo)-alquileno C0-C5]- y -[alquileno C0-C6-(heterociclo)-alquileno C0-C5]-, donde el resto enlazador está sustituido con p sustituyentes R9 (donde p es un número entero de 0 a 10); X está ausente o se selecciona entre el grupo que consiste en -O-, -S- y -NH-; R6 es un carbociclo o un heterociclo, donde dicho carbociclo o heterociclo está sustituido con 0-10 sustituyentes R10; cada R9 y R10 se selecciona independientemente entre el grupo que consiste en alquilo, alquenilo, alquinilo, alcoxi, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, haloalquilo, haloalquenilo, haloalquinilo, heterociclilo, heterociclilalquilo, halo, nitro, ciano, hidroxi, amino, carboxi, -OR11, -NHR11, -NR11R12, -C(O)H, -C(O)R11, -OC(O)R11, -C(O) OR11, -C(O)NHR11, -C(O)NR11R12, -S(O)xR11 (donde X es de 0 a 2), -S(O)2OR11, -R13-nitro, -R13-ciano, -R13-hidroxi -R13-amino, -R13-carboxi, -R13-OR11, -R13-NHR11, -R13-NR11R12, -R13-C(O)H, -R13-C(O)R11, -R13-OC(O)R11, -R13- C(O)OR11, -R13-C(O)NHR11, -R13-C(O)NR11R12, -R13-S(O)xR11 (donde X es de 0 a 2), -R13-S(O)2OR11; -O-R13-nitro, -O-R13-ciano, -O-R13-hidroxi, -O-R13-amino, -O-R13-carboxi, -O-R13-OR11, -O-R13-NHR11, -O-R13-NR11R12, -OR13- C(O)H, -O-R13-C(O)R11, -O-R13-OC(O)R11, -O-R13-C(O)OR11, -O-R13-C(O)NHR11, -O-R13-C(O)NR11R12, -OR13- S(O)xR11 (donde X es de 0 a 2), -O-R13-S(O)2OR11; -N(R14)-R13-nitro, -N(R14)-R13-ciano, -N(R14)-R13-hidroxi, -N(R14)-R13-amino, -N(R14)-R13-carboxi, -N(R14)-R13-OR11, -N(R14)-R13-NHR11, -N(R14)-R13-NR11R12, -N(R14)-R13- C(O)H, -N(R14)-R13-C(O)R11, -N(R14)-R13-OC(O)R11, -N(R14)C(O)R11-, -O-R13-N(R14)-C(O)R11-, -N(R14)-R13-C(O) OR11, -N(R14)-R13-C(O)NHR11, -N(R14)-R13-C(O)NR11R12, -N(R14)-R13-S(O)xR11 (donde X es de 0 a 2), -N(R14)-R13- S(O)2OR11, (morfolin-4-il)-alquilo C1-C6 o (morfolin-4-il)-alcoxi C1-C6; cada uno de R11 y R12 de se selecciona independientemente entre el grupo que consiste en alquilo, alquenilo, alquinilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, haloalquilo, haloalquenilo, haloalquinilo, heterociclilo, heterociclilalquilo, o si R11 y R12 están unidos los dos a un átomo de nitrógeno, junto con el átomo de nitrógeno forman un anillo de 5-7 miembros que consiste en carbono y 0-2 heteroátomos adicionales seleccionados entre el grupo que consiste en O, S y N (donde el N se une a un sustituyente adicional seleccionado entre el grupo que consiste en hidrógeno, alquilo, arilo y aralquilo), pudiendo estar el sistema de anillos parcialmente insaturado; cada R13 se selecciona independientemente entre el grupo que consiste en alquileno C1-C6, alquenileno C2-C6 y alquinileno C2-C6; cada R14 se selecciona independientemente entre el grupo que consiste en hidrógeno, alquilo, alquenilo, alquinilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, haloalquilo, haloalquenilo, haloalquinilo, heterociclilo y heterociclilalquilo; o tautómeros del mismo; en forma de un solo estereoisómero o una mezcla de estereoisómeros; o en forma de una sal farmacéuticamente aceptable del mismo.

10. 发明专利

NO20063186A 未知
公开(公告)号：NO20063186A
公开(公告)日：2006-09-20
申请号：NO20063186
申请日：2006-07-10
申请人： GPC BIOTECH INC
发明人： BOCKOVICH NICHOLAS , KLUGE ARTHUR , MURTHI KRISHNA K , RAM SIYA , HUANG JIANXING , OALMANN CHRIS , WANG ZHONGGUO
IPC分类号： C07D231/54 , C07D403/12 , C07D413/12 , C07D487/04 , C07F9/6561
CPC分类号： C07F9/6561

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