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    ANTI-CTLA4 ANTIBODY AND INDOLINONE COMBINATION THERAPY FOR TREATMENT OF CANCER
    1.
    发明申请
    ANTI-CTLA4 ANTIBODY AND INDOLINONE COMBINATION THERAPY FOR TREATMENT OF CANCER 审中-公开
    抗CTLA4抗体和吲哚宁酮治疗癌症的组合疗法

    公开(公告)号：WO2006101692A1

    公开(公告)日：2006-09-28

    申请号：PCT/US2006/007651

    申请日：2006-03-03

    Applicant: PFIZER PRODUCTS INC. ,  GOMEZ-NAVARRO, Jesus ,  BAUM, Charles, Michael

    Inventor： GOMEZ-NAVARRO, Jesus ,  BAUM, Charles, Michael

    IPC: A61K39/395 ,  A61P35/00 ,  C07K16/28

    CPC classification number: C07K16/2818 ,  A61K31/404 ,  A61K39/39541 ,  A61K45/06 ,  A61K2039/505 ,  C07K2317/21 ,  A61K2300/00

    Abstract: The invention relates to administration of an anti-CTLA4 antibody, particularly human antibodies to human CTLA4, such as those having amino acid sequences of antibodies 3.1.1 , 4.1.1 , 4.8.1 , 4.10.2, 4.13.1 , 4.14.3, 6.1.1 , ticilimumab (also referred to as 11.2.1 or CP- 675,206), 11.6.1 , 11.7.1 , 12.3.1.1 , 12.9.1.1 , and ipilimumab (also referred to as 10D1 or MDX-010), in combination with an indolinone receptor tyrosine kinase inhibitor (RTKI), e.g., N-[2-diethylamino]ethyl]-5-[(Z)-(5-fluoro-2-oxo-1 ,2-dihydro-3H-indol-3-ylidene)methyl]-2,4- dimethyl-1 H-pyrrole-3-carboxamide (compound 1 ), N-[2-(ethylamino)ethyl]-5-[(Z)-(5-fluoro-2- oxo-1 ,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1 H-pyrrole-3-carboxamide (compound 2), and 5-[(Z)-(5-fluoro-2-oxo-1 ,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2- hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1 H-pyrrole-3-carboxamide (compound 3), for treatment of cancer. The invention relates to administering a combination of an anti-CTLA4 antibody and an indolinone RTKI such as, inter alia, compound 1. The invention relates to neoadjuvant, adjuvant, first-line, second-line, and third-line therapy of cancer, whether localized or metastasized, and at any point(s) along the disease continuum (e.g., at any stage of the cancer).

    Abstract translation: 本发明涉及抗CTLA4抗体，特别是人CTLA4的人抗体的施用，例如具有抗体3.1.1,4.1.1,4.8.1,4.10.2,4.13.1,4.14的氨基酸序列的那些。 3，6.1.1，替尼米单抗（也称11.2.1或CP-675,206），11.6.1,11.7.1,12.3.1.1,12.9.1.1和ipilimumab（也称为10D1或MDX-010） ，与吲哚酮受体酪氨酸激酶抑制剂（RTKI）组合，例如N- [2-二乙基氨基]乙基] -5 - [（Z） - （5-氟-2-氧代-1,2-二氢-3H- 吲哚-3-亚基）甲基] -2,4-二甲基-1H-吡咯-3-甲酰胺（化合物1），N- [2-（乙基氨基）乙基] -5 - [（Z） - （5-氟 -2-氧代-1,2-二氢-3H-吲哚-3-亚基）甲基] -2,4-二甲基-1H-吡咯-3-甲酰胺（化合物2）和5 - [（Z） - （ 5-氟-2-氧代-1,2-二氢-3H-吲哚-3-亚基）甲基] -N - [（2S）-2-羟基-3-吗啉-4-基丙基] -2,4-二甲基 -1H-吡咯-3-甲酰胺（化合物3），用于治疗癌症。 本发明涉及施用抗CTLA4抗体和吲哚啉酮RTKI（尤其是化合物1）的组合。本发明涉及癌症的新辅助剂，佐剂，一线，二线和三线治疗， 无论是局部的还是转移的，以及沿着疾病连续体的任何点（例如，在癌症的任何阶段）。

    USES OF ANTI-CTLA-4 ANTIBODIES
    2.
    发明申请
    USES OF ANTI-CTLA-4 ANTIBODIES 审中-公开
    抗CTLA-4抗体的使用

    公开(公告)号：WO2005092380A2

    公开(公告)日：2005-10-06

    申请号：PCT/IB2005/000671

    申请日：2005-03-14

    Applicant: PFIZER PRODUCTS INC ,  GOMEZ-NAVARRO, Jesus ,  HANSON, Douglas, Charles ,  MUELLER, Eileen, Elliott ,  NOE, Dennis, Alan

    Inventor： GOMEZ-NAVARRO, Jesus ,  HANSON, Douglas, Charles ,  MUELLER, Eileen, Elliott ,  NOE, Dennis, Alan

    IPC: A61K39/395

    CPC classification number: C07K16/2818 ,  A61K9/0019 ,  A61K47/26 ,  A61K2039/505 ,  C07K2317/21 ,  C07K2317/73

    Abstract: The invention relates to treatment of cancer in a mammal who has undergone stem cell transplantation by administering an effective amount of a human anti-CTLA-4 antibody to the mammal. Stem cell transplantation may be allogeneic or autologous stem cell transplantation and may be preceded by a preparatory treatment such as chemotherapy. The methods of the invention may be combined with additional cancer treatments. Further, the invention relates to treatment of cancer using at least 10 mg/kg of a human anti-CTLA-4 antibody, and, more preferably, about 15-20 mg/kg of antibody.

    Abstract translation: 本发明涉及通过向哺乳动物施用有效量的人抗CTLA-4抗体，已经经历了干细胞移植的哺乳动物的癌症治疗。 干细胞移植可以是同种异体或自体干细胞移植，并且之前可以进行诸如化疗的预备治疗。 本发明的方法可以与另外的癌症治疗组合。 此外，本发明涉及使用至少10mg / kg人抗CTLA-4抗体，更优选约15-20mg / kg抗体治疗癌症。

    THERAPY OF PROSTATE CANCER WITH CTLA4 ANTIBODIES AND HORMONAL THERAPY
    3.
    发明申请
    THERAPY OF PROSTATE CANCER WITH CTLA4 ANTIBODIES AND HORMONAL THERAPY 审中-公开
    前列腺癌与CTLA4抗体治疗与HORMONAL THERAPY

    公开(公告)号：WO2006101691A1

    公开(公告)日：2006-09-28

    申请号：PCT/US2006/007650

    申请日：2006-03-03

    Applicant: PFIZER PRODUCTS INC. ,  GOMEZ-NAVARRO, Jesus

    Inventor： GOMEZ-NAVARRO, Jesus

    IPC: A61K39/395 ,  A61K38/09 ,  A61P35/00 ,  C07K16/28

    CPC classification number: C07K16/2818 ,  A61K38/09 ,  A61K39/39541 ,  A61K2039/545 ,  C07K2317/21 ,  A61K2300/00

    Abstract: The invention relates to methods for treating prostate cancer comprising administration of an anti-CTLA4 antibody, or an antigen-binding portion thereof, particularly a human antibody to human CTLA4, e.g., antibody 3.1.1 , 4.1.1 , 4.8.1 , 4.10.2, 4.13.1 , 4.14.3, 6.1.1 , ticilimumab (also known as 11.2.1 ), 11.6.1 , 11.7.1 , 12.3.1.1 , 12.9.1.1 , and ipilimumab (also known as MDX-010 and 10D1 ), in combination with hormonal therapy. Hormonal therapy agents include, inter alia, an anti-androgen (e.g., megestrol, cyproterone, flutamide, nilutamide, and bicalutamide), a GnRH antagonist (e.g., abarelix and histrelin), and a LH-RH agonist (e.g., leuprolide, goserelin, and buserelin). The invention relates to neoadjuvant therapy, adjuvant therapy, therapy for rising PSA, first-line therapy, second-line therapy, and third-line therapy of prostate cancer, whether localized or metastasized.

    Abstract translation: 本发明涉及治疗前列腺癌的方法，包括给予抗CTLA4抗体或其抗原结合部分，特别是对人CTLA4的人抗体，例如抗体3.1.1,4.1.1,4.8.1,4.10 .2,4.13.1,4.14.3,6.1.1，妥米单抗（也称为11.2.1），11.6.1,11.7.1,12.3.1.1,12.9.1.1和ipilimumab（也称为MDX-010 和10D1），结合激素治疗。 激素治疗剂尤其包括抗雄激素（例如，甲孕酮，环丙孕酮，氟他胺，尼鲁米汀和比卡鲁胺），GnRH拮抗剂（例如阿巴瑞克和组氨凝胺）和LH-RH激动剂（例如，亮丙瑞林，戈舍瑞林 和布舍瑞林）。 本发明涉及新辅助治疗，辅助治疗，上升PSA治疗，一线治疗，二线治疗和前列腺癌的三线治疗，无论是局部化还是转移。

    CTLA4 ANTIBODY COMBINATION THERAPY
    4.
    发明申请
    CTLA4 ANTIBODY COMBINATION THERAPY 审中-公开
    CTLA4抗体联合治疗

    公开(公告)号：WO2007113648A3

    公开(公告)日：2008-03-20

    申请号：PCT/IB2007000860

    申请日：2007-03-26

    Applicant: PFIZER PROD INC ,  GOMEZ-NAVARRO JESUS

    Inventor： GOMEZ-NAVARRO JESUS

    IPC: A61K39/395 ,  A61P31/18 ,  A61P35/00 ,  C07K16/28

    CPC classification number: C07K16/2818 ,  A61K39/39541 ,  A61K39/39558 ,  A61K2039/507 ,  C07K16/2887 ,  C07K2317/21 ,  A61K2300/00

    Abstract: The invention relates to administration of an anti-CTLA4 antibody, particularly human antibodies to human CTLA4, such as those having amino acid sequences of antibodies 3.1.1, 4.1.1, 4.8.1, 4.10.2, 4.13.1, 4.14.3, 6.1.1, 11.6.1, 11.7.1, 12.3.1.1, 12.9.1.1, CP-675,206 (11.2.1), and ipilimumab, in combination with a therapeutic agent for treatment of cancer. An exemplary method of the invention comprises administering an anti-CTLA4 antibody, preferably, CP-675,206, and a chemotherapeutic agent, preferably, gemcitabine, for treatment of pancreatic cancer, among other treatment modalities.

    Abstract translation: 本发明涉及抗CTLA4抗体，特别是对人CTLA4的人抗体的施用，例如具有抗体3.1.1,4.1.1,4.8.1,4.10.2,4.13.1,4.14的氨基酸序列的那些。 3，6.1.1,11.6.1,11.7.1,12.3.1.1,12.9.1.1，CP-675,206（11.2.1）和ipilimumab与用于治疗癌症的治疗剂组合。 本发明的示例性方法包括施用抗CTLA4抗体，优选CP-675,206和化学治疗剂，优选吉西他滨，用于治疗胰腺癌以及其它治疗方式。

    CTLA4 ANTIBODY COMBINATION THERAPY
    7.
    发明申请
    CTLA4 ANTIBODY COMBINATION THERAPY 审中-公开
    CTLA4抗体联合治疗

    公开(公告)号：WO2007113648A2

    公开(公告)日：2007-10-11

    申请号：PCT/IB2007/000860

    申请日：2007-03-26

    Applicant: PFIZER PRODUCTS INC. ,  GOMEZ-NAVARRO, Jesus

    Inventor： GOMEZ-NAVARRO, Jesus

    IPC: A61K39/395 ,  C07K16/28 ,  A61P35/00 ,  A61P31/18

    CPC classification number: C07K16/2818 ,  A61K39/39541 ,  A61K39/39558 ,  A61K2039/507 ,  C07K16/2887 ,  C07K2317/21 ,  A61K2300/00

    Abstract: The invention relates to administration of an anti-CTLA4 antibody, particularly human antibodies to human CTLA4, such as those having amino acid sequences of antibodies 3.1.1, 4.1.1, 4.8.1, 4.10.2, 4.13.1, 4.14.3, 6.1.1, 11.6.1, 11.7.1, 12.3.1.1, 12.9.1.1, CP-675,206 (11.2.1), and ipilimumab, in combination with a therapeutic agent for treatment of cancer. An exemplary method of the invention comprises administering an anti-CTLA4 antibody, preferably, CP-675,206, and a chemotherapeutic agent, preferably, gemcitabine, for treatment of pancreatic cancer, among other treatment modalities.

    Abstract translation: 本发明涉及抗CTLA4抗体，特别是对人CTLA4的人抗体的施用，例如具有抗体3.1.1,4.1.1,4.8.1,4.10.2,4.13.1,4.14的氨基酸序列的那些。 3，6.1.1,11.6.1,11.7.1,12.3.1.1,12.9.1.1，CP-675,206（11.2.1）和ipilimumab与用于治疗癌症的治疗剂组合。 本发明的示例性方法包括施用抗CTLA4抗体，优选CP-675,206和化学治疗剂，优选吉西他滨，用于治疗胰腺癌以及其它治疗方式。

    CTLA-4 ANTIBODY AND AROMATASE INHIBITOR OR COMBINATION TREATMENT FOR BREAST CANCER
    8.
    发明申请
    CTLA-4 ANTIBODY AND AROMATASE INHIBITOR OR COMBINATION TREATMENT FOR BREAST CANCER 审中-公开
    CTLA-4抗体和芳香酶抑制剂或组合治疗乳腺癌

    公开(公告)号：WO2006048749A1

    公开(公告)日：2006-05-11

    申请号：PCT/IB2005/003307

    申请日：2005-10-24

    Applicant: PFIZER PRODUCTS INC. ,  GOMEZ-NAVARRO, Jesus

    Inventor： GOMEZ-NAVARRO, Jesus

    IPC: C07K16/28 ,  A61K39/395

    CPC classification number: C07K16/2818 ,  A61K39/39541 ,  A61K2039/505 ,  C07K2317/21 ,  C07K2317/56 ,  A61K2300/00

    Abstract: The invention relates to administration of an anti-CTLA4 antibody, particularly human antibodies to human CTLA4, such as those having amino acid sequences of antibodies 3.1.1, 4.1.1, 4.8.1, 4.10.2, 4.13.1, 4.14.3, 6.1.1, 11.2.1, 11.6.1, 11.7.1, 12.3.1.1, 12.9.1.1, and 10DI (MDX-010), in combination with an aromatase inhibitor, for treatment of breast cancer. More particularly, the invention relates to administration of an anti-CTLA4 antibody and exemestane for treatment of breast cancer.

    Abstract translation: 本发明涉及抗CTLA4抗体，特别是对人CTLA4的人抗体的施用，例如具有抗体3.1.1,4.1.1,4.8.1,4.10.2,4.13.1,4.14的氨基酸序列的那些。 3，6.1.1,11.2.1,11.6.1,11.7.1,12.3.1.1,12.9.1.1和10DI（MDX-010）与芳香酶抑制剂组合用于治疗乳腺癌。 更具体地，本发明涉及用于治疗乳腺癌的抗CTLA4抗体和依西美坦的施用。

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