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    Crystalline Solid Forms of N--N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use
    27.
    发明申请
    Crystalline Solid Forms of N--N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use 审中-公开
    N-N' - （4-氟苯基）环丙烷-1,1-二甲酰胺的结晶固体形式，制备方法和使用方法

    公开(公告)号：US20170044106A1

    公开(公告)日：2017-02-16

    申请号：US15118738

    申请日：2015-02-16

    Applicant: Exelixis, Inc.

    Inventor： Dana T. Aftab ,  Nathan Guz ,  Stephen Lau ,  Noel Hamill ,  Tracy Walker ,  Jana Galbraith ,  Simon Yau ,  Khalid Shah

    IPC: C07D215/233

    CPC classification number: C07D215/233 ,  C07B2200/13 ,  C07D215/22

    Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.

    Abstract translation: 本发明涉及化合物N- {4 - [（6,7-二甲氧基喹啉-4-基）氧基]苯基} -N' - （4-氟苯基）环丙烷-1,1-二甲酰胺（ 化合物1）及其溶剂化物，包括水合物，其可用于治疗癌症。 还公开了包含结晶固体形式和用于制备结晶固体形式的方法的药物组合物，以及其用于治疗癌症，特别是甲状腺癌，前列腺癌，肝细胞癌，肾癌和非小细胞的方法 肺癌。 结晶固体形式可用于制备卡泊沙坦的L-苹果酸盐。

    Method of Treating Lung Adenocarcinoma
    28.
    发明申请
    Method of Treating Lung Adenocarcinoma 审中-公开
    肺腺癌的治疗方法

    公开(公告)号：US20170042880A1

    公开(公告)日：2017-02-16

    申请号：US15305854

    申请日：2015-04-27

    Applicant: Exelixis, Inc.

    Inventor： Dana T. Aftab ,  Peiwen Yu

    IPC: A61K31/47 ,  C12Q1/68

    CPC classification number: A61K31/47 ,  A61K31/337 ,  A61K31/517 ,  A61K31/7068 ,  C12Q1/6886 ,  C12Q2600/158 ,  A61K2300/00

    Abstract: This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with SLC34A2-ROS1, CD74-ROS1, or FIG-ROS1 fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGFR2, and ROS1 which is a compound of Formula (I): or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及治疗患者，特别是患有肺腺癌的患者，特别是患有SLC34A2-ROS1，CD74-ROS1或FIG-ROS1融合阳性非小细胞肺癌的患者，其具有 其为式（I）化合物的MET，VEGFR2和ROS1抑制剂：或其药学上可接受的盐。

    Process for Preparing Quinoline Derivatives
    29.
    发明申请
    Process for Preparing Quinoline Derivatives 有权
    喹啉衍生物的制备方法

    公开(公告)号：US20160229805A1

    公开(公告)日：2016-08-11

    申请号：US15133708

    申请日：2016-04-20

    Applicant: Exelixis, Inc.

    Inventor： Jo Ann Wilson ,  Sriram Naganathan ,  Neil G. Andersen ,  Matthew Pfeiffer

    IPC: C07D215/233 ,  C07C231/02

    CPC classification number: C07D215/233 ,  C07C231/02 ,  C07C233/58 ,  C07C233/59 ,  C07D215/00 ,  C07D239/90

    Abstract: A process for preparing a compound of Formula I is disclosed, comprising the steps: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl; R4 is (C1-C6)alkyl; and Q is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula 1.

    Abstract translation: 公开了制备式I化合物的方法，包括以下步骤：其中：R1为卤素; R2是卤素; R 3是（C 1 -C 6）烷基或任选被杂环烷基取代的（C 1 -C 6）烷基; R4是（C1-C6）烷基; Q为CH或N; 包括：（a）在极性非质子溶剂中将1,1-环丙烷二羧酸与亚硫酰氯接触; （b）向步骤（a）的混合物中加入叔胺碱，形成式A的化合物; 和（c）将式A的化合物与式B的胺偶联以形成式1的化合物。

    Process for preparing quinoline derivatives
    30.
    发明授权
    Process for preparing quinoline derivatives 有权
    制备喹啉衍生物的方法

    公开(公告)号：US09365516B2

    公开(公告)日：2016-06-14

    申请号：US14353251

    申请日：2012-10-22

    Applicant: Exelixis, Inc.

    Inventor： Jo Ann Wilson ,  Sriram Naganathan ,  Neil G. Andersen ,  Matthew Pfeiffer

    IPC: C07D239/72 ,  C07D215/00 ,  C07D215/233 ,  C07D239/90 ,  C07C231/02

    CPC classification number: C07D215/233 ,  C07C231/02 ,  C07C233/58 ,  C07C233/59 ,  C07D215/00 ,  C07D239/90

    Abstract: A process for preparing a compound of Formula I is disclosed: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl; R4 is (C1-C6)alkyl; and Q is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula I.

    Abstract translation: 公开了制备式I化合物的方法：其中：R1为卤素; R2是卤素; R 3是（C 1 -C 6）烷基或任选被杂环烷基取代的（C 1 -C 6）烷基; R4是（C1-C6）烷基; Q为CH或N; 包括：（a）在极性非质子溶剂中将1,1-环丙烷二羧酸与亚硫酰氯接触; （b）向步骤（a）的混合物中加入叔胺碱，形成式A的化合物; 和（c）将式A的化合物与式B的胺偶联以形成式I的化合物。

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