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    Substituted aromatic compounds and related method for the treatment of fibrosis
    1.
    发明授权
    Substituted aromatic compounds and related method for the treatment of fibrosis 有权

    公开(公告)号：US10023518B2

    公开(公告)日：2018-07-17

    申请号：US14776328

    申请日：2014-03-14

    申请人： PROMETIC BIOSCIENCES INC.

    发明人： Boulos Zacharie ,  Shaun Abbott ,  Lyne Gagnon ,  Pierre Laurin ,  Brigitte Grouix

    IPC分类号： C07C53/134 ,  A61K31/192 ,  C07C59/52 ,  C07C57/30 ,  C07C57/58

    摘要： The present invention relates to compounds of: or a pharmaceutically acceptable salt thereof, wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R1 is H, F or OH; R2 is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R3 is H, F, OH or CH2Ph; R4 is H, F or OH; Q is 1) (CH2)mC(O)OH wherein m is 1 or 2, 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH, or 6) C(O)—C(O)OH; and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.

    METHOD FOR THE PREPARATION OF TRIGLYCERIDES OF MEDIUM-CHAIN LENGTH FATTY ACIDS
    7.
    发明申请
    METHOD FOR THE PREPARATION OF TRIGLYCERIDES OF MEDIUM-CHAIN LENGTH FATTY ACIDS 有权
    中链长链脂肪酸螯合物的制备方法

    公开(公告)号：US20150018295A1

    公开(公告)日：2015-01-15

    申请号：US14382080

    申请日：2013-02-28

    申请人： PROMETIC BIOSCIENCES INC.

    发明人： Zacharie Boulos ,  Jean-Simon Duceppe ,  Christopher Penney

    IPC分类号： C07C67/08 ,  A61K47/14 ,  A61K45/06 ,  A61K31/23

    CPC分类号： C07C67/08 ,  A61K31/225 ,  A61K31/23 ,  A61K31/337 ,  A61K31/513 ,  A61K31/675 ,  A61K31/704 ,  A61K31/7068 ,  A61K45/06 ,  A61K47/14 ,  C11C3/02 ,  C11C3/025 ,  A61K2300/00

    摘要： A method is disclosed for the preparation of glycerol esters (triglycerides) of medium-chain length monocarboxylic fatty acids which consists of the reaction of the precursor free fatty acid and glycerol in the presence of a catalyst under partial vacuum. The process preferably uses a metal catalyst such as an oxide or a chloride of tungsten, molybdenum, calcium, zinc, chromium or magnesium. The method of the invention allows the preparation in high yield and high purity (>99.5%) of the final triglyceride. The present method allows the formation of triglycerides without solvent. Are also contemplated, the triglyceride obtained by the method, and the pharmaceutical composition containing the triglyceride as an excipient or as an active ingredient.

    摘要翻译： 公开了用于制备中链长度单羧酸脂肪酸的甘油酯（甘油三酯）的方法，其由部分真空下在催化剂存在下前体游离脂肪酸和甘油的反应组成。 该方法优选使用金属催化剂，例如钨，钼，钙，锌，铬或镁的氧化物或氯化物。 本发明的方法允许以高产率和高纯度（> 99.5％）制备最终甘油三酯。 本方法允许无溶剂形成甘油三酯。 还考虑了通过该方法获得的甘油三酯和含有甘油三酸酯作为赋形剂或作为活性成分的药物组合物。

    Substituted Aromatic Compounds and Related Method for the Treatment of Fibrosis
    9.
    发明申请
    Substituted Aromatic Compounds and Related Method for the Treatment of Fibrosis 有权
    取代芳香族化合物及相关方法治疗纤维化

    公开(公告)号：US20160039736A1

    公开(公告)日：2016-02-11

    申请号：US14776328

    申请日：2014-03-14

    申请人： PROMETIC BIOSCIENCES INC.

    发明人： Boulos ZACHARIE ,  Shaun ABBOTT ,  Lyne GAGNON ,  Pierre LAURIN ,  Brigitte GROUIX

    IPC分类号： C07C53/134

    CPC分类号： C07C53/134 ,  A61K31/192 ,  C07C57/30 ,  C07C57/58 ,  C07C59/52 ,  Y02A50/423

    摘要： The present invention relates to compounds of: or a pharmaceutically acceptable salt thereof, wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(0)-(CH2)n-CH3 or CH(OH)—(CH2)n-CH3 wherein n is 3 or 4; R1 is H, F or OH; R2 is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(0)-(CH2)n-CH3 or CH(OH)—(CH2)n-CH3 wherein n is 3 or 4; R3 is H, F, OH or CH2Ph; R4 is H, F or OH; Q is 1) (CH2)mC(0)OH wherein m is 1 or 2, 2) CH(CH3)C(0)OH, 3) C(CH3)2C(0)OH, 4) CH(F)—C(0)OH, 5) CF2-C(0)OH, or 6) C(0)-C(0)OH; and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.

    摘要翻译： 本发明涉及以下化合物：或其药学上可接受的盐，其中A为C5烷基，C6烷基，C5烯基，C6烯基，C（O） - （CH2）n-CH3或CH（OH） - （CH2） n-CH 3，其中n为3或4; R1是H，F或OH; R 2是C 5烷基，C 6烷基，C 5烯基，C 6烯基，C（O） - （CH 2）n -CH 3或CH（OH） - （CH 2）n -CH 3，其中n是3或4; R3是H，F，OH或CH2Ph; R4是H，F或OH; Q是1）（CH 2）m C（O）OH，其中m是1或2，2）CH（CH 3）C（O）OH，3）C（CH 3）2 C（O）OH，4）CH（F） C（O）OH，5）CF 2 -C（O）OH或6）C（O）-C（O）OH; 包含其的组合物和使用其的方法用于预防或治疗受试者中的各种纤维化疾病和病症，包括肺纤维化，肝纤维化，皮肤纤维化，肾纤维化，胰腺纤维化，系统性硬化，心脏纤维化或黄斑变性。

    COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CANCER
    10.
    发明申请
    COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CANCER 有权
    化合物和组合物治疗癌症

    公开(公告)号：US20150313856A1

    公开(公告)日：2015-11-05

    申请号：US14797957

    申请日：2015-07-13

    申请人： PROMETIC BIOSCIENCES, INC.

    发明人： Lyne GAGNON ,  Brigitte GROUIX ,  Lilianne GEERTS ,  Pierre LAURIN ,  Christopher PENNEY ,  Boulos ZACHARIE

    IPC分类号： A61K31/192 ,  A61K31/196 ,  A61K31/7068

    CPC分类号： A61K31/192 ,  A61K31/196 ,  A61K31/22 ,  A61K31/513 ,  A61K31/675 ,  A61K31/7068 ,  C07C57/46 ,  C07C57/48 ,  C07C59/54 ,  C07C59/84 ,  C07C62/20 ,  C07C229/18 ,  C07C229/42 ,  C07C323/52

    摘要： New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.

    摘要翻译： 苯甲酮羧酸酯化合物和式I，式I.1，式I.2，式IA，式IB，式IC和式II的取代芳族化合物及其用于治疗癌症的药学上可接受的盐的新用途。 描述了这些化合物中的两种的组合的使用，并且使用这些化合物之一与抗癌剂如脱巴嗪，多柔比星，柔红霉素，环磷酰胺，总胆固醇，白消安，长春花碱，长春新碱，博来霉素，依托泊苷，拓扑替康 ，伊立替康，泰索帝，紫杉醇，5-氟尿嘧啶，甲氨蝶呤，吉西他滨，顺铂，卡铂和苯丁酸氮芥。