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    Sulindac derivatives
    3.
    发明授权
    Sulindac derivatives 有权

    公开(公告)号：US10329249B1

    公开(公告)日：2019-06-25

    申请号：US16151291

    申请日：2018-10-03

    Applicant: KING SAUD UNIVERSITY

    Inventor： Mashooq Ahmad Bhat ,  Mohamed A. Al-Omar ,  Nawaf Abdulaziz Alsaif ,  Syed Hidayathulla

    IPC: C07C325/02 ,  A61P29/00

    Abstract: The sulindac derivatives are compounds of the formula: wherein R is one of twenty-five substituted or unsubstituted phenyl substituents; and pharmaceutically acceptable salts thereof. The sulindac derivatives are synthesized by refluxing sulindac hydrazide with appropriately substituted benzaldehydes in the presence of ethanol and catalytic amounts of glacial acetic acid. The sulindac derivatives may be used as active ingredients in pharmaceutical compositions for the treatment of inflammation or inflammatory diseases. The sulindac derivatives may also be used as analgesic and/or gastric sparing agents.

    Naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents
    4.
    发明授权
    Naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents 有权

    公开(公告)号：US10239875B2

    公开(公告)日：2019-03-26

    申请号：US15624811

    申请日：2017-06-16

    Applicant: KING SAUD UNIVERSITY

    Inventor： Nagy Mahmoud Hassan Khalifa ,  Mohamed A. Al-Omar

    IPC: C07D471/04

    Abstract: The naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents are (E)-2-(substituted benzylidene)-1-(2,7-dialkyl-1,8-naphthyridinyl) hydrazines that provide effective peripheral analgesic activity, as demonstrated using the mouse writhing test. The new target compounds include at least one compound that demonstrates higher potency in providing analgesic relief in mice (Protection (%)=81.44) compared to the reference drug acetyl salicylic acid (Protection (%)=78.47). These results demonstrated that the target compound exerts acute analgesic action, suggesting that it may represent an alternative in the development of new therapeutic strategies. Preferably, the (E)-2-(substituted benzylidene)-1-(2,7-dialkyl naphthyridinyl) hydrazine has the formula: wherein R1 and R2 are alkyl, R3 is hydrogen, and R4 is NO2.

    Abietic acid derivatives as anti-tumor agents
    5.
    发明授权
    Abietic acid derivatives as anti-tumor agents 有权

    公开(公告)号：US10064837B1

    公开(公告)日：2018-09-04

    申请号：US15897912

    申请日：2018-02-15

    Applicant: KING SAUD UNIVERSITY

    Inventor： Abd El-Galil E. Amr ,  Mohamed A. Al-Omar ,  Abdulrahman A. Almehizia

    IPC: A61K31/216 ,  A61K31/265 ,  A61K31/365 ,  A61P35/00 ,  A61K31/167

    Abstract: The abietic acid derivatives as anti-tumor agents are derivatives of abietic acid in which the hydroxyl entity (—OH) of the carboxyl entity is replaced by an electronegative substituent, which may be C6H5-O—, C6H5-S—, or C6H5-NH—, and a hydrogen atom on one of the rings is replaced by a hydroxyl (—OH) substituents, the derivatives having the formula: wherein X is O, S, or NH. The derivatives are formed by formation of an intermediate lactone from abietic acid, followed by reaction of the lactone with phenol, thiophenol, or aniline. All of the derivatives exhibited potent 5α-reductase inhibitor activity, both in vitro and in vivo, and anti-tumor activity with regard to two prostate cancer cell lines—LNCaP and PC-3. The intermediate lactones are also derivatives of abietic acid that exhibit anti-tumor activity.

    Sulfonylurea derivatives of oleanolic acid
    9.
    发明授权
    Sulfonylurea derivatives of oleanolic acid 有权

    公开(公告)号：US10137138B1

    公开(公告)日：2018-11-27

    申请号：US15991916

    申请日：2018-05-29

    Applicant: KING SAUD UNIVERSITY

    Inventor： Abd El-Galil E. Amr ,  Mohamed A. Al-Omar ,  Abdulrahman Abdulaziz Almehizia ,  Ahmed Mohamed Naglah

    IPC: A61K31/64 ,  A61P3/10 ,  A61K9/00

    Abstract: The sulfonylurea derivatives of oleanolic acid include compounds replacing the 5-chloro-2-methoxybenzoic acid moiety found in glibenclamide with oleanolic acid. The resulting triterpenoidal sulfonylurea derivatives are compounds having the following formula: or a pharmaceutically acceptable salt thereof. The derivatives are synthesized by condensation of 3-oxo-Olean-12-en-28-oic acid with 4-(2-aminoethyl)benzenesulfonamide to form an intermediate product, followed by reaction with cyclohexyl isocyanate or 4-methylcyclohexyl isocyanate to give 3a or 3b, respectively. The sulfonylurea derivative compounds were screened for their oral hypoglycemic activity in vivo using the alloxan-induced diabetic mouse model and proved more potent than either glibenclamide or oleanolic acid.

    Pyrido[2,3-d]pyrimidines as anticancer agents
    10.
    发明授权
    Pyrido[2,3-d]pyrimidines as anticancer agents 有权

    公开(公告)号：US10100054B1

    公开(公告)日：2018-10-16

    申请号：US15944734

    申请日：2018-04-03

    Applicant: KING SAUD UNIVERSITY

    Inventor： Nagy Mahmoud Hassan Khalifa ,  Mohamed A. Al-Omar ,  Hamad M. Alkahtani ,  Ahmed H. Bakheit

    IPC: C07D471/04 ,  A61P35/00

    Abstract: The pyrido[2,3-d]pyrimidine derivatives as anticancer agents include 5-(substituted-phenyl)-2-(3-methyl-5-oxo-2H-pyrazol-1(5H)-yl)-7-(pyridin-3-yl)pyrido[2,3-d]pyrimidin-4(3H)-one derivatives having the formula: where R is hydrogen; 2-halo, 3-halo, or 4-halo (Cl, Br, or F); 2-methoxy, 3-methoxy, or 4-methoxy (OCH3); 2-nitro, 3-nitro, or 4-nitro (NO2); 4-isopropyl, 4-methyl, or 4-cyano (CN); 2-hydroxy or 3-hydroxy (OH), 3-chloro and 5-chloro; 2-methoxy and 5-methoxy, 3-methoxy and 5-methoxy, or 3-methoxy and 4-methoxy; 3,4,5-trimethoxy; or 2-hydroxy and 4-hydroxy; or a pharmaceutically acceptable salt thereof. The derivatives may be useful in treating various cancers, including hepatic, colon, prostate, breast, and lung cancer.

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