The present disclosure provides a taxane compound and a preparation method and application thereof. The preparation method includes: protecting two hydroxyl groups in gemcitabine, conducting a condensation reaction between the protected gemcitabine and alkyl chloroformate, and removing of hydroxyl protecting groups to obtain an intermediate G1; protecting a first hydroxyl group of the intermediate G1, and then protecting the other one of the hydroxyl groups, and removing a protecting group of the first hydroxyl group to obtain an intermediate G2; reacting 7,10-di-troc-docetaxel with dianhydride to obtain an intermediate D1; conducting a condensation reaction between the intermediate D1 and the intermediate G2 to obtain an intermediate D2; and subjecting the intermediate D2 to hydroxyl deprotection to obtain a target product comprising the disclosed taxane compound.

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer. For example, the compounds can comprise compounds of formula

TABLE-US-00001 (SEQIDNO:1) X.sub.1X.sub.2X.sub.3X.sub.4X.sub.5GVX.sub.6AKAGVX.sub.7NX.sub.8FKSESY (I) (SEQIDNO:2) (X.sub.9).sub.nGVX.sub.10AKAGVX.sub.11NX.sub.12FKSESY (II) (SEQIDNO:3) YKX.sub.13LRRX.sub.14APRWDX.sub.15PLRDPALRX.sub.16X.sub.17L (III) (SEQIDNO:4) YKX.sub.18LRR(X.sub.19).sub.nPLRDPALRX.sub.20X.sub.21L (IV) (SEQIDNO:5) IKLSGGVQAKAGVINMDKSESM (V) (SEQIDNO:6) IKLSGGVQAKAGVINMFKSESY (VI) (SEQIDNO:7) IKLSGGVQAKAGVINMFKSESYK (VII) (SEQIDNO:8) GVQAKAGVINMFKSESY (VIII) (SEQIDNO:9) GVRAKAGVRNMFKSESY (IX) (SEQIDNO:10) GVRAKAGVRN(Nle)FKSESY (X) (SEQIDNO:11) YKSLRRKAPRWDAPLRDPALRQLL (XI) (SEQIDNO:12) YKSLRRKAPRWDAYLRDPALRQLL (XII) (SEQIDNO:13) YKSLRRKAPRWDAYLRDPALRPLL (XIII) wherein X.sub.1 to X.sub.21 and n can have various different values and wherein at least one protecting group and/or at least one labelling agent is optionally connected to said peptide compound at an N- and/or C-terminal end.

The present invention discloses therapeutic compounds of the aminoindane class, including certain short-acting ester and lactone derivatives, and pharmaceutical compositions made therewith, as well as methods of their use in the treatment of alcohol and other substance use disorders, behavioral addictions, and CNS and mental health disorders, and for the improvement of mental health and psychological functioning.

The present invention discloses therapeutic compounds of the aminoindane class, including certain short-acting ester and lactone derivatives, and pharmaceutical compositions made therewith, as well as methods of their use in the treatment of alcohol and other substance use disorders, behavioral addictions, and CNS and mental health disorders, and for the improvement of mental health and psychological functioning.

This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.

The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2-benzoyloxy-5,20-epoxy-1-hydroxy-7, 10-dimethoxy-9-oxo-tax-11-ene-13-yle, and to the preparation thereof.

The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2-benzoyloxy-5,20-epoxy-1-hydroxy-7, 10-dimethoxy-9-oxo-tax-11-ene-13-yle, and to the preparation thereof.

Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G or Formula M:

##STR00001##

with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G or Formula M:

##STR00001##

with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.