137 results about "Ester prodrug" patented technology

The present invention relates to method of sustained-delivery of an active drug to a posterior part of an eye of a mammal to treat or prevent a disease or condition affecting said mammal, wherein said disease or condition can be treated or prevented by the action of said active drug upon said posterior part of the eye, comprising administering an effective amount of an ester prodrug of the active drug subconjunctivally or periocularly. Preferably, the active drug is more than about 10 times as active as the prodrug. Other aspects of this invention deal with the treatment of certain diseases by the periocular or subconjunctival delivery of an ester prodrug, and certain pharmaceutical products containing ester prodrugs for periocular or subconjunctival administration.

The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.

A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.

The invention describes a phosphate structure containing substituted benzyl, wherein the phosphate structure is shown as a formula (I) and a formula (II). The phosphate structure can be used as prodrugs for various nucleoside analogues including non-cyclic nucleoside, carbon-cyclic nucleoside, furan-cyclic nucleoside and the like, and enhance bioactivity of nucleoside compounds, and thus the structure can be applied in treatment for virus infections and cancers.

The present invention discloses an anti-tumor compound and its preparation method,application, and pharmaceutical compositions. The anti-tumor compound is a 4 - nitro-substituted benzyl group ifosfamide ester prodrug thereof, or pharmaceuticallysalt, or solvate thereof of the structure of formula I. The structure of formula I. The present invention has the following advantage of being used for the treatment or prevention of mammalian tumor-related diseases, such as leukemia, hemangioma, glioma, Kaposi's sarcoma, ovarian cancer, breast cancer, lung cancer, pancreatic cancer, lymphoma, prostate, colon and skin tumors and their complications.

The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.

The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.

This invention provides a prodrug that help arthritis patients without increasing cardiovascular and gastrointestinal risk. A novel group of hybrid nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs), moiety attached via a one -carbon methylene spacer to the carboxylic acid group of the traditional NSAIDs aspirin, ibuprofen and indomethacin were synthesized. The ester prodrugs showed equipotent anti-inflammatory activities in vivo to that of the parent aspirin, ibuprofen and indomethacin. The simultaneous release of parent drug and nitric oxide from the NO- prodrugs constitutes a potentially beneficial property for the prophylactic prevention of thrombus formation and adverse cardiovascular events such as stroke and myocardial infarction. Data acquired in an in vivo ulcer index (UI) assay showed that this group of ester prodrugs in which no lesions were observed when compared to the parent drugs at equivalent doses. Accordingly, these hybrid NO-NSAID prodrugs possessing a diazen-1-ium-1,2-diolate moiety, represents a new approach for the rational design of anti-inflammatory drugs with reduced gastric ulcerogenicity.

The invention discloses 2,7-substituted 3H-imidazole[4,5-b]pyridine compounds shown as the structural formula I, or pharmaceutically acceptable salt, ester and precursors, and/or hydrate and medicinal compositions thereof, and a preparation method for the compounds. The compounds, or pharmaceutically acceptable salt, ester and precursors, and/or hydrate and medicinal compositions thereof can serve as antagonists of CR4 and are used for treating or preventing CXCR4 receptor activation related diseases.

The invention discloses cyclohexene compounds and an application thereof, and belongs to the field of medicinal chemistry. The cyclohexene compounds are cyclohexene compounds having a structure characteristic represented by the formula I and pharmaceutically acceptable salts and ester prodrugs or stereoisomers thereof; the cyclohexene compounds are subjected to influenza virus neuraminidase activity detection and are confirmed to have good inhibition activity on both wild type and drug-resistant mutant type influenza viruses; a part of the compounds have the inhibition activity IC50 on the wild type and drug-resistant mutant type influenza virus neuraminidase of less than 5 nM, and have the effect for significantly inhibiting the influenza viruses; the cyclohexene compounds or the pharmaceutically acceptable salts or the stereoisomers thereof are showed to have a good application prospect in preparation of anti-influenza virus drugs, thereby providing a new drug choice for clinic treatment of influenza.

The present invention is related to 10,20-di-O ester derivatives of camptothecin and pharmaceutical formulations thereof. The compounds and pharmaceutical formulations of the present invention possess increased biological life span and bioavailability and reduced toxicity, while maintaining anti-cancer activity.

Esters prodrugs that cross the blood brain barrier can be ideal drugs for treatment of diseases of the central nervous system because the cerebral spinal fluid contains an abundance of esterases. The prodrug can be hydrolyzed into an active drug and a metabolite such as cholesterol that is known to be non-toxic and is familiar to the central nervous system. This invention describes a modification of the Fischer-Speier or Fischer esterification reaction in which one reagent is lipophilic and the other reagent is hydrophilic. The reaction occurs in a heterogeneous mixture. The preferred catalyst is 1.0 M hydrochloric acid and the preferred solvent is acetone. The presence of ester synthesis was confirmed by the hydroxamic acid-ferric perchlorate reaction. The synthesis can be conducted without chemical scaffolds and without protecting functional groups.

The present invention is directed to a 2,6-substituted-4-monosubstitutedamino-pyrimidine compound of formula (I):

or an enantiomer thereof, or an ester prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.

The invention relates to sulfomorpholine compounds, a preparation method thereof and a purpose thereof, and concretely relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, free alkalis thereof, solvates thereof, esters thereof, prodrugs thereof, stereo isomers thereof, geometric isomers thereof and racemates thereof, wherein symbols in the formula (I) are shown in the specification. The invention also relates to a medicinal composition containing the compounds, a purpose of the compounds in the preparation of medicines for treating and/or preventing diseases or symptoms related with DPP-IV (dipeptidyl peptidase IV) hyperactivity or DPP-IV overexpression, and a method for treating relevant diseases with the compounds of the invention. The compounds of the invention can effectively inhibit the DPP-IV activity.

Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided:

wherein:

each (L)_k-Ar¹ is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR¹ or O and each R¹ and R² is independently H, alkyl, alkenyl or aralkyl or R¹ and R² taken together form a 5-8 membered ring; R³⁻R⁶ are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO₂, CH₂, NH, N(alkyl), or NHC(═O); and Z is OH, NR⁶R⁷, NR⁸SO₂(alkyl), NR⁸C(O)NR⁶R⁷, NR⁸C(O)O(alkyl), NR⁸-dihydrothiazole, or NR⁸-dihydroimidazole or wherein Z can fuse with Ar² to form selected heterocycles.

The invention relates to an abelmoschus manihot extract and a novel application of chemical components thereof, concretely, relates to a compound of formula I or its pharmaceutically acceptable salt, solvate, ester and prodrug, and an extract containing the compound of formula I, a composition thereof and an application thereof. The compound or extract of the invention can be used as anti-oxidative damaging agent, and can be used for treating or preventing diseases or symptoms related to oxidative damage.

The invention discloses a sulfo-Adefovir and Tenofovir liver targeting ester prodrug represented by the following general formula (I), or medicinal salt, hydrate or solvate thereof, which serves as the effective component of hepatitis B antivirus. The compound of the invention has liver targeting characteristic and better achieves the aim of small dose, high effect and low toxic or side effect.

Compounds of Formula I:

and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines

The invention discloses pyrimidine nucleoside compounds and a preparation method and application thereof, and particularly relates to 4-substituted amido-2'-deoxo-2'-fluoro-4'-azido-beta-D-cytidine compounds, a preparation method thereof and application thereof in an antiviral aspect, belonging to the field of pharmaceutical chemistry. The 4-substituted amido-2'-deoxo-2'-fluoro-4'-azido-beta-D-cytidine compounds have the following structural general formula in the specification and comprises pharmaceutically usable salt, ester, a prodrug or a metabolite thereof. In the formula, X indicates H or halogens (fluorine, chlorine, bromine and iodine) and the like. a structure as shown in the specification indicates (1) amido (NH2) and C3-C8 cyclic or non-cyclic alkylamino or derived alkylamino thereof, (2) adamantanamino and decahydronaphthalene amido or the following other substituted amido and (3) arylamino (which includes anilino, naphthylamido, heterocyclic amino and the like) or corresponding substituted arylamino. The pyrimidine nucleoside compounds disclosed by the invention have antiviral and virus infection resistant activity, is applied to the development of medicaments for treating virus infection and have good application prospect.

The invention belongs to the field of pharmaceutical chemistry, and particularly relates to pyridazinone compounds as shown in general formula I or isomers thereof or pharmaceutically acceptable salt, ester prodrug or solvate thereof, a preparation method thereof, a medicinal composition and application thereof in preparation of a tyrosine kinase inhibitor (especially c-Met inhibitor). The compounds or the medicinal composition thereof serving as a tyrosine kinase inhibitor (especially c-Met inhibitor) can be used for preventing and/or treating neoplastic diseases related to c-Met abnormality.