73 results about "Imidazoquinoline" patented technology

A method of treating dermal lesions caused by envenomation comprising applying a therapeutically effective amount of an immune response modifier compound selected from the group consisting of imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphthyridine amines, tetrahydroimidazonaphthyridine amines, oxazolopyridine amines, oxazoloquinoline amines, thiazolopyridine amines, thiazoloquinoline amines and 1,2-bridged imidazoquinoline amines to the site of the lesion is disclosed.

Aqueous gel formulations, including an immune response modifier (IRM), such as those chosen from imidazoquinoline amines, tetrahydroimidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, imidazonaphthyridine amines, imidazotetrahydronaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines, oxazolopyridine amines, thiazolopyridine amines, oxazolonaphthyridine amines, thiazolonaphthyridine amines, pyrazolopyridine amines, pyrazoloquinoline amines, tetrahydropyrazoloquinoline amines, pyrazolonaphthyridine amines, tetrahydropyrazolonaphthyridine amines, and 1H-imidazo dimers fused to pyridine amines, quinoline amines, tetrahydroquinoline amines, naphthyridine amines, or tetrahydronaphthyridine amines, are provided. Methods of use and kits are also provided.

The invention provides novel compositions comprising imidazoquinoline compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an)other agent(s).

The invention belongs to the technical field of medicines, and particularly relates to an imidazo quinoline PI3K and mTOR (mammalian target of rapamycin) dual inhibitor disclosed in a general formula (I) and clinically-acceptable salt or stereoisomer thereof, wherein R1, R2, R3, R3', R4, R4', R5 and X are defined as in a specification. The invention also relates to a preparation method of the compounds, a medicine preparation containing the compounds and the application of the compounds in preparing medicines capable of treating and / or preventing proliferative diseases.

The invention provides, inter alia, immunogenic compositions comprising a first antigen, at least two adjuvants, wherein a first adjuvant comprises a polymer derived from poly(lactides) and / or poly(lactide-co-glycolides), and wherein a second adjuvant comprises an imidazoquinoline, wherein said first antigen is encapsulated within, adsorbed or conjugated to, co-lyophilized or mixed with said first adjuvant, and a pharmaceutically acceptable excipient, wherein said composition elicits a cellular immune response when administered to a vertebrate subject. The invention also provides methods of producing immunogenic compositions, methods for producing a cytotoxic-T lymphocyte (CTL) response in a vertebrate subject, and methods of immunization.

Pharmaceutical formulations comprising an immune response modifier (IRM) chosen from imidazoquinoline amines, imidazotetrahydroquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, thiazolo-quinolineamines, oxazolo-quinolinamines, thiazolo-pyridinamines, oxazolo-pyridinamines, imidazonaphthyridine amines, tetrahydroimidazonaphthyridine amines, and thiazolonaphthyridine amines; a fatty acid; and a hydrophobic, aprotic component miscible with the fatty acid are useful for the treatment of dermal associated conditions. Novel topical formulations are provided. In one embodiment, the topical formulations are advantageous for treatment of actinic keratosis, postsurgical scars, basal cell carcinoma, atopic dermatitis, and warts.

This invention relates to novel 4-amino-imidazoquinoline compounds of the formulawherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer or infectious diseases.

The compounds of the subject invention are adjuvant molecules that comprise a imidazoquinoline molecule covalently linked to a phospho- or phosphonolipid group. The compounds of the invention have been shown to be inducers of interferon-a, IL-12 and other immunostimulatory cytokines and possess an improved activity profile in comparison to known cytokine inducers when used as adjuvants for vaccine antigens.

The present invention is directed to a method of increasing the time period between outbreaks of genital herpes comprising providing an imidazoquinolinamine formulation, disposing an amount of the imidazoquinolinamine formulation into a first nare of an individual infected with Herpes Simplex Virus type 2, covering at least a portion of the internal surface of the individual's first nare with a portion of the amount of the imidazoquinolinamine in the nare, massaging the portion of the amount of the imidazoquinolinamine into the internal surface of the first nare, disposing the amount of the imidazoquinolinamine formulation into a second nare of the individual, covering at least a portion of the internal surface of the second nare with a portion of the amount of the imidazoquinolinamine in said nare and massaging the portion of the amount of the imidazoquinolinamine into the internal surface of said nare.

Pharmaceutical formulations comprising an immune response modifier (IRM) chosen from imidazoquinoline amines, imidazotetrahydroquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, thiazolo-quinolineamines, oxazolo-quinolinamines, thiazolo-pyridinamines, oxazolo-pyridinamines, imidazonaphthyridine amines, tetrahydroimidazonaphthyridine amines, and thiazolonaphthyridine amines; a fatty acid; and a hydrophobic, aprotic component miscible with the fatty acid are useful for the treatment of dermal associated conditions. Novel topical formulations are provided. In one embodiment, the topical formulations are advantageous for treatment of actinic keratosis, postsurgical scars, basal cell carcinoma, atopic dermatitis, and warts.

The invention provides an oil-based pharmaceutical composition comprising as an active ingredient phostphatidylserine or a derivative thereof and a pharmaceutically acceptable oil-based carrier, which is formulated for topical or intratumoral administration. Preferably, the composition is an ointment or a cream. The composition can contain additional active agents as well, such as aminophospholipid translocase inhibitors, transnitrosylating agents, chemokines, cytokines, Toll-like receptor ligands, imidazoquinolines, dendritic cell differentiation factors, or combinations thereof. In another aspect, the invention provides a method of treating cancer within a patient in need of treatment by administering the inventive composition to the patient.

The compounds of the subject invention are adjuvant molecules that comprise a imidazoquinoline molecule covalently linked to a phospho- or phosphonolipid group. The compounds of the invention have been shown to be inducers of interferon-a, IL-12 and other immunostimulatory cytokines and possess an improved activity profile in comparison to known cytokine inducers when used as adjuvants for vaccine antigens.

The invention discloses a preparing method for clinic level cells for enhancing the immune modulating function of MSCs. The preparing method is suitable for culturing the mesenchymal stem cells from bone marrow, fat and the umbilical cord. A serum-free complete medium is adopted to culture the mesenchymal stem cells from umbilical cord tissue, a traditional method is improved by applying a secondary inoculation method, and the obtaining rate of primary cells is increased. Imidazoquinoline R848 with the concentration of 1-5 micrograms / milliliters and recombinant human interferon I FN-alpha-2b with the concentration of 100-200 units / milliliters are applied as pretreatment factors and obviously induce high expression of the MSCs and secretory cell factors VEGF, HGF and PGE-2, the capacity for modulating immune and promoting tissue regeneration of the MSCs is brought into play better, the multiplication capacity and the capacity for resisting NK cell killing of the MSCs can be improved obviously, and the pretreated MSCs have the enhanced capacity for suppressing lymphocyte proliferation and can be applied to treatment on the GVHD with T cells as the principal and other autoimmune diseases better.

The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereofwherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Disclosed are alkyl chain modified 1H-imidazoquinoline compounds, derivatives and analogs thereof, as Toll-like receptor-7 and -8 agonists for enhancing immune responses. Also provided are methods of making pharmaceutical compositions containing these compounds. The present disclosure also describes methods of use for the alkyl chain modified 1H-imidazoquinoline compounds, derivatives and analogs thereof, and pharmaceutical compositions containing these compounds for the treatment of disease in a subject.

The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)-active and toll-like receptor (TLR8)-active imidazoquinolines and oxoadenines.

The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.

Provided is a process for producing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod), which includes reacting 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline with a non-gaseous amine precursor. Also provided are methods for isolating highly pure imiquimod. Further provided are intermediates useful in the production of imiquimod, methods for producing such intermediates, and methods for obtaining imiquimod from such intermediates.

The invention relates to a bactericidal composition containing pyraclostrobin and imidazoquinoline copper. The active ingredient of the composition is a binary complex of the pyraclostrobin and imidazoquinoline copper, wherein the mass ratio of the pyraclostrobin to imidazoquinoline copper is (1-50):(50-1), the mass fraction of the active ingredients comprising the pyraclostrobin and imidazoquinoline copper in the preparation is 1-80%, and the composition further comprises allowed and acceptable auxiliary ingredients in pesticides. Dosage forms of the bactericidal composition disclosed by theinvention comprise missible oil, suspending agents, wettable powder, water dispersible granules, emulsion in water, micro-emulsion, granules and microcapsules. The bactericidal composition is mainly used for controlling important diseases, such as powdery mildew, rust disease, glume blight, web blotch, downy mildew, late blight and the like, in ascomycetes, basidiomycetes and oomycetes subclass.

The present invention provides a process for preparing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod). The process preferably includes heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with ammonia in a polar aprotic solvent at relatively moderate pressure to produce imiquimod, and optionally purifying the imiquimod. The process of the present invention can produce highly pure imiquimod in high yield.

Pharmaceutical compositions are provided that include an antibiotics, but that include ingredients that counteract the effect of that antibiotic on wound healing, without altering the bactericidal properties of the antibiotic. These pharmaceutical compositions include an effective amount of 1) an imidazoquinoline having toll-like receptor 7 (TLR7) ligand activity, 2) an immunostimulatory K-type CpG oligodeoxynucleotide (ODN) comprising an unmethylated CpG motif, 3) an antibiotic, and 4) a surfactant, wherein the composition is formulated for topical administration. Methods for accelerating wound healing are also provided. These methods include topically administering the disclosed compositions. The wound can be in the skin or in the eye.

The invention relates to a method for synthesizing a 3-cyano-substituted imidazo [1, 5a] quinoline compound. Particularly, the invention provides a method for constructing a 3-cyano-substituted imidazo [1, 5a] quinoline compound by using an electrocatalytic three-component reaction, and the method comprises the following steps: 1) respectively adding an electrolyte, unsubstituted or substituted 2-methylquinoline, substituted fatty amine, a cyano source and a solvent into a non-separated electrolytic cell, installing an electrode in the electrolytic cell, and performing electrifying and stirring to react; 2) separating and purifying the solution after the reaction to obtain the 3-cyano-substituted imidazo [1, 5a] quinoline compound.

The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of formula (I), and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammatory diseases and angiogenesis related disorders.

The invention provides novel compositions comprising imidazoquinoline compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an) other agent(s).

The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereofwherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.