56 results about "Chagas disease" patented technology

The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and / or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and / or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and / or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I):(wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and / or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

Molecular targets are identified in T. cruzi suitable for use in diagnosis of Chagas disease, drug development, and vaccines, including live vaccines.

Transfusion of contaminated blood has become the major route of transmission for Chagas' disease. Current screening tests are insensitive and yield conflicting results, while confirmatory assays do not exist. The present invention relates to antigens and their use for serological diagnosis of Chagas' disease. More specifically, the present invention concerns assays which are able to reliably and accurately detect the presence of antibodies to various specific antigens of Trypanosoma cruzi in a highly sensitive and specific manner.

The present invention relates to compounds of formula (1), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

Transfusion of contaminated blood has become the major route of transmission for Chagas' disease. Current screening tests are insensitive and yield conflicting results, while confirmatory assays do not exist. The present invention relates to antigens and their use for serological diagnosis of Chagas' disease. More specifically, the present invention concerns assays which are able to reliably and accurately detect the presence of antibodies to various specific antigens of Trypanosoma cruzi in a highly sensitive and specific manner.

The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.

It is intended to provide a method of diagnosing infection with Chagas disease by screening a trypanocidal drugs for Trypanosoma cruzi which is the pathogen of Chagas disease. Using a flavin protein TcOYE specific to Trypanosoma cruzi, a trypanocidal drugs effective against Trypanosoma cruzi is screened. Using the gene sequence of TcOYE and an antibody therefor, infection with Trypanosoma cruzi is diagnosed.

A vaccine against the Chagas disease, capable of stimulating the immune response against the trans-sialidase virulence factor of the Trypanosoma cruzi parasite, which is a multicomponent vaccine comprising: (a) an immunogenic portion formed by one or more recombinant or synthetic polypeptides or fractions of thereof and (b) one or more polynucleotides including the regions codifying one or more immunogenic polypeptides, or a monocomponent vaccine comprising at least one component selected among an immunogenic portion formed by one or more recombinant or synthetic polypeptides or fractions of them and a group of polynucleotides including the regions codifying one or more immunogenic polypeptides derived from Trypanosoma cruzi and pharmaceutical compositions containing said multicomponent and monocomponent vaccines, the procedures for obtaining the immunogen portion of said vaccines and the nucleic acid used in the procedure.

A vaccine against the Chagas disease, capable of stimulating the immune response against the trans-sialidase virulence factor of the Trypanosoma Cruzi parasite, which is a multicomponent vaccine comprising: (a) an immunogenic portion formed by one or more recombinant or synthetic polypeptides or fractions of thereof and (b) one or more polynucleotides including the regions that codifying one or more immunogenic polypeptides, or a monocomponent comprising at least one component selected among an immunogenic portion formed by one or more recombinant or synthetic polypeptides or fractions of them and a group of polynucleotides including the regions codifying one or more immunogenic polypeptides derived from Trypanosoma Cruzi and pharmaceutical compositions containing said multicomponent and monocomponent vaccines, the procedures for obtaining the immunogen portion of said vaccines and the nucleic acid used in the procedure.

Molecular targets are identified in T. cruzi suitable for use in diagnosis of Chagas disease, drug development, and vaccines, including live vaccines.

A peptidyl nitrile of the general formula (I) or a pharmaceutically acceptable salt or prodrug thereof, is capable of selectively inhibiting dipeptidyl-peptidase (DPP-I), also known as cathepsin C. A compound of the invention is useful as an active substance for the treatment of inflammation, type 2 diabetes, asthma, severe influenza, respiratory syncytial virus infection, CD8 T cell inhibition, inflammatory bowel diseases, psoriasis, atopic dermatitis, Papillon Lefevre syndrome, Haim Munk syndrome, gun disease, periodontitis, rheumatoid arthritis, Huntington's disease, Chagas' disease, Alzheimer's disease, sepsis or for application in target cell apoptosis.

A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof,wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; orR1 and R2 are both H;one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; orR3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group;R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; orR6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached;R8 is C1-8-alkyl or C3-8-cycloalkyl;R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.

The present invention relates to methods for the diagnosis, prevention and treatment of heart disease or heart failure in a subject. The present invention also relates to methods for the diagnosis, prevention and treatment of atherosclerosis with vulnerable plaque in a subject. Furthermore, the present invention relates to methods for the diagnosis, prevention and treatment of cardiomyopathies resulting from Chagas disease.

The invention provides compounds of the formula: wherein L1 and L2 are independently selected from O and S; R1 is C3-C6 straight or branched alkyl, C3-C7cycloalkyl, C5-C7cycloalkenyl, adamantly, phenyl or saturated heterocyclyl, any of which being optionally substituted; R2 is H, methyl or ethyl; R5 is NRxCORy, NRxRy, CH2COCH3, CH2C≡N, or a 5- or 6-membered heteroaryl group which is optionally substituted; X, Y and Z are independently N or CH; Rx is independently H or C1-C4alkyl; Ry is independently H, CrC4alkyl, phenyl or benzyl, either of which is optionally substituted; n is 0-3; salts, hydrates and N-oxides, wherein the optional substituents are further defined in the claims. The compounds have utility in the prophylaxis or treatment of trypanosomal diseases, such as T. cruzi (Chagas disease).

The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, malaria and Leishmaniasis, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.

The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal, especially a human, in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting Human African Trypanosomiasis (HAT), Chagas Disease, Malaria, Leishmaniasis, and other infectious diseases transmitted to humans and animals by exposure to parasites, the method comprising administering to a human or mammal in need of such treatment a compound of formula I as described above.

The nucleotide sequence of Tc100, a gene encoding PTc100, a new Trypanosoma antigen, and the amino acid sequence of PTc100 are described. Tc100 and PTc100, or fragments thereof, modified or otherwise, can be used directly or indirectly for the detection of Trypanosoma cruzi, or for the monitoring of the infection generated by Trypanosoma cruzi, in man or in animals.

Methods are provided to inhibit proliferation of Trypanosoma cruzi with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can be used to provide prophylaxis or treatment to a patient in need of treatment against Chagas disease.

Use of synthetic peptides derived from Trypanosoma cruzi antigens and their use in vaccination against trypomastigote infection and Chagas disease. T. cruzi uses several surface proteins to invade the host. In their role of protection, the surface protients ensure the targeting and invasion of specific cells or tissues. A conserved region in the family of mucin-associated surface proteins (MASP) was used to analyze the expression of MASP at different points of invasion and proved to be important for host cell invasion, thus suggesting MASP as a candidate for vaccine development. A synthetic peptide, MASPsyn, was studied and showed efficacy in stimulating antibody and cytokine production necessary for resistance against the parasite.

The present invention relates to compositions and methods for the reduction of atherosclerotic plaques and the decrease in the level of total serum cholesterol, triglycerides, serum LDL cholesterol, and serum HDL cholesterol. The present invention also relates to methods for the diagnosis, prevention and treatment of atherosclerosis and mycoplasma associated diseases, cardiotoxicity related to cancer treatment, and Chagas disease related cardiomyopathies.

The present invention relates to a class of novel pradimicins and analogues and derivatives thereof, including the compounds of formula A, I and 111, and / or a pharmaceutical acceptable addition salt thereof and / or a stereoisomer thereof and / or a solvate thereof and their use to treat or prevent kinetoplastid infections and their use to manufacture a medicine to treat or prevent kinetoplastid infections, particularly infections with trypanosoma and leishmania, such as Trypanosoma brucei, Trypanosoma cruzi and Leischmania donovani. wherein Ra, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the claim 1 or as described in detail in the description of the invention. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent kinetoplastid infections. The present invention further relates active ingredients, more specifically as medicaments for the treatment of kinetoplastid infections and pathologic conditions such as, but not limited to Trypanosomiasis, such as African trypanosomiasis, sleeping sickness, Chagas disease and leishmaniasis.

Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidieal agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria. African typanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).

This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesis and / or purification of certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (also known as Methylene Blue). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment, prophylaxis, and diagnosis, etc., for example, a tauopathy; a disease of tau protein aggregation; Alzheimer's disease (AD); Pick's disease; Progressive Supranuclear Palsy (PSP); fronto temporal dementia (FTD); parkinsonism linked to chromosome 17 (FTDP-17); disinhibition-dementia-parkinsonism-amyotrophy complex (DDPAC); pallido-ponto-nigral degeneration (PPND); Guam-ALS syndrome; pallido-nigro-luysian degeneration (PNLD); cortico-basal degeneration (CBD); mild cognitive impairment (MCI); skin cancer; melanoma; methemoglobinemia; a viral infection; a bacterial infection; a protozoal infection; a parasitic infection; malaria; visceral leishmaniasis; African sleeping sickness; toxoplasmosis; giardiasis; Chagas' disease; Hepatitis C virus (HCV) infection; human immunodeficiency virus (HIV) infection; West Nile virus (WNV) infection; a synucleinopathy; Parkinson's disease (PD); dementia with Lewy bodies (DLB); multiple system atrophy (MSA); drug-induced parkinsonism; and pure autonomic failure (PAF).