200 results about "Indolamines" patented technology

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and / or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.

The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunsupression associated with an infectious disease, e.g., HIV-1 infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.

The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

The present invention provides a population of connective tissue derived cells that respond to interferon-gamma (IFN-γ) by expressing indolamine-2,3-dioxygenase (IDO) for use in preventing, treating or ameliorating one or more symptoms associated with disorders in which modulation of a subject's immune system is beneficial, including, but not limited to, autoimmune diseases, inflammatory disorders, and immunologically mediated diseases including rejection of transplanted organs and tissues.

The invention relates to an indoleamine 2,3-dioxygenase inhibitor with a structure represented by the formula (I) and a preparation method and applications thereof. The indoleamine 2,3-dioxygenase (IDO) inhibitor is the derivative of (Z)-N'-hydroxyl-N-phenyl formamidine, has an extremely high activity on inhibiting IDO, can effectively inhibit the activity of IDO, and can be used to inhibit the immunity inhibition of patients. The inhibitor can be widely used to treat or prevent cancer / tumor, viral infection, depression, neurodegenerative diseases, wounds, age related cataract, organ-graft refection, and autoimmune disease, and can be advantageously to be used as a novel immune-suppressor.

The invention belongs to the medicinal field, and concretely relates to a use of a 8-nitrotryptanthrin compound as an IDO inhibitor. The 8-nitrotryptanthrin compound is a reversible IDO inhibitor, has an inhibition constant Ki of 0.054muM, has in-vitro and cell-based median effective inhibition concentrations IC50 of 0.103muM and 1.80*10<-5>muM respectively, and has an inhibition effectiveness obviously better than a present inhibitor 1-methyltryptophan (Ki of 34muM and IC50 of 340muM). 8-nitrotryptanthrin disclosed in the invention can effectively lower the abnormally-increasing IDO activity in a tumor animal model as the IDO inhibitor, and also has tumor treatment effects comprising tumor growth delaying, tumor volume reduction and in-vitro tumor cell killing. 8-nitrotryptanthrin disclosed in the invention has a wide application prospect, and can be used for treating serious diseases having the IDO mediated tryptophan metabolism approach pathology characteristics, such as cancers, the Alzheimer disease, tristimania, cataract and the like as the IDO inhibitor.

The invention belongs to the field of pharmaceutical chemistry and relates to a 1, 2, 3-triazole compound, comprising 4-(2-bromophenyl)-1H-1, 2, 3-triazole and 4-(2-chlorphenyl)-1H-1, 2, 3-triazole. The result of an inhibitory activity test of indoleamine 2, 3-dioxygenase indicates that the disclosed 1, 2, 3-triazole compound used as the indoleamine 2, 3-dioxygenase inhibitor has broad prospect of application and can be applied to the treatment of diseases with indoleamine 2, 3-dioxygenase-mediated tryptophan metabolic pathway pathological characteristics, including cancer, AIDS (Acquired Immure Deficiency Syndrome), Alzheimer disease, tristimania, cataract and other critical diseases.

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and / or inflammatory disorders utilizing the compounds of the invention.

The present invention relates to a pharmaceutical composition for treatment and / or prevention of diseases, use and a use thereof. Specifically, the invention relates to an application of an IDO (indoleamine 2, 3-dioxygenase) inhibitor containing a 1, 2, 5-oxadiazole structure to disease treatment and / or prevention in combination with other drugs. Specifically, the invention relates to a compound which can be used as an IDO inhibitor and contains a 1, 2, 5-oxadiazole structure, or an isomer, metabolite, stable isotope derivative, prodrug, pharmaceutically acceptable salt, hydrate, solvate, eutectic substance or polymorph thereof, and other drugs for combined medication. Compared with single medication, the combined medication has a good synergistic effect on abnormal cell proliferation diseases.

The invention discloses compounds represented by a general formula (I) shown in the description, wherein in the formula (I), A and B are respectively a six-membered cyclic compound containing D1, D2,D3 and D4 and a six-membered cyclic compound containing D5, D6, D7 and D8. The invention also disclose an indoleamine-2,3-dioxygenase and / or tryptophan-2,3-dioxygenase inhibitor containing the above compounds and the application of the compounds in preparation of medicaments for treating cancers. The compounds provided by the invention can effectively inhibit cell proliferation, and have good therapeutic effects on various diseases such as the cancers, significant therapeutic effects on breast cancer, cervical cancer, colon cancer, lung cancer, stomach cancer, rectal cancer, pancreatic cancer,brain cancer, skin cancer, oral cancer, prostate cancer, bone cancer, kidney cancer, ovarian cancer, bladder cancer, liver cancer, fallopian tube tumors, ovarian tumors, peritoneal tumors, stage IV melanoma, glioma, neuroblastoma, hepatocellular carcinoma, mastoid renal tumors, head and neck tumors, leukemia, lymphoma, myeloma and non-small cell lung cancers, and very broad application prospects.

The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a selective inhibitor of indoleamine 2, 3-dioxygenase 1 (IDO1), and the use of the combination therapies for the treat-ment of cancer, and in particular for treating cancers that express PD-L 1.

Disclosed herein are 5 or 8-substituted imidazo[1,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[1,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo[1,5-a]pyridines that can be useful for inhibiting indoleamine 2,3-dioxygenase and / or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

The invention discloses an application of azatryptanthrin derivatives as IDO1 (indoleamine 2,3-dioxygenase) and / or TDO (tryptophan 2,3-dioxygenase) inhibitors. The structure of the derivatives is shown as the general formula (I) in the description, wherein substituents are defined in detail in the description. The compounds shown as the general formula (I) have an inhibition effect on IDO1 and / or TDO and can be used for treating diseases having pathological characteristics of IDO1 and / or TDO mediated tryptophan metabolism, and the diseases include but are not limited to tumors, autoimmune diseases, infectious diseases, Alzheimer disease, depression and anxiety disorder.

The invention relates to application of mesenchymal stem cells in preparing medicine for treating neurodegenerative diseases. It is revealed for the first time that the relieving effect of mesenchymal stem cells on neurodegenerative diseases can be significantly promoted after mesenchymal stem cells are treated with inflammatory factors. The invention further provides a pharmaceutical composition containing the cells. The invention further discloses the key role of indoleamine 2,3-dioxygenase in treating neurodegenerative diseases with mesenchymal stem cells.

The invention relates to a genetic engineering strain capable of efficiently synthesizing melatonin and a construction method and application of the genetic engineering strain. In view of the problemsof biosynthesis of the melatonin at present that the yield is low and consumed time is long, the invention provides the genetic engineering strain capable of efficiently synthesizing the melatonin. The genetic engineering strain over-expresses a tryptophane synthase gene TRP5, an iodolamine-2,3-dioxygenase gene BNA2 is knocked out, and saccharomyces cerevisiae serves as a starting strain. The melatonin is synthesized by using the genetic engineering strain constructed by the method, the efficiency of synthesis is increased obviously, the maximum yield reaches 25.7mg / L and is increased by 12 times or more compared with that of original strains. The genetic engineering strain can be applied to industrial production of the melatonin.

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3 -dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and / or inflammatory disorders utilizing the compounds of the invention.

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and / or inflammatory disorders utilizing the compounds of the invention.

The invention relates to the field of drugs, in particular to a carbamidine derivative containing a furan structure and a composition of the carbamidine derivative. The derivative and the compositionthereof can be used for preparing drugs for treating a pathologic characteristic disease with an indoleamine 2,3-dioxygenase mediated tryptophan metabolic pathway. The invention further relates to a method for preparing the derivative and an intermediate thereof.

The invention discloses the use of azatryptanthin derivatives as IDO1 and / or TDO inhibitors. The derivatives are represented by the general formula (I), wherein the definition of each substituent is detailed in the description. The compound represented by the general formula (I) has inhibitory effect on indoleamine-2,3-dioxygenase 1 (IDO1) and / or tryptophan-2,3-dioxygenase (TDO), and can be used For the treatment of diseases with pathological features of tryptophan metabolism mediated by IDO1 and / or TDO, including but not limited to tumors, autoimmune diseases, infectious diseases, Alzheimer's disease, depression, anxiety.

The invention relates to a compound, which is one or a plurality of indoleamine 2,3-dioxygenase inhibitors. The present invention further provides a pharmaceutical component containing the compound, apreparation containing the compound, and uses of the indoleamine 2,3-dioxygenase inhibitors, wherein the compound can be used for treating indoleamine 2,3-dioxygenase related symptoms through singlemedication or combination with other drugs.