30 results about "Autotaxin" patented technology

To provide a peritoneal function evaluation marker, peritoneal function evaluation kit, and peritoneal dialysis drainage measurement method that can measure D / P Cr or D / D0 Glu by a PET or an amount of drainage by a peritoneal dialysis upon implementing an ordinary peritoneal dialysis, by a simple method, and by a simple index, or can evaluate a peritoneal function equaling to a measurement of dip Na, and what is more, can take an appropriate action to prolong a peritoneal dialysis period as long as possible, and can contribute to improvement in quality of life of a patient, and an extention of the peritoneal dialysis period and life expectancy period, and improvement in medical economy.SOLUTION: A peritoneal function evaluation marker is composed of autotaxin. A peritoneal function evaluation kit includes a reagent that detects the peritoneal function evaluation marker composed of the autotaxin. A peritoneal dialysis drainage measurement method is configured to detect the peritoneal function evaluation marker composed of the autotaxin in peritoneal dialysis drainage.SELECTED DRAWING: None

The present invention provides: a novel azabicyclo derivative compound, a hydrate thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating autotaxin-related diseases, comprising the same as an active ingredient. The azabicyclo derivative compound according to the present invention exhibits excellent inhibitory activity against autotaxin, and thus can be used for treating and preventing diseases associated with autotaxin inhibition. The compounds can be used for treating diseases such as fibrotic diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, metabolic diseases, cancers and cancer metastases, ocular diseases, cholestatic and other forms of chronic pruritus, and acute or chronic organ transplant rejection.

An anhydrous crystalline form of autotaxin (ATX) inhibitor and methods to prepare the same. Pharmaceutical formulations comprising autotaxin (ATX) inhibitor or a pharmaceutically acceptable salt thereof

The present invention relates to a novel benzimidazolone derivative compound as an autotaxin inhibitor.

The present invention provides a novel heterocyclic compound, a hydrate thereof, a solvate thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a disease associated with autotaxin activity. The heterocyclic compound of the present invention exhibits excellent inhibitory activity against autotaxin, and can be usefully used in the treatment and prevention of diseases associated with the inhibition of autotaxin, such as fibrotic diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, metabolic diseases, cancer and cancer metastasis, ocular diseases, cholestatic forms and other forms of chronic pruritus, and acute or chronic organ transplant rejection.

The present invention provides a novel heterocyclic compound, a hydrate thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for preventing or treating an autotaxin activity-related disease containing the same as an active ingredient. The heterocyclic compound according to the present invention exhibits excellent inhibitory activity against autotaxin, and is useful for the treatment and prevention of fibrotic diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, metabolic diseases, cancer and cancer metastasis, eye diseases, cholestatic forms and other forms of chronic pruritus, and acute or chronic organ transplant rejection reactions, which are autotaxin-inhibiting related diseases.

Disclosed herein are autotaxin inhibitor compounds, polymorphic forms, pharmaceutical compositions, and methods of use and preparation thereof. Some embodiments relate to crystalline forms of Compound 1 and salts thereof. # imgabs0 #

The present invention relates to a compound having autotaxin (ATX) inhibitory activity, a pharmaceutical composition comprising same as an active ingredient, and pharmaceutical uses thereof. The compound according to the present invention exhibits excellent ATX inhibitory activity and can be effectively used for preventing or treating ATX activity-related diseases.

Disclosed herein are autotaxin inhibitor compounds, polymorphic forms thereof, pharmaceutical compositions, and methods of use and preparation. Some embodiments relate to crystalline forms of Compound 1 and salts thereof. 【Chemical 1】 JPEG2025516335000046.jpg7689

The present invention relates to novel pyridazines, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment and / or prevention of diseases and disorders mediated by Autotaxin.

The pharmaceutical compound or the pharmaceutically acceptable salt thereof is used for preventing or treating the following diseases by simultaneously inhibiting autotaxin (ATX) and activating peroxisome proliferator-activated receptor gamma (PPAR gamma): a) fibroproliferative diseases, in particular interstitial lung diseases (ILD) and / or liver diseases, and b) fibroproliferative diseases, in particular interstitial lung diseases (ILD) and / or liver diseases; the present invention relates to a pharmaceutical composition for treating hepatitis, such as various hepatitis and / or non-alcoholic fatty liver disease (NAFLD) and / or non-alcoholic steatohepatitis (NASH) and / or cirrhosis, where said ILD may be a primary disease, preferably idiopathic pulmonary fibrosis and / or sarcoidosis and / or interstitial pneumonia, or said ILD is a complication associated with an autoimmune and / or inflammatory and / or metabolic disease, or a pharmaceutical composition comprising said ILD. Preferably rheumatoid arthritis ILD and / or scleroderma ILD and / or myositis ILD and / or diabetes ILD and / or cardiovascular disease ILD; and / or b) inflammatory and / or autoimmune diseases, preferably rheumatoid arthritis and / or scleroderma; and / or c) cancer, in particular lung and / or hepatocellular carcinoma and / or pancreatic cancer and / or glioblastoma and / or neuroblastoma; and / or d) a metabolic disease, in particular diabetes mellitus type 1 and / or diabetes mellitus type 2 and / or obesity, having a formula selected from the group consisting of formulae (A), (B), (C), (D), (E), (F), (G) and (H).

Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.

Disclosed herein are autotaxin inhibitor compounds, polymorphic forms, pharmaceutical compositions, and the method of use and preparation thereof. Some embodiments relate to crystalline forms of Compound 1 and salts thereof.

An autotaxin (ATX) inhibitor or a pharmaceutically acceptable salt thereof for use in a method of treatment of pancreatic cancer in a patient, optionally wherein the method further comprises administration of a TGF-β pathway inhibitor and / or an additional chemotherapeutic agent.

The present invention provides: a novel heterocyclic compound, a hydrate thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating diseases associated with autotaxin activity, comprising the same as an active ingredient. The heterocyclic compound according to the present invention exhibits excellent inhibitory activity against autotaxin, and thus can be used for treating and preventing diseases associated with autotaxin inhibition. The compounds can be used for treating diseases such as fibrotic diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, metabolic diseases, cancers and cancer metastases, ocular diseases, chronic pruritus in cholestatic and other forms, and acute or chronic organ transplant rejection.

Disclosed herein are autotaxin inhibitor compounds, polymorphic forms, pharmaceutical compositions, and the method of use and preparation thereof. Some embodiments relate to crystalline forms of Compound 1 and salts thereof.

Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.

To provide means for treating inflammatory airway or fibrotic diseases.SOLUTION: The present invention relates to N-methyl, N-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (ATX) modulators for the treatment of inflammatory airway or fibrotic diseases such as e.g. idiopathic lung disease (IPF) or systemic sclerosis (SSc). The present description discloses exemplary compounds (e.g. pages 57 to 75; examples 1.1 to 5) as well as relevant biological data thereof (e.g. pages 15 to 21, tables 1 to 9). An exemplary compound is e.g. 1-(6-(4-(((6-((6-(trifluoromethyl) pyridin-3-yl)methoxy)pyridazin-3-yl)amino)methyl)phenyl)-2,6- diazaspiro[3.3]heptan-2-yl)ethan-1-one (example 1.1).SELECTED DRAWING: None

The present invention provides novel azabicycle derivative compounds, their hydrates, their solvates, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions for the prevention or treatment of autotaxin-related diseases containing them as active ingredients. The azabicycle derivative compounds according to the present invention exhibit excellent inhibitory activity against autotaxin and can be usefully used for the treatment and prevention of autotaxin inhibition-related diseases, including fibrous diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, metabolic diseases, cancer and cancer metastasis, ocular diseases, cholestatic and other forms of chronic pruritus, and acute or chronic organ transplant rejection.

To provide means for treating inflammatory airway or fibrotic diseases.SOLUTION: The present invention relates to N-methyl, N-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (ATX) modulators for the treatment of inflammatory airway or fibrotic diseases such as e.g. idiopathic lung disease (IPF) or systemic sclerosis (SSc). The present description discloses exemplary compounds (e.g. pages 57 to 75; examples 1.1 to 5) as well as relevant biological data thereof (e.g. pages 15 to 21, tables 1 to 9). An exemplary compound is e.g. 1-(6-(4-(((6-((6-(trifluoromethyl) pyridin-3-yl)methoxy)pyridazin-3-yl)amino)methyl)phenyl)-2,6- diazaspiro[3.3]heptan-2-yl)ethan-1-one (example 1.1).SELECTED DRAWING: None

This invention relates to a novel benzimidazolon derivative compound as an autotaxin inhibitor.

The present invention provides a solid form of a compound of formula (I) or a solvate thereof having autotaxin (ATX) inhibitory activity, wherein the solid form comprises a crystalline form and / or an amorphous form. The crystalline form comprises two non-solvate crystalline forms: crystalline form A and crystalline form L; six hydrate crystalline forms: crystalline form B (dihydrate), crystalline form D (trihydrate), crystalline form G (tetrahydrate), crystalline form H (monohydrate), crystalline form K (dihydrate) and crystalline form M-1 (monohydrate); and seven solvate crystalline forms: crystalline form C (hemitoluene solvate), crystalline form E (chloroform solvate), crystalline form N (dichloromethane solvate), crystalline form P (isopropanol solvate), crystalline form J-1 (hemisec-butyltetrahydrofuran solvate), crystalline form J-2 (methyl isobutyl ketone solvate) and crystalline form M-2 (acetonitrile solvate). The solid form can be used for treating and / or preventing diseases related to autotaxin (ATX).

The present invention relates to N-methyl, N-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (ATX) modulators for the treatment of inflammatory airway or fibrotic diseases such as e.g. idiopathic lung disease (IFF) or systemic sclerosis (SSc). The present description discloses the preparation of exemplary compounds (e.g. pages 37 to 45; examples 1.1 to 1.13) as well as relevant biological data thereof (e.g. pages 12 to 17, tables 1 to 9). An exemplary compound is e.g. 1-[4-(4-{1-[(6-{[6-(trifluoromethyl) pyridin-3-yl]methoxy}pyridazin-3-yl)amino]cyclopropyl}-phenyl) piperazin-1-yl]ethan-1-one (example 1.1).

The present invention relates to a pharmaceutical composition comprising an autotaxin inhibitor as an active ingredient for preventing or treating calcification-related diseases. Specifically, the autotaxin inhibitor is useful for the prevention or treatment of calcification-related diseases such as vascular calcification, vascular stiffening, vascular inflammation, vascular fibrosis, vascular stenosis, valvular calcification, valvular inflammation, valvular fibrosis, aortic valve stenosis, and calcinosis cutis.

A method for treating or preventing a disease involving autotaxin including administering a carboxylic acid compound of formula (1)or a pharmacologically acceptable salt thereof to a patient in need thereof.

To provide a novel compound having autotaxin (ATX) inhibitory activity for the treatment of diseases involving ATX, specifically kidney diseases, liver diseases, chronic inflammatory disorders or inflammatory diseases, respiratory diseases, vascular and cardiovascular diseases, fibrotic diseases, and cancers, or a pharmaceutically acceptable salt, a solvate or a salt of the solvate, or a composition including the compound.SOLUTION: The present invention discloses, for example, an aminoazine amide compound represented by the following formula, or a pharmaceutically acceptable salt, a solvate or a salt of the solvate, or a composition including the compound.SELECTED DRAWING: None

Disclosed are a tricyclic derivative and a preparation method therefor and an application thereof. Specifically, disclosed are a compound shown in formula (I) and an optical isomer thereof or a pharmaceutically acceptable salt thereof, and an application of the compound as an Autotaxin inhibitor.

The present invention provides a new class of aromatic heterocyclic compounds as ATX (Autotaxin) inhibitors, pharmaceutical compositions comprising the compounds, and the use of the compounds and compositions in the treatment of diseases in mammals having a pathological characteristic of increased expression of ATX (Autotaxin), wherein the compounds have the structure of Formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, tautomer, nitroso, metabolite, prodrug, or mixture thereof; wherein, R 1 , Ar 1 , Ar 2 , Ar 3 , W, Y, Z and Cy have the definitions described in the present invention.

The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same.The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.