46 results about "Autotaxin" patented technology

The present invention discloses compounds according to Formula I:Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein.The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and / or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and / or abnormal angiogenesis associated diseases by administering the compound of the invention.

Novel and optimized classes of pipemidic acid derivative compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes of compounds exhibit exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include thioureas, diphenyldiazerenes, xanthenes, and isoindoles and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and / or prophylaxis of physiological and / or pathophysiological conditions, which are caused, mediated and / or propagated by increased lysophosphatic acid levels and / or the activation of autotaxin, in particular of different cancers.

Provided is a compound superior in an autotaxin inhibitory action and the like, effective as a prophylactic or therapeutic drug for diseases involving ATX. The present invention relates to a compound represented by the following formula (I):[wherein each symbol is as described in the DESCRIPTION], which has a superior autotaxin inhibitory action and is useful as a prophylactic or therapeutic drug for diseases involving ATX.

The present invention relates to pyridopyrimidine derivatives according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and / or prophylaxis of physiological and / or pathophysiological conditions, which are caused, mediated and / or propagated by increased lysophosphatic acid levels and / or the activation of autotaxin, in particular of different cancers.

The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and / or prophylaxis of physiological and / or pathophysiological conditions, which are caused, mediated and / or propagated by increased lysophosphatic acid levels and / or the activation of autotaxin, in particular of different cancers.

Stabilized benzyl phosphonic acid and naphthyl phosphonic acid analog compounds are effective in inhibiting the activity of autotaxin.

The present invention discloses compounds according to Formula I:Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and / or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and / or abnormal angiogenesis associated diseases by administering the compound of the invention.

A compound of formula (I) wherein variables are as defined herein having an autotaxin inhibitory effect and a pharmaceutical composition comprising the same.

The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.

The present invention relates, in general, to autotaxin. In particular, the present invention relates to a DNA segment encoding autotaxin; recombinant DNA molecules containing the DNA segment; cells containing the recombinant DNA molecule; a method of producing autotaxin; antibodies to autotaxin; and identification of functional domains in autotaxin.

A screening method is provided for antibody specifically recognizing naturally-occurring form of human autotaxin in a state in which it is present in the body without being denatured, comprising the steps of: binding a binding factor capable of capturing a candidate antibody of the antibody to a solid phase; binding the candidate antibody of the antibody to the binding factor; allowing naturally-occurring form of human autotaxin to react on a system in which the candidate antibody has reacted; and selecting an antibody that specifically recognizes the naturally-occurring form of human autotaxin by using as an indicator thereof the binding strength of the naturally-occurring form of human autotaxin to the antibody. Moreover, a detecting method for malignant lymphoma is provided comprising: measuring the concentration of autotaxin in a human specimen, and judging to be a malignant lymphoma in the case that value exhibits a significantly higher value than normal values comprised of measured values from normal healthy subjects.

Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.

The present invention provides an aptamer binding to an autotaxin, which contains a nucleotide sequence represented by the formula:(SEQ ID NO: 42)GWAACAGGUUUUGCUwherein W is A or U (provided uracil is optionally thymine), and which is the following (a) or (b):(a) an aptamer wherein, in the nucleotides contained in the aptamer,(i) the 2′-position of the ribose of each pyrimidine nucleotide is a fluorine atom,(ii) the 2′-position of the ribose of each purine nucleotide is a hydroxy group;(b) the aptamer of (a), wherein(i) the fluorine atom at the 2′-position of the ribose of each pyrimidine nucleotide is independently unsubstituted, or substituted by an atom or group selected from the group consisting of a hydrogen atom, a hydroxy group and a methoxy group,(ii) the hydroxy group at the 2′-position of the ribose of each purine nucleotide is independently unsubstituted, or substituted by an atom or group selected from the group consisting of a hydrogen atom, a methoxy group and a fluorine atom.

The present invention relates to compounds of formula I, wherein A1, A2, A3, R1, R2, R3, R4, R5, R6, L, Ar and Q are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions (e.g. fibrosis) in which ATX activity is implicated.

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.

The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX) / histone deacetylase (HDAC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.

The present invention discloses compounds according to Formula I:Wherein R1a, R1b, R2, R4, R5, R6, R7, R8, W, X, Y, Z, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and / or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and / or abnormal angiogenesis associated diseases by administering the compound of the invention.

Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include thioureas, diphenyldiazerenes, xanthenes, and isoindoles and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.