50 results about "PTPN1" patented technology

Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatases, such as protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders, and conditions that respond favorably to PTPN1 or PTPN2 inhibitor treatment, such as cancer or metabolic diseases.

Provided herein are degrader compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders, and conditions favorably responsive to PTPN1 or PTPN2 degrader treatment, e.g., a cancer or a metabolic disease.

Provided herein are methods using a combination comprising a protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and an additional therapeutic agent for treating diseases favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.

The invention discloses a thiadiazolidinone compound and a preparation method and application thereof, the thiadiazolidinone derivative is a compound with a structure shown as a general formula (I) or pharmaceutically acceptable salt of the compound, and the invention further discloses application of the thiadiazolidinone derivative in medicine for treating PTPN2 / PTPN1 mediated diseases. The compound disclosed by the invention has obvious inhibitory activity on PTPN2 / PTPN1 phosphatase, has important influence on occurrence and development of tumors and immune response, can also be used in combination with an immunosuppressant to treat related immune diseases, can be developed into an anti-tumor drug with high activity, good selectivity and small toxic and side effects, and has the characteristics of strong plasticity and great future modification potential. # imgabs0 #

Provided herein are compounds, compositions, and methods that are useful for inhibiting protein tyrosine phosphatases, such as protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and that are useful for treating related diseases, disorders, or conditions, such as cancer or metabolic diseases, that respond favorably to treatment with a PTPN1 or PTPN2 inhibitor.

The invention belongs to the field of medical chemistry, and particularly discloses a protein tyrosine phosphatase inhibitor, such as type 2 non-receptor protein tyrosine phosphatase (PTPN2) and / or type 1 non-receptor protein tyrosine phosphatase (PTPN1) inhibitor, a pharmaceutical composition and application thereof. The invention discloses a method for treating related diseases such as cancers and metabolic diseases by using the protein tyrosine phosphatase inhibitor.

The present invention relates to novel compounds, to said compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of PTPN2 and / or PTPN1, yet more in particular for the prevention or treatment of cancer or metabolic diseases. The present invention also relates to a method for the prevention or treatment of said diseases comprising the use of the novel compounds. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds as well as to said compositions or preparations for use as a medicine, more preferably for the prevention or treatment of diseases mediated by activity of PTPN2 and / or PTPN1, yet more in particular for the prevention or treatment of cancer or metabolic diseases. The present invention also relates to processes for the preparation of said compounds.

Provided in the present invention is a class of compounds. Specifically, provided in the present invention is a compound having a structure as shown in the following formula (I), or an optical isomer, pharmaceutically acceptable salt, prodrug, deuterated derivative, hydrate, or solvate thereof. The compound is capable of effectively inhibiting PTPN2 and / or PTPN1, and can be used for treating or preventing diseases or conditions associated with the activity or expression level of PTPN2 and / or PTPN1.

The present invention relates to novel compounds of Formulas (I) and (III), with said compounds for use as a medicament, more particularly for the prevention or treatment of diseases mediated by PTPN2 and / or PTPN1 activity, and even more particularly for the prevention or treatment of cancer or metabolic diseases. The present invention also relates to a method for the prevention or treatment of such diseases comprising the use of the novel compounds. The present invention further relates to pharmaceutical compositions or combination preparations of the novel compounds, as well as to said compositions or preparations for use as a medicament, most preferably for the prevention or treatment of diseases mediated by PTPN2 and / or PTPN1 activity, and even more particularly for the prevention or treatment of cancer or metabolic diseases.The invention also relates to processes for the preparation of said compounds.

The present invention is generally directed to inhibitors of protein tyrosine phosphatase enzymes (PTPN1 and / or PTPN2) useful in the treatment of diseases and disorders modulated by said enzymes and having the Formula (I):

The invention provides a CD40 targeted medicine for realizing tumor immunodiagnosis and treatment by regulating PTPN1 / PTPN2 as well as a preparation method and application of the CD40 targeted medicine. The drug comprises a drug-loading membrane layer, perfluorinated compound PFC and glycerin are wrapped in the drug-loading membrane layer, the drug-loading membrane layer is coupled with a CD40 agonist, and the drug-loading membrane layer comprises phospholipid, cholesterol, a functionalized lipid polymer and AC484. The drug shows excellent biological stability and can be delivered to tumor tissue through a respiratory tract or a vein route; according to the medicine, accumulation and distribution of the medicine in the body are dynamically monitored through a 1H / 19F magnetic resonance imaging technology, noninvasive evaluation of the tumor state is achieved, immunotherapy is accurately guided, and therefore the tumor treatment effect is remarkably improved.

The invention discloses a 1, 2, 5-thiadiazole compound substituted by a 4-position tetrahydronaphthalene or tetrahydroisoquinoline structure and application of the 1, 2, 5-thiadiazole compound, and belongs to the field of medicines. The invention provides a 4-position tetrahydronaphthalene or tetrahydroisoquinoline structure substituted 1, 2, 5-thiadiazole compound with a structure shown as a formula (I) or a pharmaceutically acceptable salt thereof, and the compound has excellent protein tyrosine phosphatase inhibitory activity and can be used for preparing a medicine for preventing and treating diseases. A method of treatment of a disease or condition (e.g., cancer, type 2 diabetes, obesity, metabolic disease or any other disease, condition or condition) that is positively responsive to a protein tyrosine phosphatase (PTPN2 or PTPN1) inhibitor is provided.

The present invention relates to a benzo ring-containing compound as a PTPN1 and / or PTPN2 inhibitor and use thereof, and particularly relates to a compound of formula (I), a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, a method for preparing same, and use thereof in the preparation of a medicament for treating a PTPN1 and / or PTPN2-related disease.

The present invention relates to antisense oligonucleotides (ASO) for use in treating, preventing, or ameliorating the progression of conditions such as type 2 diabetes mellitus (T2DM) and insulin resistance, leptin resistance, and obesity, Rater Syndrome, and cancer. Specifically, a thiomorpholino-containing ASO targets a protein tyrosine phosphatase non-receptor type 1 (PTPN1) gene transcript and induces exon skipping (including exon 2) of the transcript during RNA processing, thereby inhibiting expression of the protein tyrosine phosphatase-1B (PTP1B) protein.

The present invention relates to a double bond substituent containing compound serving as a PTPN1 and / or PTPN2 inhibitor, and a use thereof, and in particular to a compound represented by formula (I), a tautomer, a stereoisomer, or a pharmaceutically acceptable salt thereof, and a preparation method therefor, and a use in the preparation of a drug for treating diseases related to PTPN1 and / or PTPN2.

To provide compounds and compositions for treating cancer, type-2 diabetes, obesity, a metabolic disease, or any other disease, disorder or ailment favorably responsive to PTPN2 or PTPN1 inhibitor treatment, and methods of treating the diseases.SOLUTION: Provided herein are: compounds with an effect of inhibiting PTPN2 and / or PTPN1 illustrated by the compound Y in the figure; pharmaceutically acceptable compositions comprising the compounds and pharmaceutically acceptable carriers; and methods of treatment by administering the compositions.SELECTED DRAWING: None

The invention relates to a benzoring-containing compound serving as a PTPN1 and / or PTPN2 inhibitor and application thereof, in particular to a compound shown in a formula (I), a tautomer, a stereoisomer or pharmaceutically acceptable salt of the compound, a preparation method of the compound, and application of the compound to preparation of drugs for treating PTPN1 and / or PTPN2 related diseases. (I)

Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders, and conditions favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.

Provided herein are useful for degrading protein tyrosine phosphatase, such as protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and useful for treating related diseases, disorders and conditions that contribute to the treatment of PTPN1 or PTPN2 degrading agents, degradation agent compounds, compositions, and methods for treating cancer, such as cancer or metabolic diseases.

The present invention relates to novel compounds, to said compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of PTPN2 and / or PTPN1, yet more in particular for the prevention or treatment of cancer or metabolic diseases. The present invention also relates to a method for the prevention or treatment of said diseases comprising the use of the novel compounds. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds as well as to said compositions or preparations for use as a medicine, more preferably for the prevention or treatment of diseases mediated by activity of PTPN2 and / or PTPN1, yet more in particular for the prevention or treatment of cancer or metabolic diseases. The present invention also relates to processes for the preparation of said compounds.

The invention relates to a compound containing double bond substitution as a PTPN1 and / or PTPN2 inhibitor and application thereof, in particular to a compound shown in a formula (I), a tautomer, a stereoisomer or pharmaceutically acceptable salt of the compound, a preparation method of the tautomer, the stereoisomer or the pharmaceutically acceptable salt of the compound, and application of the tautomer, the stereoisomer or the pharmaceutically acceptable salt in preparation of drugs for treating PTPN1 and / or PTPN2 related diseases.

Provided herein are methods of using a combination comprising protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1) and an additional therapeutic agent to treat a disease (e.g., cancer or metabolic disease) that produces an advantageous response to PTPN1 or PTPN2 inhibitor treatment.

The invention discloses a novel BimBH3 mimic peptide analogue constructed on the basis of a nailing and fatty acid acylation dual-modification strategy and application of the novel BimBH3 mimic peptide analogue serving as a PTPN1 inhibitor to development of a long-acting hypoglycemic drug. The structural general formula of the BimBH3 mimic peptide analogue is as shown in a formula I. The structural general formula of the BimBH3 mimic peptide analogue is as shown in a formula I. The invention provides the BimBH3 mimic peptide analogue with a novel structure, and the BimBH3 mimic peptide analogue is constructed by adopting a nailing and fatty acid acylation dual-modification strategy and has the structural general formula as shown in the formula I. The invention further provides a preparation method of the BimBH3 mimic peptide analogue. On the basis of a BimBH3 functional domain core sequence, the novel BimBH3 mimic peptide analogue has target inhibitory activity, metabolic stability and in-vivo action durability through second-site lysine substitution, N-terminal palmitic acid conjugation and fifth, sixth and ninth site glutamic acid side chain mediated synthesis ring nailing modification, and the synthesis ring nailing mode is molecular lactam cyclization. Experiments show that the compound can efficiently inhibit PTPN1 activity, has a long-acting hypoglycemic effect in a type 2 diabetes animal model, and has the potential of being developed into a long-acting antidiabetic drug which is administered once a week. The invention also discloses a solid-phase synthesis preparation method of the compound and application of the compound as a potential PTPN1 inhibitor drug.

The present invention is generally directed to inhibitors of protein tyrosine phosphatase enzymes (PTPN1 and / or PTPN2) useful in the treatment of diseases and disorders modulated by said enzymes and having the Formula (I). Further disclosed a method of treating a disease or disorder associated with PTPN1 / PTPN2, comprising of administering to a subject a compound or a pharmaceutical composition.

The present invention belongs to the technical field of medicine, and specifically relates to a PTPN2 / PTPN1 inhibitor, a preparation method therefor, and the medical use thereof. Provided are a compound represented by formula (I), a composition thereof and the use thereof. The compound can be used for treating or preventing PTPN2 / PTPN1-mediated diseases or disorders.

To provide compounds, compositions and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders and conditions favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.SOLUTION: The invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, ester, N-oxide, stereoisomer or isotopically enriched variant thereof.SELECTED DRAWING: None

Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders, and conditions favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.

An isolated or purified antisense oligomer targeted to a nucleic acid molecule encoding a PTPN1 pre-mRNA, wherein the antisense oligomer inhibits expression of PTP1B.

Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders and conditions favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.