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30 results about "JNK Pathway" patented technology
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JNK (c-Jun N-terminal kinase) is a group of kinases belong to the mitogen-activated protein kinase family and also play a role in T cell differentiation and the cellular apoptosis pathway.
Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto
Owner:SIGNAL PHARMA LLC
Methods for Treating Pressure Induced Optic Neuropathy, Preventing Neuronal Degeneration and Promoting Neuronal Cell Survival Via Administration of LINGO-1 Antagonists and TrkB Agonists
InactiveUS20100297121A1High activityPromote cell activationOrganic active ingredientsSenses disorderNeuronal degenerationMedicine
This invention relates to methods for promoting neuronal survival and regeneration using LINGO-1 antagonists and TrkB agonists. Additionally, the invention relates to methods for treating pressure induced optic neuropathies using LINGO-1 antagonists. The invention also relates generally to methods for increasing TrkB activity and inhibiting JNK pathway signaling using a LINGO-1 antagonist.
Owner:BIOGEN MA INC
Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases
The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl which is substituted with at least one ionizable moiety to which a lipophilic chain is attached and which is containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.
Owner:MERCK SERONO SA
Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith
Provided herein are Aminopurine Compounds having the following structure: (I) wherein R<1 >, R<2> and and R<3> are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
Owner:SIGNAL PHARMA LLC +1
Haloaryl Substituted Aminopurines, Compositions Thereof, And Methods Of Treatment Therewith
Provided herein are Aminopurine Compounds having the following structure: (I) wherein R<1 >, R<2> and and R<3> are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
Owner:SIGNAL PHARMA LLC +1
Methods and compositions for inhibition of axonal degeneration by modulation of the dlk/jnk pathway
InactiveUS20100056609A1Shorten the progressInhibit axonal degenerationCompound screeningOrganic active ingredientsWallerian degenerationAxon degeneration
Methods of reducing Wallerian degeneration are disclosed. These methods comprise inhibiting expression or activity of a mixed lineage kinas such as a dual leucine-zipper-bearing kinase (DLK), inhibiting expression or activity of a molecule acting downstream from DLK, such as a c-Jun N-terminal kinase (JNK), or a combination thereof. Further disclosed are methods of screening candidate compounds for DLK inhibition activity. These methods comprise providing a neuronal culture comprising a plurality of axons; contacting the culture with a candidate compound and with an axon degeneration-triggering agent; and comparing axonal degeneration in the culture to a control culture comprising the axon degeneration-triggering agent but not the candidate compound.
Owner:WASHINGTON UNIV IN SAINT LOUIS
Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases
The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.
Owner:MERCK SERONO SA
Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases
Owner:MERCK SERONO SA
Methods of modulating inflammatory cell recruitment and gene expression using haloaryl substituted aminopurines
Provided herein are Aminopurine Compounds having the following structure:wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
Owner:SIGNAL PHARMA LLC
Methods and compositions for inhibition of axonal degeneration by modulation of the dlk/jnk pathway
Owner:WASHINGTON UNIV IN SAINT LOUIS
Benzazole derivatives and their use as JNK modulators
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and / or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation.X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl;G is an unsubstituted or substituted pyrimidinyl group.
Owner:MERCK SERONO SA
Methods for Treating Pressure Induced Optic Neuropathy, Preventing Neuronal Degeneration and Promoting Neuronal Cell Survival Via Administration of Lingo-1 Antagonists and TrkB Agonists
InactiveUS20160354465A1High activityPromote cell activationOrganic active ingredientsSenses disorderNeuronal degenerationMedicine
This invention relates to methods for promoting neuronal survival and regeneration using LINGO-1 antagonists and TrkB agonists. Additionally, the invention relates to methods for treating pressure induced optic neuropathies using LINGO-1 antagonists. The invention also relates generally to methods for increasing TrkB activity and inhibiting JNK pathway signaling using a LINGO-1 antagonist.
Owner:BIOGEN MA INC
Serum-free medium for mesenchymal stem cells
PendingCN113403271ACulture processMammal material medical ingredientsMesenchymal stem cellBiochemistry
The invention belongs to the field of biological medicines and relates to a serum-free medium for mesenchymal stem cells. The serum-free medium provided by the invention comprises a basic medium and additive components, wherein the additive components comprise a JNK pathway inhibitor, an ERK1 / 2 pathway inhibitor, a P38MAPK pathway inhibitor and aminoethanol; the JNK pathway inhibitor comprises but is not limited to SP600125; the ERK1 / 2 pathway inhibitor comprises but is not limited to PD0325901; and the P38MAPK pathway inhibitor comprises at least one of SB202190, SB203580 and BIRB796. The medium for mesenchymal stem cells disclosed by the invention does not contain FBS and does not contain any heterologous animal-derived component, the probability of cell contamination is reduced, and an effect of promoting MSC amplification is achieved.
Owner:国家卫生健康委科学技术研究所
Pharmaceutically active sulfonamide derivatives
The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6 membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.
Owner:MERCK SERONO SA
Arylsulfonamide derivatives as C-Jun-N-Terminal Kinases (JNK's) inhibitors
InactiveUS7683078B2Using treatment methodBiocideSenses disorderAutoimmune diseasePharmaceutical formulation
Owner:MERCK SERONO SA
Arylsulfonamide derivatives as c-jun-n-terminal kinases (jnk's) inhibitors
The present invention relates to sulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.Ar1 is a substituted or unsubstituted aryl or heteroaryl group;X is O or S, preferably O;Ar2 a substituted or unsubstituted arylene or heteroarylene group;R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group;
Owner:LAB SERONO SA
Application of chiral nano bionic photosensitive protein in preparation of medicine for promoting regeneration of damaged neuron axons
The invention relates to application of chiral nano bionic photosensitive protein in preparation of a medicine for promoting regeneration of axons of damaged neurons. Chiral nickel hydroxide ultra-small nanoparticles with characteristics similar to photosensitive protein are utilized, can penetrate through a blood brain barrier, enter damaged neuronal cells in the brain of an AD mouse and are combined with a cell membrane receptor, calcium ion flow is caused under the action of near-infrared light, and then a Wnt5a / JNK pathway is activated. Through illumination treatment for two months, the expression quantities of RhoA and ROCK in the brain of the AD mouse are reduced, axons of damaged neurons regrow, meanwhile, the content of marker protein in cerebrospinal fluid of the AD mouse is reduced, and the memory and cognitive abilities are recovered. The method can be applied to neuronal repair of AD model mice, and provides possibility for relieving central nervous system diseases such as neuronal injury.
Owner:JIANGNAN UNIV
Method of inhibiting the expression and/or the activity of jnk
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and / or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl; G is an unsubstituted or substituted pyrimidinyl group.
Owner:MERCK SERONO SA
Pharmaceutically active sulfonyl hydrazide derivatives
The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation. In Formula (I) Ar1 and Ar2 are independently from each other an unsubstituted or substituted aryl or beteroaryl group, X1 and X2 are independently from each other O or S; R1, R2, R3 are independently from each other hydrogen or a C1-C6-alkyl substituent or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; or R2 and R3 form a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8 membered heterocycle containing at least one heteroatom, or G is a substituted or unstibstituted C1-C6-alkyl group.
Owner:MERCK SERONO SA
Targeted anti-cancer polypeptide for inhibiting signal transmission of MKK7-JNK pathway and application of polypeptide
ActiveCN111217890AGood curative effectPromote growthPeptide/protein ingredientsPeptidesIn vivoTumor cells
The invention discloses a polypeptide for inhibiting signal transmission of an MKK7-JNK pathway in tumor cells and an application of the polypeptide. The polypeptide has an amino acid sequence shown in SEQ ID NO.1 in a sequence table. The polypeptide provided by the invention can enter cells, specifically bind to MKK7 in vivo and in vitro, further inhibit the signal transmission of the MKK7-JNK pathway by inhibiting the binding of the MKK7 to RACK1, and finally inhibit the growth of tumor cells.
Owner:深圳市健翔生物制药有限公司
Application of CTSG (cathepsin G) cell factor in preparation of medicaments to treat hepatic failure
InactiveCN110201149ASuppress deathInhibit apoptosisPeptide/protein ingredientsDigestive systemUpper gastrointestinalCathepsin G
The invention discloses application of a CTSG (cathepsin G) cell factor in the preparation of medicaments to treat hepatic failure. Death of mass hepatic cells occurs during the course of hepatic failure; the CTSG cell factor helps overcome the aforementioned problem. CTSG JNK (c-Jun N-terminal kinase) is one of MAPK (mitogen-activated protein kinase) family members; JNK pathway can inhibit apoptosis of hepatic cells by regulating the expression of CTSG. The CTSG cell factor can be applied to the preparation of medicaments to treat hepatic failure to significantly increase biochemical indexesof a patient, reduce bilirubin level, lower aminotransferase, improve the coagulation function, inhibit cell apoptosis, promote the regeneration of hepatic cells and bile duct cells, prevent occurrence of fatal complications, such as massive alimentary tract bleeding, severe hepatic encephalopathy and hepatorenal syndrome, extend the survival time of the patient significantly, and increase the survival rate.
Owner:杭州笙源生物科技有限公司
Composition for enhancing trail sensitivity comprising inhibitors for expression or activity of tip41 as a target gene of trail sensitizer
ActiveUS20120315284A1Shrink tumorIncreasing TRAIL sensitivityOrganic active ingredientsSenses disorderCancer preventionAdjuvant
The present invention relates to a pharmaceutical composition, including inhibitors for expression or activity of TIP41 protein, for prevention and treatment of cancer. When the liver cancer cell lines, showing resistance to TRAIL, are treated with TIP41 siRNA and TRAIL, apoptosis is induced in cancer cell. The same effect is found in cases of lung cancer and colon cancer with resistance against TRAIL. Moreover, this induction of apoptosis by TIP41 siRNA and TRAIL was confirmed in tumor xenograft, which was injected with Huh7 liver cancer cells and then was subjected to TIP41 siRNA transfection and TRAIL treatment. In addition, it was confirmed through animal experiments in which the tumor size has reduced and apoptosis was induced by treatment with TIP41 siRNA and TRAIL. Of note, MKK7 / JNK pathway was confirmed to mediate the apoptosis induced by the application of TIP41 siRNA and TRAIL. The apoptosis were verified to be caused by the activation of MKK7 / JNK signaling pathway. Taken together, the present invention provide the strong evidence that the pharmaceutical composition, including inhibitors for TIP41 expression or activity can be used for cancer prevention and treatment as well as an anti-cancer adjuvant. Taken together, the pharmaceutical composition comprising inhibitors for expression or activity of TIP41 protein may be used for prevention and treatment of cancer or as an anti-cancer adjuvant.
Owner:KOREA RES INST OF BIOSCI & BIOTECH
Application of PPAR (peroxisome proliferators-activated receptor) gamma cytokine to preparation of hepatic failure treatment drug
InactiveCN110279850ASuppress deathInhibit apoptosisPeptide/protein ingredientsDigestive systemAntioxidantHepatocyte apoptosis
The invention discloses an application of a PPAR (peroxisome proliferators-activated receptor) gamma cytokine to preparation of a hepatic failure treatment drug. The drug comprises a pharmaceutically acceptable excipient, antioxidant and carrier of the PPAR gamma cytokine. The problem that a large number of hepatocytes are dead in the course of hepatic failure can be solved by the PPAR gamma cytokine. PPAR gamma JNK (jun n-terminal kinase) is one of family members of MAPK, and a JNK pathway can inhibit hepatocyte apoptosis by regulating and controlling expression of PPAR gamma. Besides, damage of the liver and other organs is further aggravated due to the fact that serious liver metabolism dysfunction can appear in the hepatic failure process. PPAR gamma plays a pivotal role in lipid metabolism, and researches show that a PPAR gamma deficient type neonatal mouse has severe lipodystrophy shortly after birth.
Owner:杭州笙源生物科技有限公司
Application of AMPH (amphiphilic protein) cytokine to preparation of hepatic failure treatment drug
InactiveCN110279848ASuppress deathInhibit apoptosisPeptide/protein ingredientsDigestive systemAntioxidantHepatocyte apoptosis
The invention discloses an application of an AMPH (amphiphilic protein) cytokine to preparation of a hepatic failure treatment drug. The drug comprises a pharmaceutically acceptable excipient, antioxidant and carrier of the AMPH cytokine. On the basis of multi-center and large prospective cohort populations and samples, cross validation is executed from different angles with multiple techniques including transcriptome sequencing, multi-omics association analysis, qRT-PCR (quantitative reverse transcription-polymerase chain reaction), in-vivo validation in animal experiments and the like, and it is indicated that the AMPH cytokine can be applied to effective preparation of the hepatic failure treatment drug and the AMPH cytokine can cooperate with different solvents and stabilizers for producing drugs of different forms and dosages. Selectable administration modes in the using process comprise intravenous injection, intramuscular injection, hypodermic injection and oral administration. AMPH JNK (Jun N-terminal kinase) is one of MAPK family members, and a JNK pathway can inhibit hepatocyte apoptosis by regulating and controlling expression of AMPH.
Owner:杭州笙源生物科技有限公司
Composition for enhancing TRAIL sensitivity comprising inhibitors for expression or activity of TIP41 as a target gene of TRAIL sensitizer
ActiveUS8703732B2High sensitivityShrink tumorOrganic active ingredientsSenses disorderCancer preventionAdjuvant
Owner:KOREA RES INST OF BIOSCI & BIOTECH
Application of mir‑127 inhibitors in anti-inflammatory and lung injury protection drugs
ActiveCN104548132BInhibit inflammationAvoid damageAntipyreticGenetic material ingredientsLung InflammationsMechanism of action
Owner:HANGZHOU NORMAL UNIVERSITY
Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein junkinases
The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O;R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1;n is an integer from 0 to 5, preferably between 1-3 and most preferred 1;Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl which is substituted with at least one ionisable moiety to which a lipophilic chain is attached and which is containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.
Owner:LAB SERONO SA
Pharmaceutically active sulfonyl amino acid derivatives
The present invention is related to sulfonyl amino acid derivatives of formula (I), notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl amino acid derivatives. Said sulfonyl amino acid are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 33. The present invention is furthermore related to novel sulfonyl amino acid derivatives as well as to methods of their preparation.
Owner:MERCK SERONO SA
Regulation of JNK activity by modulation of the interaction between the endocytic protein endophilin and the germinal center kinase-like kinase
InactiveUS20020164672A1Alter abilityAltering abilityCompound screeningApoptosis detectionHuntingtons choreaEndophilin I
Endophilin I is a brain-specific protein functioning in clathrin-mediated endocytosis. The present invention is based on the finding that the rat germinal center kinase-like kinase (rGLK), a member of the germinal center kinase (GCK) family of c-jun N-terminal kinase (JNK) activating enzymes, is a novel endophilin I-binding partner. In a first aspect of the present invention, the novel interaction between endophilin I and rGLK is put to use in a novel screening assay. In a second aspect of the present invention, the interaction between endophilin I and GLK is modulated for therapeutic purposes, namely for the prevention and / or curtailment of neurological disorders associated with the JNK pathway. JNK-mediated neuronal cell death is believed to play an important role in injuries and diseases involving neuronal degeneration, such as Huntington's disease.
Owner:MCGILL UNIV
Application of MSC in reducing cytokine storm influence
InactiveCN111467376AInhibition of activationInhibition formationCell dissociation methodsAntiviralsCombined treatmentTherapeutic group
The invention specifically discloses an application of MSC in reducing cytokine storm influence, in particular to an application of MSC in reducing cytokine storm influence of a viral infection patient, and relates to the technical field of biomedical engineering. A prepared MSC preparation is added into an MSC treatment group to carry out combined treatment on the viral infection patient, AP-1 / JNK pathway activation can be effectively inhibited, the generation of cytokines is reduced, and the formation of cytokine storms is inhibited, so that the injury of the cytokine storms to the tissues in the body of the patient can be effectively reduced by combined treatment of the MSC treatment group.
Owner:HUNAN YUANPIN CELL TECH CO LTD
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