158326-84-2

Usage

Uses

Used in Pharmaceutical Industry:
6-bromo-3,3-dimethylindolin-2-one is used as a potential pharmaceutical candidate for various applications due to its unique chemical structure and properties. The presence of the bromine atom and methyl groups may contribute to its potential therapeutic effects and interactions with biological targets.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 6-bromo-3,3-dimethylindolin-2-one is utilized for the development of new drugs and therapeutic agents. Its chemical structure can be further modified or optimized to enhance its pharmacological properties, making it a valuable compound for drug discovery and design.

Upstream product

• 83-34-1 3-Methylindole 
• 99365-40-9 6-bromo-2,3-dihydro-1H-indole-2-one 
• 74-88-4 methyl iodide 
• 544709-66-2 2-(4-bromo-2-nitro-phenyl)-2-methyl-propionic acid methyl ester 
• 1190861-71-2 N'-(3-bromophenyl)isobutyrohydrazide 
• 90725-50-1 (3-RS)-6-bromo-2,3-dihydro-3-methyl-1H-indole-2-one 
• 65617-24-5 2,6-dibromo-3-methyl-indole 
• 40887-80-7 3-bromophenylhydrazine 

Downstream Products

• 1190861-74-5 3,3-dimethyl-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indolin-2-one 
• 127267-57-6 3,3-dimethyl-2-oxoindolin-6-carboxylic acid 
• 1581753-96-9 6-benzylamino-1-isopropyl-3,3-dimethyl-1,3-dihydroindol-2-one 
• 158326-85-3 6-Bromo-3,3-dimethyl-dihydroindole 

Relevant academic research and scientific papers

SUBSTITUTED TRICYCLIC COMPOUNDS

Disclosed are compounds of the general formula (I), its tautomeric form, its stereoisomer, its pharmaceutically acceptable salt, its polymorph, or solvate thereof, wherein, ring A, ring B, R1 to R4, and n are as defined herein, for use as SOS1 inhibitors in the treatment of proliferative, infectious and RASopathy diseases or disorders. Also disclosed are methods of synthesizing the compound of formula I, pharmaceutical compositions containing the compound of formula I, method of treatment of proliferative, infectious and RASopathy diseases or disorder, for example, a cancer, by administering the said compound and combinations of the compound of formula I with other active ingredients.

PYRIDINONE DERIVATIVES AND THEIR USE AS SELECTIVE ALK-2 INHIBITORS

The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES

The present invention is concerned with indolin-2-one and l,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula (I) wherein Ar1 is phenyl, pyridinyl or pyrimidinyl; Ar2 is a 5 or 6 membered heteroaryl group, containing 2 or 3 heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, halogen or lower alkoxy; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, lower alkyl substituted by hydroxy, cycloalkyl, oxetan-3-yl, pyridinyl, imidazolyl, pyrazolyl, pyrimidinyl, which rings may optionally substituted by lower alkyl, or is -(CH2)3-S(O)2-cyclopropyl; X is CH or N; n is 1 or 2; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof, for use in the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

INDOLIN-2-ONE OR PYRROLO-PYRIDIN-2-ONE DERIVATIVES

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+-(O-); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+-(O-), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, epilepsy, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems.

2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein (N1) is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; (N2) is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R1 may be the same or not; R2/R2' are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C3-6-cycloalkyl ring; R3 is lower alkyl, C3-6-cycloalkyl, CH2-C3-6-cycloalkyl, C3-6-cycloalkyl wherein one ring-carbon atom is replaced by -O-, (CH2)3-O-C3-6-cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH2)3-S(O)2-C3-6-cycloalkyl or (CH2)2-S(O)2-lower alkyl; R4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R4 may be the same or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar is a heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o-O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o-S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o-S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3; R3 is halogen or lower alkyl; X is CH or N; X1 is CH or N; n is 1 or 2; o is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line is a bond or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

RING-FUSED COMPOUND

The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below. [in the formula, R1 is -Q1-A1 and the like; ---- is a double bond or a single bond; when ---- is a double bond, W1 is a nitrogen atom or a group represented by the general formula: =C(Ra)-, and W2 is a nitrogen atom or a group represented by the general formula: =C(Rb) -; when ---- is a single bond, W1 is a group represented by the general formula: -C(Raa)(Rab)- or a group represented by the general formula: -(C=O) -, and W2 is a group represented by the general formula: C(Rba)(Rbb)-, a group represented by the general formula: - (C=O) - or a group represented by the general formula: -N(Rbc)-; W3, W4 and W5 are each independently a nitrogen atom or a methine group and the like that may have a substituent; X is a single bond, an oxygen atom and the like; Y is a single bond or (CRYiRYi')n; and Z is a hydroxyl group or COOR2 and the like.

8 - SUBSTITUTED 2 -AMINO - [1,2,4] TRIAZOLO [1, 5 -A] PYRAZINES AS SYK TRYROSINE KINASE INHIBITORS AND GCN2 SERIN KINASE INHIBITORS

Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus

TRIAZOLOPYRAZINE DERIVATIVES

Compounds of the formula (I) in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.

Indolin-2-one p38α inhibitors I: Design, profiling and crystallographic binding mode

The use of structure-based design and molecular modeling led to the discovery of indolin-2-one derivatives as potent and selective p38α inhibitors. The predicted binding mode was confirmed by X-ray crystallography.