Patent classifications
C07D295/027
3-(benzylamino)-4-(cyclohexylamino)-n-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 analogues as cell death inhibitors for treating e.g. stroke
The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate.
Apparatus and process for the automated chemical synthesis of compounds
Provided is an apparatus for the automated synthesis of at least one chemical compound including: at least one cartridge including at least one first compartment for providing at least one first reagent for the chemical synthesis of the at least one compound; at least one second compartment for providing at least one second reagent for the chemical synthesis of the at least one compound, and at least one third compartment for purifying the at least one synthesized compound; at least one reaction container for providing the compounds to be fed into at least one of the compartments of the cartridge and/or collecting the reaction product from at least one of the compartments of the cartridge; at least one solvent container at least two flow path selecting valves and at least one pump.
Apparatus and process for the automated chemical synthesis of compounds
Provided is an apparatus for the automated synthesis of at least one chemical compound including: at least one cartridge including at least one first compartment for providing at least one first reagent for the chemical synthesis of the at least one compound; at least one second compartment for providing at least one second reagent for the chemical synthesis of the at least one compound, and at least one third compartment for purifying the at least one synthesized compound; at least one reaction container for providing the compounds to be fed into at least one of the compartments of the cartridge and/or collecting the reaction product from at least one of the compartments of the cartridge; at least one solvent container at least two flow path selecting valves and at least one pump.
Dual NAV1.2/5HT2a inhibitors for treating CNS disorders
Compounds of formula I: ##STR00001##
are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.
Dual NAV1.2/5HT2a inhibitors for treating CNS disorders
Compounds of formula I: ##STR00001##
are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.
Method for depleting 2-methoxyethanol (MOE)
A process for the depletion of 2-methoxyethanol (MOE) from a mixture comprising predominantly morpholine (MO) (crude morpholine), wherein crude morpholine is distilled in a distillation column in the presence of an alkali metal compound of the general formula M.sup.+[RO.sup.−] (M.sup.+ is alkali metal cation and R is hydrogen (H), methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, sec-butyl or tert-butyl), where MO and a compound of the general formula R—OH are distilled off and an alkali metal methoxyethoxide of the general formula M.sup.+[MeOEtO.sup.−] is obtained in the bottom of the column.
Method for depleting 2-methoxyethanol (MOE)
A process for the depletion of 2-methoxyethanol (MOE) from a mixture comprising predominantly morpholine (MO) (crude morpholine), wherein crude morpholine is distilled in a distillation column in the presence of an alkali metal compound of the general formula M.sup.+[RO.sup.−] (M.sup.+ is alkali metal cation and R is hydrogen (H), methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, sec-butyl or tert-butyl), where MO and a compound of the general formula R—OH are distilled off and an alkali metal methoxyethoxide of the general formula M.sup.+[MeOEtO.sup.−] is obtained in the bottom of the column.
Ammonium carboxylate compound, crystalline form, amorphous form and preparation method thereof
The present disclosure belongs to the field of chemical synthesis, and in particular relates to an ammonium carboxylate compound, a crystalline form and an amorphous form, and a preparation method thereof. The present disclosure prepares the compound and the crystalline form I and its single crystal, amorphous form and crystalline form II thereof. The compound, the crystalline forms, the single crystal and the amorphous form can stably exist and exhibit good solid forms, suitable for medicine-making. Furthermore, these products possess high purity and less single impurity. Moreover, the preparation methods of the present disclosure are easy to implement due to the simple processes with mild reaction conditions, and could produce products of high yield and high purity without complex purification steps. Furthermore, the preparation methods may facilitate safety, environmental protection, and industrial production.
NOVEL SALTS AND POLYMORPHIC FORM OF BEMPEDOIC ACID
The present invention relates to novel pharmaceutically acceptable salts of Bempedoic acid, novel intermediates of Bempedoic acid, novel crystalline form of Bempedoic acid and novel processes for the preparation of Bempedoic acid or its intermediates thereof.
HYDROGENATION CATALYST FOR USE IN HYDROGENATING AMIDE COMPOUND AND METHOD FOR PRODUCING AMINE COMPOUND USING SAME
Provided is a hydrogenation catalyst for an amide compound, containing hydroxyapatite and platinum and vanadium that are fixed on the hydroxyapatite, 15 to 80% of the surface of the platinum being covered with vanadium. The hydrogenation catalyst can promote a reduction reaction in which an amide compound is converted into an amine compound, can be used under mild conditions, and has such durability that the catalyst can be repeatedly used while retaining a high activity.