C07D311/22

NOVEL TNF ACTIVITY INHIBITOR COMPOUND, AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
20230271925 · 2023-08-31 · ·

The present invention relates to a novel TNF activity inhibitor compound and a pharmaceutically acceptable salt thereof, a method for prevention, alleviation or treatment comprising administering the compound of the present invention, a method for preparing the compound of the present invention, and a pharmaceutical composition comprising the compound.

IRE-1α inhibitors

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.

IRE-1α inhibitors

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.

Biheterocyclic compound

The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter ##STR00001##
wherein R.sup.1-L- is R.sup.1—OC(O)—, or the like, R.sup.1 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R.sup.2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R.sup.3 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like, the part of X, Y, and Z is X═Y—Z, X—Y═Z, or X—Y—Z, X is nitrogen atom, NR.sup.4 (R.sup.4 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.

Biheterocyclic compound

The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter ##STR00001##
wherein R.sup.1-L- is R.sup.1—OC(O)—, or the like, R.sup.1 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R.sup.2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R.sup.3 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like, the part of X, Y, and Z is X═Y—Z, X—Y═Z, or X—Y—Z, X is nitrogen atom, NR.sup.4 (R.sup.4 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.

Synthesis of intermediates for the preparation of alpha-tocopherol

The present invention relates to a novel synthetic pathway for alpha-tocopherol. The invention discloses different reactions yielding some new intermediates in a very high yield and stereoselectivity.

Synthesis of intermediates for the preparation of alpha-tocopherol

The present invention relates to a novel synthetic pathway for alpha-tocopherol. The invention discloses different reactions yielding some new intermediates in a very high yield and stereoselectivity.

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.

METHODS FOR PREPARING SUBSTITUTED CHROMANONE DERIVATIVES

The present disclosure relates to a method for preparing a compound of formula (I).

##STR00001##

In the compound of formula (I), n may be 0 to 5 and each of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 may be independently selected from the group consisting of H, —O-Alkyl, halo, alkyl, —CN, or —NO.sub.3.