261896-27-9Relevant academic research and scientific papers
1-CYANO-PYRROLIDINE DERIVATIVES AS DUB INHIBITORS
-
Paragraph 0649-0650, (2020/11/30)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.
Chemical synthesis method of (3R,4S)-4-methyl pyrrolidine-3-yl carbamic acid tert-butyl ester hydrochloride
-
Paragraph 0023-0025; 0036-0038; 0049-0051, (2019/01/08)
The invention relates to a chemical synthesis method of (3R,4S)-4-methyl pyrrolidine-3-yl carbamic acid tert-butyl ester hydrochloride. The method comprises the following six steps: dissolving (E)-but-2-enoic acid ethyl ester in dichloromethane, adding N-
METHODS OF MAKING AND USING PDE9 INHIBITORS
-
Paragraph 0153; 0157-0159, (2018/12/13)
The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyperplasia, beta thalassemia, and sickle cell disease.
PDE9 INHIBITORS FOR TREATMENT OF PERIPHERAL DISEASES
-
Paragraph 00195; 00252, (2018/09/25)
The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyperplasia, beta thalassemia, and sickle cell disease.
Chemical synthesis method of (3S,4R)-4-methylpyrrolidin-3-yl tert-butyl carbamate hydrochloride
-
Paragraph 0025-0027; 0040-0042; 0055-0057, (2019/01/06)
The invention relates to a chemical synthesis method of (3S,4R)-4-methylpyrrolidin-3-yl tert-butyl carbamate hydrochloride. The chemical synthesis method comprises the following seven steps: (1) adding ethyl (E)-2-butenoate into a dichloromethane solvent,
PDE9 INHIBITORS WITH IMIDAZO TRIAZINONE BACKBONE AND IMIDAZO PYRAZINONE BACKBONE FOR TREATMENT OF PERIPHERAL DISEASES
-
Page/Page column 41; 42, (2017/02/09)
The present invention relates to PDE9 inhibitors and their use for treatment of benign prostate hyperplasia and sickle cell disease.
NOVEL COMPOUNDS FOR USE IN COGNITION IMPROVEMENT
-
Page/Page column 47, (2016/04/19)
Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a -(C=O)NRaRb moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases.
NOVEL COMPOUNDS
-
Page/Page column 61-62, (2016/04/20)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.
NOVEL COMPOUNDS AS DUAL INHIBITORS OF PHOSPHODIESTERASES AND HISTONE DEACETYLASES
-
Page/Page column 74, (2014/09/16)
It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein B1 is a radical selected from the group consisting of formula (A"), formula (B"), formula (C"), and formula (D"):
NOVEL TRICYCLIC COMPOUNDS
-
, (2013/03/28)
The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
