C07D417/06

SOLID FORMS OF(Z)-4-(5-((3-BENZYL-4-OXO-2-THIOXOTHIAZOLIDIN-5-YLIDENE)METHYL)FURAN-2-YL)BENZOIC ACID
20230227443 · 2023-07-20 ·

The present invention provides new salts and crystalline forms of leukadherin LA1 [(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid] according to Formula I. Methods for preparation of the salts and crystalline forms are also described, as well as methods for treating β2 integrin-mediated diseases and conditions using the salts and crystalline forms.

SOLID FORMS OF(Z)-4-(5-((3-BENZYL-4-OXO-2-THIOXOTHIAZOLIDIN-5-YLIDENE)METHYL)FURAN-2-YL)BENZOIC ACID
20230227443 · 2023-07-20 ·

The present invention provides new salts and crystalline forms of leukadherin LA1 [(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid] according to Formula I. Methods for preparation of the salts and crystalline forms are also described, as well as methods for treating β2 integrin-mediated diseases and conditions using the salts and crystalline forms.

METHODS AND COMPOSITIONS OF INHIBITING DCN1-UBC12 INTERACTION

In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

METHODS AND COMPOSITIONS OF INHIBITING DCN1-UBC12 INTERACTION

In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

HETEROCYCLIC COMPOUNDS FOR MEDICAL TREATMENT

The present invention provides heterocyclic compounds that bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation in a human or other host. The present invention also provides compounds that can be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.

COMPOUND HAVING LYSOPHOSPHATIDIC ACID RECEPTOR AGONIST ACTIVITY AND PHARMACEUTICAL USE THEREOF

A pharmaceutical containing a compound having an agonist activity for LPA3 as an active ingredient, wherein the compound is of formula (IY):

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wherein all symbols represent the same meaning as described in the specification, and which is useful as a preventive and/or therapeutic agent for, e.g., essential thrombocythemia or reactive thrombocytosis.

Sulfamoylamide Derivatives

The invention relates to a compound of formula (I) wherein R1-R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

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Sulfamoylamide Derivatives

The invention relates to a compound of formula (I) wherein R1-R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

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NOVEL 2-ARYLTHIAZOLE DERIVATIVE OR SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
20230219908 · 2023-07-13 · ·

Provided are a 2-arylthiazole derivative or pharmaceutically acceptable salt thereof having a specific carboxamide moiety, including a substituted aminoalkyl-carboxamide moiety, a N-containing heterocyclic-alkyl-carboxamide moiety, or a N-containing heterocyclic-carboxamide moiety, a process for the preparation thereof, and a pharmaceutical composition comprising the same.

NOVEL 2-ARYLTHIAZOLE DERIVATIVE OR SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
20230219908 · 2023-07-13 · ·

Provided are a 2-arylthiazole derivative or pharmaceutically acceptable salt thereof having a specific carboxamide moiety, including a substituted aminoalkyl-carboxamide moiety, a N-containing heterocyclic-alkyl-carboxamide moiety, or a N-containing heterocyclic-carboxamide moiety, a process for the preparation thereof, and a pharmaceutical composition comprising the same.