Patent classifications
A61K31/438
NITROGEN-CONTAINING SPIRO CYCLIC COMPOUNDS AND PHARMACEUTICAL USES THEREOF
A compound of the following general formula [I]:
##STR00001##
wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.
NITROGEN-CONTAINING SPIRO CYCLIC COMPOUNDS AND PHARMACEUTICAL USES THEREOF
A compound of the following general formula [I]:
##STR00001##
wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.
PIPERIDINYL-3-(ARYLOXY)PROPANAMIDES AND PROPANOATES
Disclosed are compounds of Formula 1,
##STR00001##
stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R.sup.5, R.sup.6, R.sup.7, R.sup.9, R.sup.10, R.sup.11, R.sup.12, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.13, and X.sup.14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.
PIPERIDINYL-3-(ARYLOXY)PROPANAMIDES AND PROPANOATES
Disclosed are compounds of Formula 1,
##STR00001##
stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R.sup.5, R.sup.6, R.sup.7, R.sup.9, R.sup.10, R.sup.11, R.sup.12, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.13, and X.sup.14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.
(R)-4-(1-(6-(4-(TRIFLUOROMETHYL)BENZYL)-6-AZASPIRO[2.5] OCTANE-5-CARBOXAMIDO)-CYCLOPROPYL) BENZOIC ACID OR ITS SALT ALSO IN POLYMORPHIC FORM A FOR USE IN THE PREVENTION OF HETEROTOPIC OSSIFICATION
There is described a compound of formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl)benzoic acid or a pharmaceutically acceptable salt thereof or the form A of its sodium salt for use in the prevention of heterotopic ossification. Preferably such a compound is effective in a specific dose range.
(R)-4-(1-(6-(4-(TRIFLUOROMETHYL)BENZYL)-6-AZASPIRO[2.5] OCTANE-5-CARBOXAMIDO)-CYCLOPROPYL) BENZOIC ACID OR ITS SALT ALSO IN POLYMORPHIC FORM A FOR USE IN THE PREVENTION OF HETEROTOPIC OSSIFICATION
There is described a compound of formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl)benzoic acid or a pharmaceutically acceptable salt thereof or the form A of its sodium salt for use in the prevention of heterotopic ossification. Preferably such a compound is effective in a specific dose range.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
IMPROVED TREATMENT OF ATOPIC DERMATITIS WITH TRADIPITANT
The disclosure relates generally to improvements in the treatment of pruritus, atopic dermatitis (AD), and associated symptoms with tradipitant. More particularly, it relates to a method for increasing the likelihood of achieving optimal therapeutic response in the treatment of an AD patient, where the AD patient is one for whom a potential therapy of choice may include the administration of an amount of an NK-1 antagonist, e.g. tradipitant effective to treat the patient's AD.
Toxic aldehyde related diseases and treatment
The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.
Toxic aldehyde related diseases and treatment
The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.