Patent classifications
C07D333/38
COMPOSITIONS AND METHODS FOR TREATMENT
The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
COMPOSITIONS AND METHODS FOR TREATMENT
The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS
A process for preparing and purifying a compound of Formula I is provided:
##STR00001##
thereof, wherein the subscript m is an integer of from 0 to 3; each R.sup.a is independently selected from the group consisting of (C.sub.3-C.sub.8)cycloalkyl, (C.sub.1-C.sub.4)haloalkyl, halogen, —OH, —OR.sup.1, —SH, —SR.sup.1, —S(O)R.sup.1, —S(O).sub.2R.sup.1, —SO.sub.2NH.sub.2, —C(O)NH.sub.2, —C(O)NHR.sup.1, —C(O)N(R.sup.1).sub.2, —C(O)R.sup.1, —C(O)H, —CO.sub.2H, —CO.sub.2R.sup.1, —NO.sub.2, —NH.sub.2, —NHR.sup.1, —N(R.sup.1).sub.2, wherein each R.sup.1 is independently (C.sub.1-C.sub.8)alkyl; L is a linking group selected from the group consisting of a bond or CH.sub.2; Q.sup.a, Q.sup.b, and Q.sup.c are each members independently selected from the group consisting of N, S, O and C(R.sup.q) wherein each R.sup.q is independently selected from the group consisting of H, C.sub.1-8 alkyl, halo and phenyl, and the ring having Q.sup.a, Q.sup.b, Q.sup.c and Y as ring vertices is a five-membered ring having two double bonds; and
Y is selected from the group consisting of C and N.
PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS
A process for preparing and purifying a compound of Formula I is provided:
##STR00001##
thereof, wherein the subscript m is an integer of from 0 to 3; each R.sup.a is independently selected from the group consisting of (C.sub.3-C.sub.8)cycloalkyl, (C.sub.1-C.sub.4)haloalkyl, halogen, —OH, —OR.sup.1, —SH, —SR.sup.1, —S(O)R.sup.1, —S(O).sub.2R.sup.1, —SO.sub.2NH.sub.2, —C(O)NH.sub.2, —C(O)NHR.sup.1, —C(O)N(R.sup.1).sub.2, —C(O)R.sup.1, —C(O)H, —CO.sub.2H, —CO.sub.2R.sup.1, —NO.sub.2, —NH.sub.2, —NHR.sup.1, —N(R.sup.1).sub.2, wherein each R.sup.1 is independently (C.sub.1-C.sub.8)alkyl; L is a linking group selected from the group consisting of a bond or CH.sub.2; Q.sup.a, Q.sup.b, and Q.sup.c are each members independently selected from the group consisting of N, S, O and C(R.sup.q) wherein each R.sup.q is independently selected from the group consisting of H, C.sub.1-8 alkyl, halo and phenyl, and the ring having Q.sup.a, Q.sup.b, Q.sup.c and Y as ring vertices is a five-membered ring having two double bonds; and
Y is selected from the group consisting of C and N.
COMPOUNDS AND MODULES FOR INHIBITION OF PRE-miR-21 AND THEIR USE IN TREATMENT OF CERTAIN CANCERS
Small molecule compounds and corresponding dimers having inhibitory activity against pre-miR-21 RNA and related methods for treatment of neoplastic disease such as cancer and especially cancers expressing miR-21 are disclosed.
Silicon-based energy storage devices with functional thiophene compounds or derivatives of thiophene containing electrolyte additives
Electrolytes and electrolyte additives for energy storage devices comprising functional thiophene compounds are disclosed. The energy storage device comprises a first electrode and a second electrode, wherein at least one of the first electrode and the second electrode is a Si-based electrode, a separator between the first electrode and the second electrode, an electrolyte, and at least one electrolyte additive selected from a thiophene compound.
Silicon-based energy storage devices with functional thiophene compounds or derivatives of thiophene containing electrolyte additives
Electrolytes and electrolyte additives for energy storage devices comprising functional thiophene compounds are disclosed. The energy storage device comprises a first electrode and a second electrode, wherein at least one of the first electrode and the second electrode is a Si-based electrode, a separator between the first electrode and the second electrode, an electrolyte, and at least one electrolyte additive selected from a thiophene compound.
KCNT1 INHIBITORS AND METHODS OF USE
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
KCNT1 INHIBITORS AND METHODS OF USE
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
ACLY inhibitors and uses thereof
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.