Patent classifications
A61P13/10
PURINE DIONES AS WNT PATHWAY MODULATORS
The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
Biphenyl derivatives and methods for preparing same
Provided are biphenyl derivatives having the structure of Formula 1: ##STR00001##
stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein R.sub.1 is hydrogen, halogen, hydroxy, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or C.sub.1-C.sub.6 alkoxy; R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, halogen, substituted or unsubstituted amino, nitro, cyano, hydroxy, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, substituted or unsubstituted C.sub.1-C.sub.6 alkoxy, or —C(O)R.sub.6; R.sub.5 is hydrogen or C.sub.1-C.sub.6 alkyl; n is 0 or 1; and R.sub.6 is hydrogen or amino, methods for preparing the same, and a pharmaceutical composition containing the same. The biphenyl derivatives having the structure of Formula 1 act as muscarinic M3 receptor antagonists, and thus are useful for the prevention or treatment of a disease selected from among chronic obstructive pulmonary disease, asthma, irritable bowel syndrome, urinary incontinence, rhinitis, spasmodic colitis, chronic cystitis, Alzheimer's disease, senile dementia, glaucoma, schizophrenia, gastroesophageal reflux disease, cardiac arrhythmia, and hyper-salivation syndromes.
ANTI-C5 ANTIBODIES AND USES THEREOF
The present invention provides monoclonal antibodies that bind to the complement factor 5 (C5) protein, and methods of use thereof. In various embodiments of the invention, the antibodies are fully human antibodies that bind to C5 protein. In some embodiments, the antibodies of the invention are useful for inhibiting or neutralizing C5 activity, thus providing a means of treating or preventing a C5-related disease or disorder in humans. In some embodiments, the invention provides for an anti-C5 antibody that has improved pharmacokinetic and pharmacodynamic properties, e.g., a half-life of more than 10 days.
BIOMARKERS AND METHODS OF TREATING PD-1 AND PD-L1 RELATED CONDITIONS
Provided herein are biomarkers for the treatment of pathological conditions, such as cancer, and method of using PD-1/PD-L1 pathway antagonists. In particular, provided are biomarkers for patient selection and prognosis in cancer, as well as methods of therapeutic treatment, articles of manufacture and methods for making them, diagnostic kits, methods of detection and methods of advertising related thereto.
Purine Diones As Wnt Pathway Modulators
The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
AMINO-SUBSTITUTED ISOTHIAZOLES
The present invention relates to amino-substituted isothiazoles of general formula (I): in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
##STR00001##
DERMAL FILLER BASED ON CROSSLINKED HYALURONIC ACID AND CARBOXYMETHYL CELLULOSE LUBRICANT
The present invention relates to injectable dermal filler compositions in the form of a gel, comprising hyaluronic acid (HA), carboxymethyl cellulose (CMC) and, optionally, microparticles such as calcium hydroxyapatite (CaHAP) microparticles. The injectable dermal filler compositions have improved rheological properties while at the same time have low extrusion forces. The present invention further relates to a method for preparing such injectable dermal filler compositions and their use for cosmetic and therapeutic purposes.
METHOD FOR TREATING UNDERACTIVE BLADDER SYNDROME
Disclosed are nonlimiting embodiments comprising novel methods for treating underactive bladder in a subject, including administering an effective amount of a pharmaceutical composition comprising an M1-selective muscarinic agonist to the subject. In some embodiments, the M1-selective muscarinic agonist is cevimeline.
Certain chemical entities, compositions and methods
Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.
1,2,4-Oxadiazole Derivatives as Immunomodulators
The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I)
##STR00001##
In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.