Abstract: Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.

Abstract: Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor.

Abstract: The present invention relates to the use of a novel class of cancer stem cell pathway (CSCP) inhibitors; to methods of using such compounds to treat refractory, recurrent, or metastatic cancers; to methods of selective killing cancer cells by using such compounds with specific administration regimen; to methods of targeting cancer stem cells by inhibiting Stat3 pathway; to methods of using novel compounds in the treatment of conditions or disorders in a mammal related to aberrant Stat3 pathway activity; and to processes for preparing such compounds and intermediates thereof, and to the pharmaceutical composition of relevant compounds, and to the specific methods of administration of these compounds.

Abstract: Systems and methods are disclosed for cosmetic augmentation by forming a biocompatible cross-linked polymer having a multi-phase mixture with a time release catalyst; injecting the mixture into a patient as a viscous fluid; after injection, activating the catalyst to cross-link the polymer after a predetermined period after injection into a patient; and augmenting soft tissue with the biocompatible cross-linked polymer.

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

Abstract: The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.

Abstract: The invention generally relates to compounds that function as TP antagonists for treating thrombosis and other cardiovascular, renal, or pulmonary diseases. In some embodiments, the invention provides a compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating thrombosis by administering an antithrombotic compound that preferentially binds to a thromboxane receptor, has preferential binding for either TPalpha (TP?) or TPbeta (TP?) receptor subtype.

Abstract: The present invention discloses the potential of Calebin A in attenuating high fat diet (HFD) induced hepatic steatosis in mammals.

Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.

Abstract: The invention relates to a method for controlling woolly apple aphid insect comprising contacting the insect or a locus, where control of the insect is desired, with a combination of at least one neonicotinoid compound and at least one benzoylphenyl urea compound.

Abstract: The present invention relates to the composition and methods of use of Stat3 pathway inhibitors or cancer stem cell inhibitors in combination treatment of cancer.

Abstract: The present application is directed to an aqueous pharmaceutical formulation comprising less than about 5% w/v sodium deoxycholate maintained at a pH sufficient to substantially inhibit precipitation of the sodium deoxycholate. Also disclosed herein, are methods for inhibiting precipitation of sodium deoxycholate in an aqueous solution comprising less than about 5% w/v of sodium deoxycholate, said method comprising maintaining pH of the solution of from at least about 8.0 to about 8.5.

Abstract: Provided are inclusion complexes comprising fulvestrant and a cyclodextrin. The complexes may be useful for treating various conditions, such as cancer and systemic lupus crythematosus. Also provided are methods of producing the inclusion complexes, methods of using the inclusion complexes in therapy, and kits and unit dosages comprising the complexes.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

Abstract: The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.

Abstract: Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: Disclosed are near IR emitting fluorescent compounds; methods of making and kits containing the described compounds; and their use in fluorescence-based detection of biological materials.

Abstract: Methods are provided for treating conditions including chronic pelvic pain, in which there are palpable trigger points of local areas of muscle restriction and spasticity that recreate or refer pain of patients complaints upon palpation, chronic pelvic pain syndrome, pelvic floor myalgia, pelvic floor dysfunction, interstitial cystitis, levator ani syndrome, coccygodynia, prostatodynia, piriformis syndrome, anal sphincter pain, bowel movement pain, post bowel movement pain, ejaculatory pain, post ejaculatory pain, sitting pain, post bowel movement pain, rectal pain, tailbone pain, urinary frequency, urinary urgency, urinary hesitancy, post urinary pain, overactive bladder, perineal pain, penile pain, vaginismus, anismus, sexual dysfunction, reduced level of ejaculate or reduced penile erection, myofascial pain in muscle tissue of a patient who has one or more trigger points in the muscle tissue, or the pain/sensitivity of pelvic floor muscle trigger points and specific areas of myofascial restriction detected

Abstract: The present invention provides novel 3,4-disubstituted-1H-pyrrolo[2,3-b]pyridine derivatives and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and X are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ?Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ?Z is ?O, etc.; and n is an integer of 0 to 4.