Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C?, D, E, F, G, H?, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
Abstract: A method for treating phytophotodermatitis including the steps of applying an isothiocyanate functional surfactant to an area affected by phytophotodermatitis, wherein said isothiocyanate functional surfactant comprises at least one isothiocyanate functional group associated with an aliphatic and/or aromatic carbon atom of the isothiocyanate functional surfactant.
Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I) wherein R1, R2, R3, R4, R5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts.
Abstract: The present disclosure is related to percarboxylic acid compositions formed in situ in non-equilibrium reactions. The peroxycarboxylic acid compositions are formed using ester based starting materials. Methods for using the percarboxylic acid compositions are also disclosed.
Type:
Grant
Filed:
September 26, 2014
Date of Patent:
September 19, 2017
Assignee:
Ecolab USA Inc.
Inventors:
Junzhong Li, David D. McSherry, Richard Staub
Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble.
Type:
Grant
Filed:
January 3, 2014
Date of Patent:
September 19, 2017
Assignee:
COLLEGIUM PHARMACEUTICAL, INC.
Inventors:
Jane Hirsh, Alison Fleming, Roman Rariy, Alexander Klibanov
Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent the presence or absence of a double bond which can be in the cis or trans configuration and A, B, Z, X, R1 and R2 are as defined in the specification and a penetration enhancer. Such compositions are used in stimulating hair growth of human or non-human animals.
Type:
Grant
Filed:
August 18, 2015
Date of Patent:
September 19, 2017
Assignee:
ALLERGAN, INC.
Inventors:
John T. Trogden, Adnan K. Salameh, Chetan P. Pujara
Abstract: [Problem] Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain. [Means for Solution] The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11?-hydroxydehydrogenase type 1 (11?-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11?-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).
Abstract: Irreversible inhibitors of K-Ras, H-Ras or N-ras protein comprising a G12C mutation are provided. Also disclosed are methods to regulate the activity of K-Ras, H-Ras or N-ras protein comprising G12C mutation and methods to disease mediated by K-Ras, H-Ras or N-ras G12C.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
August 29, 2017
Assignee:
ARAXES PHARMA LLC
Inventors:
Pingda Ren, Yi Liu, Liansheng Li, Jun Feng
Abstract: The present invention relates to compounds of Formula (I), along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).
Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
Type:
Grant
Filed:
October 21, 2015
Date of Patent:
August 8, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Steven Clareen, Veronique Plantevin-Krenitsky, Moorthy Palanki, Yoshitaka Satoh
Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
Type:
Grant
Filed:
September 17, 2014
Date of Patent:
August 1, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Ri are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstjtuted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.
Abstract: An aqueous pharmaceutical solution composition comprising between about 20 mg/ml to about 100 mg/ml of a radioprotective ?,?-unsaturated aryl sulfone, a cosolvent comprising polyethylene glycol (PEG), polypropylene glycol, polyglycerol, DMA, propylene glycol, glycerol, ethanol, sorbitol, isopropyl alcohol, or a combination thereof in an amount between about 25% and about 90% w/v, and a water soluble Vitamin E derivative, wherein the composition has a pH within the range of about 7.0 to about 9.5.
Abstract: Provided herein is a pharmaceutical composition comprising an isoflavonoid derivative and a cyclodextrin. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions. In specific instances, provided herein are intravenous compositions and therapies.
Abstract: The present invention relates to novel benzimidazole derivatives of the general formula processes for their preparation and their use for the production of pharmaceutical compositions for the treatment of diseases and indications that are connected with the receptor EP4.
Type:
Grant
Filed:
December 3, 2013
Date of Patent:
July 18, 2017
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Olaf Peters, Nico Bräuer, Thorsten Blume, Antonius Ter Laak, Ludwig Zorn, Jens Nagel, Stefan Kaulfuss, Gernot Langer, Joachim Kuhnke
Abstract: The present invention relates to a composition comprising metformin as an active ingredient for preventing or treating inflammatory bowel disease. The metformin compound or the metformin-etanercept (product name: Enbrel) composite according to the present invention may have excellent effects of maintaining the thickness of the small intestine and length of the large intestine normal, inhibiting or decreasing the activity of IL-17 and TNF-a, and promoting or increasing the activity of IFNr, and therefore can be effectively used as a pharmaceutical composition for preventing or treating autoimmune diseases including inflammatory bowel disease.
Type:
Grant
Filed:
March 19, 2015
Date of Patent:
July 11, 2017
Assignee:
Catholic University Industry Academic Cooperation Foundation
Abstract: Provided herein is a pharmaceutical composition comprising at least one isoflavonoid. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions.
Type:
Grant
Filed:
November 1, 2011
Date of Patent:
May 30, 2017
Assignee:
MEI PHARMA, INC.
Inventors:
George Jeoffreys, Alison Johnson, Andrew Heaton, Ofir Moreno
Abstract: A personal product antimicrobial preservative composition for preservation of topical personal care formulations is provided and includes [A] one or more undecylenic acid derivatives depicted by Formula (I), [B] one or more octanoic acid derivatives depicted by Formula (II), and [C] 2-phenoxy ethanol or 2-ethyl hexyl glyceryl ether or mixture of these two ‘liquid alcohol ethers’; wherein, each of the two components [A] and [B] is present in the range of 5 to 20% by weight and together [A] and [B] constitute 10 to 30% by weight and the ‘liquid alcohol ether’, component [C], is present 70 to 90% by weight of the total preservative composition. A method for preserving personal care product from microbial attack is provided containing an aqueous phase comprising three component composition from about 0.5 to 2.5% by weight of the total personal care formulation.
Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
Type:
Grant
Filed:
September 10, 2014
Date of Patent:
May 30, 2017
Assignee:
ALLERGAN, INC.
Inventors:
Haiqing Yuan, Richard L. Beard, Michael E. Garst, John E. Donello, Xiaoxia Liu, Veena Viswanath
Abstract: This invention provides a method for treating or for reducing ambulatory deterioration in a human patient diagnosed to be afflicted with relapsing-remitting multiple sclerosis (RRMS) and having a high baseline disability score according to the Kurtzke Expanded Disability Status Scale (EDSS), comprising periodically administering to only the patient diagnosed with RRMS and having a high baseline disability score an amount of laquinimod effective to treat the patient or to reduce ambulatory deterioration. This invention further provides pharmaceutical compositions and packages comprising an effective amount of laquinimod for treating a human patient diagnosed to be afflicted with RRMS and having a high baseline disability score according to the EDSS.