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公开(公告)号：US20170239257A1
公开(公告)日：2017-08-24
申请号：US15277550
申请日：2016-09-27
Inventor： Nestor F. Gonzalez-Cadavid , Jacob Rajfer
IPC: A61K31/53 , A61K31/519 , A61K9/00 , A61K31/4985
CPC classification number: A61K31/53 , A61K9/0053 , A61K31/00 , A61K31/4985 , A61K31/519 , A61K48/00 , A61K48/005 , A61K2201/094 , C12N15/86 , C12N2710/10343 , C12N2830/008 , C12N2830/85
Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart. In certain embodiments, the compositions may comprise a PDE-4 inhibitor, a PDE-5 inhibitor, a compound that elevates cGMP and/or PKG, a stimulator of guanylyl cyclase and/or PKG, a combination of a compound that elevates cGMP, PKG or NO with an antioxidant that decreases ROS, or a compound that increases MMP activity.
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公开(公告)号：US09737543B2
公开(公告)日：2017-08-22
申请号：US15342309
申请日：2016-11-03
Applicant: Strategic Science & Technologies, LLC
Inventor： Eric T. Fossel
IPC: A61K31/53 , A61K47/06 , A61K47/14 , A61K47/26 , A61K47/02 , A61K47/22 , A61K9/00 , A61K9/06 , A61K9/107 , A61K31/198 , A61K31/495 , A61K31/506 , A61K31/519 , A61K47/36 , A61K31/4985 , A61K47/10 , A61K47/16 , A61K47/18 , A61K47/12
CPC classification number: A61K31/53 , A61K9/0014 , A61K9/0034 , A61K9/06 , A61K9/107 , A61K31/198 , A61K31/495 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K47/02 , A61K47/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/16 , A61K47/183 , A61K47/22 , A61K47/26 , A61K47/36 , A61K2300/00
Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a phosphodiesterase type 5 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.
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公开(公告)号：US09737542B2
公开(公告)日：2017-08-22
申请号：US15027585
申请日：2014-10-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Carolyn Diane Dzierba , Bireshwar Dasgupta , John E. Macor , Joanne J. Bronson , Ramkumar Rajamani , George N. Karageorge
IPC: A61K31/53 , A61K31/5377
CPC classification number: A61K31/53 , A61K31/5377
Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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公开(公告)号：US20170231931A1
公开(公告)日：2017-08-17
申请号：US15504281
申请日：2015-08-25
Inventor： María del Mar CUADRADO TEJEDOR , Ana María GARCÍA OSTA , Julen OYARZABAL SANTAMARINA , Maria Obdulia RABAL GRACIA
IPC: A61K31/167 , A61K31/519 , A61K31/4985 , A61K31/53
CPC classification number: A61K31/167 , A61K31/4985 , A61K31/519 , A61K31/53 , A61K45/06 , A61K2300/00
Abstract: The invention relates to a product that comprises a compound of formula (1-01) to (1-47) and a compound of formula (2-01) to (2-26), or their pharmaceutically or veterinary acceptable salts thereof, or any stereoisomers either of the compounds or of any of their pharmaceutically or veterinary acceptable salts. The invention also relates to said product for use in the treatment and/or prevention of a neurological disorder coursing with a cognition deficit or impairment, or a neurodegenerative disease.
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公开(公告)号：US09730928B2
公开(公告)日：2017-08-15
申请号：US14896906
申请日：2014-06-13
Applicant: University of Utah Research Foundation
Inventor： Vincente Planelles , Alberto Bosque-Pardos , Chris M. Ireland , Ryan Van Wagoner , Mary Kay Harper-Ireland , John Alan Maschek
IPC: A61K31/501 , A61K31/416 , A61K31/53 , A61K45/06 , C07D231/54 , C07D249/04 , A61K31/4192 , A61K31/437 , C07D249/18 , C07D253/08 , C07D403/04 , C07D471/04
CPC classification number: A61K31/501 , A61K31/416 , A61K31/4192 , A61K31/437 , A61K31/53 , A61K45/06 , C07D231/54 , C07D249/04 , C07D249/18 , C07D253/08 , C07D403/04 , C07D471/04 , A61K2300/00
Abstract: In one aspect, the invention relates to triazol-1-ol compounds, analogs thereof, compositions comprising same, and methods of using same, alone or in combination with other agents, to reactivate latent retroviruses, and more particularly to reactivate latent HIV-1. Such compounds, compositions, and methods can be used, for example, in connection with diagnosing and/or treating a retrovirus, and more specifically HIV-1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US20170224657A1
公开(公告)日：2017-08-10
申请号：US15382448
申请日：2016-12-16
Applicant: BOARD OF REGENTS OF NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF UNIVERSITY OF NEVADA, RENO
Inventor： Dean Burkin , Ryan Wuebbles
IPC: A61K31/404 , A61K45/06
CPC classification number: A61K31/404 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/36 , A61K31/37 , A61K31/381 , A61K31/4025 , A61K31/4035 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K31/4365 , A61K31/4402 , A61K31/4418 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/5365 , A61K31/5375 , A61K31/5377 , A61K31/5383 , A61K31/541 , A61K31/551 , A61K31/57 , A61K31/575 , A61K31/661 , A61K38/05 , A61K38/39 , A61K45/06
Abstract: Disclosed herein are α7β1 integrin modulatory agents and methods of using such to treat conditions associated with decreased α7β1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an α7β1 integrin modulatory agent to the subject with muscular dystrophy, wherein the α7β1 integrin modulatory agent increases α7β1 integrin expression or activity as compared to α7β1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing α7β1 integrin expression by use of the disclosed α7β1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
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公开(公告)号：US09724294B2
公开(公告)日：2017-08-08
申请号：US13564525
申请日：2012-08-01
Applicant: Jay Richard Ray, II , Charles D. Hodge
Inventor： Jay Richard Ray, II , Charles D. Hodge
IPC: A61K31/54 , A61K9/00 , A61K31/5415 , A61K31/167 , A61K31/53 , A61K31/7048 , A61K9/06
CPC classification number: A61K9/0014 , A61K9/06 , A61K31/167 , A61K31/53 , A61K31/5415 , A61K31/7048 , A61K2300/00 , A61K31/63
Abstract: The present embodiments relate to topically delivered compounded medications. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include low concentrations of local anesthetics, a NSAID, an anticonvulsant, and/or other active ingredients. For instance, the transdermal cream may include lidocaine, prilocaine, meloxicam, and lamotrigine and/or topiramate. Alternatively, the transdermal cream may include a lidocaine/prilocaine base cream to which is added a fine powder of one or more ground up medications to form a compounded medication. The compounded medication in powder form may be generated from grinding up tablets of NSAIDs, anticonvulsants, nerve depressants, antidepressants, muscle relaxants, NMDA receptor antagonists, opiate or opioid agonists, and/or other agents. The compounded medication in powder form may include meloxicam, lamotrigine, topiramate, and/or other active ingredients. In another aspect, the present embodiments relate to methods of compounding medications and transdermal creams or gels.
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公开(公告)号：US09718828B2
公开(公告)日：2017-08-01
申请号：US15250978
申请日：2016-08-30
Applicant: MERCK SHARP & DOHME CORP. , MERCK SHARP & DOHME B.V.
Inventor： Adrianus Petrus Antonius De Man , Jan-Gerard Sterrenburg , Hans C. A. Raaijmakers , Allard Kaptein , Arthur A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Jacobus C. H. M. Wijkmans , Tjeerd A. Barf , Alan B. Cooper , Ronald M. Kim , Sobhana Babu Boga , Hugh Y. Zhu , Xiaolei Gao , Xin Yao , Rajan Anand , Hao Wu , Shilan Liu , Chundao Yang , Abdul-Basit Alhassan , James Wang , Younong Yu , Jian Liu , Henry M. Vaccaro
IPC: C07D487/04 , C07D497/02 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/52 , A61K31/53 , A61P19/02 , C07D519/00 , A61K45/06 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D513/04 , C07D471/04
CPC classification number: C07D487/04 , A61K31/4985 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D471/04 , C07D513/04 , C07D519/00
Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
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公开(公告)号：US09718788B2
公开(公告)日：2017-08-01
申请号：US15249851
申请日：2016-08-29
Applicant: MILLENNIUM PHARMACEUTICALS, INC.
Inventor： Christopher F. Claiborne , Stephen Critchley , Steven P. Langston , Hirotake Mizutani , Edward J. Olhava , Stephane Peluso , Irache Visiers , Stepan Vyskocil
IPC: C07D213/82 , C07D239/48 , C07D487/04 , C07D239/42 , C07D213/56 , C07D213/69 , C07D401/04 , C07D403/04 , C07D471/04 , C07D471/08 , C07D473/34 , C07D473/30 , A61K31/53 , C07D251/18 , C07D251/48 , C07D213/74 , C07D401/06 , C07D213/81 , C07D239/36
CPC classification number: C07D239/42 , A61K31/53 , C07D213/56 , C07D213/69 , C07D213/74 , C07D213/81 , C07D213/82 , C07D239/36 , C07D239/48 , C07D251/18 , C07D251/48 , C07D401/04 , C07D401/06 , C07D403/04 , C07D471/04 , C07D471/08 , C07D473/30 , C07D473/34 , C07D487/04
Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
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公开(公告)号：US20170209394A1
公开(公告)日：2017-07-27
申请号：US15339346
申请日：2016-10-31
Applicant: Elcelyx Therapeutics, Inc.
Inventor： Alain D. BARON , Mark S. FINEMAN , Nigel R.A. BEELEY
IPC: A61K31/155 , A61K31/485 , A61K31/137 , A61K31/35 , A61K45/06 , A61K31/55
CPC classification number: A61K31/155 , A61K9/2086 , A61K9/2806 , A61K9/4808 , A61K31/137 , A61K31/341 , A61K31/35 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4196 , A61K31/4453 , A61K31/454 , A61K31/485 , A61K31/53 , A61K31/55 , A61K45/06 , A61K2300/00
Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
