Patent classifications
A01N43/00
NOVEL PYRAZOLO-PYRROLO-PYRIMIDINE-DIONE DERIVATIVES AS P2X3 INHIBITORS
The present invention covers substituted. Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R.sup.1, R.sup.2 and R.sup.3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.
##STR00001##
NONMUSCLE MYOSIN II INHIBITORS FOR SUBSTANCE USE RELAPSE
The invention can provide compounds, analogs of blebbistatin, effective and selective inhibitors of nonmuscle myosin II relative to cardiac myosin II. Compounds can be used in the method of treating a disease, disorder, or medical condition in a patient, comprising modulating myosin II ATPase, such as treatment of substance abuse relapse disorder, or of renal disease, cancer and metastasis, benign prostate hyperplasia, hemostasis or thrombosis, nerve injury including retinal damage, lung fibrosis, liver fibrosis, arthrofibrosis, wound healing, spinal cord injury, periodontitis, glaucoma and immune-related diseases including multiple sclerosis; or wherein the disease, disorder, or medical condition comprises addiction including abuse of or addiction to anything classified as a Substance-Related or Addictive Disorder in the Diagnostic and Statistical Manual of Mental Disorders (DSM), such as, but not limited to, cocaine, opioids, amphetamines, ethanol, cannabis/marijuana, nicotine, and activities including gambling Compounds are of general formula (I) with substituents as defined herein.
UBIQUITIN-SPECIFIC-PROCESSING PROTEASE 7 (USP7) MODULATORS AND USES THEREOF
Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of USP7 activity.
KRAS G12C INHIBITORS
- John P. Fischer ,
- Jay Bradford Fell ,
- James F. Blake ,
- Ronald Jay Hinklin ,
- Macedonio J. MEJIA ,
- Erik James Hicken ,
- Mark Joseph Chicarelli ,
- John J. Gaudino ,
- Guy P.A. Vigers ,
- Laurence E. Burgess ,
- Matthew Arnold Marx ,
- James Gail Christensen ,
- Matthew Randolf LEE ,
- Pavel Savechenkov ,
- Henry J. Zecca ,
- Tony P. Tang
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
NOVEL HETEROARYL HETEROCYCLYL COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
The present invention relates to compounds of formula (I), ab (I), wherein R1 to R3 and L are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
##STR00001##
Use of anti-connexin agents for modulating the therapeutic effect of psychotropic drugs
The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-β-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid. The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-β-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid.
Combinations of a muscarinic receptor antagonist and a beta-2 adrenoreceptor agonist
Combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, and methods of using them are provided.
Method of treatment using nanoparticulate ganaxolone formulations
In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
COMPOUNDS THAT INHIBIT MCL-1 PROTEIN
- Sean P. Brown ,
- David Karl BEDKE ,
- Micheal R. DEGRAFFENREID ,
- Jiasheng Fu ,
- Zhihong Li ,
- Felix GONZALEZ LOPEZ TURISO ,
- Ana Gonzalez Buenrostro ,
- Micheal W. GRIBBLE, JR. ,
- Micheal G. JOHNSON ,
- Todd J. KOHN ,
- Kexue LI ,
- Yunxiao LI ,
- Mike Elias Lizarzaburu ,
- Yosup Rew ,
- Joshua TAYGERLY ,
- Yingcal WANG ,
- Xuelei Yan ,
- Ming Yu ,
- Jiang Zhu ,
- Manuel Zancanella ,
- Xian Yun Jiao ,
- Liusheng Zhu ,
- Xianghong Wang ,
- Julio C. Medina ,
- Jason A. Duquette ,
- Jonathan B. HOUZE ,
- Marc VIMOLRATANA ,
- Marlo G. CARDOZO ,
- Alan C. Cheng
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I,
##STR00001##
and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
Method for reducing itching in atopic dermatitis
This invention relates to a method for treating atopic dermatitis, comprising administering an effective amount of N-acyltryptamine represented by Formula (I): ##STR00001##
wherein R represents a saturated aliphatic hydrocarbon group having 2 to 29 carbon atoms; or a pharmaceutically acceptable salt, hydrate or solvate thereof to a subject in need thereof.