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Patent # Description
2018/0237441 Chemical Compounds
The invention is directed to substituted pyrrolidinone and imidazolidinone derivatives. Specifically, the invention is directed to compounds according to...
2018/0237440 JANUS KINASE 1 SELECTIVE INHIBITOR AND PHARMACEUTICAL USE THEREOF
Janus kinase 1 selective inhibitors and pharmaceutical use thereof are provided.
2018/0237439 PYRAZOLE DERIVATIVES USEFUL AS 5-LIPOXYGENASE ACTIVATING PROTEIN (FLAP) INHIBITORS
The present application relates to novel compounds of formula (I) to their utility in treating and/or preventing clinical conditions including cardiovascular...
2018/0237438 CRYSTAL FORM OF BISULFATE OF JAK INHIBITOR AND PREPARATION METHOD THEREFOR
A crystal form I of a Janus Kinase (JAK) inhibitor (3aR,5s,6aS)-N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2- ...
2018/0237437 NOVEL PROCESS
A process for making certain spiroheterocyclic pyrrolidine dione derivatives.
2018/0237436 HYDANTOIN DERIVATIVE
The present invention provides compounds represented by formula (1) below and pharmacologically acceptable salts thereof: ##STR00001## wherein R.sub.1, R.sub.2,...
2018/0237435 GUANIDINE SUBSTITUTED IMIDAZO[4,5-c] RING COMPOUNDS
Imidazo[4,5-c] ring compounds, (particularly imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and...
2018/0237434 MICROBIOCIDAL HETEROBICYCLIC DERIVATIVES
Compounds of the formula (I) wherein Q.sub.1, Q.sub.2, Y--X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.b, R.sub.c, R.sub.d, R.sub.5, R.sub.6, R.sub.7, Ra, m...
2018/0237433 PROCESS DEVELOPMENT OF A PYRIDINE-CONTAINING NK-1 RECEPTOR ANTAGONIST
The disclosure provides process developments and novel routes for the preparation of the NK-1 receptor antagonist, Compound (I) and intermediates in those...
2018/0237432 BRIDGED PIPERIDINE DERIVATIVES
The present invention relates to compounds of formula ##STR00001## hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S...
2018/0237431 COMPOSITIONS, FORMULATIONS AND METHODS FOR TREATING OCULAR DISEASES
Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions...
2018/0237430 COMPOSITIONS, FORMULATIONS AND METHODS FOR TREATING OCULAR DISEASES
Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions...
2018/0237429 COMPOSITIONS, FORMULATIONS AND METHODS FOR TREATING OCULAR DISEASES
Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions...
2018/0237428 NOVEL COMPOUNDS AS ROR GAMMA MODULATORS
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R.sup.1, R.sup.2,...
2018/0237427 INHIBITORS OF BETA-HYDROXYLASE FOR TREATMENT OF CANCER
The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel ...
2018/0237426 HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
2018/0237425 PROCESSES FOR THE PREPARATION OF BENZODIAZEPINE DERIVATIVES
The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of...
2018/0237424 FGFR3 ANTAGONISTS
The invention pertains to novel FG-FR3antagonists of general formula (I), The compounds are useful for the treatments and prevention of achondroplasia and...
2018/0237423 NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula: ##STR00001## where X, R.sup.a, R.sup.b, R.sup.2, and R.sup.7 are as defined in the ...
2018/0237422 TRIAZOLYL PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS
The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous...
2018/0237421 SUBSTITUTED PYRAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS
There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin and/or kallikrein, which compounds include substituted...
2018/0237420 BENZIMIDAZOLE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS
The invention relates to benzimidazole-carboxamide 5-HT.sub.4 receptor agonist compounds of formula (I) ##STR00001## wherein R.sup.1 and X are as defined in the...
2018/0237419 AZETIDINE COMPOUNDS AS GRP119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
The present disclosure relates to azetidine compounds. The azetidine compounds are GPR119 modulators and useful for the prevention and/or treatment of...
2018/0237418 MODULATORS OF ESTROGEN RECEPTOR PROTEOLYSIS AND ASSOCIATED METHODS OF USE
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present...
2018/0237417 SUBSTITUTED BENZIMIDAZOLES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
This application relates to substituted benzimidazoles, compositions comprising them and their uses in the treatment of diseases and conditions in which...
2018/0237416 INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS
Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an...
2018/0237415 AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to amide derivatives having dual pharmacological activity towards both the sigma (.sigma.) receptor, and the .mu.-opioid...
2018/0237414 METHOD FOR THE PREPARATION OF THE METABOLITES OF (4S)- AND ...
The present invention relates to a novel method for preparing (4R)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-na- ...
2018/0237413 HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
2018/0237412 SELECTIVE MATRIX METALLOPROTEINASE INHIBITORS
The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix...
2018/0237411 ISOFLAVONOID COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER
Provided herein is a pharmaceutical composition comprising an isoflavonoid derivative and a cyclodextrin. Also provided herein are methods of treating cancer,...
2018/0237410 HYDROPHILIC COMPOUNDS FOR OPTICALLY ACTIVE DEVICES
The present invention relates to novel compounds, particularly to hydrophilic compounds, comprising a photoactive unit, said novel compounds being particularly...
2018/0237409 COMPOUNDS FOR OPTICALLY ACTIVE DEVICES
The present invention relates to novel compounds, particularly to compounds comprising a photoactive unit, said novel compounds being particularly suitable for...
2018/0237408 METHOD OF PRODUCING BERAPROST
An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d...
2018/0237407 PHENYLSULFONAMIDO-BENZOFURAN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF PROLIFERATIVE DISEASES
Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions,...
2018/0237406 PHENYLSULFONAMIDO-BENZOFURAN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF PROLIFERATIVE DISEASES
Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions,...
2018/0237405 TREATMENT OF MULTIPLE SCLEROSIS AND PSORIASIS USING PRODRUGS OF METHYL HYDROGEN FUMARATE
Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering...
2018/0237404 HETEROCYCLIC COMPOUND
Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom...
2018/0237403 SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF...
A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: ...
2018/0237402 AZAQUINAZOLINE CARBOXAMIDE DERIVATIVES
Novel azaquinazoline carboxamide derivatives of formula (I) ##STR00001## wherein W.sup.1, W.sup.2, W.sup.3, W.sup.4, R.sup.1, R.sup.2, R.sup.3 and m which are...
2018/0237401 TRIAZOLE DERIVATIVES
The present invention relates to compounds of formula I ##STR00001## wherein R.sup.1' is CH.sub.3 R.sup.1 is methyl, ethyl, CF.sub.3, CH.sub.2OH, cyclopropyl or...
2018/0237400 Synthesis Of Benzodiazepine Derivatives
The invention relates to processes for the synthesis of benzodiazepine derivatives of Formula I: (I) ##STR00001##
2018/0237399 COMPOUNDS HAVING AGONISTIC EFFECT AGAINST GPR84, PREPARATION METHOD FOR COMPOUNDS AND USE OF COMPOUNDS
The present invention relates to a class of compounds represented by the formula I, or pharmaceutically acceptable salts thereof, methods for their...
2018/0237398 UREA DERIVATIVE AND USE THEREFOR
A compound has inhibitory activity on Discoidin Domain Receptor 1. A urea derivative is represented by the formula (I) or a pharmaceutically acceptable salt...
2018/0237397 PYRAZOLE DERIVATIVES AS ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein...
2018/0237396 Processes For Preparing AG-10, Its Intermediates, and Salts Thereof
Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of...
2018/0237395 (--)-HUPERZINE A PROCESSES AND RELATED COMPOSITIONS AND METHODS OF TREATMENT
The invention provides (1) processes for making substantially-pure (-) huperzine A and substantially-pure (-) huperzine A derivatives; (2) compositions useful...
2018/0237394 COMPOSITIONS AND METHODS FOR TREATING TUBERCULOSIS
The present invention provides compounds for the treatment of a bacterial infection. Additionally, the present invention provides compositions and methods for...
2018/0237392 CHARGED ION CHANNEL BLOCKERS AND METHODS FOR USE
The invention provides compounds, compositions, methods, and kits for the treatment of pain, itch, and neurogenic inflammation.
2018/0237391 OCTAHYDROCYCLOPENTAPYRROLES, THEIR PREPARATION AND USE
The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when...
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