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Patent # Description
2017/0217968 PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME
Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: ##STR00001## or a pharmaceutically...
2017/0217967 POLYMORPH OF SYK INHIBITORS
Polymorphs of a bis-mesylate salt of a compound of Formula I: ##STR00001## or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a...
2017/0217966 PYRAZOLOPYRIMIDINE COMPOUNDS
The present teachings provide a compound represented by structural formula (I-0), or a pharmaceutically acceptable salt thereof. Also described are...
2017/0217965 NEW BENZODIAZEPINE DERIVATIVE AND USE THEREOF
The present invention relates to a new benzodiazepine derivative, pharmaceutically acceptable salt thereof, preparation method therefor, and use thereof. The...
2017/0217964 AMINOTETRAHYDROPYRAN DERIVATIVE USED AS DIPEPTIDYL PEPTIDASEIV INHIBITOR
Provided is an Aminotetrahydropyran derivative represented by general formula (I), a preparation method for the derivative, a pharmaceutical composition...
2017/0217963 SPHINOGOSINE-1-PHOSPHATE RECEPTOR MODULATORS FOR TREATMENT OF CARDIOPULMONARY DISORDERS
The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension...
2017/0217962 A PROCESS FOR THE PREPARATION OF PALBOCICLIB
The present invention relates to a process for the preparation of palbociclib utilizing a silyl-protected crotonic acid derivative to produce a...
2017/0217961 PYRIMIDINE-2,4-DIAMINE DERIVATIVES FOR TREATMENT OF CANCER
A compound of formula I, ##STR00001## or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may...
2017/0217960 IMMUNOMODULATORS AND IMMUNOMODULATOR CONJUGATES
The invention provides compounds of formula I: ##STR00001## wherein R.sub.1--R.sub.3, R.sup.a, and R.sup.b have any of the values defined herein, and salts...
2017/0217959 NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula: ##STR00001## where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a...
2017/0217958 PYRAZOLE DERIVATIVE MANUFACTURING METHOD
The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided are a method for manufacturing a ...
2017/0217957 METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NA- ...
The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihy- ...
2017/0217956 AZAINDOLE RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
Provided herein are compounds of the formulas (I) and (II), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those...
2017/0217955 INHIBITORS OF HISTONE DEACETYLASE
The present invention relates to compounds of formula (I): ##STR00001## or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U,...
2017/0217954 CYANO-SUBSTITUTED IMIDAZO[1,2-A]PYRIDINECARBOXAMIDES AND THEIR USE
The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or...
2017/0217953 PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUNDS
The present invention relates to a process for the preparation of a compound of formula (I) wherein A.sub.1 and A.sub.2 are C--H, or one of A.sub.1 and A.sub.2...
2017/0217952 CRYSTALLINE FORM
The invention provides a crystalline form of the compound of formula (Ia), methods for making the crystalline form of the compound of formula (Ia), and...
2017/0217951 Metabotropic Glutamate Receptor Negative Allosteric Modulators (NAMS) and Uses Thereof
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the...
2017/0217950 Bicyclo[3.2.1]Octyl Amide Derivatives and Uses of Same
The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): ##STR00001## wherein L, R.sup.1 and R.sup.2 are as defined herein, or a ...
2017/0217949 4-ARYL-N-PHENYL-1,3,5-TRIAZIN-2-AMINES CONTAINING A SULFOXIMINE GROUP
The present invention relates to 4-aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia) as described and defined...
2017/0217948 XANTHINE OXIDASE INHIBITOR
Provided are a xanthine oxidase inhibitor, a drug for improving vascular endothelial function, and an excellent therapeutic or prophylactic drug for diseases...
2017/0217946 AMINO-SUBSTITUTED ISOXAZOLES
The present invention relates to amino-substituted isoxazoles of general formula (I): in which A, R1 and R2 are as defined in the claims, to methods of...
2017/0217945 BENZOXAZINONE AMIDES AS MINERALOCORTICOID RECEPTOR MODULATORS
Disclosed are certain derivatives of benzoxazinone amides of formula (I), or pharmaceutically acceptable salts thereof, (Formula (I)) that act as ...
2017/0217944 TAXIFOLIN DERIVATIVE WITH SUPERIOR ANTIOXIDANT EFFECT AND COSMETIC COMPOSITION CONTAINING THE SAME
Disclosed are taxifolin derivative with superior antioxidant effect, a method of synthesizing the same and a cosmetic composition containing the same. In...
2017/0217943 SMALL MOLECULE INHIBITORS OF FIBROSIS
Described herein are compounds and compositions for the treatment of a fibrotic disease.
2017/0217942 [7,6]-FUSED BICYCLIC ANTIDIABETIC COMPOUNDS
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may...
2017/0217941 SUBSTITUTED BENZENE AND 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS
The present invention relates to substituted benzene compounds and bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical...
2017/0217940 FUSED TETRACYCLIC HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A', R.sup.2A, R.sup.2B, R.sup.7, R.sup.8,...
2017/0217939 CRYSTALLINE FORMS OF VILAZODONE HYDROCHLORIDE AND VILAZODONE FREE BASE
The present application relates to crystalline and amorphous Vilazodone hydrochloride. The present application further relates to amorphous solid dispersions...
2017/0217938 FLUORINATED BENZOFURANYL-PYRIMIDINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP
The present invention relates to fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined...
2017/0217937 ADDITIVE FOR IMPARTING ULTRAVIOLET ABSORBENCY AND/OR HIGH REFRACTIVE INDEX TO MATRIX, AND RESIN MEMBER USING SAME
Provided is an additive for imparting ultraviolet absorbency, or an additive for imparting a high refractive index, which has satisfactory compatibility with a...
2017/0217936 PYRROLIDINYL UREA, PYRROLIDINYL THIOUREA AND PYRROLIDINYL GUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R.sup.1, R.sup.2, R.sup.a,...
2017/0217935 SALT OF MONOCYCLIC PYRIDINE DERIVATIVE AND CRYSTAL THEREOF
The present invention provides salts consisting of an organocarboxylic acid selected from the group consisting of succinic acid and maleic acid and a compound...
2017/0217934 METHOD FOR PRODUCING SUBSTITUTED ANTHRANILIC ACID DERIVATIVES
The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) ##STR00001## in which R.sup.1, R.sup.2,...
2017/0217933 APOPTOSIS SIGNAL-REGULATING KINASE INHIBITOR
The present invention relates to a compound of formula (I): ##STR00001## The compound has apoptosis signal-regulating kinase ("ASK1") inhibitory activity, and is...
2017/0217932 Nrf2 Activating Compounds and Uses Thereof
Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may find use in the treatment of autoimmune and inflammatory diseases...
2017/0217931 COMPOUNDS FOR USE IN ANTHELMINTHIC TREATMENT
Disclosed are compounds of formula (I) which possess anthelminthic properties wherein the structural elements have the meaning as indicated in the description....
2017/0217930 PYRROLIDINE GPR40 MODULATORS FOR THE TREATMENT OF DISEASES SUCH AS DIABETES
The present invention provides compounds of Formula (I) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein all of...
2017/0217929 TREATMENT OF SOLID TUMORS BY INHIBITING MRK/ZAK
Methods and compounds are described for treating solid tumors, and in particular, malignant, neoplastic solid tumors such as glioblastoma and medulloblastoma,...
2017/0217928 PESTICIDALLY ACTIVE HETEROCYCLIC DERIVATIVES WITH SULPHUR CONTAINING SUBSTITUENTS
Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers,...
2017/0217927 AMORPHOUS FORM OF TETRACYCLIC COMPOUND
An amorphous form of 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihy- dro-5H-benzo[b]carbazole-3-carbonitrile and a solid dispersion...
2017/0217926 ETHYNYL DERIVATIVES
The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment...
2017/0217925 PROCESS FOR PREPARING 3-[(S)-7-BROMO-2-(2-OXOPROPYLAMINO)-5-PYRIDIN-2-YL-3H-1,4-BENZODIAZEPIN-3- ...
A process for preparing 3-[(S)-7-bromo-2-(2-oxo-propylamino)-5-pyridin-2-yl-3H-1,4,-benzodiazepin- -3-yl]propionic acid methyl ester at a high conversion rate...
2017/0217924 PROCESS FOR THE PREPARATION OF 3-(3-CHLORO-1H-PYRAZOL-1-YL)PYRIDINE
This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the...
2017/0217923 THERAPEUTIC COMPOUNDS AND RELATED METHODS OF USE
Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include...
2017/0217922 Nrf2 Activating Compounds and Uses Thereof
Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and...
2017/0217921 COFORMER SALTS OF (2S,3S)-METHYL 7-FLUORO-2-(4-FLUOROPHENYL)-3-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-4-OXO-1,2,- ...
Described herein are coformer salts of (2S,3S)-methyl 7-fluoro-2-(4-fluorophenyl)-3-(1-methyl-1H-1,2,4-triazol-5-yl)-4-oxo-1,2,- ...
2017/0217920 ANTIDIABETIC BICYCLIC COMPOUNDS
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may...
2017/0217919 Catalytic Enantioselective Synthesis of 2-Aryl Chromenes and Related Phosphoramidite Ligands and Catalyst Compounds
Methods to access 2-aryl chromene compounds via an asymmetric catalytic process.
2017/0217918 ANTIDIABETIC BICYCLIC COMPOUNDS
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof are agonists of G-protein coupled receptor 40 (GPR40) and may...
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