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Patent # Description
US-9,353,150 Substituted pyrazino[1',2':1 ,5]pyrrolo[2,3-b]-indole-1,4-diones for cancer treatment
The present application provides, among other things, a compound of Formula I-a and/or I-b, ##STR00001## or a pharmaceutically acceptable salt thereof,...
US-9,353,149 Compounds, compositions and methods for the treatment of diseases through inhibiting TGF-.beta. activity
The present disclosure relates to compounds, compositions and methods for the treatment of diseases through inhibiting the activity of the transforming growth...
US-9,353,148 Method for producing peptide
The present invention provides a production method of a protected amino acid, protected peptide or peptide, including precipitation and solid-liquid separation...
US-9,353,147 Method for producing peptide
The present invention provides a production method of peptide, which includes the following step (1). (1) removing N-terminal Fmoc group of N-Fmoc C-protected...
US-9,353,146 Acylation derivatives of paridis saponins I, preparation method therefor and application thereof
The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and relates to novel Polyphyllin I derivatives of formula (I) that...
US-9,353,145 Process for preparing 17-substituted steroids
The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing...
US-9,353,144 Vascular leakage inhibitor
The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present invention inhibits the apoptosis of...
US-9,353,143 Ecdysterone compounds
An ecdysterone compound is described. An ecdysterone compound may include ecdysterone and decanoic acid. An ecdysterone compound may further include ecdysterone...
US-9,353,142 Protecting group for indole group, nucleic acid-synthesizing amidite and nucleic acid-synthesizing method
A protecting group for 1-nitrogen atom of an indole group including a sulfonylethyl carbamate group, wherein the protecting group is represented by the...
US-9,353,141 Galectoside inhibitors of galectins
The present invention relates to novel compounds prepared from readily accessible 3-O-propargyl-D-galactopyranoside derivatives and having an effect as i.a.,...
US-9,353,140 BQC-G, a tumor-selective anti-cancer prodrug
The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative...
US-9,353,139 Metal complexes with N-Aminoamidinate ligands
The invention relates to new metal complexes having N-aminoamidinate ligands, more particularly metal complexes having N,N'-bis(dimethylamino)acetamidinate, ...
US-9,353,137 Method for separation and purification of phosphatidylcholine employing magnetic nanoparticles and compositions...
A process for separation and purification of phosphatides, especially phosphatidylcholine, from vegetable lecithins, comprising deoiling with acetone, dissolved...
US-9,353,136 Process for preparing (meth)acrylamido-functional silanes by the reaction of aminoalkyl alkoxysilanes with...
The invention relates to a process for preparing (meth)acrylamido-functional silanes.
US-9,353,135 Silicone compound and a use thereof
One of the purposes of the present invention is to provide a compound which is a polymerizable monomer having a specific number of silicon atoms and a specific...
US-9,353,134 Silicon-containing carboxylic acid derivative
A compound represented by the formula (I) [at least one of R.sup.1, R.sup.2, and R.sup.3 represents a cyclic alkyl group, the remaining represents a linear or...
US-9,353,133 Boron-containing small molecules
This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal...
US-9,353,132 Boron-based 4-hydroxytamoxifen and endoxifen prodrugs as treatment for breast cancer
The present disclosure relates to boron-based 4-hydroxytamoxifen and endoxifen prodrugs and the synthesis of the same. Further, the present disclosure teaches...
US-9,353,131 Methods for forming protected organoboronic acids
Described are methods of forming protected boronic acids that provide in a manner that is straightforward, scalable, and cost-effective a wide variety of...
US-9,353,130 Process for the in situ activation of zinc metal
A non-carcinogenic process for the activation of zinc metal in a medium polarity solvent, wherein said zinc metal is activated by the reaction thereof with a...
US-9,353,129 Microporous coordination complex and method of making the same
Disclosed herein is a three-dimensional coordination complex that includes a plurality of inorganic centers; a plurality of a first bis(bidentate) linker; and a...
US-9,353,128 Disubstituted naphthoheterodiazole compounds
Disubstituted naphthoheterodiazole compound having general formula (I): ##STR00001## wherein: Z represents a heteroatom selected from oxygen (O), sulfur (S),...
US-9,353,127 Methods of preparation of conjugates
The present invention is directed to methods of preparing a conjugate of a cell-binding agent and a drug (such as a cytotoxic compound). The methods comprise...
US-9,353,126 Substituted triazoles useful as Axl inhibitors
Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein...
US-9,353,125 Process for the preparation of benzohetero [1,3]-diazole compounds disubstituted with heteroaryl groups
Process for the preparation of a benzohetero[1,3]diazole compound disubstituted with heteroaryl groups which comprises reacting at least one...
US-9,353,124 Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting...
US-9,353,123 Therapeutic compounds and uses thereof
Described herein are compounds of Formula (I)-(III), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are...
US-9,353,122 Therapeutic compounds and uses thereof
Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided...
US-9,353,121 Anti-cancer compounds targeting Ral GTPases and methods of using the same
The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also...
US-9,353,120 Tetraaza macrocyclic compound, preparation method thereof and use thereof
Provided are a cross-bridged tetraaza macrocyclic compound of a novel structure that can be used, for example, as a contrast agent for diagnostic imaging or a...
US-9,353,119 Composition for preventing and treating non-small cell lung cancer, containing pyrazino-triazine derivatives
Disclosed is a composition comprising a pyrazino-triazine derivative, an isomer thereof or a pharmaceutically acceptable salt thereof. It is very effective for...
US-9,353,117 Substituted pyrazolopyrimidines as glucocerebrosidase activators
Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and...
US-9,353,116 Methods and compositions for kinase inhibition
The present invention sets forth a new chemical genetic approach for engineering kinase enzymes with a cysteine gatekeeper residue as well as for developing...
US-9,353,115 Immune system modulators
The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the...
US-9,353,114 Process for the preparation of dipeptidylpeptidase inhibitors
Provided is a process for the preparation of linagliptin of Formula I, comprising deprotecting a compound of Formula II wherein R.sub.1 and R.sub.2 together...
US-9,353,113 Tetrahydrocarboline derivative
An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a...
US-9,353,112 Synthesis of polycyclic alkaloids
Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having...
US-9,353,111 Carboxamide compounds and methods for using the same
Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure ##STR00001## ...
US-9,353,110 Fused heterocyclic compound
There is provided a compound having an excellent controlling effect on pests represented by the formula (1): ##STR00001## wherein, A.sup.1 represents...
US-9,353,109 Flindersia alkaloids, derivatives and analogs: compositions and methods for producing the same
The present invention provides methods for chemically synthesizing analogs and derivatives of naturally-occurring Flindersia alkaloids. Generally, the precursor...
US-9,353,108 Tetrahydronaphthyridine somatostatin receptor 5 antagonists
A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following...
US-9,353,107 3-(pyrazolyl)-1H-pyrrolo[2,3-b]pyridine derivatives as kinase inhibitors
The present application relates to novel 3-(pyrazolyl)-1H-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. ##STR00001## The...
US-9,353,106 Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
The invention provides novel quinolinone-carboxamide 5-HT.sub.4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising...
US-9,353,105 Complex targeting hepatitis B virus
A compound medicine for treating acute and chronic hepatitis B, includes a polyphenolic selenium compound having a functional group of alkali metal ion and...
US-9,353,104 Substituted pyridizinone derivatives as PDE10 inhibitors
The present invention is directed to substituted pyridizinone compounds of formula I which are useful as therapeutic agents for the treatment of central nervous...
US-9,353,103 Macrocyclic inhibitors of hepatitis C virus
Inhibitors of HCV replication of formula (I) ##STR00001## and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double...
US-9,353,102 Non-annulated thiophenylamides
The invention provides novel compounds having the general formula (I) ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A, E...
US-9,353,101 Cyclic amine substituted heterocyclic CETP inhibitors
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising...
US-9,353,100 Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating HCV...
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation...
US-9,353,099 Compounds that modulate intracellular calcium
Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels....
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