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Patent # Description
US-1,013,8272 Matriptase and u-plasminogen activator substrates and other cleavable moieties and methods of use thereof
The invention relates generally to polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and...
US-1,013,8271 Native and agonist CTL epitopes of the MUC1 tumor antigen
The invention provides peptides comprising a human cytolytic T lymphocyte (CTL) epitope from the human tumor-associated antigen (TAA) mucin 1 (MUC1) and analogs...
US-1,013,8270 Synthetic peptide amides
The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low...
US-1,013,8269 Method for producing amino acid crystals and method for producing protein crystals
A method for producing a crystalline amino acid involves a step of irradiating a saturated solution of an amino acid with an optical vortex and depositing a...
US-1,013,8268 Peptide fragment condensation and cyclisation using a subtilisin variant with improved synthesis over...
The invention relates to a method for enzymatically synthesizing an (oligo)peptide, comprising coupling (a) an (oligo)peptide C-terminal ester or thioester and...
US-1,013,8267 Bioconjugates of heterocyclic compounds
The invention provides bioconjugates of heterocylic compounds such as S-adenosylmethionine and S-adenosylhomocysteine with biotin or digoxigenin. The...
US-1,013,8266 Method of cutting out RNA oligonucleotide
The invention provides a cut-out method capable of suppressing production of a byproduct, wherein the object RNA oligonucleotide is not cleaved from a universal...
US-1,013,8265 Uridine nucleoside derivatives, compositions and methods of use
This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods...
US-1,013,8264 Recombined molecules and preparation thereof
The invention relates to novel molecules and libraries thereof as well as methods for their production. Methods of producing the novel molecules include the...
US-1,013,8263 Non-caloric sweetener
Disclosed is a steviol glycoside referred to as rebaudioside D2. Rebaudioside D2 has five .beta.-D-glucosyl units connected to the aglycone steviol. Also...
US-1,013,8262 Reactive multi-functional additives for coatings compositions
A composition comprising: (a) from 20 to 60 wt % of a saccharide component comprising from two to five sugar ring units having polymerized units of at least...
US-1,013,8261 Ferrocenyl compounds
A ferrocenyl compound having the general formula (I): (I) Het is a substituted or unsubstituted heterocyclic moiety. L1, L2 and L3 are each a linker...
US-1,013,8260 Compounds of phosphinanes and azaphosphinanes, a process for their preparation and pharmaceutical compositions...
Compounds of formula (I) ##STR00001## wherein: Ak.sub.1 represents an alkyl chain, X represents --(CH.sub.2).sub.m--, --CH(R)--, --N(R)--, --CH.sub.2--N(R)--,...
US-1,013,8258 Cyclic siloxane compounds and compositions comprising the same
A composition comprises a plurality of cyclic siloxane compounds. At least a portion of the cyclic siloxane compounds comprise first and second siloxane...
US-1,013,8257 Transition metal complexes, production and use thereof
Phosphasalen transition metal complexes are disclosed for use in alkene polymerization to produce polyolefins. The transition metal complexes are represented by...
US-1,013,8256 MK2 inhibitors and uses thereof
The present invention provides compounds, compositions thereof, and methods of using the same.
US-1,013,8255 Piperazine derivatives as HIV protease inhibitors
The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease,...
US-1,013,8254 Bicyclic compounds as pest control agents
The present application relates to novel bicyclic compounds, to their use for controlling animal pests and to processes and intermediates for their preparation.
US-1,013,8253 Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the...
US-1,013,8252 Lactones
The present disclosure relates to novel lactones such as dihydropyrrole-fused furanones, a novel palladium-catalyzed carbonylation method to make the novel...
US-1,013,8251 Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors
The present invention encompasses compounds of formula (I) ##STR00001## wherein the groups R.sup.1 to R.sup.7, V, W, X, Y, n and q are defined herein, their...
US-1,013,8250 Salt of pyrrolo[2,3-D]pyrimidine compound and novel polymorph of salt
The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyr- imidine-6-carboxylic acid...
US-1,013,8249 Triazolopyridines and triazolopyrazines as LSD1 inhibitors
The present invention is directed to [1,2,4]triazolo[4,3-a]pyridine and [1,2,4]triazolo[4,3-a]pyrazine derivatives which are LSD1 inhibitors useful in the...
US-1,013,8248 Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted...
This application relates to compounds of Formula (I): ##STR00001## or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of...
US-1,013,8247 7-(morpholin-4-yl)pyrazole[1,5-A]pyrimidine derivatives as PI3 kinase inhibitors
A compound of the general formula (I) wherein Y represents --CH.sub.2-- or >C=0; R.sup.1 is selected from the group consisting of A1, A2 and A3; R.sup.2...
US-1,013,8246 Deuterated triazolopyridazine as a kinase modulator
The invention is directed to a triazolopyridazine compound of formula (I), N-oxides, pharmaceutically acceptable salts and solvates thereof, wherein D...
US-1,013,8244 Triazolopyrazinone derivative useful as a human PDE1 inhibitor
The present invention provides a compound of Formula I: ##STR00001## or a pharmaceutically acceptable salt thereof, for use as a human PDE1 inhibitor.
US-1,013,8243 Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors
Provided herein are compounds of the General Formula I: ##STR00001## and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A,...
US-1,013,8242 Pyrazolopyridine derivatives and their use in therapy
The present invention relates to pyrazolopyridine derivatives, which are useful as medicaments, pharmaceutical compositions comprising one or more of the...
US-1,013,8241 Substituted benzamides as RIPK2 inhibitors
The present invention relates to compounds of formula (I): ##STR00001## or pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, X, Y, and HET...
US-1,013,8240 Crystal of 5-hydroxy-4-(trifluoromethyl)pyrazolopyridine derivative
A crystal of a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is...
US-1,013,8239 Preparation method of crystalline form a of PCI-32765
A preparation method of PCI-32765 crystalline form A, which comprises the following steps: 1) dissolving free base of PCI-32765 in a good solvent; 2) the...
US-1,013,8238 Pesticidally active polycyclic derivatives with sulfur containing substituents
Polycyclic derivatives of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers,...
US-1,013,8237 1,2,4-triazolo[4,3-a]pyridine compounds and their use as positive allosteric modulators of mGluR2 receptors
The present invention relates to novel 1,2,4-triazolo[4,3-a]pyridine compounds as positive allosteric modulators (PAMs) of the metabotropic glutamate receptor...
US-1,013,8236 Factor xia-inhibiting pyridobenzazepine and pyridobenzazocine derivatives
The invention relates to substituted pyridobenzazepine and pyridobenzazocine derivatives and to processes for preparation thereof, and also to the use thereof...
US-1,013,8235 Pyrazolopyridine derivatives, preparation process therefor and therapeutic use thereof
The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) ##STR00001## to a process for preparing them and to the...
US-1,013,8234 2-phenyl or 2-hetaryl imidazol[1,2-a]pyridine derivatives
The invention relates to compounds of formula I: ##STR00001## and to pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1-R.sup.6,...
US-1,013,8233 Imidazole compounds as modulators of FSHR and uses thereof
The present invention relates to imidazole compounds, and pharmaceutically acceptable compositions thereof, useful as positive allosteric modulators of follicle...
US-1,013,8232 Naphthyridinedione derivatives
The invention relates to compound of the formula (I') ##STR00001## or a salt thereof, wherein the substituents are as defined in the specification; to its...
US-1,013,8231 Tricyclic and tetracyclic systems acting upon the vascular and central nervous systems
Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The...
US-1,013,8230 Autotaxin inhibitors
The present invention relates to compounds of formula (I): wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4a, R.sub.4b, R.sub.4C, R.sub.4d, L, A, Q, W and HET are...
US-1,013,8229 Heteroaromatic compounds as BTK inhibitors
The present invention encompasses compounds of the formula (I) ##STR00001## wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the...
US-1,013,8228 Isoxazole derivatives as FXR agonists and methods of use therof
The present invention provides compounds of Formula I: ##STR00001## and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising...
US-1,013,8227 Heteroaryl substituted pyridines and methods of use
The invention discloses compounds of Formula I, ##STR00001## wherein X.sup.1, X.sup.2, R.sup.1, and R.sup.2 are as defined herein. The present invention...
US-1,013,8226 Benzimidazol-2-amines as MIDH1 inhibitors
The present invention relates to benzimidazol-2-amines of general formula (I) in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8,...
US-1,013,8225 Amide compounds for treatment of medical disorders
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition...
US-1,013,8224 Preparation method of rociletinib
Disclosed is a method for preparing Rociletinib. 2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5 -(trifluoromethyl)-pyrimidin-4-one is obtained by means...
US-1,013,8223 Stable crystal form of tipiracil hydrochloride and crystallization method for the same
An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride....
US-1,013,8222 Substituted benzamides as RIPK2 inhibitors
The present invention relates to compounds of formula (I): ##STR00001## or pharmaceutically acceptable salts thereof, wherein R.sup.1--, R.sup.2--, X, Y, and...
US-1,013,8221 Salts of nilotinib and polymorphs thereof
The present invention provides novel salts of nilotinib and polymorphs thereof. The acid addition salts of nilotinib with benzenesulfonic acid, butanedisulfonic...
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