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63 results about "Analogs & derivatives" patented technology
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Used with drugs and chemicals for substances that share the same parent molecule or have similar electronic structure but differ by the addition or substitution of other atoms or molecules. It is used when the specific chemical heading is not available and no appropriate group heading exists.
Vitamin receptor binding drug delivery conjugates
The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
Owner:ENDOCTYE INC
Novobiocin analogues as anticancer agents
Novel analogues and derivatives of novobiocin are provided, including compounds having modifications to the amide side chain, coumarin ring, and sugar moieties. The compounds of the present invention are useful as heat shock protein 90 inhibitors, and may be used as anticancer and neuroprotective agents.
Owner:UNIVERSITY OF KANSAS +1
Use of glp-1 analogs and derivatives administered peripherally in regulation of obesity
Owner:DIMARCHI RICHARD +1
G-csf site-specific mono-conjugates
Novel site-specific mono-conjugates of Granulocyte Colony Stimulating Factor (G-CSF) are hereby described, with analogues and derivatives thereof, which stimulate proliferation and differentiation of progenitor cells to mature neutrophiles. These conjugates have been obtained using transglutaminase to covalently and site-specifically bind a hydrophilic, non-immunogenic polymer to a single glutamine residue of the human G-CSF native sequence and analogues thereof. These novel site-specific mono-conjugated derivatives are recommended for therapeutic use since they are stable in solution and exhibit significant biological activity in vitro and a longer bloodstream half-life, as compared to the non-conjugated protein, with a consequent prolonged pharmacological activity.
Owner:BIO KER
Triazine compounds and their analogs, compositions, and methods
The present invention relates to triazine compounds and their analogs and derivatives, and methods and compositions comprising these compounds. The compounds and compositions of this invention are useful for, among other things, treating pathophysiological conditions arising from inflammatory responses, inhibiting or blocking glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells, inhibiting smooth muscle proliferation, treating vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis, and the like.
Owner:DR REDDYS LAB LTD
Azacytosine analogs and derivatives
Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 4- and 6-position of the triazine ring, at the 1′-6′position of the ribose ring, or combinations thereof. Methods of synthesizing and manufacturing these analogs and derivatives are also provided. These compounds can be formulated into pharmaceutical compositions that can be used for treating any disease that is sensitive to the treatment with decitabine or azacitidine, such as hematological disorders and cancer.
Owner:SUPERGEN
Cobalamin mediated delivery of nucleic acids, analogs and derivatives thereof
InactiveUS20060074034A1Prevent significant uncouplingImprove stabilityBiocideSugar derivativesCobalaminMedicinal chemistry
Owner:MAYO FOUND FOR MEDICAL EDUCATION & RES
Macrocyclic depsipeptide antibody-drug conjugates and methods
InactiveUS20090226465A1Prevent proliferationInhibit tumor cell growthImmunoglobulins against animals/humansAntibody ingredientsDiseaseKahalalide F
The present invention relates to antibody-drug conjugate compounds of Formula I: Ab (L D)p I where one or more macrocyclic depsipeptide drug moieties (D), selected from Aplidin, Didemnin B, Kahalalide F, and analogs and derivatives therefrom, are covalently attached by a linker (L) to an antibody (Ab) which binds to one or more tumor-associated antigens or cell-surface receptors. These compounds may be useful in methods of diagnosis or treatment of cancer, and other diseases and disorders.
Owner:GENENTECH INC
Peptides, derivatives and analogs thereof, and methods of using same
InactiveUS20070087971A1Promoting beta cell regenerationIncrease satietyOrganic active ingredientsSenses disorderHuman Proislet PeptideProgenitor
Human proIslet Peptides (HIP) and HIP analogs and derivatives thereof, derived from or homologous in sequence to the human REG3A protein, chromosome 2p12, are able to induce islet neogenesis from endogenous pancreatic progenitor cells. Human proIslet Peptides are used either alone or in combination with other pharmaceuticals in the treatment of type 1 and type 2 diabetes and other pathologies related to aberrant glucose, carbohydrate, and / or lipid metabolism, insulin resistance, overweight, obesity, polycystic ovarian syndrome, eating disorders and the metabolic syndrome.
Owner:CUREDM GRP HLDG
Synthesis and use of omega-3 and omega 6 very long chain polyunsaturated fatty acids (VLC-PUFA)
InactiveUS20130190399A1BiocideCarboxylic acid esters preparationFatty acids.polyunsaturatedTreatment use
The invention provides methods of synthesizing omega-3 and omega-6 very long chain polyunsaturated fatty acids (VLC-PUFAs, C28-C42:4, 5 and 6), analogs and derivatives thereof, pharmaceutical compositions containing these isolated VLC-PUFA compounds and therapeutic uses therefor.
Owner:DSM IP ASSETS BV
Azacytosine analogs and derivatives
Owner:SUPERGEN
Azacytosine analogs and derivatives
InactiveUS20060205687A1Decrease electrophilicityBiocideSugar derivativesAbnormal tissue growthPyrimidine analogue
Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 2-, 4-, or 6-position of the triazine ring, at the 1′-6′position of the ribose ring, or combinations thereof. Methods of using, synthesizing and manufacturing these analogs and derivatives are also provided. These compounds can be formulated into pharmaceutical compositions that can be used for treating any disease associated with aberrant DNA methylation, or a disease or condition that is sensitive to the treatment with decitabine or azacitidine, such as hematological disorders, tumors and cancers.
Owner:SUPERGEN
Method of Determining, Identifying or Isolating Cell-Penetrating Peptides
InactiveUS20140141452A1Reduce dilution effectReduce surfacePeptide/protein ingredientsAntibody mimetics/scaffoldsCell membranePeptide library
The present invention provides a method of determining or identifying or isolating a cell-penetrating peptide (CPP) or analog or derivative thereof having cell-type selectivity and / or at least capable of passing through a Blood Brain Barrier of an animal subject. This invention also provides CPPs and analogs and derivatives thereof, such as those set forth in SEQ ID NOs: 1-27 of the Sequence Listing, and compositions comprising one or more of the CPPs, including conjugates in which a CPP or analog or derivative thereof is linked to a cargo molecule. The invention also provides methods for transporting cargo molecules across cell membranes to specific locations within cells, and for treating, preventing and / or diagnosing diseases that are treatable by a cargo molecule to which a CPP or analog or derivative of the invention is attached. The invention also provides tailored peptide libraries for use in identifying or isolating CPPs.
Owner:PHYLOGICA
Luciferyl peptide substrate
InactiveUS20060073529A1Promote localizationPeptide/protein ingredientsMicrobiological testing/measurementLuciferase GeneCell membrane
Provided are luciferyl peptide substrates that are produced by attaching specifically prepared peptide conjugates to luciferin, and / or its analogs and derivatives. The luciferyl peptide substrates are incapable of penetrating cell membranes and tissue barriers. Cleavage of the peptide conjugates from the luciferyl peptide substrates releases the luciferin, which upon contact with luciferase emits photons for easy detection. The luciferyl peptide substrates may be used in assays to detect pathogens, test protease inhibitors, probe cell physiology, assess protease activity in oncogenesis, and improve specific and regulated drug delivery.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
Betulinic acid, derivatives and analogs thereof and uses therefor
Provided herein provided herein are novel analogs and derivatives of betulinic acid. Also provided is a method for inhibiting an activity of one or more specificity protein (Sp) transcription factors cells associated with a neoplastic disease using betulinic acid, betulinic acid analog(s) and / or derivative(s) effective to decrease expression of a microRNA with concomitant increase in Sp suppressor gene expression. The betulinic acid analogs and derivatives also are effective in methods provided herein for inhibiting proliferation of cells associated with a neoplastic disease for treating a cancer or for reducing toxicity of a cancer therapy in a subject via administration of an analog or derivative of betulinic acid and, optionally, another anticancer drug.
Owner:SAFE STEPHEN H +1
Use of dianhydrogalactitol and analogs and derivatives thereof to treat glioblastoma multiforme
ActiveUS20140221442A1Improve survivalFree of side effectBiocideNervous disorderDianhydrogalactitolGlioblastoma
The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.
Owner:DEL MAR PHARMA
Truncated glp-1 derivaties and their therapeutical use
InactiveUS20100292133A1Nervous disorderPeptide/protein ingredientsAmino acid substitutionExtracellular Structure
The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.
Owner:NOVO NORDISK AS
Processes for preparing tubulysins
InactiveUS20130137139A1Low yieldDifficult to remove impurityOrganic active ingredientsPeptide/protein ingredientsStereochemistryCombinatorial chemistry
Owner:ENDOCTYE INC
Process of preparation of formulations of the peptide angiotensin-(1-7) and its analogues, agonistic and antagonists using cyclodextrins, lipossomes and biodegradable polymers and/or mixtures and products thereof
The prior art lacks a formulation, application or product of D-Ala7-Angiotensin-(1-7) (A-779) and analogues and derivatives, D-Pro7-Angiotensin-(1-7) and analogues or derivatives or of Ang-(1-7) analogues or derivatives using ciclodextrines, lipossomes, biodegradable polymers and its derivatives for the study or treatment of arterial hypertension and other cardiovascular diseases, wounds, burns, erithema, tumors, diabetes mellitus, sperm mobility, nephropathy, gastrointestinal and gynaecological disorders, angiogenesis, angioplatsy, alopecia and blood diseases in warm blooded animals, or as ligands for de G-protein-coupled receptor MAS. This characterizes the present invention as a more effective option for the study and treatment of pathologies associated or not to this receptor. A combination of two different technologies are provided: the molecular encapsulament of the peptide angiotensin-(1-7) and its analogues and derivates in cyclodextrin and the microencapsulament in biodegradable polymers and lipossomes. It is also characterized by the increase of this peptides and its analogues and derivatives using the formulation.
Owner:UNIVERSIDADE FEDERAL DE MINAS GERAIS
Disialyllacto-n-tetraose (DSLNT) or variants, isomers, analogs and derivatives thereof to prevent or inhibit bowel disease
ActiveUS20130315990A1Prevent and treat bowel diseasePrevent and treat and inflammationBiocideOrganic active ingredientsBowels diseasesDisialyllacto-N-tetraose
Owner:RGT UNIV OF CALIFORNIA
Toll-Like Receptor 4 (Tlr-4) Agonist Peptides For Modulating Tlr-4 Mediated Immune Response
InactiveUS20140220074A1Increase secretionBacterial antigen ingredientsCell receptors/surface-antigens/surface-determinantsInfectious DisorderPharmaceutical drug
Peptides including an amino acid sequence of a fragment of mammalian Toll-like receptor-4 (TLR-4), analogs and derivatives thereof, and pharmaceutical compositions including these peptides. Methods for modulating a TLR-4 mediated immune response, particularly stimulating TLR-4 mediated immune response, thereby treating infectious diseases and cancer.
Owner:YEDA RES & DEV CO LTD
Use of GLP-1 analogs and derivatives administered peripherally in regulation of obesity
InactiveCN1242707ALose weightReduce healingPeptide/protein ingredientsMetabolism disorderObesityMedicinal chemistry
The present invention relates to the use of glucagon-like peptides such as GLP-1, GLP-1 analogs or GLP-1 derivatives in weight reduction methods and compositions.
Owner:ELI LILLY & CO
Processes for preparing tubulysins
Owner:ENDOCTYE INC
Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof
InactiveCN101516835AImprove drug deliveryReduce manufacturing costOrganic chemistrySelective androgen receptor modulatorSelective receptor modulator
Owner:THE OHIO STATE UNIV RES FOUND +1
Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
ActiveUS20160220537A1Increase profitAvoid repairsOrganic active ingredientsMicrobiological testing/measurementAnthraceneSide effect
Owner:RACE ONCOLOGY LTD
Nicotinic receptor agonists and analogues and derivatives thereof for the treatment of inflammatory diseases
InactiveUS20070249622A1Minimize impactMinor side effectsOrganic active ingredientsOrganic chemistrySide effectAntiinflammatory drug
Owner:UNIV LAVAL
Compositions and methods for treating hyperpigmentation
InactiveUS20020141953A1Reduce retention timeImprove shipping rateBiocideCosmetic preparationsPerilla oilCarboxylic acid
There is provided a topical composition for treating, preventing or ameliorating hyperpigmentation in human skin. The composition has a de-pigmenting agent in an amount effect to reduce or diminish pigmentation at an area of skin to which it is applied, and a cosmetically or pharmaceutically acceptable vehicle. Suitable de-pigmenting agents include 3,3'-thiodipropionic acid, thiazolidine-2-carboxylic acid, kaempferol-7-glucoside, perilla oil, and clofibrate and clofibrate analogs and derivatives. There is also provided methods for treating, preventing or ameliorating hyperpigmentation in human skin.
Owner:AVON PROD INC
Truncated GLP-1 Derivatives and Their Therapeutical Use
InactiveUS20140296131A1Nervous disorderPeptide/protein ingredientsAmino acid substitutionExtracellular Structure
Owner:NOVO NORDISK AS
Combination therapy
InactiveUS20070031374A1Reduce tumor burdenEnhance immune responseBiocideOrganic active ingredientsCombination therapyCancer research
Owner:NOVO NORDISK AS
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