The present disclosure is directed to antibody radioisotope construct comprising: a radioisotope; a chelating linker; and an antibody moiety specific for human urokinase plasminogen activator receptor (uPAR), wherein the chelating linker comprises one or more squaramide moieties. Also provided are methods of treating a disease or disorder in a patient in need thereof using the antibody radioisotope constructs, and methods of diagnosing a disease or disorder in a patient using the antibody radioisotopes disclosed herein.
Antibodies specific for uPAR and uPA-uPAR complexes in the form of radioconjugates with alpha particle-emitting radionuclides are disclosed as is their use in treating severe respiratory diseases such as severe COVID-19.
A targeted radiopharmaceutical of chemical Formula I, below, is disclosed wherein Q+3 is a
A targeted radiopharmaceutical of chemical Formula I, below, is disclosed wherein Q+3 is a
trivalent radioactive isotope ion; M is a proton (H+), an ammonium ion or an alkali metal ion; “g” is a number that is 1 to about 12; the boxed mAb MNPR-101 represents the chemically-bonded humanized mAb MNPR-101; and Y− is an optional anion present in an amount needed to balance the ionic charge. A pharmaceutical composition that comprises a theranostic effective amount of a Formula I targeted radiopharmaceutical dissolved or dispersed in a pharmaceutically acceptable diluent is also disclosed, as are a method for treating and/or diagnosing a mammalian host having a disease, disorder or condition characterized by undesired angiogenesis, tumor growth and/or tumor metastasis. A targeted pro-radiopharmaceutical construct similar to that of Formula I but without the radioisotope (Formula III) is also contemplated.
A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes
A61K 51/10 - Antibodies or immunoglobulinsFragments thereof
5.
Trivalent Radioisotope Bio-Targeted Radiopharmaceutical, Methods Of Preparation And Use
A targeted radiopharmaceutical comprising a targeting species chemically-bonded to a PCTA-chelated Q+3 trivalent radioactive ion of Formula I
A targeted radiopharmaceutical comprising a targeting species chemically-bonded to a PCTA-chelated Q+3 trivalent radioactive ion of Formula I
A targeted radiopharmaceutical comprising a targeting species chemically-bonded to a PCTA-chelated Q+3 trivalent radioactive ion of Formula I
is disclosed. Six of R1 through R7 are H and the seventh is a reacted functionality, Z, that forms the chemical bond with the targeting species, T. “g” is a number whose average value is 1 to about 12. X1, X2, and X3, are substituent groups that can coordinate to the Q+3 ion and/or help neutralize the ionic charge. Anion Y− is optionally present to balance the ionic charge. A pharmaceutical composition comprising a theranostic effective amount of a targeted radiopharmaceutical of Formula I in a pharmaceutically acceptable diluent is also contemplated, as are a method for treating and/or diagnosing a mammalian host having a disease, disorder or condition characterized by undesired angiogenesis, tumor growth and/or tumor metastasis.
A targeted radiopharmaceutical comprising a targeting species chemically-bonded to a PCTA-chelated Q+3 trivalent radioactive ion of Formula I is disclosed. Six of R1through R7are H and the seventh is a reacted functionality, Z, that forms the chemical bond with the targeting species, T. "g" is a number whose average value is 1 to about 12. X1, X2, and X3, are substituent groups that can coordinate to the Q+3 ion and/or help neutralize the ionic charge. Anion Y- is optionally present to balance the ionic charge. A pharmaceutical composition comprising a theranostic effective amount of a targeted radiopharmaceutical of Formula I in a pharmaceutically acceptable diluent is also contemplated, as are a method for treating and/or diagnosing a mammalian host having a disease, disorder or condition characterized by undesired angiogenesis, tumor growth and/or tumor metastasis.
C07D 487/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains two hetero rings
A targeted radiopharmaceutical of chemical Formula I, below, is disclosed wherein Q+3 is a trivalent radioactive isotope ion; M is a proton (H+), an ammonium ion or an alkali metal ion; "g" is a number that is 1 to about 12; the boxed mAb MNPR- 101 represents the chemically-bonded humanized mAb MNPR-101; and Y- is an optional anion present in an amount needed to balance the ionic charge, A pharmaceutical composition that comprises a theranostic effective amount of a Formula I targeted radiopharmaceutical dissolved or dispersed in a pharmaceutically acceptable diluent is also disclosed, as are a method for treating and/or diagnosing a mammalian host having a disease, disorder or condition characterized by undesired angiogenesis, tumor growth and/or tumor metastasis. A targeted pro-radiopharmaceutical construct similar to that of Formula I but without the radioisotope (Formula III) is also contemplated.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 51/10 - Antibodies or immunoglobulinsFragments thereof
C07F 5/00 - Compounds containing elements of Groups 3 or 13 of the Periodic Table
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Antibodies specific for uPAR and uPA-uPAR complexes in the form of radioconjugates with alpha particle—emitting radionuclides are disclosed as is their use in treating severe respiratory diseases such as severe COVID-19.
A61P 35/04 - Antineoplastic agents specific for metastasis
A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes
9.
3'DEAMINO-3'-(2"-PYRROLINE-1"-YL)-5-IMINO-13-DEOXYANTHRACYCLINES AND METHODS OF PREPARATION
2-pyrrolino- 13-deoxyanthracycline derivatives, medical uses thereof, and a process for making them. A 2-pyrrolino- 13-deoxyanthracycline and a 13-deoxyanthracycline can be administered to a patient simultaneously or sequentially in amounts to produce a synergistic therapeutic effect with increased potency and efficacy, compared to the sum of the effects of each drug when administered alone. A composition or preparation of a 2-pyrrolino- 13- deoxyanthracycline and a 13-deoxyanthracycline for producing a potent anticancer therapeutic effect is also provided.
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
C07H 15/24 - Condensed ring systems having three or more rings
2-pyrrolino-13-deoxyanthracycline derivatives, medical uses thereof, and a process for making them. A 2-pyrrolino-13-deoxyanthracycline and a 13-deoxyanthracycline can be administered to a patient simultaneously or sequentially in amounts to produce a synergistic therapeutic effect with increased potency and efficacy, compared to the sum of the effects of each drug when administered alone. A composition or preparation of a 2-pyrrolino-13-deoxyanthracycline and a 13-deoxyanthracycline for producing a potent anticancer therapeutic effect is also provided.
C07H 15/24 - Condensed ring systems having three or more rings
C07H 15/252 - Naphthacene radicals, e.g. daunomycins, adriamycins
C07H 19/04 - Heterocyclic radicals containing only nitrogen as ring hetero atom
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
11.
Clonidine and/or clonidine derivatives for use in the prevention of skin injury resulting from radiotherapy
The present invention pertains to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and Clonidine and/or Clonidine derivatives as a sole active ingredient for use in the prevention of skin injury resulting from radiotherapy by transmucocal administration.
The present invention pertains to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and Clonidine and/or Clonidine derivatives as a sole active ingredient for use in the prevention of skin injury resulting from radiotherapy by transmucocal administration.
The present invention pertains to specific clonidine and/or clonidine derivatives for use in the prevention and/or treatment of adverse side effects of alkylating agent chemotherapy, other than those resulting from mucosal inflammation. It also pertains to the use of this clonidine and/or clonidine derivative for the manufacture of a pharmaceutical composition intended to prevent and/or alleviate the adverse side effects of alkylating agent chemotherapy, other than those resulting from mucosal inflammation. This invention is further directed to a kit comprising: (a) a clonidine and/or clonidine derivative, and (b) at least one alkylating chemotherapeutic agent, as a combined preparation for simultaneous, separate or sequential use in the treatment of cancer.
The present invention concerns a pharmaceutical composition comprising an alpha-2 adrenergic receptor agonist for preventing or treating inflammatory pain and diseases in mucosa of oral cavity, pharynx and larynx. In another aspect the present invention provides mucosal bioadhesive slow release carriers for the extended and controlled release of alpha-2 adrenergic receptor agonists that can be used on mucosal surfaces for preventing or treating inflammatory pain and diseases in mucosa of oral cavity.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Bio-adhesive pharmaceutical preparations with slow-release
of an anti-inflammatory agent used for treating inflammatory
diseases and particularly mucitis.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Bioadhesive pharmaceutical preparations for prolonged release of an anti-inflammatory agent used for the treatment of inflammatory diseases and in particular mucosal inflammation.
17.
Anticancer treatment with a combination of taxanes and 13-deoxyanthracyclines
A 13-deoxy anthracycline and a taxane can be administered to a patient simultaneously, separately, sequentially, or consecutively to produce a therapeutic anticancer effect with reduced toxicity and side effect profile, compared to the administration of equieffective amounts of either compound alone. A composition or preparation of a 13-deoxy anthracyclines and a taxane for producing a potent anticancer therapeutic effect is also provided.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
A 13-deoxy anthracycline and a taxane can be administered to a patient simultaneously, separately, sequentially, or consecutively to produce a therapeutic anticancer effect with reduced toxicity and side effect profile, compared to the administration of equieffective amounts of either compound alone. A composition or preparation of a 13-deoxy anthracyclines and a taxane for producing a potent anticancer therapeutic effect is also provided.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
Antibodies specific for uPAR and uPA-uPAR complexes in the form of radioconjugates with alpha particle?emitting radionuclides are disclosed as is their use in treating severe respiratory diseases such as severe COVID-19.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A targeted radiopharmaceutical of chemical Formula I, below, is disclosed wherein Q+3 is a trivalent radioactive isotope ion; M is a proton (H+), an ammonium ion or an alkali metal ion; "g" is a number that is 1 to about 12; the boxed mAb MNPR- 101 represents the chemically-bonded humanized mAb MNPR-101; and Y- is an optional anion present in an amount needed to balance the ionic charge, A pharmaceutical composition that comprises a theranostic effective amount of a Formula I targeted radiopharmaceutical dissolved or dispersed in a pharmaceutically acceptable diluent is also disclosed, as are a method for treating and/or diagnosing a mammalian host having a disease, disorder or condition characterized by undesired angiogenesis, tumor growth and/or tumor metastasis. A targeted pro-radiopharmaceutical construct similar to that of Formula I but without the radioisotope (Formula III) is also contemplated.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 51/10 - Antibodies or immunoglobulinsFragments thereof
C07F 5/00 - Compounds containing elements of Groups 3 or 13 of the Periodic Table
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
21.
3'-DEAMINO-3'-(2"-PYRROLINE-1"-YL)-5-IMINO-13-DEOXYANTHRACYCLINES AND METHODS OF PREPARATION
2-pyrrolino- 13-deoxyanthracycline derivatives, medical uses thereof, and a process for making them. A 2-pyrrolino- 13-deoxyanthracycline and a 13-deoxyanthracycline can be administered to a patient simultaneously or sequentially in amounts to produce a synergistic therapeutic effect with increased potency and efficacy, compared to the sum of the effects of each drug when administered alone. A composition or preparation of a 2-pyrrolino- 13- deoxyanthracycline and a 13-deoxyanthracycline for producing a potent anticancer therapeutic effect is also provided.
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
The present invention pertains to a clonidine and/or clonidine derivative formulated for transmucosal administration, for use in the prevention and/or treatment of asthenia and/or fatigue due to alkylating agent chemotherapy. The clonidine and/or clonidine derivative is selected from compounds having the following formula, in which R1 and R2 are independently selected from H and -OCOR; R3 is selected from H, -CH2OH, -OCOR, -COOR, -NH2, -NHR, -NRR' and -NHCOR; and R and R independently designate a linear or branched alkyl group having from 1 to 6 carbon atoms, which may be substituted by one or more groups selected from a halogen atom, an amino group and an alkylamino group which alkyl part is a linear or branched alkyl having from 1 to 6 carbon atoms, and tautomer forms and pharmaceutically acceptable salts thereof
