Compounds having activity as modulators of phosphodiesterase 7 (PDE 7) are provided. The compounds have the following Structures (I) or (II):
Compounds having activity as modulators of phosphodiesterase 7 (PDE 7) are provided. The compounds have the following Structures (I) or (II):
Compounds having activity as modulators of phosphodiesterase 7 (PDE 7) are provided. The compounds have the following Structures (I) or (II):
as a stereoisomer, enantiomer, or tautomer thereof or a mixture thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein each of R1, R2, R3, R4a, R4b, ring A, ring B, ring A′ and ring B′ (i.e., {circle around (A)}, {circle around (B)}, , and as shown in Structure (I) and (II), respectively) are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of phosphodiesterase 7 (PDE 7) are also provided.
Compounds having activity as modulators of phosphodiesterase 7 (PDE 7) are provided. The compounds have the following Structures (I) or (II): (I) (II) as a stereoisomer, enantiomer, or tautomer thereof or a mixture thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein each of R1, R2, R3, R4a, R4b, ring A, ring B, ring A' and ring B' (i.e.,, B, A', and B' as shown in Structure (I) and (II), respectively) are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of phosphodiesterase 7 (PDE 7) are also provided.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact. In another aspect, the invention provides compositions for inhibiting the effects of lectin-dependent complement activation, comprising a therapeutically effective amount of a MASP-2 inhibitory agent and a pharmaceutically acceptable carrier.
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
5.
Methods for Inhibiting Fibrosis in a Subject in Need Thereof
In one aspect, the invention provides methods for treating, inhibiting, alleviating or preventing fibrosis in a mammalian subject suffering, or at risk of developing a disease or disorder caused or exacerbated by fibrosis and/or inflammation. In one embodiment, the invention provides methods of treating a subject suffering from renal fibrosis. In one embodiment, the invention provides methods of reducing proteinuria in a subject suffering from a renal disease or condition associated with proteinuria. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation.
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Biological preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; preparations for diagnostic purposes are specifically excluded from all of the foregoing goods.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Biological preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; preparations for diagnostic purposes are specifically excluded from all of the foregoing goods.
9.
METHODS FOR INHIBITING ANGIOGENESIS IN A SUBJECT IN NEED THEREOF
In one aspect, the present invention provides methods for preventing, treating, reverting and/or delaying angiogenesis in a mammalian subject suffering from, or at risk for developing, an angiogenesis-dependent disease or condition, comprising administering to the subject an amount of a MASP-2 inhibitory agent effective to inhibit angiogenesis. In some embodiments of these aspects of the invention, the MASP-2 inhibitory agent is a MASP-2 antibody or fragment thereof.
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to MASP-3 inhibitory antibodies and compositions comprising such antibodies for use in inhibiting the adverse effects of MASP-3 dependent complement activation.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a human subject suffering from TMA associated with hematopoietic stem cell transplant. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation.
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
This disclosure is directed to compounds, compositions, and methods for the treatment of various diseases and/or conditions related to G protein-coupled receptor 174 (e.g., cancers).
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
15.
Methods for Treating and/or Preventing Graft-Versus-Host Disease and/or Diffuse Alveolar Hemorrhage and/or Veno-Occlusive Disease Associated with Hematopoietic Stem Cell Transplant
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a human subject suffering from graft-versus-host disease and/or diffuse alveolar hemorrhage and/or veno-occlusive disease associated with a hematopoietic stem cell transplant. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Biochemical preparations for medical purposes, namely, for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; chemical preparations for medical purposes, namely, for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; therapeutic preparations for medical purposes, namely, for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders.
17.
Compositions and Methods of Inhibiting MASP-1 and/or MASP-2 and/or MASP-3 for the Treatment of Various Diseases and Disorders
In one aspect, the invention provides methods and compositions for inhibiting MASP-3-dependent complement activation in a subject suffering from or at risk for developing, a disease or disorder selected from the group consisting of paroxysmal nocturnal hemoglobinuria, age-related macular degeneration, arthritis, disseminated intravascular coagulation, thrombotic microangiopathy, asthma, dense deposit disease, pauci-immune necrotizing crescentic glomerulonephritis, traumatic brain injury, aspiration pneumonia, endophthalmitis, neuromyelitis optica and Behcet's disease by administering to the subject a composition comprising an amount of a MASP-3 inhibitory agent in an amount effective to inhibit MASP-3-dependent complement activation. In some embodiments, the subject is administered a MASP-2 inhibitory agent and a MASP-1 inhibitory agent, a MASP-2 inhibitory agent and a MASP-3 inhibitory agent administered, a MASP-3 inhibitory agent and a MASP-1 inhibitory agent, or a MASP-1 inhibitory agent, a MASP-2 inhibitory agent and a MASP-3 inhibitory agent.
The present invention relates to therapeutic methods of using stable, high-concentration low-viscosity formulations of MASP-2 inhibitory antibodies, and kits comprising the formulations for treating subjects suffering from atypical hemolytic uremic syndrome (aHUS).
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; biologics for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; preparations for diagnostic purposes are
specifically excluded from all of the foregoing goods.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; biologics for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; preparations for diagnostic purposes are
specifically excluded from all of the foregoing goods.
21.
METHODS FOR TREATING CONDITIONS ASSOCIATED WITH MASP-2 DEPENDENT COMPLEMENT ACTIVATION
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact. In another aspect, the invention provides compositions for inhibiting the effects of lectin-dependent complement activation, comprising a therapeutically effective amount of a MASP-2 inhibitory agent and a pharmaceutically acceptable carrier.
The disclosure provides synthetic compositions useful as inhibitors of mannan-binding lectin-associated serine protease-2 (MASP-2), including compositions that selectively inhibit MASP-2 over thrombin, as well as methods for the manufacture and use thereof.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
23.
THERAPEUTIC METHODS AND USES FOR ANTIBODIES TO HUMAN MASP-3
Methods of treating paroxysmal nocturnal hemoglobinuria, complement 3 glomerulopathy, or idiopathic immune complex-mediated glomerulonephritis using MASP-3 serine protease inhibitors are provided. In some embodiments, the MASP-3 serine protease inhibitors are anti-MASP-3 antibodies. Also provided are uses of MASP-3 serine protease inhibitors in treatment of paroxysmal nocturnal hemoglobinuria, complement 3 glomerulopathy, or idiopathic immune complex-mediated glomerulonephritis and for manufacture of a medicament for treatment of paroxysmal nocturnal hemoglobinuria, complement 3 glomerulopathy, or idiopathic immune complex-mediated glomerulonephritis.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a human subject suffering from, or at risk for developing HSCT-IPS and/or suffering from, or at risk for developing HSCT-CLS and/or suffering from, or at risk for developing HSCT-FO and/or suffering from, or at risk for developing HSCT-ES. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Biochemical preparations for medical purposes, namely, for
the treatment of endothelial diseases and disorders, renal
diseases, transplant complications, and hematological,
neurological, immunological and inflammation-related disease
and disorders; chemical preparations for medical purposes,
namely, for the treatment of endothelial diseases and
disorders, renal diseases, transplant complications, and
hematological, neurological, immunological and
inflammation-related disease and disorders; therapeutic
preparations for medical purposes, namely, for the treatment
of endothelial diseases and disorders, renal diseases,
transplant complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Biological and pharmaceutical preparations for the treatment of transplant complications, ischemia-reperfusion injury, and endothelial, renal, cardiovascular, infectious, hematological, oncological, pulmonary, autoimmune, neurological, psychiatric, endocrine, metabolic, inflammatory, immunological, ocular, and addiction- and compulsion-related diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Biological and pharmaceutical preparations for the treatment of transplant complications, ischemia-reperfusion injury, and endothelial, renal, cardiovascular, infectious, hematological, oncological, pulmonary, autoimmune, neurological, psychiatric, endocrine, metabolic, inflammatory, immunological, ocular, and addiction- and compulsion-related diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for complement-mediated diseases, addiction and oncology, none of the foregoing in connection with pharmaceutical preparations for the treatment of dermatological diseases and conditions
The disclosure provides synthetic compositions useful as inhibitors of mannan-binding lectin-associated serine protease-2 (MASP-2), including compositions that selectively inhibit MASP-2 over thrombin, as well as methods for the manufacture and use thereof.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; biologics for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; preparations for diagnostic purposes are
specifically excluded from all of the foregoing goods.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; biologics for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, and hematological, neurological,
immunological and inflammation-related disease and
disorders; preparations for diagnostic purposes are
specifically excluded from all of the foregoing goods.
32.
THERAPEUTIC METHODS AND USES FOR ANTIBODIES TO HUMAN MASP-3
Methods of treating paroxysmal nocturnal hemoglobinuria, complement 3 glomerulopathy, or idiopathic immune complex-mediated glomerulonephritis using MASP-3 serine protease inhibitors are provided. In some embodiments, the MASP-3 serine protease inhibitors are anti-MASP-3 antibodies. Also provided are uses of MASP-3 serine protease inhibitors in treatment of paroxysmal nocturnal hemoglobinuria, complement 3 glomerulopathy, or idiopathic immune complex-mediated glomerulonephritis and for manufacture of a medicament for treatment of paroxysmal nocturnal hemoglobinuria, complement 3 glomerulopathy, or idiopathic immune complex-mediated glomerulonephritis.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject suffering from, or at risk for developing a thrombotic microangiopathy (TMA). The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Biochemical preparations for medical purposes, namely, for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; chemical preparations for medical purposes, namely, for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; therapeutic preparations for medical purposes, namely, for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders
35.
Therapeutic antibodies that bind to the serine protease domain of MASP-2 and uses thereof
Isolated monoclonal antibodies and antigen-binding fragments thereof are provided that specifically bind to an epitope within the serine protease domain of human MASP-2. In some embodiments, the antibodies or antigen-binding fragments thereof inhibit lectin pathway complement activation. Also provided are polynucleotides encoding the disclosed monoclonal antibodies or antigen-binding fragments thereof, and cloning vectors or expression cassettes comprising such polynucleotides. Further provided are methods of inhibiting lectin pathway complement activation and methods of treating lectin pathway diseases and disorders.
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present invention relates to anti-MASP-2 inhibitory antibodies and compositions comprising such antibodies for use in inhibiting the adverse effects of MASP-2 dependent complement activation.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact. In another aspect, the invention provides compositions for inhibiting the effects of lectin-dependent complement activation, comprising a therapeutically effective amount of a MASP-2 inhibitory agent and a pharmaceutically acceptable carrier.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact.
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Medical and scientific research information in the field of pharmaceuticals, biopharmaceuticals, and clinical trials; Research and development in the pharmaceutical and biotechnology fields Providing medical information
42.
MASP-2 AND MASP-3 INHIBITORS, AND RELATED COMPOSITIONS AND METHODS, FOR TREATMENT OF SICKLE CELL DISEASE
The present disclosure relates to the use of MASP-2 inhibitors and/or MASP-3 inhibitors and compositions comprising the same for treatment of sickle cell disease, including treatment, reduction, and/or prevention of sickle cell disease symptoms or manifestations.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact. In another aspect, the invention provides compositions for inhibiting the effects of lectin-dependent complement activation, comprising a therapeutically effective amount of a MASP-2 inhibitory agent and a pharmaceutically acceptable carrier.
The present invention relates to novel chimeric molecules of ficolin-associated polypeptides, such as fusion polypeptides for the use in the treatment of conditions associated with inflammation, apoptosis, autoimmunity, coagulation, thrombotic or coagulopathic related diseases. The present invention further relates to nucleic acid molecules encoding such fusion polypeptides, vectors and host cells used in the production of the fusion polypeptides.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Medical and scientific research information in the field of
pharmaceuticals, biopharmaceuticals, and clinical trials;
research and development in the field of pharmaceuticals and
biotechnology for medicine. Providing medical information.
46.
MASP-2 AND MASP-3 INHIBITORS, AND RELATED COMPOSITIONS AND METHODS, FOR TREATMENT OF SICKLE CELL DISEASE
The present disclosure relates to the use of MASP-2 inhibitors and/or MASP-3 inhibitors and compositions comprising the same for treatment of sickle cell disease, including treatment, reduction, and/or prevention of sickle cell disease symptoms or manifestations.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; preparations for diagnostic purposes are specifically excluded from all of the foregoing goods
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; preparations for diagnostic purposes are specifically excluded from all of the foregoing goods
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; preparations for diagnostic purposes are specifically excluded from all of the foregoing goods
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, and hematological, neurological, immunological and inflammation-related disease and disorders; preparations for diagnostic purposes are specifically excluded from all of the foregoing goods
51.
THERAPEUTIC ANTIBODIES THAT BIND TO THE SERINE PROTEASE DOMAIN OF MASP-2 AND USES THEREOF
Isolated monoclonal antibodies and antigen-binding fragments thereof are provided that specifically bind to an epitope within the serine protease domain of human MASP-2. In some embodiments, the antibodies or antigen-binding fragments thereof inhibit lectin pathway complement activation. Also provided are polynucleotides encoding the disclosed monoclonal antibodies or antigen-binding fragments thereof, and cloning vectors or expression cassettes comprising such polynucleotides. Further provided are methods of inhibiting lectin pathway complement activation and methods of treating lectin pathway diseases and disorders.
The present invention relates to stable, high-concentration low-viscosity formulations of MASP-2 inhibitory antibodies, kits comprising the formulations and therapeutic methods using the formulations and kits for inhibiting the adverse effects of MASP-2 dependent complement activation.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Biological and pharmaceutical preparations for the treatment
of transplant complications, ischemia-reperfusion injury,
and endothelial, renal, cardiovascular, infectious,
hematological, oncological, pulmonary, autoimmune,
neurological, psychiatric, endocrine, metabolic,
inflammatory, immunological, ocular, and addiction- and
compulsion-related diseases and disorders. Providing information about medical research, namely,
providing information about the results of clinical trials
for pharmaceutical products, medical and scientific research
with respect to transplant complications,
ischemia-reperfusion injury, and endothelial, renal,
cardiovascular, infectious, hematological, oncological,
pulmonary, autoimmune, neurological, psychiatric, endocrine,
metabolic, inflammatory, immunological, ocular, and
addiction- and compulsion-related diseases and disorders.
54.
Compositions and Methods of Inhibiting MASP-2 for the Treatment of Various Thrombotic Diseases and Disorders
In one aspect, the invention provides compositions and methods for preventing, reducing, and/or treating a disease, disorder or condition associated with fibrin-induced activation of the complement system and the associated activation of the coagulation and/or contact systems comprising administering a therapeutic amount of a MASP-2 inhibitory antibody to a subject in need thereof. In some embodiments, the methods of the invention provide anticoagulation and/or antithrombosis and/or antithrombogenesis without affecting hemostasis. In one embodiment of this aspect of the invention, the compositions and methods are useful for treating a subject is suffering from, or at risk of developing, a disease, disorder or condition associated with complement-related inflammation, excessive coagulation or contact system activation initiated by fibrin or activated platelets.
Isolated monoclonal antibodies and antigen-binding fragments thereof are provided that specifically bind, to an epitope within the serine protease domain of human MASP-2. In some embodiments, the antibodies or antigen-binding fragments thereof inhibit lectin pathway complement activation. Also provided are polynucleotides encoding the disclosed monoclonal antibodies or antigen-binding fragments thereof, and cloning vectors or expression cassettes comprising such polynucleotides. Further provided are methods of inhibiting lectin pathway complement activation and methods of treating lectin pathway diseases and disorders.
Isolated monoclonal antibodies and antigen-binding fragments thereof are provided that specifically bind, to an epitope within the serine protease domain of human MASP-2. In some embodiments, the antibodies or antigen-binding fragments thereof inhibit lectin pathway complement activation. Also provided are polynucleotides encoding the disclosed monoclonal antibodies or antigen-binding fragments thereof, and cloning vectors or expression cassettes comprising such polynucleotides. Further provided are methods of inhibiting lectin pathway complement activation and methods of treating lectin pathway diseases and disorders.
In one aspect, the present disclosure provides targeted complement-activating molecules comprising a target-binding domain and a complement-activating serine protease effector domain. In some embodiments, the target-binding domain is derived from an antibody or an antigen-binding fragment thereof. Also provided are compositions and methods for treating cancer, autoimmune disease, or microbial infection, including bacterial, viral, fungal, or parasitic infection, using targeted complement-activating molecules.
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
G01N 33/569 - ImmunoassayBiospecific binding assayMaterials therefor for microorganisms, e.g. protozoa, bacteria, viruses
G01N 33/543 - ImmunoassayBiospecific binding assayMaterials therefor with an insoluble carrier for immobilising immunochemicals
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07C 235/88 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having the nitrogen atom of at least one of the carboxamide groups further acylated
C07C 251/24 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 217/14 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
C07D 231/44 - Oxygen and nitrogen or sulfur and nitrogen atoms
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 235/30 - Nitrogen atoms not forming part of a nitro radical
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 295/033 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Biological and pharmaceutical preparations for the treatment of transplant complications, ischemia-reperfusion injury, and endothelial, renal, cardiovascular, infectious, hematological, oncological, pulmonary, autoimmune, neurological, psychiatric, endocrine, metabolic, inflammatory, immunological, ocular, and addiction- and compulsion-related diseases and disorders. (1) Providing information about medical research, namely, providing information about the results of clinical trials for pharmaceutical products, medical and scientific research with respect to transplant complications, ischemia-reperfusion injury, and endothelial, renal, cardiovascular, infectious, hematological, oncological, pulmonary, autoimmune, neurological, psychiatric, endocrine, metabolic, inflammatory, immunological, ocular, and addiction- and compulsion-related diseases and disorders.
62.
TARGETED CATALYTIC COMPLEMENT-ACTIVATING MOLECULES AND METHODS OF USE THEREOF
In one aspect, the present disclosure provides targeted complement-activating molecules comprising a target-binding domain and a complement-activating serine protease effector domain. In some embodiments, the target-binding domain is derived from an antibody or an antigen-binding fragment thereof. Also provided are compositions and methods for treating cancer, autoimmune disease, or microbial infection, including bacterial, viral, fungal, or parasitic infection, using targeted complement-activating molecules.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
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
In one aspect, the present disclosure provides targeted complement-activating molecules comprising a target-binding domain and a complement-activating serine protease effector domain. In some embodiments, the target-binding domain is derived from an antibody or an antigen-binding fragment thereof. Also provided are compositions and methods for treating cancer, autoimmune disease, or microbial infection, including bacterial, viral, fungal, or parasitic infection, using targeted complement-activating molecules.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 37/00 - Drugs for immunological or allergic disorders
C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
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
64.
TREATMENT OF ADDICTION AND IMPULSE-CONTROL DISORDERS USING PDE7 INHIBITORS
This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/385 - Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
Compounds, compositions, and methods for generating T cells with altered phenotype are disclosed. The phenotype-altered T cells have increased persistence, prolonged survival, and increased antitumor activity and are useful for treatment of cancers.
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Medical and scientific research information in the field of pharmaceuticals, biopharmaceuticals, and clinical trials; Research and development in the field of pharmaceuticals and biotechnology for medicine Providing medical information
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Providing information concerning medical and scientific research with respect to transplant complications, ischemia-reperfusion injury, and endothelial, renal, cardiovascular, infectious, hematological, oncological, pulmonary, autoimmune, neurological, psychiatric, endocrine, metabolic, inflammatory, immunological, ocular, and addiction- and compulsion-related diseases and disorders Medical information services, namely, providing information relating to diagnostic, prophylactic, and therapeutic properties of pharmaceutical products with respect to transplant complications, ischemia-reperfusion injury, and endothelial, renal, cardiovascular, infectious, hematological, oncological, pulmonary, autoimmune, neurological, psychiatric, endocrine, metabolic, inflammatory, immunological, ocular, and addiction- and compulsion-related diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Biological and pharmaceutical preparations for the treatment of transplant complications, ischemia-reperfusion injury, and endothelial, renal, cardiovascular, infectious, hematological, oncological, pulmonary, autoimmune, neurological, psychiatric, endocrine, metabolic, inflammatory, immunological, ocular, and addiction- and compulsion-related diseases and disorders
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Providing medical and scientific research information in the
fields of pharmaceuticals and biopharmaceuticals. Medical information services, namely, providing information
concerning pharmaceutical and biopharmaceutical products,
and therapeutic methods in the fields of endothelial
diseases and disorders, renal diseases, transplant
complications, ischemia reperfusion injury, hematological,
autoimmune, immunological, and inflammatory related diseases
and disorders, and oncology, addiction, compulsive, and
movement related diseases and disorders.
70.
BIOMARKER FOR ASSESSING THE RISK OF DEVELOPING ACUTE COVID-19 AND POST-ACUTE COVID-19
THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF CAMBRIDGE (United Kingdom)
OMEROS CORPORATION (USA)
Inventor
Demopulos, Gregory A.
Dudler, Thomas
Lynch, Nicholas James
Schwaeble, Hans-Wilhelm
Shaffer, Kathleen
Yabuki, Munehisa
Abstract
Disclosed herein are compositions, kits and methods for determining the concentration of fluid-phase MASP-2/C1-INH complex in a biological fluid, such as a biological fluid obtained from a subject infected with SARS-CoV-2. Also disclosed are methods of using said compositions, methods and kits for detection of MASP-2/C1-INH complex to determine the status of lectin pathway activation in a mammalian subject and thereby assess the risk of a subject that is or has been infected with SARS-CoV-2 for developing COVID-19-related ARDS or other poor outcome, or determine the need for treatment or efficacy of treatment of a subject in need thereof with a complement inhibitor such as a MASP-2 inhibitory agent.
05 - Pharmaceutical, veterinary and sanitary products
16 - Paper, cardboard and goods made from these materials
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical preparations for the treatment of endothelial
diseases and disorders, renal diseases, transplant
complications, ischemia-reperfusion injury and
hematological, autoimmune, neurological, immunological and
inflammation-related disease and disorders; biologics for
the treatment of endothelial diseases and disorders, renal
diseases, transplant complications, ischemia-reperfusion
injury and hematological, autoimmune, neurological,
immunological and inflammation-related disease and
disorders. Printed publications in the nature of brochures, pamphlets,
newsletters, written articles and guidebooks in the field of
medical information and patient support. Providing medical and scientific research information in the
fields of pharmaceuticals and biopharmaceuticals. Medical information services, namely, providing information
concerning pharmaceutical and biopharmaceutical products,
and therapeutic methods in the fields of endothelial
diseases and disorders, renal diseases, transplant
complications, ischemia reperfusion injury, hematological,
autoimmune, immunological and inflammatory related diseases
and disorders.
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
(1) Providing medical and scientific research information in the fields of pharmaceuticals and biopharmaceuticals.
(2) Medical information services, namely, providing information concerning pharmaceutical and biopharmaceutical products, and therapeutic methods in the fields of endothelial diseases and disorders, renal diseases, transplant complications, ischemia reperfusion injury, hematological, autoimmune, immunological, and inflammatory related diseases and disorders, and oncology, addiction, compulsive, and movement related diseases and disorders.
73.
BIOMARKER FOR ASSESSING THE RISK OF DEVELOPING ACUTE COVID-19 AND POST-ACUTE COVID-19
Disclosed herein are compositions, kits and methods for determining the concentration of fluid-phase MASP-2/C1-INH complex in a biological fluid, such as a biological fluid obtained from a subject infected with SARS-CoV-2. Also disclosed are methods of using said compositions, methods and kits for detection of MASP-2/C1-INH complex to determine the status of lectin pathway activation in a mammalian subject and thereby assess the risk of a subject that is or has been infected with SARS-CoV-2 for developing COVID-19-related ARDS or other poor outcome, or determine the need for treatment or efficacy of treatment of a subject in need thereof with a complement inhibitor such as a MASP-2 inhibitory agent.
Disclosed herein are compositions, kits and methods for determining the concentration of fluid-phase MASP-2/C1-INH complex in a biological fluid, such as a biological fluid obtained from a subject infected with SARS-CoV-2. Also disclosed are methods of using said compositions, methods and kits for detection of MASP-2/C1-INH complex to determine the status of lectin pathway activation in a mammalian subject and thereby assess the risk of a subject that is or has been infected with SARS-CoV-2 for developing COVID-19-related ARDS or other poor outcome, or determine the need for treatment or efficacy of treatment of a subject in need thereof with a complement inhibitor such as a MASP-2 inhibitory agent.
In one aspect, the invention provides methods and compositions for inhibiting MASP-3-dependent complement activation in a subject suffering from paroxysmal nocturnal hemoglobinuria by administering to the subject a composition comprising an amount of a MASP-3 inhibitory agent in an amount effective to inhibit MASP-3-dependent complement activation. In another aspect, the invention provides methods and compositions for increasing the survival of red blood cells in a subject suffering from paroxysmal nocturnal hemoglobinuria by administering to the subject a composition comprising an amount of at least one of a MASP-1 inhibitory agent and/or a MASP-3 inhibitory agent effective to increase the survival of red blood cells. In some embodiments, the subject is administered a MASP-2 inhibitory agent and a MASP-1 inhibitory agent, a MASP-2 inhibitory agent and a MASP-3 inhibitory agent administered, a MASP-3 inhibitory agent and a MASP-1 inhibitory agent, or a MASP-1 inhibitory agent, a MASP-2 inhibitory agent and a MASP-3 inhibitory agent.
05 - Pharmaceutical, veterinary and sanitary products
16 - Paper, cardboard and goods made from these materials
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
(1) Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological diseases and disorders, autoimmune diseases and disorders, neurological diseases and disorders, namely, Alzheimer's, Huntington's Disease, cerebral palsy, brain injury, spinal cord injury, seizure disorders, cerebrovascular accident (stroke), Parkinson's disease, multiple sclerosis, myasthenia gravis, immunological diseases and disorders and inflammation-related disease and disorders, namely, inflammatory bowel diseases, inflammatory connective tissue diseases, inflammatory muscle diseases and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological diseases and disorders, autoimmune, diseases and disorders neurological diseases and disorders, namely, Alzheimer's, Huntington's Disease, cerebral palsy, brain injury, spinal cord injury, seizure disorders, cerebrovascular accident (stroke), Parkinson's disease, multiple sclerosis, myasthenia gravis, immunological diseases and disorders and inflammation-related disease and disorders, namely, inflammatory bowel diseases, inflammatory connective tissue diseases, inflammatory muscle diseases and disorders.
(2) Printed publications in the nature of brochures, pamphlets, newsletters, written articles and guidebooks in the field of medical information and patient support. (1) Providing medical and scientific research information in the fields of pharmaceuticals and biopharmaceuticals.
(2) Medical information services, namely, providing information concerning pharmaceutical and biopharmaceutical products, and therapeutic methods in the fields of endothelial diseases and disorders, renal diseases, transplant complications, ischemia reperfusion injury, hematological, autoimmune, immunological and inflammatory related diseases and disorders.
16 - Paper, cardboard and goods made from these materials
35 - Advertising and business services
36 - Financial, insurance and real estate services
41 - Education, entertainment, sporting and cultural services
Goods & Services
Printed publications in the nature of brochures, pamphlets, newsletters, written articles and guidebooks in the field of medical information and patient support Promoting awareness of patient support offerings for endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; business administration of reimbursement and medical benefit information for endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders and their treatment; and business administrative services for medical referrals Providing a website featuring financial information regarding medical benefits and reimbursements available for medical expenses related thereto; insurance services, namely, benefits verification in the nature of insurance claims administration; and providing online information and financial assistance with insurance benefits and coverage for health care providers and patients in the field of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders Educational services, namely, conducting educational programs in the fields of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders and treatment and patient support options for these conditions
16 - Paper, cardboard and goods made from these materials
35 - Advertising and business services
36 - Financial, insurance and real estate services
41 - Education, entertainment, sporting and cultural services
Goods & Services
Printed publications in the nature of brochures, pamphlets, newsletters, written articles and guidebooks in the field of medical information and patient support Promoting awareness of patient support offerings for endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; business administration of reimbursement and medical benefit information for endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders and their treatment; and business administrative services for medical referrals Providing a website featuring financial information regarding medical benefits and reimbursements available for medical expenses related thereto; insurance services, namely, benefits verification in the nature of insurance claims administration; and providing online information and financial assistance with insurance benefits and coverage for health care providers and patients in the field of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders Educational services, namely, conducting educational programs in the fields of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders and treatment and patient support options for these conditions
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Medical information services, namely, providing information concerning pharmaceutical and biopharmaceutical products, and therapeutic methods in the fields of endothelial diseases and disorders, renal diseases, transplant complications, ischemia reperfusion injury, hematological, autoimmune, immunological, and inflammatory related diseases and disorders, and oncology, addiction, compulsive, and movement related diseases and disorders
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact. In another aspect, the invention provides compositions for inhibiting the effects of lectin-dependent complement activation, comprising a therapeutically effective amount of a MASP-2 inhibitory agent and a pharmaceutically acceptable carrier.
Disclosed herein are monoclonal antibodies that specifically bind to human mature Factor D and that do not bind to human Pro-Factor D, monoclonal antibodies that specifically bind to human Pro-Factor D and do not bind to human mature Factor D, and monoclonal antibodies that bind to both human mature Factor D and human Pro-Factor D. Also disclosed are methods of using the monoclonal antibodies, and compositions comprising the same, for detection of the mature and/or the pro-form of Factor D in biological samples, to determine the status of the Alternative Pathway of Complement (APC ) in a mammalian subject, or to determine the status of Factor D after treatment with a MASP-3 inhibitory agent which inhibits the conversion of Pro-Factor D to mature Factor D.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
83.
MONOCLONAL ANTIBODIES, COMPOSITIONS AND METHODS FOR DETECTING COMPLEMENT FACTOR D
Disclosed herein are monoclonal antibodies that specifically bind to human mature Factor D and that do not bind to human Pro-Factor D, monoclonal antibodies that specifically bind to human Pro-Factor D and do not bind to human mature Factor D, and monoclonal antibodies that bind to both human mature Factor D and human Pro-Factor D. Also disclosed are methods of using the monoclonal antibodies, and compositions comprising the same, for detection of the mature and/or the pro-form of Factor D in biological samples, to determine the status of the Alternative Pathway of Complement (APC ) in a mammalian subject, or to determine the status of Factor D after treatment with a MASP-3 inhibitory agent which inhibits the conversion of Pro-Factor D to mature Factor D.
Disclosed herein are monoclonal antibodies that specifically bind to human mature Factor D and that do not bind to human Pro-Factor D, monoclonal antibodies that specifically bind to human Pro-Factor D and do not bind to human mature Factor D, and monoclonal antibodies that bind to both human mature Factor D and human Pro-Factor D. Also disclosed are methods of using the monoclonal antibodies, and compositions comprising the same, for detection of the mature and/or the pro-form of Factor D in biological samples, to determine the status of the Alternative Pathway of Complement (APC) in a mammalian subject, or to determine the status of Factor D after treatment with a MASP-3 inhibitory agent which inhibits the conversion of Pro-Factor D to mature Factor D.
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Pharmaceutical preparations for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders; biologics for the treatment of endothelial diseases and disorders, renal diseases, transplant complications, ischemia-reperfusion injury and hematological, autoimmune, neurological, immunological and inflammation-related disease and disorders Printed publications in the nature of brochures, pamphlets, newsletters, written articles and guidebooks in the field of medical information and patient support Providing medical and scientific research information in the fields of pharmaceuticals and biopharmaceuticals Medical information services, namely, providing information concerning pharmaceutical and biopharmaceutical products, and therapeutic methods in the fields of endothelial diseases and disorders, renal diseases, transplant complications, ischemia reperfusion injury, hematological, autoimmune, immunological and inflammatory related diseases and disorders
86.
METHODS FOR INHIBITING FIBROSIS IN A SUBJECT IN NEED THEREOF
In one aspect, the invention provides methods for treating, inhibiting, alleviating or preventing fibrosis in a mammalian subject suffering, or at risk of developing a disease or disorder caused or exacerbated by fibrosis and/or inflammation. In one embodiment, the invention provides methods of treating a subject suffering from renal fibrosis. In one embodiment, the invention provides methods of reducing proteinuria in a subject suffering from a renal disease or condition associated with proteinuria. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation.
In one aspect, the invention provides methods for treating, inhibiting, alleviating, or preventing acute respiratory distress syndrome, pneumonia, or some other pulmonary or other manifestation of coronavirus infection, such as thrombosis, in a mammalian subject infected with coronavirus, such as SARS-CoV-2. The methods comprise the step of administering to a subject infected with coronavirus an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In one embodiment, the MASP-2 inhibitory agent is a MASP-2 monoclonal antibody, or fragment thereof that specifically binds to a portion of SEQ ID NO:6. In one embodiment, the MASP-2 inhibitory agent is a small molecule MASP-2 inhibitory compound. In one embodiment, the subject is a human subject suffering from COVID-19-induced acute respiratory distress syndrome (ARDS) and requires supplemental oxygen prior to treatment and the MASP-2 inhibitory agent is administered in an amount sufficient to discontinue the need for supplemental oxygen.
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a human subject suffering from graft-versus-host disease and/or diffuse alveolar hemorrhage and/or veno-occlusive disease associated with a hematopoietic stem cell transplant. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation.
In one aspect, the invention provides methods for treating, inhibiting, alleviating, or preventing acute respiratory distress syndrome, pneumonia, or some other pulmonary or other manifestation of coronavirus infection, such as thrombosis, in a mammalian subject infected with coronavirus, such as SARS-CoV-2. The methods comprise the step of administering to a subject infected with coronavirus an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In one embodiment, the MASP-2 inhibitory agent is a MASP-2 monoclonal antibody, or fragment thereof that specifically binds to a portion of SEQ ID NO:6. In one embodiment, the MASP-2 inhibitory agent is a small molecule MASP-2 inhibitory compound. In one embodiment, the subject is a human subject suffering from COVID- 19-induced acute respiratory distress syndrome (ARDS) and requires supplemental oxygen prior to treatment and the MASP-2 inhibitory agent is administered in an amount sufficient to discontinue the need for supplemental oxygen.
In one aspect, the invention provides methods for treating, inhibiting, alleviating, or preventing acute respiratory distress syndrome, pneumonia, or some other pulmonary or other manifestation of coronavirus infection, such as thrombosis, in a mammalian subject infected with coronavirus, such as SARS-CoV-2. The methods comprise the step of administering to a subject infected with coronavirus an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In one embodiment, the MASP-2 inhibitory agent is a MASP-2 monoclonal antibody, or fragment thereof that specifically binds to a portion of SEQ ID NO:6. In one embodiment, the MASP-2 inhibitory agent is a small molecule MASP-2 inhibitory compound. In one embodiment, the subject is a human subject suffering from COVID- 19-induced acute respiratory distress syndrome (ARDS) and requires supplemental oxygen prior to treatment and the MASP-2 inhibitory agent is administered in an amount sufficient to discontinue the need for supplemental oxygen.
The present invention relates to MASP-3 inhibitory antibodies and compositions comprising such antibodies for use in inhibiting the adverse effects of MASP-3 dependent complement activation.
In one aspect, the present invention provides methods for preventing, treating, reverting and/or delaying angiogenesis in a mammalian subject suffering from, or at risk for developing, an angiogenesis-dependent disease or condition, comprising administering to the subject an amount of a MASP-2 inhibitory agent effective to inhibit angiogenesis. In some embodiments of these aspects of the invention, the MASP-2 inhibitory agent is a MASP-2 antibody or fragment thereof.
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
C07D 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/662 - Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
