612344 are described herein. The invention also relates to the use of the compounds, salts, or compositions described herein in methods of inhibiting sPLA2-X enzymes in a sample. The invention also relates to the use of the compounds, salts, or compositions in methods of treating or lessening the severity of an sPLA2-X mediated disease in a subject.
C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/85 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 345/00 - Heterocyclic compounds containing rings having selenium or tellurium atoms as the only ring hetero atoms
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
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 405/04 - 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 two hetero rings directly linked by a ring-member-to-ring- member bond
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
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
35 - Advertising and business services
Goods & Services
Cosmetics, eyebrow and eyelash enhancers, skin cream and body lotions. Retail store services provided in relation to cosmetics, eyebrow and eyelash enhancers, skin cream and body lotions; wholesale and retail services, including online wholesale and retail services, provided in relation to cosmetics, eyebrow and eyelash enhancers, skin cream and body lotions.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Kits and reagents consisting of lipid nanoparticles for scientific research purposes; kits comprising lipids, and reagents used to formulate lipid nanoparticles for scientific research purposes
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Membrane-based screening tests comprised of diagnostic and chemical reagents for the identification of protein-lipids interactions and characteristics for scientific research purposes
Disclosed herein are compounds of formula (I)
6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
C07D 409/06 - 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 only aliphatic carbon atoms
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 31/4015 - 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
A61L 24/00 - Surgical adhesives or cementsAdhesives for colostomy devices
A61L 24/02 - Surgical adhesives or cementsAdhesives for colostomy devices containing inorganic materials
A61L 27/12 - Phosphorus-containing materials, e.g. apatite
A61L 27/36 - Materials for prostheses or for coating prostheses containing ingredients of undetermined constitution or reaction products thereof
A61L 27/54 - Biologically active materials, e.g. therapeutic substances
A61L 27/58 - Materials at least partially resorbable by the body
C07D 409/06 - 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 only aliphatic carbon atoms
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
Disclosed herein are compounds of formula (I)
6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
C07D 409/06 - 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 only aliphatic carbon atoms
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 31/4015 - 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
A61L 24/00 - Surgical adhesives or cementsAdhesives for colostomy devices
A61L 24/02 - Surgical adhesives or cementsAdhesives for colostomy devices containing inorganic materials
A61L 27/12 - Phosphorus-containing materials, e.g. apatite
A61L 27/36 - Materials for prostheses or for coating prostheses containing ingredients of undetermined constitution or reaction products thereof
A61L 27/54 - Biologically active materials, e.g. therapeutic substances
A61L 27/58 - Materials at least partially resorbable by the body
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
(1) Chemicals, namely, standard solutions and reagents used in analytical chemistry; Analytical standard solutions and reagents for scientific, research, and clinical laboratory use; Chemical preparations for analyses in laboratories, namely, forensic testing, environmental testing, pharmaceutical testing, biomedical research, industrial testing, food testing, safety testing, wellness testing, and proficiency testing.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Chemicals, namely, standard solutions and reagents used in analytical chemistry; Analytical standard solutions and reagents for scientific, research, and clinical laboratory use; Chemical preparations for analyses in laboratories, namely, forensic testing, environmental testing, pharmaceutical testing, biomedical research, industrial testing, food testing, safety testing, wellness testing, and proficiency testing.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Chemicals, namely, standard solutions and reagents used in analytical chemistry; Analytical standard solutions and reagents for scientific, research, and clinical laboratory use; Chemical preparations for analyses in laboratories, namely, forensic testing, environmental testing, pharmaceutical testing, biomedical research, industrial testing, food testing, safety testing, wellness testing, and proficiency testing.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Chemicals, namely, standard solutions and reagents used in analytical chemistry; analytical standard solutions in the nature of chemicals for scientific, research, and clinical laboratory use; reagents for scientific, research, and clinical laboratory use; chemical preparations for analyses in laboratories, namely, forensic testing, environmental testing, pharmaceutical testing, biomedical research, industrial testing, food testing, safety testing, wellness testing, and proficiency testing
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Chemicals, namely, standard solutions and reagents used in analytical chemistry; Analytical standard solutions in the nature of chemicals for scientific, research, and clinical laboratory use; Reagents for scientific, research, and clinical laboratory use; Chemical preparations for analyses in laboratories, namely, forensic testing, environmental testing, pharmaceutical testing, biomedical research, industrial testing, food testing, safety testing, wellness testing, and proficiency testing
Disclosed herein are compounds of formula (I)
6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.
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 31/4025 - 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
C07D 409/06 - 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 only aliphatic carbon atoms
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
A61L 24/00 - Surgical adhesives or cementsAdhesives for colostomy devices
A61L 24/02 - Surgical adhesives or cementsAdhesives for colostomy devices containing inorganic materials
A61L 27/12 - Phosphorus-containing materials, e.g. apatite
A61L 27/36 - Materials for prostheses or for coating prostheses containing ingredients of undetermined constitution or reaction products thereof
A61L 27/54 - Biologically active materials, e.g. therapeutic substances
A61L 27/58 - Materials at least partially resorbable by the body
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Products for use in mass spectrometry, namely, assays, reagents, and analytical reference standards used to identify and quantify biomarkers in biological samples for research purposes
20.
ANTI-CITRULLINATED HLA POLYPEPTIDE ANTIBODIES AND USES THEREOF
The present invention relates to methods for treating an autoimmune disease in a human subject mediated by the presence of a citrullinated epitope QKCitAA, QRCitAA, or RRCitAA in the subject, the method comprising administering a therapeutically effective amount of an antibody or a specific binding fragment thereof that specifically binds to citrullinated epitope QKCitAA, QRCitAA, or RRCitAA. Further aspects of the invention include an antibody or a specific binding fragment thereof, that specifically binds to a human citrullinated epitope QKCitAA, QRCitAA, or RRCitAA.
Disclosed herein are compositions and methods of treating osteroporosis, bone fracture, bone loss, and increasing bone density by administration of compounds of formula (I)
6, and s are as defined in the specification.
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 31/4025 - 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
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
C07D 409/06 - 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 only aliphatic carbon atoms
A61L 24/00 - Surgical adhesives or cementsAdhesives for colostomy devices
A61L 24/02 - Surgical adhesives or cementsAdhesives for colostomy devices containing inorganic materials
A61L 27/12 - Phosphorus-containing materials, e.g. apatite
A61L 27/36 - Materials for prostheses or for coating prostheses containing ingredients of undetermined constitution or reaction products thereof
A61L 27/54 - Biologically active materials, e.g. therapeutic substances
A61L 27/58 - Materials at least partially resorbable by the body
23.
Methods, systems, and compositions for promoting bone growth
The present invention relates to novel bone compositions for locally delivering a therapeutic agent to the site of a bone defect. Therapeutic agents may promote repair of the bone defect and/or treat conditions or disorders such as pain, inflammation, cancer, and infection. The compositions include calcium phosphate cements and a demineralized bone matrix or a collagen sponge. The compositions are useful for implantation in a patient at the site of a bone defect.
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 31/4025 - 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
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
C07D 409/06 - 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 only aliphatic carbon atoms
A61L 27/36 - Materials for prostheses or for coating prostheses containing ingredients of undetermined constitution or reaction products thereof
A61L 27/42 - Composite materials, i.e. layered or containing one material dispersed in a matrix of the same or different material having an inorganic matrix
A61L 27/54 - Biologically active materials, e.g. therapeutic substances
Disclosed herein are compounds of formula (I)
4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
C07D 417/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 409/06 - 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 only aliphatic carbon atoms
Disclosed herein are compounds of formula (I)
4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 417/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 409/06 - 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 only aliphatic carbon atoms
26.
Chiral compounds, compositions, products and methods employing same
Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.
C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
C07D 313/04 - Seven-membered rings not condensed with other rings
C07D 313/18 - Eight-membered rings not condensed with other rings
C07H 15/203 - Monocyclic carbocyclic rings other than cyclohexane ringsBicyclic carbocyclic ring systems
C07D 311/02 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
C07D 215/22 - Oxygen atoms attached in position 2 or 4
C07D 319/12 - 1,4-DioxanesHydrogenated 1,4-dioxanes not condensed with other rings
C07D 333/48 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom by oxygen atoms
Disclosed herein are compounds of formula (I)
6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.
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 31/4025 - 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
C07D 409/06 - 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 only aliphatic carbon atoms
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
28.
Difluorolactam compounds as EP4 receptor-selective agonists for use in the treatment of EP4-mediated diseases and conditions
Disclosed herein are compounds of formula (I)
6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.
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 31/4025 - 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
C07D 409/06 - 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 only aliphatic carbon atoms
29.
Difluorolactam compositions for EP4-mediated osteo related diseases and conditions
Disclosed herein are compositions and methods of treating osteoporosis, bone fracture, bone loss, and increasing bone density by administration of compounds of formula (I)
6, and s are as defined in the specification.
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 31/4025 - 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
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
C07D 409/06 - 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 only aliphatic carbon atoms
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Assays and reagents for research purposes; assays and reagents for profiling enzymes and proteins; assays and reagents for research purposes for profiling enzymes and proteins; diagnostic kits for research purposes comprising assays and reagents; diagnostic kits comprising assays and reagents; diagnostic kits for research purposes comprising assays and reagents for profiling enzymes and proteins. Assays and reagents for medical purposes for profiling enzymes and proteins; diagnostic kits for medical purposes comprising assays and reagents for profiling enzymes and proteins; assays and reagents for medical purposes; diagnostic kits for medical purposes comprising assays and reagents.
The present invention relates to novel bone compositions for locally delivering a therapeutic agent to the site of a bone defect. Therapeutic agents may promote repair of the bone defect and/or treat conditions or disorders such as pain, inflammation, cancer, and infection. The compositions include calcium phosphate cements and a demineralized bone matrix or a collagen sponge. The compositions are useful for implantation in a patient at the site of a bone defect.
A61L 27/36 - Materials for prostheses or for coating prostheses containing ingredients of undetermined constitution or reaction products thereof
A61L 27/54 - Biologically active materials, e.g. therapeutic substances
A61L 27/42 - Composite materials, i.e. layered or containing one material dispersed in a matrix of the same or different material having an inorganic matrix
(2)The present invention relates to processes and intermediates for preparing compounds of formula (2), wherein R13 is defined herein. Compounds of formula (2) are useful as intermediates for preparing compounds which are EP4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.
C07C 69/63 - Halogen-containing esters of saturated acids
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 409/06 - 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 only aliphatic carbon atoms
The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R1, R4, R5, R6, and L1 are as defined herein. Compounds of formula (IA) have been found useful as EP4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.
C07D 409/06 - 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 only aliphatic carbon atoms
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
Disclosed herein are compounds of formula (I) wherein L1, L2, L3, R1, R4, R5, and R6 are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
C07D 417/06 - 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 carbon chain containing only aliphatic carbon atoms
Disclosed herein are compounds of formula (I) wherein L1, L2, L3, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
C07D 417/06 - 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 carbon chain containing only aliphatic carbon atoms
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Assays and reagents for research purposes; Diagnostic kits comprising assays and reagents for research purposes; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for electron transport chain inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for beta oxidation inhibition; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for ATP-ase inhibition.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
(1) Assays and diagnostic reagents for medical research purposes; Diagnostic kits comprising assays and reagents for medical research purposes; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for electron transport chain inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for beta oxidation inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for ATP-ase inhibition.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
(1) Assays and diagnostic reagents for medical research purposes; Diagnostic kits comprising assays and reagents for medical research purposes; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for electron transport chain inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for beta oxidation inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for ATP-ase inhibition.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Assays and reagents for research purposes; Diagnostic kits comprising assays and reagents for research purposes; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for electron transport chain inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for beta oxidation inhibition; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for ATP-ase inhibition.
The present invention provides processes for preparing a prostacyclin analogue of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R10 is a linear or branched C1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
C07C 205/57 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Assays and reagents for research purposes; Diagnostic kits comprising assays and reagents for research purposes; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for electron transport chain inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for beta oxidation inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for ATP-ase inhibition
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
Assays and reagents for research purposes; Diagnostic kits comprising assays and reagents for research purposes; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for electron transport chain inhibition; diagnostic kits for research purposes comprising assays and reagents for testing a composition for beta oxidation inhibition; Diagnostic kits for research purposes comprising assays and reagents for testing a composition for ATP-ase inhibition
52.
DIFLUOROLACTAM COMPOSITIONS FOR EP4-MEDIATED OSTEO RELATED DISEASES AND CONDITIONS
Disclosed herein are compositions and methods of treating osteroporosis, bone fracture, bone loss, and increasing bone density by administration of compounds of formula (I) or compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier, wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification.
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 31/4025 - 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
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
53.
DIFLUOROLACTAM COMPOUNDS AS EP4 RECEPTOR-SELECTIVE AGONISTS FOR USE IN THE TREATMENT OF EP4-MEDIATED DISEASE AND CONDITIONS
Disclosed herein are compounds of formula (I) and therapeutic methods of treatment with compounds of formula (I), wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.
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 207/20 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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 31/4025 - 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
Disclosed herein are compositions and methods of treating osteroporosis, bone fracture, bone loss, and increasing bone density by administration of compounds of formula (I) or compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier, wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification.
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 31/4025 - 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
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
55.
Chiral compounds, compositions, products and methods employing same
Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.
C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
A61K 8/49 - Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
C07D 311/02 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
C07D 215/22 - Oxygen atoms attached in position 2 or 4
C07D 319/12 - 1,4-DioxanesHydrogenated 1,4-dioxanes not condensed with other rings
C07D 333/48 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom by oxygen atoms
Assay methods may generally comprise forming homogeneous assay mixtures comprising target SAM-utilizing protein, fluorescent detection analyte, and test compound, incubating, and measuring FP or TR-FRET signal emitted in order to determine a measure of test compound-SAM -utilizing protein binding. Assay mixtures comprise a SAM-utilizing protein, and a fluorescent detection analyte that binds with the SAM-utilizing protein in the absence of test compound. Assay mixtures may further comprise a test compound. Assay mixture embodiments may generate FP or TR-FRET signal properties that are a function of the inherent binding interactions of both the test compound and the detection analyte with the SAM-utilizing protein. Fluorescent detection analytes comprise a fluorophore moiety, a covalent linker moiety, and a SAM-utilizing protein ligand moiety and could be utilized in FP or TR-FRET assays to measure test compound binding.
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
Assay methods may generally comprise forming homogeneous assay mixtures comprising target SAM-utilizing protein, fluorescent detection analyte, and test compound, incubating, and measuring FP or TR-FRET signal emitted in order to determine a measure of test compound-SAM-utilizing protein binding. Assay mixtures comprise a SAM-utilizing protein, and a fluorescent detection analyte that binds with the SAM-utilizing protein in the absence of test compound. Assay mixtures may further comprise a test compound. Assay mixture embodiments may generate FP or TR-FRET signal properties that are a function of the inherent binding interactions of both the test compound and the detection analyte with the SAM- utilizing protein. Fluorescent detection analytes comprise a fluorophore moiety, a covalent linker moiety, and a SAM-utilizing protein ligand moiety and could be utilized in FP or TR-FRET assays to measure test compound binding.
C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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
58.
Process for the preparation of F-series prostaglandins
A process for the synthesis and purification of F-series prostaglandin compounds and synthetic intermediates used to prepare them. The synthetic intermediates are solid and may be purified by precipitation and therefore may form the representative F-series prostaglandin compounds such as latanoprost, bimatoprost, fluprostenol, cloprostenol, and substituted analogs therefrom in highly pure forms.
C07D 405/00 - 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
C07D 307/935 - Not further condensed cyclopenta [b] furans or hydrogenated cyclopenta [b] furans
59.
TETRANOR-PGDM/PGJM SPECIFIC IMMUNOGENS, ANTIBODIES, TRACERS, ASSAY KITS AND METHODS FOR MAKING SAME
Tetranor-PGDM/tetranor-PGJM-specific antibodies, immunogens used to generate them, the processes of their manufacture, and their uses in assay kits for detecting and quantifying tetranor-PGDM and tetranor-PGJM in biological fluids for determining biosynthesis of PGD2 in a subject or patient.
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
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
C07C 51/347 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups
C07C 59/82 - Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings the keto group being part of a ring
61.
TETRANOR-PGEM/PGAM SPECIFIC IMMUNOGENS, ANTIBODIES, TRACERS, ASSAY KITS AND METHODS FOR MAKING SAME
Tetranor-PGEM/tetranor-PGAM-specific antibodies, immunogens used to generate them, the processes of their manufacture, and their uses for detecting and quantifying tetranor-PGEM in biological fluids for determining biosynthesis of PGE2 in a subject or patient.
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
Methods, compositions and kits are provided for measuring aspirin's anti-thrombotic effectiveness on a subject. Included are a novel assay for quickly and specifically measuring TxA2 metabolite levels in urine and correlating the levels with aspirin dose in a subject. The methods, compositions and kits utilize a novel anti TxA2 metabolite antibody.
A process for the synthesis and purification of F-series prostaglandin compounds and synthetic intermediates used to prepare them. The synthetic intermediates are solid and may be purified by precipitation and therefore may form the representative F-series prostaglandin compounds such as latanoprost, bimatoprost, fluprostenol, cloprostenol, and substituted analogs therefrom in highly pure forms.
A61K 31/34 - 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
A61P 9/02 - Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
64.
Methods and kits for detection of thromboxane A2 metabolites
Methods, compositions and kits are provided for measuring aspirin's anti-thrombotic effectiveness on a subject. Included are a novel assay for quickly and specifically measuring TxA2 metabolite levels in urine and correlating the levels with aspirin dose in a subject. The methods, compositions and kits utilize a novel anti TxA2 metabolite antibody.
Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
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 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 401/04 - 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 directly linked by a ring-member-to-ring- member bond
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 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
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N- terminus of the enzyme.
A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.
A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.
A METHOD FOR SCREENING OF PROSTAGLANDIN COMPOUNDS COMPRISING AN OPTIMAL FORMULATION FOR THE ENHANCEMENT OF HAIR GROWTH AND THE STIMULATION OF FOLLICULAR ANAGEN AND FORMULATIONS RESULTING THEREFROM
A method for developing Prostaglandin F2α analogs for enhancing and sustaining the growth of eye lashes. The exemplary method first provides a method for determining the ability of a FP receptor agonist test compound having unknown hair growth ability to induce hair growth in its free acid form. The test compound may then be provided in its amide, or slowly hydrolyzing form and ester form, or rapidly hydrolyzing form to determine the relative hydrolysis rate within corneal tissue. Depending upon its hair growth ability and relative hydrolysis rates, the Prostaglandin F2α analog in one or more forms may be used an ingredient in a binary cosmetic prodrug designed for enhancing and sustaining the growth of eye lashes.
Disclosed are systems and methods for providing expedited, unlimited, unrestricted, free or minimal cost access to information such as scientific research results. The methods and systems include receiving information, identifying at least one product included in the received information, retrieving links associated with the identified product or products, publishing the received information and the retrieved links, and receiving revenue from the entities associated with the identified products. A portion of the received revenue is then expended on one or more of the costs of providing access to the received information. In one aspect of the invention, information is received and provided via the Internet, advertising links are provided in the form of thumbnail images, and revenue is generated for each click of a thumbnail image.
