PROLYL HYDROXYLASE INHIBITORS

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) 2. The method according to wherein:X is O;Y is O;{'sup': 1', '4, 'sub': 1-', '10', '2-', '10', '2-', '10', '3', '8', '3', '8', '1-', '10', '5', '8', '5', '8', '1-', '10', '3', '8', '3', '8', '1-', '10', '1-', '10', '1-', '10, 'Rand Rare each independently selected from the group consisting of hydrogen, CCalkyl, CCalkenyl, CCalkynyl, C-Ccycloalkyl, C-Ccycloalkyl-CCalkyl, C-Ccycloalkenyl, C-Ccycloalkenyl-CCalkyl, C-Cheterocycloalkyl, C-Cheterocycloalkyl-CCalkyl, aryl, aryl-CCalkyl, heteroaryl and heteroaryl-CCalkyl;'}{'sup': 2', '7', '8', '9, 'Ris —NRRor —OR;'}{'sup': '3', 'sub': 1-', '4, 'claim-text': [{'sup': 7', '8, 'sub': 1-', '10', '2-', '10', '2-', '10', '3', '8', '3', '8, 'where Rand Rare each independently selected from the group consisting of hydrogen, CCalkyl, CCalkenyl, CCalkynyl, C-Ccycloalkyl, C-Cheterocycloalkyl, aryl and heteroaryl, and'}, {'sup': '9', 'sub': 1-', '10', '3', '6, 'Ris H or a cation, or CCalkyl which is unsubstituted or substituted with one or more substituents independently selected from the group consisting of C-Ccycloalkyl, heterocycloalkyl, aryl and heteroaryl,'}, {'sup': 1', '2', '3', '4', '7', '8', '9', '10', '5', '6', '10', '10', '10', '10', '10', '5', '6', '5', '6', '5', '10', '5', '10', '5', '6', '5', '5', '6', '5', '6', '5', '10', '5', '6', '10, 'sub': 1', '6', '1', '6', '2', '2', '2', '2', '10', '2', '10', '3', '6', '3', '6', '1', '6', '1', '6', '1-', '10', '2-', '10', '2-', '10', '1', '4', '3', '6', '3', '6', '2', '1', '4', '3', '8', '3', '8', '6', '14', '1-', '10', '1-', '10, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'where any carbon or heteroatom of R, R, R, R, R, R, Ris unsubstituted or is substituted with one or more substituents independently selected from C-Calkyl, C-Chaloalkyl, halogen, —OR, —NRR, oxo, cyano, nitro, —C(O)R, —C(O)OR, —SR, —S(O)R, —S(O)R, —NRR, —CONRR, —N(R)C(O)R, —N(R)C(O)OR, —OC(O) ...

THROMBOPOIETIN MIMETICS

Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative. 150-. (canceled)52. The method of wherein Q is —COOH claim 51 , which is the compound 3′-{N′-[1-(3 claim 51 ,4-Dimethylphenyl)-3-methyl-5-oxo-1 claim 51 ,5-dihydropyrazol-4-ylidene]hydrazino}-2′-hydroxybiphenyl-3-carboxylic acid or a pharmaceutically acceptable salt thereof.53. The method of wherein Q is tetrazol-5-yl claim 51 , which is the compound 3-{N′-[1-(3 claim 51 ,4-dimethylphenyl)-3-methyl-5-oxo-1 claim 51 ,5-dihydropyrazol-4-ylidene]hydrazino}-2-hydroxy-3′-tetrazol-5-ylbiphenyl or a pharmaceutically acceptable salt thereof.54. The method of wherein the compound is administered orally.55. The method of wherein the compound is administered parenterally.56. The method of further comprising co-administering a therapeutically effective amount of an agent selected from the group consisting of: a colony stimulating factor claim 51 , cytokine claim 51 , chemokine and an interleukin or cytokine receptor agonist or antagonist.57. The method of wherein the agent is selected from the group consisting of: G-CSF claim 56 , GM-CSF claim 56 , TPO claim 56 , M-CSF claim 56 , EPO claim 56 , Gro-beta claim 56 , IL-11 claim 56 , SCF claim 56 , FLT3 ligand claim 56 , LIF claim 56 , IL-3 claim 56 , IL-6 claim 56 , IL-1 claim 56 , NESP claim 56 , SD-01 claim 56 , IL-8 and IL-5.59. The method of wherein Q is —COOH claim 58 , which is the compound 3′-{N′-[1-(3 claim 58 ,4-Dimethylphenyl)-3-methyl-5-oxo-1 claim 58 ,5-dihydropyrazol-4-ylidene]hydrazino}-2′-hydroxybiphenyl-3-carboxylic acid or a pharmaceutically acceptable salt thereof.60. The method of wherein Q is tetrazol-5-yl claim 58 , which is the compound 3-{N′-[1-( ...

INTELLIGENT BACKHAUL SYSTEM

A intelligent backhaul system is disclosed to manage and control multiple intelligent backhaul radios within a geographic zone. The intelligent backhaul system includes multiple intelligent backhaul radios (IBRs) that are able to function in both obstructed and unobstructed line of sight propagation conditions, one or more intelligent backhaul controllers (IBCs) connecting the IBRs with other network elements, and an intelligent backhaul management system (IBMS). The IBMS may include a private and/or public server and/or agents in one or more IBRs or IBCs. 1. An intelligent backhaul system comprising: a plurality of receive RF chains;', 'one or more transmit RF chains;', 'an antenna array comprising a plurality of directive gain antenna elements, wherein each directive gain antenna element is couplable to at least one receive RF or transmit RF chain;', 'a radio resource controller, wherein the radio resource controller sets or causes to be set a certain RF carrier frequency or channel bandwidth for at least one of the receive or transmit RF chains;', 'an interface bridge configured to couple the intelligent backhaul radio to a data network, the interface bridge comprising one or more Ethernet interfaces to couple the interface bridge to the data network, the interface bridge multiplexing and buffering the one or more Ethernet interfaces; and', 'a media access controller to exchange data to and from the data network via coupling to at least the interface bridge and to and from at least one other intelligent backhaul radio,, 'a plurality of intelligent backhaul radios, each of the plurality of intelligent backhaul radios comprisingwherein one or more of the plurality of intelligent backhaul radios comprises an intelligent backhaul management system agent coupled to the radio resource controller, and wherein said intelligent backhaul management system agent sets or causes to be set certain policies related to the RF carrier frequency or channel bandwidth for at least ...

Intelligent Backhaul Radio with Multi-Interface Switching

A intelligent backhaul system is disclosed to manage and control multiple intelligent backhaul radios within a geographic zone. The intelligent backhaul system includes multiple intelligent backhaul radios (IBRs) that are able to function in both obstructed and unobstructed line of sight propagation conditions, one or more intelligent backhaul controllers (IBCs) connecting the IBRs with other network elements, and an intelligent backhaul management system (IBMS). The IBMS may include a private and/or public server and/or agents in one or more IBRs or IBCs. 1. An intelligent backhaul radio with combined switch comprising:a plurality of network interfaces;a managed switch coupled to the plurality of network interfaces;a plurality of receive RF chains;one or more transmit RF chains;an antenna array comprising a plurality of directive gain antenna elements, wherein each directive gain antenna element is couplable to at least one receive RF or transmit RF chain;a modem comprising one or more modulator cores and comprising one or more demodulator cores, wherein each of the one or more modulator cores is coupled to at least one of the one or more transmit RF chains and each of the one or more demodulator cores is coupled to at least one of the plurality of receive RF chains;a media access controller coupled to the modem and an interface bridge;the interface bridge specifically coupled to the managed switch via at least one of the plurality of network interfaces or via at least one of one or more internal ports of the managed switch; andone or more wireless adapters,wherein at least one wireless adapter is specifically coupled to the managed switch via at least one of the plurality of network interfaces or via at least one of one or more internal ports of the managed switch, andwherein the managed switch determines parameters based upon at least one policy, the parameters associated with an exchange of traffic between the at least one wireless adapter specifically coupled ...

Intelligent Backhaul Management System

A intelligent backhaul system is disclosed to manage and control multiple intelligent backhaul radios within a geographic zone. The intelligent backhaul system includes multiple intelligent backhaul radios (IBRs) that are able to function in both obstructed and unobstructed line of sight propagation conditions, one or more intelligent backhaul controllers (IBCs) connecting the IBRs with other network elements, and an intelligent backhaul management system (IBMS). The IBMS may include a private and/or public server and/or agents in one or more IBRs or IBCs.

Intelligent Backhaul Controller

A intelligent backhaul system is disclosed to manage and control multiple intelligent backhaul radios within a geographic zone. The intelligent backhaul system includes multiple intelligent backhaul radios (IBRs) that are able to function in both obstructed and unobstructed line of sight propagation conditions, one or more intelligent backhaul controllers (IBCs) connecting the IBRs with other network elements, and an intelligent backhaul management system (IBMS). The IBMS may include a private and/or public server and/or agents in one or more IBRs or IBCs. 1. An intelligent backhaul controller comprising:a plurality of network interfaces;a host controller;an intelligent backhaul management system agent; anda managed switch coupled to the plurality of network interfaces and the host controller,wherein the intelligent backhaul management system agent is capable of communicating with or comprised within either of the host controller or the managed switch, andwherein the intelligent backhaul management system agent is capable of communicating with either a server or at least one of one or more other intelligent backhaul management system agents to exchange at least one policy that affects operation of the managed switch.2. The intelligent backhaul controller of further comprising:a power supply configured to receive a power input;and a remote power switch coupled to the power supply and the plurality of network interfaces.3. The intelligent backhaul controller of further comprising a battery backup coupled to the power supply.4. The intelligent backhaul controller of wherein the intelligent backhaul management system agent or the host controller is capable of communicating with the remote power switch.5. The intelligent backhaul controller of wherein the intelligent backhaul management system agent or the host controller directs the remote power switch to restrict or terminate power to one or more of the plurality of network interfaces based on at least one of one or ...

Chemical Compounds

The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: 2. A compound of Formula (I) claim 1 , as described in claim 1 , wherein:{'sup': '3', 'claim-text': hydrogen, and', {'sub': '3', '—OCH,'}], 'Ris selected fromor a salt thereof including a pharmaceutically acceptable salt thereof.5. A compound of selected from:5-({3-(aminocarbonyl)-7-[2,4-bis(methyloxy)-5-pyrimidinyl]-4-quinolinyl}amino)-3-biphenylcarboxylic acid;5-({3-(aminocarbonyl)-7-[2,6-bis(methyloxy)-3-pyridinyl]-4-quinolinyl}amino)-1,3-benzenedicarboxylic acid;3-({3-(aminosulfonyl)-7-[2,4-bis(methyloxy)-5-pyrimidinyl]-4-quinolinyl}amino)-5-cyclopentylbenzoic acid;3-({3-(aminosulfonyl)-7-[2,4-bis(methyloxy)-5-pyrimidinyl]-4-quinolinyl}amino)benzoic acid; and3-({3-(aminocarbonyl)-7-[2,4-bis(methyloxy)-5-pyrimidinyl]-4-quinolinyl}amino)-5-cyclopentylbenzoic acid;or a salt thereof including a pharmaceutically acceptable salt thereof.6. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.7. A method of treating or lessening the severity of cancer in a mammal in need thereof claim 1 , which comprises administering to such mammal a therapeutically effective amount of a compound of Formula I claim 1 , as described in or a pharmaceutically acceptable salt thereof.8. The method of wherein the mammal is a human.9. A method of treating or lessening the severity of cancer in a mammal in need thereof claim 4 , which comprises administering to such mammal a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.10. The method of wherein the mammal is a human.11. The method according to wherein said cancer is selected from: brain (gliomas) claim 7 , glioblastomas claim 7 , Bannayan-Zonana syndrome claim 7 , Cowden disease claim 7 , Lhermitte-Duclos disease claim 7 , breast claim 7 , colon claim 7 ...

METHOD FOR DEPLOYING A BACKHAUL RADIO WITH ANTENNA ARRAY

A intelligent backhaul system is disclosed to manage and control multiple intelligent backhaul radios within a geographic zone. The intelligent backhaul system includes multiple intelligent backhaul radios (IBRs) that are able to function in both obstructed and unobstructed line of sight propagation conditions, one or more intelligent backhaul controllers (IBCs) connecting the IBRs with other network elements, and an intelligent backhaul management system (IBMS). The IBMS may include a private and/or public server and/or agents in one or more IBRs or IBCs. 1. A method for deploying a first backhaul radio capable of communicating with one or more second backhaul radios , wherein the first backhaul radio comprises at least a backhaul management system agent for exchanging information with at least a server and an antenna array comprising at least a plurality of directive gain antenna elements , said method comprising:receiving at least configuration information from the server;determining a favored one of the one or more second backhaul radios from at least association information comprised within the configuration information;associating via a first wireless link with the favored one of the one or more second backhaul radios;processing signals transmitted or received via at least one of the plurality of directive gain antenna elements based at least upon one or more operational parameters of the first wireless link; andreporting at least one of the one or more operational parameters to the server; a link quality metric;', 'a link performance metric;', 'an operational statistic;', 'a resource selection;', 'a timing parameter;', 'a measured interference level;', 'an internal topology characteristic;', 'an access control setting; or', 'combinations thereof., 'wherein the one or more operational parameters comprises one or more of2. The method of claim 1 , said method further comprising:determining a favored RF spectrum resource selection from at least RF spectrum ...

Novel Compounds

A compound of Formula (I) 127.-. (canceled)29. A compound of claim 28 , or a pharmaceutically acceptable salt thereof claim 28 , wherein:{'sup': '35', 'Ris selected from: F and OH; and'}{'sup': '36', 'Ris selected from: F and OH;'}{'sup': 35', '36, 'provided: at least one of Rand Ris F.'}30. A compound of claim 28 , or a pharmaceutically acceptable salt thereof claim 28 , wherein:{'sup': '35', 'Ris OH; and'}{'sup': '36', 'Ris F.'}32. A pharmaceutical composition comprising a compound of claim 28 , or a pharmaceutically acceptable salt thereof claim 28 , and one or more of pharmaceutically acceptable excipients.33. A method of treating a disease state selected from: inflammation claim 28 , allergic diseases claim 28 , autoimmune diseases claim 28 , human immunodeficiency virus (HIV) claim 28 , infectious diseases claim 28 , cancer claim 28 , and pre-cancerous syndromes claim 28 , in a mammal in need thereof claim 28 , which comprises administering to such mammal a therapeutically effective amount of a compound of Formula IV claim 28 , or a pharmaceutically acceptable salt thereof claim 28 , as described in .34. The method of wherein the mammal is a human.35. A composition comprising a compound of claim 28 , or a pharmaceutically acceptable salt thereof claim 28 , and an antigen or antigen composition.36. A vaccine composition comprising an antigen or antigen composition and a compound of claim 28 , or a pharmaceutically acceptable salt thereof.37. An immugenic composition comprising an antigen or antigen composition and a compound of claim 28 , or a pharmaceutically acceptable salt thereof.38. A composition comprising a compound of claim 28 , or a pharmaceutically acceptable salt thereof claim 28 , and one or more immunostimulatory agents.39. A method of treating a disease selected from: HBV claim 28 , HCV claim 28 , influenza claim 28 , skin warts claim 28 , multiple sclerosis claim 28 , and allergic inflammation claim 28 , in a human in need thereof claim 28 , ...

Prolyl Hydroxylase Inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) 7. A pharmaceutical composition which comprises a compound as described in and one or more of pharmaceutically acceptable carriers claim 1 , diluents and excipients.8. A method of treating anemia in a mammal in need thereof which comprises administering to such mammal a therapeutically effective amount of a compound as described in of .9. The method of wherein the mammal is a human.10. A method of inhibiting HIF prolyl hydroxylases in a mammal in need thereof which comprises administering to such mammal a therapeutically effective amount of a compound as described in .11. The method of wherein the mammal is a human.12. A method of treating Ischemia in a mammal in need thereof which comprises administering to such mammal a therapeutically effective amount of a compound as described in .13. The method of wherein the mammal is a human.14. A method of treating myocardial infarction in a mammal in need thereof which comprises administering to such mammal a therapeutically effective amount of a compound as described in .15. The method of wherein the mammal is a human.16. A method of treating diseases of the hematopoietic system claim 14 , in a mammal in need thereof claim 14 , which comprises: administering to such mammal a therapeutically effective amount of{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) a compound as described in ; and'}b) EPO or a derivative thereof.17. A process for preparing a pharmaceutical composition containing a pharmaceutically acceptable carrier or diluent and an effective amount of a compound as described in which process comprises bringing the compound as described in into association with a pharmaceutically acceptable carrier or diluent. This application is a Continuation of Ser. No. 16/023,058 filed Jun. 29, 2018, which is Allowed; which is a Continuation of Ser. No. 15/187,075 filed Jun. 20, 2016, which is now U.S. Pat. ...

METHOD FOR DEPLOYING A BACKHAUL RADIO WITH ANTENNA ARRAY

An intelligent backhaul system is disclosed to manage and control multiple intelligent backhaul radios within a geographic zone. The intelligent backhaul system includes multiple intelligent backhaul radios (IBRs) that are able to function in both obstructed and unobstructed line of sight propagation conditions, one or more intelligent backhaul controllers (IBCs) connecting the IBRs with other network elements, and an intelligent backhaul management system (IBMS). The IBMS may include a private and/or public server and/or agents in one or more IBRs or IBCs. 1receiving at least configuration information from the server;determining a favored one of the one or more second backhaul radios from at least association information comprised within the configuration information;associating via a first wireless link with the favored one of the one or more second backhaul radios;processing signals transmitted or received via at least one of the plurality of directive gain antenna elements based at least upon one or more operational parameters of the first wireless link; andreporting at least one of the one or more operational parameters to the server; a link quality metric;', 'a link performance metric;', 'an operational statistic;', 'a resource selection;', 'a timing parameter;', 'a measured interference level;', 'an internal topology characteristic;', 'an access control setting; or', 'combinations thereof., 'wherein the one or more operational parameters comprises one or more of. A method for deploying a first backhaul radio capable of communicating with one or more second backhaul radios, wherein the first backhaul radio comprises at least a backhaul management system agent for exchanging information with at least a server and an antenna array comprising at least a plurality of directive gain antenna elements, said method comprising: The present application is a continuation application of U.S. patent application Ser. No. 14/964,292, filed Dec. 9, 2015, currently pending, ...

Novel anti-infectives

Compounds useful as HCV anti-infectives having the formula: wherein the formula variables are as defined herein, are disclosed. Also disclosed are methods of making and using the same.

Prolyl hydroxylase inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

G-csf mimetics

Invented are G-CSF mimetics. Also invented are selected octacyclic compounds , pharmaceutical compositions containing these compounds, and methods of using these compounds as G-CSF mimetics. Also invented are novel processes used in preparing these compounds.

G-CSF mimetics

G-CSF mimetics

Hexacyclic g-csf mimetics

Invented are G-CSF mimetics. Also invented are selected hexacyclic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds as G-CSF mimetics. Also invented are novel processes used in preparing these compounds.

Hexacyclic g-csf mimetics

Invented are G-CSF mimetic. Also invented are selected hexacyclic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds as G-CSF mimetic. Also invented are novel processes used in preparing these compounds.

Novel chemical compounds

(5Z) -5- (6-QUINOXALINYL METHYLIDENE) -2 - [(2,6-DICHLOROPHENYL) AMINO] -1,3-THIAZOL-4 (5H) -ONE

REFERIDA A UN COMPUESTO (5Z)-5-(6-QUINOXALINILMETILIDENO)-2- (2,6-DICLOROFENIL)AMINO -1,3-TIAZOL-4(5H)-ONA, Y/O SUS SALES, HIDRATOS, SOLVATOS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHO COMPUESTO ES INHIBIDOR DE LA PROTEINA hYAK3 Y ES UTIL PARA TRATAR O PREVENIR DEFICIENCIAS EN CELULAS ERITROIDES Y HEMATOPOYETICAS TALES COMO ANEMIA, ANEMIA APLASICA, MIELOSUPRESION, CITOPENIA, ENTRE OTRAS

(5z)-5-(6-quinoxalinylmethylidene)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazol-4(5h)-one

Invented is the compound (5Z)-5-(6-quinoxalinylmethylidene)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazol-4(5H)-one, and/or pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are pharmaceutical compositions containing this compound, methods of preparing this compound and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are methods of using this compound as an inhibitor of hYAK3 proteins.

(5z) -5- (6-quinoxalinylmethylidene) -2 - [(2,6-dichlorophenyl) mino] -1,3-thiazol-4 (5h) -one

(5Z) -5- (6-QUINOXALINILMETILIDENO) -2-1(2,6-DICLOROFENIL)ANINO]-1,3-TIAZOL-4 (5H) -ONA. A presente invenção se refere ao composto (5Z)-5- (6-quinoxalinilmetilideno)-2-[ (2, 6-diclorofenil)amino] -1,3- tiazol-4(5H)-ona, e/ou aos sais, hidratos, solvatos e pró- fármacos farmaceuticamente aceitáveis do mesmo. Ainda se refere às composições farmacêuticas contendo o referido composto, métodos de preparação do referido composto e os sais, hidratos, solvatos e prá-fármacos farmaceuticamente aceitáveis do mesmo. Também se refere aos métodos de uso do referido composto como um inibidor de proteínas hYAK3. (5Z) -5- (6-Quinoxyalkylmethylidene) -2-1 (2,6-Dichlorophenyl) Anino] -1,3-Thiazole-4 (5H) -ON. The present invention relates to (5Z) -5- (6-quinoxalinylmethylidene) -2 - [(2,6-dichlorophenyl) amino] -1,3-thiazol-4 (5H) -one, and / or salts pharmaceutically acceptable hydrates, solvates and prodrugs thereof. It further relates to pharmaceutical compositions containing said compound, methods of preparing said compound and the pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof. It also relates to methods of using said compound as an hYAK3 protein inhibitor.

Cyclic purine dinucleotides as modulators of sting

A compound of Formula (I) wherein Y 1, Y2, X 1, X 2, R 1, R 2, R3, R4, R5, R6, R8, and R9 are as defined herein; and pharmaceutically acceptable salts and tautomers thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, in the treatment of diseases in which modulation of STING (Stimulator of Interferon Genes) is beneficial, for example inflammation, allergic and autoimmune diseases, infectious diseases, cancer, pre-cancerous syndromes and as vaccine adjuvants.

Novel chemical compounds

Prolyl hydroxylase inhibitors

The invention described herein relates to certain pyrimidinetrione N-subs tituted glycine derivatives of formula (I), which are antagonists of HIF pro lyl hydroxylases and are useful for treating diseases benefiting from the in hibition of this enzyme, anemia being one example.

Thrombopoietin-mimetic

Prolyl hydroxylase inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Thrombopoietin mimetics

Chemical compounds

The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R, R 1 , R 2 , R 3 and R 4 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Method for deploying a backhaul radio with antenna array

A intelligent backhaul system is disclosed to manage and control multiple intelligent backhaul radios within a geographic zone. The intelligent backhaul system includes multiple intelligent backhaul radios (IBRs) that are able to function in both obstructed and unobstructed line of sight propagation conditions, one or more intelligent backhaul controllers (IBCs) connecting the IBRs with other network elements, and an intelligent backhaul management system (IBMS). The IBMS may include a private and/or public server and/or agents in one or more IBRs or IBCs.

Thrombopoietin mimetics

Thrombopoietin (TPO) mimetics and their use as promoters of thrombopoiesis and megakaryocytopoiesis are disclosed. Also disclosed are processes and intermediates used in the preparation of these compounds; a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative. (62) Divided out of 522474

Thrombopoietin mimetics

Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azo-naphthalene derivative.

Methods of treatment

This invention relates to a method of treating a disease state selected from: Alzheimer's disease, Down's syndrome, mental retardation, memory defects, memory loss, pancreatic cancer, bone resorption disease, osteoporosis, sickle cell anemia, chronic kidney disease, diabetes, depression, and subsets of depression including: alcoholism, anxiety, obsessive compulsive disorder, panic disorder, chronic pain, obesity, senile dementia, migraine, bulimia, anorexia, social phobia, pre-menstrual syndrome (PMS), adolescent depression, trichotillomania, dysthymia and substance abuse, in a mammal in need thereof, including a human, which comprises administering to such mammal a therapeutically effective amount of a selected substituted thiazol compound. The invention also relates to a method of enhancing cognition in a mammal in need thereof which comprises administering to such mammal a therapeutically effective amount of a selected substituted thiazol compound.

5(Z)-5-(6-quinoxalinylmethylidene)-2-[2,6-dichlorophenyl)amino]-1,3-thiazol-4(5H)-one

Invented is the compound (5Z)-5-(6-quinoxalinylmethylidene)-2-[(2,6 -dichlorophenyl)amino]-1,3-thiazol-4(5H)-one, and/or pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are pharmaceutical compositions containing this compound, methods of preparing this compound and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are methods of using this compound as an inhibitor of hYAK3 proteins.

Cordless voice and data application in a broadband gateway

A broadband gateway 10 that communicates with a broadband computer network 30 and narrow band cordless devices 34 is provided. The gateway 10 houses together a connector 12 to a broadband network, which is connected to a broadband modem 14. The broadband modem 14 provides a broadband computer network outlet 16. The broadband modem 14 is also connected to a narrow band cordless device 40. The narrow band cordless device 40 may be formed by a translation board 18 connected to the broadband modem 14, a microprocessor 20 connected to the translation board 18, a burst mode controller 22 connected to the microprocessor 20 and the translation board 18, and a transceiver 24 electrically connected to the burst mode controller 22. A codec device 26 may also be connected to the burst mode controller 22 to allow the use of a conventional telephone 32.

Thrombopoietin mimetics

Prolyl hydroxylase inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Prolyl hydroxylase inhibitors

THE INVENTION DESCRIBED HEREIN RELATES TO CERTAIN PYRIMIDINETRIONE N-SUBSTITUTED GLYCINE DERIVATIVES OF FORMULA (I), WHICH ARE ANTAGONISTS OF HIF PROLYL HYDROXYLASES AND ARE USEFUL FOR TREATING DISEASES BENEFITING FROM THE INHIBITION OF THIS ENZYME, ANEMIA BEING ONE EXAMPLE.

Thrombopoietin mimetics

Compounds

A compound of Formula (I) wherein Y 1 , Y 2 , X 1 , X 2 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , and R 9 are as defined herein; and pharmaceutically acceptable salts and tautomers thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, in the treatment of diseases in which modulation of STING (Stimulator of Interferon Genes) is beneficial, for example inflammation, allergic and autoimmune diseases, infectious diseases, cancer, pre-cancerous syndromes and as vaccine adjuvants.

HYDROXYL POSITION Suspensions

Η εφεύρεση που περιγράφεται εδώ σχετίζεται με ορισμένα παράγωγα πυριμιδινοτριόνης Ν-υποκατεστημένης γλυκίνης του τύπου (I), (I) που είναι ανταγωνιστές των HIF προλυλο υδροξυλασών και είναι χρήσιμα για τη θεραπεία ασθενειών που επωφελούνται από την αναστολή αυτού του ενζύμου, παράδειγμα των οποίων είναι η αναιμία. The invention described herein relates to certain N-substituted glycine pyrimidinotrione derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for the treatment of diseases that benefit from inhibition of this enzyme, examples of which are anemia.

Prolyl hydroxylase inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Novel chemical compounds

This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.

Regulated activation of cell-membrane receptors by metal-chelating agonists

Thrombopoietin mimetics

Thrombopoietin mimetics

Compounds, compositions and methods

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Protease inhibitors

Thrombopoietin mimetics

Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

Prolyl hydroxylase inhibitors

Pyridazine-dione N-substituted glycine derivatives as HIF hydroxylase inhibitors

The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Thrombopoietin mimetics

Invented are non-peptide TPO mimetics. also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted thiosemicarbazone derivative.

Chemical compounds

The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to FormµLa (I): wherein R, R1,P, X, Y, and Z are as defined herein; or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be usefµL in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Thrombopoietin mimetics

Anti-infectives

Compounds useful as HCV anti-infectives are disclosed. Also disclosed are methods of making and using the same.

N-substituted glycine derivatives: hydroxylase inhibitors

The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Thiadiazolyl compounds as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives Formula (I): (I) that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

MICROSOFT THROMOPOYTINE

Εφευρεθέντα είναι μιμητικά ΤΡΟ μη-πεπτίδια. Επίσης, εφευρεθέντα είναι νέες μέθοδοι και ενδιάμεσα χρήσιμα στη παρασκευή των προσφάτως εφευρεθεισών ενώσεων. Επίσης, εφευρεθείσα είναι μία μέθοδος θεραπείας θρομβοκυτοπενίας σε ένα θηλαστικό, που συμπεριλαμβάνει έναν άνθρωπο που έχει ανάγκη αυτής, που περιλαμβάνει χορήγηση σε ένα τέτοιο θηλαστικό μιας αποτελεσματικής ποσότητας ενός επιλεγέντος παραγώγου υδροξυ-1 -αζοβενζολίου. Invented are TPO mimetic non-peptides. Also invented are new methods and intermediates useful in the preparation of recently invented compounds. Also invented is a method of treating thrombocytopenia in a mammal, comprising a human in need thereof, comprising administering to such a mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

N-substituted glycine derivatives: hydroxylase inhibitors

The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

N-substituted glycine derivatives: hydroxylase inhibitors

The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Novel chemical compounds

This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.

Anti-infectives

Compounds useful as HCV anti-infectives having the formula (I) wherein the formula variables are as defined herein, are disclosed. Also disclosed are methods of making and using the same.

Prolyl Hydroxylase Inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Dinucleótidos cíclicos de purina moduladores de sting

Reivindicación 1: Un compuesto difosfatriciclo[13.2.1.0⁶,¹⁰]octadecano-3,12-diona caracterizado porque tiene la fórmula (1) en donde: Y¹ y Y² son independientemente CH₂ u O; X¹ y X² son independientemente S u O; R¹ es OH y R² es NH₂ o R¹ es NH₂ y R² es H; R³ es OH y R⁴ es NH₂ o R³ es NH₂ y R⁴ es H; R⁵ se selecciona de: F, OH y OC(O)R⁷; R⁶ se selecciona de: F, OH y OC(O)R⁷; siempre que: cuando R⁵ o R⁶ sea F, al menos uno de Y¹ y Y² sea CH₂; y R⁸ y R⁹ se seleccionan independientemente de: H, CH₂OC(O)R⁷, CH₂OCO₂R⁷, CH₂CH₂SC(O)R⁷ y CH₂CH₂SSCH₂R⁷; siempre que: cuando X¹ y X² sean O, al menos uno de R⁸ y R⁹ no sea H; donde R⁷ se selecciona de: arilo, heteroarilo, heterocicloalquilo, cicloalquilo, alquilo C₁₋₂₀ y alquilo C₁₋₂₀ sustituido con uno a 5 sustituyentes seleccionados independientemente de: arilo, cicloalquilo, hidroxi y F; o una sal farmacéuticamente aceptable del mismo.

Μιμητικα θρομβοποιητινης

Μιμητικά ΤΡΟ μη-πεπτίδιο έχουν εφευρεθεί. Επίσης έχουν εφευρεθεί νέες μέθοδοι και ενδιάμεσα που χρησιμοποιούνται στην παρασκευή των προσφάτων εφευρεθεισών ενώσεων. Επίσης έχει εφευρεθεί μία μέθοδος για θεραπεία θρομβοκυτοπενίας σε ένα θηλαστικό που συμπεριλαμβάνει έναν άνθρωπο που έχει ανάγκη αυτής που περιλαμβάνει χορήγηση σε ένα τέτοιο θηλαστικό μιας αποτελεσματικής ποσότητος ενός επιλεγέντος παραγώγου υδροξυ-1-αζοβενζολίου.

Compostos, sais farmaceuticamente aceitáveis dos mesmos, composição farmacêutica e composição imunogênica compreendendo ditos compostos e usos terapêuticos dos mesmos

NOVOS COMPOSTOS. Um composto com a Fórmula (I) em que Y1, Y2, X1, X2, R1, R2, R3, R4, R5, R6, R8 e R9 são tal como definidos aqui; e sais farmaceuticamente aceitáveis e tautômeros dos mesmos, composições, combinações e medicamentos contendo os referidos compostos e processos para a preparação dos mesmos. A invenção também se refere ao uso dos referidos compostos, combinações, composições e medicamentos no tratamento de doenças em que a modulação de STING (Estimulador dos Genes de Interferon) é benéfica, por exemplo, em inflamação, doenças alérgicas e autoimunes, doenças infecciosas, câncer, síndromes pré-cancerosas e como adjuvantes de vacinas.

Thrombopoietinmimetika

Inhibidores de proteasas

La presente invención proporciona compuestos que inhiben proteasas, incluyendo catepsina K, composiciones farmacéuticas de tales compuestos, y métodos para tratar enfermedades de excesiva pérdida ósea o degeneración de cartílago o degradación de cartílago o matriz, incluyendo osteoporosis; enfermedad gigival, incluyendo gingivitis y periodontitis; artritis, más especificamente, osteoartritis y artritis reumatoide; enfermedad de Paget; hipercalcemia de enfermedades malignas; y enfermedad ósea metabólica, que comprende inhibir dicha pérdida ósea o degeneración excesiva de cartílago o matriz administrando un compuesto de la presente invención a un paciente con necesidad de ello.

Compostos de tiadiazolil o-ligados como inibidores de dna polimerase theta

compostos de tiadiazolil o-ligados como inibidores de dna polimerase theta. são revelados no presente documento certos derivados de tiadiazolila da fórmula (i): que inibem a atividade de dna polimerase theta (pol), em particular inibem a atividade de pol¿ ao inibir a atividade do domínio de helicase dependente de atp de pol¿. além disso, são reveladas composições farmacêuticas que compreendem esses compostos e métodos para tratar e/ou prevenir doenças tratáveis pela inibição de pol como câncer, incluindo cânceres deficientes de recombinação homóloga (hr).

Novel anti-infectives

Novel chemical compounds

This invention relates to newly identified compounds for inhibiting YAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of YAK3 proteins.

Thrombopoietin-mimetika

O-linked thiadiazolyl compounds as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives Formula (I): (I) that inhibit DNA Polymerase Theta (Pol) activity, in particular inhibit Pol activity by inhibiting ATP dependent helicase domain activity of Pol. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Pol such as cancer, including homologous recombination (HR) deficient cancers.

Thrombopoietin-mimetika

Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives of Formula (I), (II), (III), or (IV): (I), (II), (III), (IV) that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

O-linked thiadiazolyl compounds as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives Formula (I): (I) that inhibit DNA Polymerase Theta (Pol) activity, in particular inhibit Pol activity by inhibiting ATP dependent helicase domain activity of Pol. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Pol such as cancer, including homologous recombination (HR) deficient cancers.

Thrombopoietin mimetics

Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted naphthimidazole derivative.

Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives of Formula (I), (II), (III), or (IV): (I), (II), (III), (IV) that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

Compuestos de 1,3-tiazol-4(5h)-ona como inhibidores de yak3

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R ES ARILO, HETEROARILO, ALCOXI, ENTRE OTROS; Q ES (a) , DONDE A, B, D, E Y G FORMAN UN ANILLO QUE CONTIENE 1 A 2 ENLACES DOBLES Y DE 1 A 4 ATOMOS DE NITROGENO, ADEMAS A y B SON C, N Y G, E y D SON CR20, O, S y N; X, Y y Z SON CR20; R20 ES H, HALOGENO, AMINO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (5Z)-2-[(2,6-DICLOROFENIL)AMINO]-5-(PIRAZOLO[1,5-a]PIRIDIN-5-ILMETILIDENO)-1,3-TIAZOL-4(5H)-ONA; (5Z)-2-[(2,6-DICLOROFENIL)AMINO]-5-(IMIDAZO[1,2-a]PIRIDIN-6-ILMETILIDENO)-1,3-TIAZOL-4(5H)-ONA; ENTRE OTROS. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. LOS COMPUESTOS DESCRITOS SON INHIBIDORES DE PROTEINAS YAK3, UTILES EN EL TRATAMIENTO DE ENFERMEDADES DE LOS SISTEMAS ERITROIDE Y HEMATOPOYETICO TALES COMO ANEMIA, ANEMIA APLASTICA, MIELOSUPRESION, CITOPENIA

Novel chemical compounds

This invention relates to newly identified compounds for inhibiting YAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of YAK3 proteins.

O-linked thiadiazolyl compounds as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives Formula (I): (I) that inhibit DNA Polymerase Theta (Pol?) activity, in particular inhibit Pol? activity by inhibiting ATP dependent helicase domain activity of Pol?. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Pol? such as cancer, including homologous recombination (HR) deficient cancers.

Compuestos de tiadiazolilo unidos a un átomo de oxígeno como inhibidores de dna polimerasa θ

RESUMEN Se divulgan en el presente documento determinados derivados de tiadiazolilo de Fórmula (I): (I) que inhiben la actividad de DNA Polimerasa Theta (Pol), en particular, inhiben la actividad de Pol mediante la inhibición de la actividad del dominio de la helicasa dependiente de ATP de Pol. Además, se divulgan composiciones farmacéuticas que comprenden dichos compuestos.

Novel chemical compounds

Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives of Formula (I), (II), (III), or (IV): (I), (II), (III), (IV) that inhibit DNA Polymerase Theta (Pol?) activity, in particular inhibit Pol? activity by inhibiting ATP dependent helicase domain activity of Pol?. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Pol? such as cancer, including homologous recombination (HR) deficient cancers.

Compuestos de tiadiazolilo unidos a un atomo de oxigeno como inhibidores de dna polimerasa (theta).

Se divulgan en el presente documento determinados derivados de tiadiazolilo de Fórmula (I): (ver Fórmula) (I) que inhiben la actividad de DNA Polimerasa Theta (Pol?), en particular, inhiben la actividad de Pol? mediante la inhibición de la actividad del dominio de la helicasa dependiente de ATP de Pol?. Además, se divulgan composiciones farmacéuticas que comprenden dichos compuestos.

O-linked thiadiazolyl compounds as dna polymerase theta inhibitors

Disclosed herein are certain thiadiazolyl derivatives Formula (I): that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

DERIVADOS SUSTITUIDOS DE TIADIAZOLILO COMO INHIBIDORES DE LA DNA POLIMERASA q

Se divulgan en el presente documento determinados derivados de tiadiazolilo de fórmula (1), (2), (3) ó (4) que inhiben la actividad de DNA Polimerasa q (Polq), en particular inhiben la actividad de Polq mediante la inhibición de la actividad del dominio de la helicasa dependiente de ATP de Polq. Además, se divulgan composiciones farmacéuticas que comprenden dichos compuestos y métodos para tratar y/o prevenir enfermedades tratables mediante la inhibición de Polq, tales como el cáncer, incluidos los cánceres deficientes en recombinación homóloga (HR).

Compuestos de tiadiazolilo unidos a un átomo de oxígeno como inhibidores de dna polimerasa theta

Se divulgan en el presente documento determinados derivados de tiadiazolilo de Fórmula (I): que inhiben la actividad de DNA Polimerasa Theta (Pol theta), en particular, inhiben la actividad de Pol theta mediante la inhibición de la actividad del dominio de la helicasa dependiente de ATP de Pol theta. Además, se divulgan composiciones farmacéuticas que comprenden dichos compuestos.

Compuestos de tiadiazolilo unidos a un átomo de oxígeno como inhibidores de dna polimerasa q

Se divulgan en el presente documento determinados derivados de tiadiazolilo de fórmula (1) que inhiben la actividad de DNA Polimerasa Theta (Polq), en particular, inhiben la actividad de Polq mediante la inhibición de la actividad del dominio de la helicasa dependiente de ATP de Polq. Además, se divulgan composiciones farmacéuticas que comprenden dichos compuestos.