Derivatives of n-(arylamino)sulfonamides as inhibitors of mek

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof

The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.

Process for Preparing Form A of Atazanavir Sulfate

A process of making Form A of atazanavir sulfate comprises: a) mixing atazanavir free base with a solvent selected from the group consisting of methanol (MeOH), ethanol (EtOH), isopropanol (IPA), N-methylprrolidone (NMP) and combinations thereof; b) reacting sulfuric acid with the atazanavir free base in the mixture formed in step a) to form a reaction solution comprising atazanavir sulfate; c) mixing an antisolvent with the reaction solution; d) seeding the mixture formed in step c) with an effective amount of Form A of atazanavir sulfate to form a seeded mixture comprising Form A of atazanavir sulfate; and e) isolating Form A of atazanavir sulfate in solid form from the seeded mixture; wherein the antisolvent is selected from the group consisting of methyl tert-butyl ether (MTBE), ethyl acetate (EtOAc), acetonitrile (MeCN), isopropyl acetate (IPAc), cyclohexane, and combinations thereof. In one alternative, step c) may be performed before step b). In another alternative, step d) may be carried out concurrent with or prior to step c).

BIARYL OXYACETIC ACID COMPOUNDS

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 2. A compound or salt according to wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen and methyl.3. (canceled)4. A compound or salt according to claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl and isopropyl.5. (canceled)6. A compound or salt according to claim 1 , wherein Ris selected from aryl and heteroaryl claim 1 , each optionally substituted with one to four substituents independently selected from halogen claim 1 , cyano claim 1 , (C-C) haloalkyl claim 1 , (C-C) alkoxy claim 1 , (C-C) haloalkoxy claim 1 , (C-C) alkyl claim 1 , and (C-C) alkylsulfonyl.9. A compound or salt according to claim 8 , wherein Ris selected from hydrogen claim 8 , methyl claim 8 , fluoro claim 8 , chloro claim 8 , cyano claim 8 , —CFand methoxy; and Ris selected from hydrogen claim 8 , fluoro claim 8 , chloro claim 8 , methyl claim 8 , methoxy claim 8 , cyano claim 8 , —CFand —SOCH.10. A compound or salt according to wherein Rand Rare each independently selected from fluoro claim 9 , chloro claim 9 , methoxy and hydrogen.11. (canceled)13. A compound or salt according to wherein Ris selected from naphthyl claim 6 , pyridinyl and quinolinyl claim 6 , each optionally substituted with one to four substituents independently selected from halogen claim 6 , cyano claim 6 , (C-C) haloalkyl claim 6 , (C-C) alkoxy claim 6 , (C-C) haloalkoxy claim 6 , (C-C) alkyl and alkylsulfonyl.14. A compound or salt according to claim 1 , wherein Rand Rare each hydrogen.15. A compound or salt according to claim 1 , wherein A is selected from phenyl claim 1 , pyridinyl claim 1 , benzimidazolyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , pyrimidinyl and imidazopyridinyl.16. A compound ...

COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITION AND METHODS OF MAKING SAME

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals. 2. The compound of claim 1 , wherein X is selected from the group consisting of hydrogen claim 1 , heteroalkyl claim 1 , substituted heteroalkyl claim 1 , heteroaryl claim 1 , substituted heteroaryl claim 1 , heteroarylalkyl claim 1 , substituted heteroarylalkyl claim 1 , CN claim 1 , S(O)R claim 1 , CONRR claim 1 , —COR claim 1 , SONRR claim 1 , NRSOR claim 1 , NRSONRR claim 1 , B(OR)(OR) claim 1 , P(O)(OR)(OR) claim 1 , and P(O)(R)(OR).7. A composition comprising one or more compounds of claim 1 , or a salt claim 1 , hydrate claim 1 , solvate or N oxide thereof claim 1 , and one or more pharmaceutically acceptable carriers.8. The composition of claim 7 , which is a food claim 7 , beverage or medicament for human consumption.9. A coffee or coffee flavored food or beverage or medicament composition that comprises at least one compound of or a salt claim 1 , hydrate claim 1 , solvate or N oxide thereof.10. The composition of claim 9 , which is an instant coffee claim 9 , ground coffee claim 9 , or brewed coffee.11. The composition of claim 9 , which is an instant coffee.12. A food claim 1 , beverage claim 1 , or medicament composition having a bitter taste wherein said bitter taste is alleviated or eliminated by the addition of an effective amount of a compound of or a salt claim 1 , hydrate claim 1 , ...

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Compounds of the formula I: 2. The compound of claim 1 , wherein C is a group of formula (i).3. The compound of claim 2 , wherein A is a group of formula (a).4. The compound of claim 3 , wherein B is a group of formula (e).5. The compound of claim 3 , wherein B is a group of formula (f).6. The compound of claim 3 , wherein m is 0.7. The compound of claim 3 , wherein m is 1.8. The compound of claim 3 , wherein Rand Rare hydrogen.9. The compound of claim 3 , wherein Rand Rare hydrogen.10. The compound of claim 3 , wherein Ris: Calkyl; Ccycloalkyl; or Ccycloalkyl-Calkyl; each of which may be optionally substituted one or more times with halo.11. The compound of claim 3 , wherein Ris Calkyl.12. The compound of claim 3 , wherein Ris isobutyl.14. The compound of claim 13 , wherein Ris: —SO—R; —(CH)—C(O)—NRR; —(CH)—SO—NRR; —(CH)—NR—C(O)—R; or —(CH)—NR—SO—R.18. A composition comprising:(a) a pharmaceutically acceptable carrier; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) a compound of .'}19. A method for treating arthritis claim 1 , said method comprising administering to a subject in need thereof an effective amount of a compound of . This application claims the benefit under 35 USC §119 of U.S. Provisional Application Ser. No. 61/579,255 filed on Dec. 22, 2011, the disclosure of which is incorporated herein by reference.The invention pertains to compounds that modulate the function of retinoid-receptor related orphan receptor RORc (RORγ) and use of such compounds for treatment of autoimmune diseases.T helper 17 cells (Th17) are interleukin (IL)-17 secreting CD4+ T cells involved in pathogenesis of autoimmune diseases such as rheumatoid arthritis, irritable bowel disease, psoriasis, psoriatic arthritis and spondyloarthridities. The retinoic acid-related orphan receptor γ (RORγ or RORc) is recognized as a transcription factor necessary for Th17 cell differentiation. RORc is an orphan member of the nuclear hormone receptor subfamily that includes RORα (RORa) ...

CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS

The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection. 4. The compound of wherein (G) is a heterocyclyl.5. (canceled)6. The compound of wherein (G) is phenyl.78-. (canceled)9. The compound of wherein E is —X═X— claim 1 , and X claim 1 , X claim 1 , Xand Xare independently C(R2) or N.10. The compound of wherein E is —X═X— claim 1 , and X claim 1 , X claim 1 , Xand Xare independently C(R2).1112-. (canceled)13. The compound of wherein E is —S— claim 1 , and Xand Xare independently C(R2) or N.1420-. (canceled)21. The compound of wherein each (R1) is independently chosen from alkyl claim 1 , aryl claim 1 , amino claim 1 , amido claim 1 , nitro claim 1 , halo claim 1 , haloalkyl claim 1 , haloalkoxy claim 1 , cyano claim 1 , heterocycle claim 1 , sulfonyl claim 1 , sulfonamide claim 1 , hydroxyl claim 1 , or alkoxy.22. The compound of wherein each (R1) is independently chosen from —CF claim 1 , —F claim 1 , —Cl claim 1 , —CN claim 1 , —CH claim 1 , —OH claim 1 , —OCH claim 1 , —C(═O)NH claim 1 , —NH—CO—CH claim 1 , —NH—SO—CH claim 1 , —NH—SO—CH—CH claim 1 , —NH—SO—CH(CH)—CH claim 1 , —NH—SO—(CH) claim 1 , —NH—SO—(CH)—CN claim 1 , —NHSOCF claim 1 , or —S(═O)NHCH.2328-. (canceled)30. The compound of wherein E is —S— or —X═X—.3137-. (canceled)38. The compound of wherein (G) is an aryl or heterocyclyl.3941-. (canceled)42. The compound of wherein each (R1) is independently chosen from alkyl claim 29 , aryl claim 29 , amino claim 29 , amido claim 29 , nitro claim 29 , halo claim 29 , haloalkyl claim 29 , cyano claim 29 , heterocyclyl claim 29 , sulfonyl claim 29 , sulfonamide claim 29 , hydroxyl claim 29 , or alkoxy.4446-. (canceled)47. The compound of wherein (G) is an aryl or heterocyclyl.4850-. (canceled)51. The compound of wherein each (R1) is independently chosen from alkyl claim 43 , aryl ...

SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN

In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 5. The compound of claim 1 , wherein the compound exhibits inhibition of STAT with an ICof less than about 300 μM.6. The compound of claim 1 , wherein the compound exhibits inhibition with an Kof less than about 300 μM.7. A pharmaceutical composition comprising a therapeutically effective amount of a compound of and a pharmaceutically acceptable carrier.12. The method of claim 8 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.13. The method of claim 8 , wherein the disorder is selected from psoriasis and pulmonary arterial hypertension.14. The method of claim 8 , wherein the disorder is a disease of uncontrolled cellular proliferation.15. The method of claim 14 , wherein the disease of uncontrolled cellular proliferation is a cancer selected from cancers of the head claim 14 , neck claim 14 , pancreas claim 14 , brain claim 14 , colon claim 14 , rectum claim 14 , skin claim 14 , ovary claim 14 , kidney claim 14 , prostate claim 14 , breast claim 14 , lung claim 14 , colon claim 14 , uterus claim 14 , and liver.18. The method of claim 16 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.19. The method of claim 16 , wherein the disorder is a disease of uncontrolled cellular proliferation.20. The method of claim 19 , ...

Tableted compositions containing atazanavir

Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV.

MULTI-MODALITY MOLECULAR IMAGING HIGH-THROUGHPUT ASSAY FOR IDENTIFYING HEAT SHOCK PROTEIN 90 (HSP90) INHIBITORS

High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90α or Hsp90β and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. A-D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives. 2. The therapeutic composition of claim 1 , wherein Ris a thiophene claim 1 , a furan claim 1 , or a substituted phenyl claim 1 , wherein the substituted phenyl is a methoxyphenyl claim 1 , an halogenated phenyl claim 1 , or a dimethoxyphenyl.3. The therapeutic composition of claim 1 , wherein the inhibitor has the formula I and is selected from compounds CP9 and A1-A62 of .5. The therapeutic composition of claim 4 , wherein Ris a thiophene claim 4 , a furan claim 4 , phenyl claim 4 , or a substituted phenyl claim 4 , wherein the substituted phenyl is a methoxyphenyl claim 4 , an halogenated phenyl claim 4 , or a dimethoxyphenyl.6. The therapeutic composition of claim 4 , wherein the inhibitor is selected from compounds CP9 and A1-A62 of .8. The therapeutic composition of claim 1 , wherein the inhibitor is CP9 claim 1 , A17 claim 1 , A29 claim 1 , or A61 claim 1 , or a combination thereof.9. The therapeutic composition of further comprising a pharmaceutically acceptable carrier.11. The method of claim 10 , wherein Ris a thiophene claim 10 , a furan claim 10 , phenyl claim 10 , or a substituted phenyl claim 10 , wherein the substituted phenyl is a methoxyphenyl claim 10 , an halogenated phenyl claim 10 , or a dimethoxyphenyl.12. The method of claim 10 , wherein the inhibitor has the formula I and is selected from compounds CP9 and A1-A62 of .14. The method of claim 13 , wherein Ris a thiophene claim 13 , a furan claim 13 , ...

Sulfonamide-Containing Compounds

This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of γ-secretase. 2. The compound of claim 1 , wherein W claim 1 , W claim 1 , W claim 1 , and Ware defined according to definition (A).3. (canceled)4. The compound according to claim 1 , wherein each of W claim 1 , W claim 1 , W claim 1 , and Wis CH.512-. (canceled)13. The compound according to claim 1 , wherein Ris selected from —COH; —C(O)OR; —NHC(O)OR; —N(CH)C(O)OR; —C(O)N(R)(R); —C(O)R; —CN; and —SO(R).14. The compound according to claim 13 , wherein Ris —COH.15. The compound according to claim 13 , wherein Ris —COR.16. (canceled)17. The compound according to claim 13 , wherein Ris —SO(R).18. (canceled)19. The compound according to claim 13 , wherein Ris —C(O)N(R)(R).2027-. (canceled)28. The compound of claim 1 , wherein Ris C-Caryl claim 1 , which is optionally substituted with from 1-3 independently selected R.29. The compound of claim 28 , wherein Ris phenyl claim 28 , which is optionally substituted with from 1-3 independently selected R.30. The compound of claim 29 , wherein claim 29 , Ris unsubstituted phenyl.31. The compound according to claim 1 , wherein Ris C-Calkyl claim 1 , which is optionally substituted with a substituent selected from —OH and —CN.32. The compound of claim 31 , wherein Ris —CHCHor —CH.3338-. (canceled)39. The compound according to claim 1 , wherein the carbon attached to Rand Rhas the S configuration.40. The compound according to claim 1 , wherein Ris C-Caryl claim 1 , which is optionally substituted with from 1-3 independently selected R.41. (canceled)42. The compound of claim 40 , wherein Ris 4-chloro-phenyl claim 40 , 4-fluoro-phenyl claim 40 , or 2 claim 40 ,4-difluorophenyl.4346-. (canceled)47. The compound according to claim 1 , wherein A is CH.48. A pharmaceutical composition comprising a compound of formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , as claimed in claim 1 , and a pharmaceutically ...

Compounds and therapeutic uses thereof

The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.

SELECTIVE HYDROXAMIC ACID BASED MMP-12 AND MMP-13 INHIBITORS

The present invention provides a compound of formula (I): 1. A compound or salt thereof selected from the group consisting of:(R)—N-Hydroxy-2-[(1-hydroxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[Benzyl-(7-ethoxy-naphthalene-2-sulfonyl)-amino]-N-hydroxy-3-methyl-butyramide;N-isoamyl-N-(6-ethyl naphthalene-2-sulfonyl)-D-valine hydroxamic acid;N-Hydroxy-2-[(6-hydroxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[(6-Amino-naphthalene-2-sulfonyl)-(3-phenyl-propyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Acetylamino-naphthalene-2-sulfonyl)-(3-phenyl-propyl)-amino]-N-hydroxy-3-methyl-butyramide;N-isoamyl-N-(6-methoxy naphthalene-2-sulfonyl)-D-valine hydroxamic acid;N-isoamyl-N-(6-hydroxy naphthalene-2-sulfonyl)-D-valine hydroxamic acid;2-[(7-Amino-naphthalene-2-sulfonyl)-(3-phenyl-propyl)-amino]-N-hydroxy-3-methyl-butyramide;(R)—N-Hydroxy-2-[(7-methoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[(6-Ethoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[Benzyl-(6-p-tolylamino-naphthalene-2-sulfonyl)-amino]-N-hydroxy-3-methyl-butyramide;N-Hydroxy-3-methyl-2-[[6-(3-methyl-butoxy)-naphthalene-2-sulfonyl]-(3-methyl-butyl)-amino]-butyramide;2-[(7-Ethoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;N-Hydroxy-2-[(6-isobutoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[(6-Amino-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Benzyloxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Acetylamino-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;N-Hydroxy-3-methyl-2-{(3-methyl-butyl)-[7-(3-methyl-butylamino)-naphthalene-2-sulfonyl]-amino}-butyramide;2-[(7-Acetylamino-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Allyloxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N- ...

TUNABLE PHENYLACETYLENE HOSTS

A compound, or a salt thereof, having the formula 7. The compound of claim 1 , wherein X is halogen and m is 5.8. The compound of claim 1 , wherein the polyether moiety is a poly(ethylene oxide) moiety.10. The compound of claim 9 , wherein X is a polyether moiety claim 9 , a lower alkoxy claim 9 , a lower alkyl claim 9 , or halogen.12. The compound of claim 11 , wherein X is a polyether moiety claim 11 , a lower alkoxy claim 11 , a lower alkyl claim 11 , or halogen.15. The compound of claim 13 , wherein R is —COOR″ wherein R″ is a lower alkyl.16. The compound of claim 14 , wherein R is —COOR″ wherein R″ is a lower alkyl.18. The compound of claim 5 , wherein Ris lower alkyl and Ris aryl or substituted aryl.19. The compound of claim 17 , wherein Ris lower alkyl and Ris aryl or substituted aryl. This application claims the benefit of U.S. Provisional Application No. 61/576,940, which was filed on Dec. 16, 2011, and is incorporated herein by reference in its entirety.This invention was made with government support under grant number GM087398-01A1 awarded by the National Institutes of Health, grant number CHE-0718242 awarded by the National Science Foundation, grant number GK12 (DGE-0742540) awarded by the National Science Foundation, and grant number IGERT (DGE-0549503). The government has certain rights in the invention.The synthesis of new molecules designed to bind or sense and report the presence of a particular substrate is an area of chemistry that is attracting attention. There exists a general lack of ligand-specific host molecules, such as specific hosts for toxic ions and small molecules of interest. There also is a dearth of specific hosts that report binding events, for example by exhibiting a spectral shift upon binding, such as an altered fluorescent response. In fact, structures of fluorescent coordination complexes are generally poorly understood, which makes the rational design of functional hosts and sensors a challenging undertaking.The detection of ...

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 2. The conjugate of claim 1 , wherein L is OR.3. The conjugate of claim 2 , wherein R is Cto Calkyl.4. The conjugate of claim 2 , wherein OR is selected from O-p-toluenesulfonate claim 2 , O-methanesulfonate claim 2 , O-trifluoromethanesulfonate claim 2 , O-benzenesulfonate claim 2 , and O-m-nitrobenzenesulfonate.5. The conjugate of claim 1 , wherein the target molecule is a polypeptide.6. The conjugate of claim 5 , wherein the polypeptide is an antibody.7. The conjugate of claim 6 , wherein the antibody is selected from trastuzumab claim 6 , rituximab and cetuximab.8. The conjugate of claim 1 , wherein the target molecule is a peptide.9. The conjugate of claim 8 , wherein the peptide is a targeting peptide.10. The conjugate of claim 9 , wherein the targeting peptide is selected from a cyclic RGD sequence claim 9 , bombesin and glu-N(CO)N-lys PSMA. This application is a Continuation of U.S. patent application Ser. No. 15/963,599, filed Apr. 26, 2018, which is a Continuation of U.S. patent application Ser. No. 15/518,333, filed Apr. 11, 2017, now U.S. Pat. No. 9,980,930, issued on May 29, 2018 and is a National Stage Application, filed under 35 U.S.C. 371, of International Application No. PCT/AU2015/050640, filed on Oct. 16, 2015, which claims priority to, and the benefit of, AU Application No. 2014904138, filed Oct. 16, 2014. The contents of each of these applications are incorporated by reference in their entirety.The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting ...

Heterocyclic compound

The present invention relates to a compound represented by the formula (I), which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. In the formula (I), each symbol is as defined in the specification.

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I) 2. The compound according to claim 1 , wherein Rrepresents a 3-7 membered saturated ring claim 1 , containing one or more heteroatoms each independently selected from the group consisting of O claim 1 , S and N claim 1 , such 3-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halo claim 1 , C-Calkyloxy claim 1 , C(═O)—C-Calkyl claim 1 , C-Calkyl claim 1 , OH claim 1 , CN claim 1 , CFH claim 1 , CFH and CF;{'sub': 1', '2', '1', '4', '1', '3', '1', '4', '2', '2', '3, 'Or RRtogether with the Nitrogen to which they are attached form a 5-7 membered saturated ring, optionally containing one or more additional heteroatoms each independently selected from the group consisting of O, S and N, such 5-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen, halo, CCalkyloxy, oxo, C(═O)—C-Calkyl, C-Calkyl, OH, CN, CFH, CFH and CF.'}3. The compound according to wherein Rrepresents a 4-7 membered saturated ring containing carbon and one or more oxygen atoms claim 1 , such 4-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halo claim 1 , CCalkyloxy claim 1 , C(═O)—C-Calkyl claim 1 , C-Calkyl claim 1 , OH claim 1 , CN claim 1 , CFH claim 1 , CFH and CF.4. The compound according to claim 1 , wherein B represents phenyl or thiophene claim 1 , optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halogen claim 1 , C-Calkyl claim 1 , CN claim 1 , CFH claim 1 , CFH and CF.5. The compound according to claim 1 , wherein Rrepresents C-Calkyl-Ror a 4-7 membered saturated ring consisting of carbon atoms and one or more heteroatoms each independently ...

SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN

In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 220.-. (canceled) This application is a continuation application of U.S. application Ser. No. 13/813,916 filed May 10, 2013, while is a national phase application of PCT/US2011/046340 filed Aug. 2, 2011, which claims priority to U.S. Application No. 61/369,796 filed Aug. 2, 2010 and to U.S. Application No. 61/422,046 filed Dec. 10, 2010, each of which is hereby incorporated by reference in its entirety.This invention was made with government support under grant numbers CA106439 and CA128865 awarded by the National Cancer Institute of the National Institutes of Health. The United States government has certain rights in the invention.STAT proteins were originally discovered as latent cytoplasmic transcription factors that mediate cytokine and growth factor responses (Darnell, J. E., Jr. (1996) Recent Prog. Norm. Res. 51, 391-403; Darnell. J. E. (2005) Nat. Med. 11, 595-596). Seven members of the family, STAT1, STAT2, STAT3, STAT4, STAT5a and STAT5b, and STATE, mediate several physiological effects including growth and differentiation, survival, development and inflammation. STATs are SH2 domain-containing proteins. Upon ligand binding to cytokine or growth factor receptors. STATs become phosphorylated on critical Tyr residue (Tyr705 for STAT3) by growth factor receptors, cytoplasmic Janus kinases (Jaks) or Src family kinases. Two phosphorylated ...

SYNTHESIS OF THE RADIOLABELED PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITORDCFPYL

Methods, and related compositions, for the improved synthesis of [F]DCFPyL are disclosed. Also provided are methods, and related compositions, for the use of [F]DCFPyL so produced. 1. A method of synthesizing 2-(3-{1-carboxy-5-[(6-[F]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioic acid ([F]DCFPyL) , the method comprising:(i) radiofluorinating a DCFPyL precursor comprising ester moiety protecting groups to form a radiofluorinated DCPFPyL precursor;{'sup': '18', '(ii) deprotecting the ester moiety protecting groups of the radiofluorinated DCPFPyL precursor of step (i) with phosphoric acid to form [F]DCFPyL in a reaction mixture; and'}{'sup': 18', '18, '(iii) purifying the [F]DCFPyL from the reaction mixture of step (ii) to provide [F]DCFPyL.'}2. The method of claim 1 , wherein the protecting groups are selected from the group consisting of benzyl claim 1 , p-methoxybenzyl claim 1 , tertiary butyl claim 1 , methoxymethyl claim 1 , methoxyethoxymethyl claim 1 , methylthiomethyl claim 1 , tetrahydropyranyl claim 1 , tetrahydrofuranyl claim 1 , benzyloxymethyl claim 1 , trimethylsilyl claim 1 , triethylsilyl claim 1 , t-butyldimethylsilyl (TBDMS) claim 1 , and triphenylmethyl.3. The method of claim 1 , wherein step (i) and step (ii) are performed in one reactor.4. The method of claim 1 , wherein the synthesizing is automated by use of a radiofluorination module (RFM) comprising a heating block claim 1 , two syringe pumps claim 1 , a multi-port cap claim 1 , and valved reagent addition vials.5. The method of claim 4 , wherein the RFM further comprises a thermal heating cavity.6. The method of claim 1 , wherein the synthesizing is automated by use of an automated radiochemistry synthesizer.7. The method of claim 4 , wherein components of the RFM or the automated radiochemistry synthesizer are free of fluorine.8. The method of claim 1 , wherein the DCFPyL precursor is 5-(((S)-6-(tert-butoxy)-5-(3-((S)-1 claim 1 ,5-di-tert-butoxy-1 claim 1 ,5-dioxopentan-2-yl) ...

3,6-DISUBSTITUTED-2-PYRIDINALDOXIME SCAFFOLDS

The present invention relates to a compound of formula (I), or one of its pharmaceutically acceptable salts: (I) wherein R1, R2 and —X—Y— have specific definitions. It also relates to the use of such a compound in therapy; and to a process for preparing it. 5. Compound according to claim 3 , wherein R2 is alkyl claim 3 , heteroaryl claim 3 , aralkyl or —R3-N(R4)(R5) claim 3 ,wherein R3 is a C1-C4 alkyl group,R4 is H, andR5 is chosen from a naphthyl radical, a 5-fluoroquinolin-4-yl radical, a quinolin-4-yl radical or a 8-methoxyquinolin-4-yl radical.6. Compound according to claim 3 , wherein R2 is —R3-N(R4)(R5) claim 3 , wherein R3 is a C1-C4 alkyl group claim 3 , andR4 and R5 form together with the nitrogen atom a 4-benzyl-piperazin-1-yl radical or a3,7-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl radical.8. Compound according to claim 7 , wherein R2 is alkyl claim 7 , aryl claim 7 , aralkyl or —R3-N(R4)(R5) claim 7 ,wherein R3 is a C1-C4 alkyl group,R4 is H, andR5 is chosen from a naphthyl radical, a 5-fluoroquinolin-4-yl radical, a quinolin-4-yl radical or a 8-methoxyquinolin-4-yl radical.9. Compound according to claim 7 , wherein R2 is —R3-N(R4)(R5) claim 7 , wherein R3 is a C1-C4 alkyl group claim 7 , andR4 and R5 form together with the nitrogen atom a 4-benzyl-piperazin-1-yl radical.13. Process for preparing a compound of formula (I) according claim 1 , wherein —X—Y— is —CH2-CH2- or —C≡C— claim 1 , comprising performing a Sonogashira coupling reaction between a 6-bromopyridinaldoxime and a compound comprising a terminal alkyne claim 1 , optionally followed by a reduction step by reaction with hydrogen.14. A method for treating a disease or condition in a subject in need thereof claim 1 , comprising administering to said subject a therapeutically effective amount of at least one compound according to claim 1 , wherein the disease or condition is:a nervous and/or respiratory failure due to intoxication with at least one organophosphorous nerve agent; a ...

SULFONAMIDE COMPOUNDS USEFUL AS CYP17 INHIBITORS

Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R, R, R, Rand Rare defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds. 6. The compound according to claim 5 , wherein:{'sup': '1', 'sub': 3', '3', '2', '3', '3', '2', '2', '2', '2', '2', '3, 'Ris H, Cl, —CH, —OH, —OCH, —OCHCH, —OCF, —OCHCHF, —OCHCHF, or —OCHCF; and'}{'sup': '7', 'sub': 3', '2', '3', '2', '2', '3', '3', '2', '2', '3', '2', '3', '3', '2', '3', '2', '3', '2', '2', '2', '2', '2, 'Ris F, Cl, —CH, —CHCH, —(CH)CH, —CF, —CHF, —CHOH, —CHOCH, —NHCHCF, —OCH, —OCHCH, —OCHCF, —OCHCHF, —OCHCHF, —O(CH)(cyclopropyl), or cyclopropyl.'}10. The compound according claim 9 , wherein:{'sup': '1', 'sub': 3', '3', '3', '3', '2', '2', '2', '3, 'Ris H, —CH, —CF, —OCH, —OCF, —OCHCHF, or —OCHCF.'}11. The compound according to claim 1 , or a stereoisomer claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein said compound is selected from: N-(3-methyl-4-(4-methyl-3-pyridinyl)phenyl)methanesulfonamide (1); N-(4-(4-methoxypyridin-3-yl)-3-methylphenyl)methanesulfonamide (2); 4-chloro-N-(4-(4-methyl-3-pyridinyl)phenyl)benzenesulfonamide (3); 3 claim 1 ,4-dichloro-N-(4-(4-methyl-3-pyridinyl)phenyl)benzenesulfonamide (4); 4-chloro-N-(3-methyl-4-(4-methyl-3-pyridinyl)phenyl)benzene sulfonamide (5); 1-((1S)-7 claim 1 ,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl)-N-(3-methyl-4-(4-methyl-3-pyridinyl)phenyl)methanesulfonamide (6); 4-chloro-N-(4-(4-methoxypyridin-3-yl)-3-methylphenyl)benzenesulfonamide (7); 4-chloro-N-(4-(4-phenyl-3-pyridinyl) phenyl)benzenesulfonamide (8); 1-phenyl-N-(4-(4-phenyl-3-pyridinyl)phenyl) methanesulfonamide (9); N-(3-methyl-4-(4-phenyl-3-pyridinyl)phenyl)-1-phenylmethane sulfonamide (10); N-(4-((3-methyl-4-(4-phenyl-3-pyridinyl)phenyl)sulfamoyl)phenyl) ...

TABLETED COMPOSITIONS CONTAINING ATAZANAVIR

Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV. 1. A compressed tablet comprising 300 mg of atazanavir as atazanavir sulfate , an intragranular lubricant , and an extragranular lubricant wherein said atazanavir sulfate and the intragranular lubricant are blended intragranularly in the presence of a fluid to form wet granules and the extragranular lubricant is added extragranularly prior to tableting.2. A compressed tablet according to comprising:(a) from about 10 to 98.9% of the atazanavir sulfate;(b) from about 0.1 to 10% of the intragranular lubricant;(c) from about 0.1 to 3.0% of the extragranular lubricant and(d) from about 1 to 20% of a disintegrant;based on the total weight of the compressed tablet.3. A compressed tablet according to wherein at least a portion of the disintegrant is blended intragranularly.4. A compressed tablet according to wherein the intragranular lubricant is stearic acid.5. A compressed tablet according to wherein the extragranular lubricant is magnesium stearate.10. A compressed tablet according to having a % label claim dissolved of 97% at 60 minutes.11. A compressed tablet according to having a % label claim dissolved of 93% at 30 minutes.12. A compressed tablet according to having a % label claim dissolved of 96% at 45 minutes.13. A compressed tablet comprising 300 mg of atazanavir as atazanavir sulfate claim 1 , an intragranular lubricant claim 1 , and an extragranular lubricant prepared by a process comprising the steps of:(a) blending atazanavir sulfate and an intragranular lubricant to form a first blend;(b) granulating the first blend in the presence of a fluid to form wet granules;(c) removing at least a portion of ...

N-BENZYL-N-ARYLSULFONAMIDE DERIVATIVE AND PREPARATION AND USE THEREOF

The invention provides an N-benzyl-N-arylsulfonamide derivative, which is an N-benzyl-N-arylsulfonamide compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof. The N-benzyl-N-arylsulfonamide derivative is obtained by condensing a substituted nitrobenzene with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B), reducing the nitro group to an amino group, and subjecting the amino group to reductive amination, sulfonamidation; or by subjecting a substituted nitrobenzene to nitro reduction, reductive amination and sulfonamidation, and condensing the resultant intermediate with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B). It has been experimentally demonstrated that the N-benzyl-N-arylsulfonamide derivative of the invention can specifically bind to Kv1.3 potassium channel and inhibit or decrease its activity, and is useful in the treatment of autoimmune diseases caused by abnormal activation of the Kv1.3 potassium channel in human or animals. The invention further provides a medicament or a pharmaceutical composition comprising the N-benzyl-N-arylsulfonamide derivative. 4. The N-benzyl-N-arylsulfonamide derivative according to claim 1 , characterized in that the N-benzyl-N-arylsulfonamide derivative is selected from the group consisting of the following compounds:ethyl 4-(2-cyano-4-((4-fluoro-N-propylphenyl)sulfonamido)phenyl) piperazin-1-formate,ethyl 4-(2-cyano-4-(N-(4-fluorobenzyl)propanesulfonamido)phenyl) piperazin-1-formate,ethyl 4-(2-cyano-4-(N-isobutylphenylsulfonamido)phenyl)piperazin-1-formate,N-(3-cyano-4-(4-hydroxypiperidin-1-yl)phenyl)-N-(4-fluorobenzyl) propane-1-sulfonamide,4-(2-cyano-4-(N-(4-fluorobenzyl)propyl)phenyl)-N,N-dimethyl piperazin-1-formamide,ethyl 4-(4-(N-benzylpropanesulfonamido)2-cyanophenyl)piperazin-1-formate,ethyl 4-(2-cyano-4-(N-(3-fluorobenzyl)propanesulfonamido)phenyl) piperazin-1-formate,ethyl 4-(4-(4-(N-(4-chlorobenzyl)propanesulfonamido)2- ...

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Compounds of the formula I: 119-. (canceled)21. The compound of claim 20 , wherein C is a group of formula (i).22. The compound of claim 20 , wherein A is a group of formula (a).23. The compound of claim 20 , wherein B is a group of formula (e).24. The compound of claim 20 , wherein B is a group of formula (f).25. The compound of claim 20 , wherein m is 0.26. The compound of claim 20 , wherein m is 1.27. The compound of claim 20 , wherein Rand Rare hydrogen.28. The compound of claim 20 , wherein Rand Rare hydrogen.29. The compound of claim 20 , wherein Ris: Calkyl; Ccycloalkyl; or Ccycloalkyl-Calkyl; each of which may be optionally substituted one or more times with halo.30. The compound of claim 20 , wherein Ris Calkyl.31. The compound of claim 20 , wherein Ris isobutyl.33. The compound of claim 32 , wherein Ris: —SO—R; —(CH)—C(O)—NRR; —(CH)—SO—NRR; —(CH)—NR—C(O)—R; or —(CH)—NR—SO—R.37. A composition comprising:(a) a pharmaceutically acceptable carrier; and{'claim-ref': {'@idref': 'CLM-00020', 'claim 20'}, '(b) a compound of .'}38. A method for treating arthritis claim 20 , said method comprising administering to a subject in need thereof an effective amount of a compound of . This application claims the benefit under 35 USC §119 of U.S. Provisional Application Ser. No. 61/579,255 filed on Dec. 22, 2011, the disclosure of which is incorporated herein by reference.The invention pertains to compounds that modulate the function of retinoid-receptor related orphan receptor RORc (RORγ) and use of such compounds for treatment of autoimmune diseases.T helper 17 cells (Th17) are interleukin (IL)-17 secreting CD4+ T cells involved in pathogenesis of autoimmune diseases such as rheumatoid arthritis, irritable bowel disease, psoriasis, psoriatic arthritis and spondyloarthridities. The retinoic acid-related orphan receptor γ (RORγ or RORc) is recognized as a transcription factor necessary for Th17 cell differentiation. RORc is an orphan member of the nuclear hormone receptor ...

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 115-. (canceled)17. The conjugate of claim 16 , wherein L is OR.18. The conjugate of claim 17 , wherein R is Cto Calkyl.19. The conjugate of claim 17 , wherein OR is selected from O-p-toluenesulfonate claim 17 , O-methanesulfonate claim 17 , O-trifluoromethanesulfonate claim 17 , O-benzenesulfonate claim 17 , and O-m-nitrobenzenesulfonate.20. The conjugate of claim 16 , wherein the target molecule is a polypeptide.21. The conjugate of claim 20 , wherein the polypeptide is an antibody.22. The conjugate of claim 21 , wherein the antibody is selected from trastuzumab claim 21 , rituximab and cetuximab.23. The conjugate of claim 16 , wherein the target molecule is a peptide.24. The conjugate of claim 23 , wherein the peptide is a targeting peptide.25. The conjugate of claim 24 , wherein the targeting peptide is selected from a cyclic RGD sequence claim 24 , bombesin and glu-N(CO)N-lys PSMA. The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting radionuclide that is used in medical imaging applications. In particular, it is used in positron emission tomography (PET) for cancer detection and imaging. It has a longer half-life (t=79.3 hours) than other radionuclides used for medical imaging, such as F. For example, F has a tof 110 minutes, which means that its use requires close proximity to a cyclotron facility and rapid and high-yielding synthesis techniques for the preparation of the agents into which it is incorporated. Zr is not plagued by these same problems, which makes ...

SERS Reporter Molecules and Methods

A SERS tag comprising a core comprising at least two aggregated particles of a SERS enhancing material wherein the contact point between the particles defines a crevice; and a reporter molecule having a length sufficiently short to fit into the crevice and a conjugated path length which is as large as possible, provided the overall reporter molecule length is maintained sufficiently short to fit into the crevice. 1. A method of providing a SERS tag having maximized scattering intensity comprising:aggregating a core from at least two particles of a SERS enhancing material wherein a contact area between the aggregated particles defines a crevice;providing a reporter molecule comprising at least two metal binding functional groups and at least one aromatic ring conjugated with one or more unsaturated groups, wherein the reporter molecule is further selected to maximizing the Raman cross section of the reporter molecule while not exceeding a length between the two metal binding functional groups which is sufficiently short to permit the molecule to fit into a region of near-field electromagnetic enhancement created by the crevice; andassociating the reporter molecule with the aggregated core at the region of near-field electromagnetic enhancement created by the crevice.2. The method of further comprising aggregating the core from at least two particles of a SERS enhancing material each having a diameter of between about 40 nm and 120 nm3. The method of further comprising providing a reporter molecule having a length of less than or equal to 1.2 nm.4. The method of further comprising providing a reporter molecule having a length of about 1.2 nm.5. The method of wherein the reporter molecule is one of 1 claim 1 ,8-diethynyl-4 claim 1 ,5-bis(4-pyridylethenyl)anthracene claim 1 , 1 claim 1 ,8 claim 1 ,9-triethynyl-10-(4-pyridylethenyl)anthracene claim 1 , 6 claim 1 ,13-bisethynylpentacene claim 1 , 5 claim 1 ,7 claim 1 ,12 claim 1 ,14-tetraethynylpentacene claim 1 , 9 claim ...

COMPOUNDS AND COMPOSITIONS FOR USE AS ALKYLATING AGENT SENSORS AND METHODS OF USE THEREOF

This invention provides compound having a structure of Formula I: 2. The compound of claim 1 , wherein{'sub': 1', '3', '3', '3', '2', '2', '2, 'Ais selected from H, Me, Et, Pr, Bu, F, Br, I, OJ, OC(O)J, CF, CCl, CN, SOH, C(O)OH, CHO, C(O)OJ, COJ, C(O)OK, C(O)NJ, C(O)N(J)(H), C(NJ)J, C(S)NH, C(S)NJand C(S)N(J)(H);'}{'sub': 2', '3', '3', '3', '2', '2', '2, 'Ais selected from H, Me, Et, Pr, Bu, F, Br, I, OJ, OC(O)J, CF, CCl, CN, SOH, C(O)OH, CHO, C(O)OJ, COJ, C(O)OK, C(O)NJ, C(O)N(J)(H), C(NJ)J, C(S)NH, C(S)NJand C(S)N(J)(H);'}{'sub': 1', '3', '3', '3', '2', '2', '2', '2, 'Eis selected from H, F, Br, I, OC(O)L, CF, CCl, CN, SOH, C(O)OH, CHO, CHOH, C(O)OL, COL, C(O)OK, C(O)NL, C(O)N(L)(H), C═NL, C(NL)L, C(S)NH, C(S)NLand C(S)N(L)(H);'}{'sub': 2', '3', '3', '3', '2', '2', '2', '2, 'Eis selected from H, F, Br, I, OC(O)L, CF, CCl, CN, SOH, C(O)OH, CHO, CHOH, C(O)OL, COL, C(O)OK, C(O)NL, C(O)N(L)(H), C═NL, C(NL)L, C(S)NH, C(S)NLand C(S)N(L)(H);'}{'sup': b', 'a', 'b', 'b', 'b', 'b', 'b', 'b', 'b, 'sub': 2', '3', '3', '3', '2', '2', '2, 'D is selected from H, Cl, Br, I, OC(O)T, NO, CF, CCl, CN, SOH, C(O)OH, CHO, C(O)OT, COT, C(O)OK, C(O)NT, C(O)N(T)(H), C(NT)T, C(S)NH, C(S)NTand C(S)N(T)(H);'}{'sub': 1', '2', '3', '3', '3', '2', '2', '2, 'sup': a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a, 'Gis selected from H, F, Cl, Br, I, NO, CF, CCl, CN, SOH, C(O)OH, CHO, OC(O)M, C(O)OM, COM, C(O)OK, C(O)NM, C(O)N(M)(H), C(NM)M, C(S)NH, C(S)NMand C(S)N(M)(H);'}{'sub': 2', '2', '3', '3', '3', '2', '2', '2, 'sup': a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a, 'Gis selected from H, Et, Pr, Bu, F, Cl, Br, I, OH, NO, CF, CCl, CN, SOH, C(O)OH, CHO, OC(O)M, C(O)OM, COM, C(O)OK, C(O)NM, C(O)N(M)(H), C(NM)M, C(S)NH, C(S)NMand C(S)N(M)(H);'}{'sub': 1', '2, 'sup': 'b', 'Qis selected from H, Et, Pr, Bu, Br, I, OH, OMand NO;'}{'sub': 2', '2, 'sup': 'b', 'Qis selected from H, Et, Pr, Bu, Br, I, OH, OMand NO;'}{'sub': 2', '2', '3, 'J is independently selected from a 1-20 carbon alkyl, 1-20 carbon aryl or 1-20 ...

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I) 113-. (canceled)15. The compound of claim 14 , wherein Ris hydrogen.16. The compound of claim 14 , wherein Ris a 4-7 membered saturated ring optionally containing one or more heteroatoms each independently selected from the group consisting of O claim 14 , S and N claim 14 , said 4-7 membered saturated ring optionally substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 14 , halogen claim 14 , C-Calkyloxy claim 14 , C-Calkyloxycarbonyl claim 14 , C(═O)—C-Calkyl claim 14 , C-Calkyl claim 14 , OH claim 14 , CN claim 14 , CFH claim 14 , CFH and CF.17. The compound of claim 14 , wherein Ris C-Ccycloalkyl.18. The compound of claim 14 , wherein B is imidazolyl or thiazolyl claim 14 , each optionally substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 14 , halogen claim 14 , C-Calkyl claim 14 , CN claim 14 , CFH claim 14 , CFH and CF.19. A compound of claim 14 , wherein at least one Ris fluoro claim 14 , and one other Ris selected from the group consisting of C-Calkyl claim 14 , C-Calkenyl claim 14 , CHFand cyclopropyl.20. A compound of claim 14 , wherein one Ris fluoro and one other Ris selected from methyl or CHF claim 14 , and wherein the location of said fluoro is on the para position related to the nitrogen(*) claim 14 , and the location of said methyl or CHFis on the meta position related to the nitrogen(*).21. The compound of claim 14 , wherein each Ris hydrogen.23. A pharmaceutical composition comprising at least one compound of and a pharmaceutically acceptable carrier.24. A product containing (a) at least one compound of claim 14 , and (b) an HBV inhibitor claim 14 , as a combined preparation for simultaneous claim 14 , separate or sequential use in the treatment of HBV infection.25. A method of preventing or treating an HBV infection in a subject in need thereof claim 14 , comprising administering ...

Novel cannabinoid receptor cb2 ligand 4-(aminomethyl)-n,n-dialkylanilines

Disclosed herein are novel cannabinoid receptor-2 (CB2) agonists and inverse agonists represented by Formula (I), and method of modulating the activity of CB2 by contacting the CB-2 receptor with a compound of Formula (I). Also, disclosed are methods for treating multiple myeloma or osteoporosis in a mammal in need thereof by modulating the activity of a cannabinoid receptor-2 (CB2).

Acly inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

SULFONAMIDE COMPOUNDS AND THEIR USE IN THE MODULATION RETINOID-RELATED ORPHAN RECEPTOR

The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ 134-. (canceled)36. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein Rand Rare CH.37. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein Ris isobutyl.38. A compound according to claim 36 , or a pharmaceutically acceptable salt thereof claim 36 , wherein Ris isobutyl.40. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein r is 1 and Ris CHOH.41. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein Rand Rare CH claim 35 , Ris isobutyl claim 35 , r is 1 and Ris CHOH.42. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein s is 0.43. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein t is 1 and X is O.44. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein each Ris H.47. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , wherein Rand Rare CH claim 35 , Ris isobutyl claim 35 , r is 1 claim 35 , Ris CHOH claim 35 , wherein t is 1 claim 35 , and X is O.50. A compound according to claim 35 , or a pharmaceutically acceptable salt thereof claim 35 , which is selected from the group consisting of:N-(4-butyl-2-methylphenyl)-N-isobutyl-4-(pyridin-4-yloxy)benzenesulfonamide;N-(4-butyl-2-methylphenyl)-4-{[(3,5-dimethyl-4-isoxazolyl)methyl]oxy}-N-(2-methylpropyl)benzenesulfonamide;4-((3,5-dimethylisoxazol-4-yl)methoxy)-N-(2,4-dimethylphenyl)-N-isobutylbenzenesulfonamide;4-{[(3,5-dimethyl-4-isoxazolyl)methyl] ...

Heterocyclic compound

wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

Improved synthesis of the radiolabeled prostate-specific membrane antigen (psma) inhibitordcfpyl

Methods, and related compositions, for the improved synthesis of [ 18 F]DCFPyL are disclosed. Also provided are methods, and related compositions, for the use of [ 18 F]DCFPyL so produced.

SELECTIVE INHIBITORS INTERFERING WITH FIBROBLAST GROWTH FACTOR RECEPTOR AND FRS2 INTERACTION FOR THE PREVENTION AND TREATMENT OF CANCER AND OTHER DISEASES

The present technology relates to medicine and includes the use of inhibitors which selectively interfere with the interaction between a fibroblast growth factor receptor and FRS2, and with the interaction with other components of the FRS2 complex. Use of the selective inhibitors described in the present technology leads to a proven increase in anti-tumor efficacy relative to other inhibitors and monoclonal antibodies, a decrease in the toxicity of treatment, and the possibility of achieving complete blockage using a low agent concentration and of conducting long-term treatment. The advantage of the technology includes the development of a novel class of medicinal agents for treating malignant neoplasms and other diseases. 5. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to and at least one pharmaceutically acceptable carrier.6. The pharmaceutical composition according to claim 5 , comprising at least one additional therapeutically active agent.7. A method for prevention or treatment of cancer comprising administration of compounds according to to the patient in a therapeutically effective amount. The present application claims convention priority to EA Patent Application No. 201400495, filed on May 22, 2014, entitled “ , FRS2, ”. This application is incorporated by reference herein in its entirety. The present application is a continuation of International Patent Application no. PCT/EA2014/000013, filed on Jun. 6, 2014, entitled “SELECTIVE INHIBITORS INTERFERING WITH FIBROBLAST GROWTH FACTOR RECEPTOR AND FRS2 INTERACTION FOR THE PREVENTION AND TREATMENT OF CANCER AND OTHER DISEASES”. This application is incorporated by reference herein in its entirety.The present technology relates to medicine and includes the use of inhibitors, which selectively interfere with interaction of the fibroblast growth factor receptor with FSR2, and also interaction with other components of FRS2 complex. The use of selective ...

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions. 2. The compound of claim 1 , wherein D is a bridged monocyclic cycloalkyl optionally substituted with 1-4 R.3. The compound of any one of - claim 1 , wherein D is a bridged 4-6 membered monocyclic cycloalkyl optionally substituted with 1-4 R.4. The compound of any one of - claim 1 , wherein D is bicyclo[1.1.1]pentane optionally substituted with 1-4 R.7. The compound of any one of - claim 1 , wherein D is substituted with 0 R.9. The compound of any one of - claim 1 , wherein at least one of Land Lis independently 2-7-membered heteroalkylene optionally substituted by 1-5 R.10. The compound of any one of - claim 1 , wherein Lis 2-7-membered heteroalkylene and Lis independently selected from C-Calkylene or 2-7-membered heteroalkylene claim 1 , wherein each alkylene and heteroalkylene is optionally substituted by 1-5 R.11. The compound of any one of - claim 1 , wherein both of Land Lare independently 2-7-membered heteroalkylene substituted by 0 R.12. The compound of any one of - claim 1 , wherein each Land Lis independently selected from —CH—* claim 1 , —CHCH—* claim 1 , CHCHCH—* claim 1 , —CH(CH)—* claim 1 , —CH(CH)CH—* claim 1 , CHO—* or CHCHO—* claim 1 , and “—*” indicates the attachment point to A and W claim 1 , respectively.13. The compound of any one of - claim 1 , wherein Lis independently selected from CHO—* or CHCHO—* claim 1 , Lis independently selected from —CH—* claim 1 , —CHCH—* claim 1 , CHCHCH—* claim 1 , —CH(CH)—* claim 1 , —CH(CH)CH—* claim 1 , CHO—* or CHCHO—* claim 1 , and “—*” indicates the attachment point to A and W claim 1 , respectively.14. The compound of any one of - claim 1 , wherein Rand Rare each hydrogen or C-Calkyl.15. The compound of any one of - claim 1 , wherein A is phenyl and W is independently phenyl or 5-6 membered heteroaryl optionally substituted with 1-5 R ...

METHOD FOR PRODUCING POLYGUANIDINES

A method for preparing polycondensation products of guanidine, aminoguanidine or diaminoguanidine G with one or more benzyl or allyl derivatives BA according to the following reaction scheme is provided: 121.-. (canceled)23. The method of claim 22 , wherein Ris a divalent residue selected from the group consisting of optionally substituted benzene claim 22 , divinylbenzene claim 22 , furan claim 22 , pyrrole claim 22 , thiophene claim 22 , pyridine claim 22 , biphenyl claim 22 , fluorene and ethylene.24. The method of claim 23 , wherein Ris a divalent residue selected from the group consisting of benzene claim 23 , divinylbenzene claim 23 , pyridine claim 23 , biphenyl and ethylene.25. The method of claim 22 , wherein the leaving group is selected from the group consisting of chlorine claim 22 , bromine claim 22 , iodine claim 22 , mesylate claim 22 , triflate and tosylate.26. The method of claim 22 , wherein the at least one benzyl or allyl derivative BA is reacted with guanidine claim 22 , aminoguanidine or diaminoguanidine G by heating the reactants at a temperature above their melting temperatures.27. The method of claim 22 , wherein the reaction is conducted for a period of at least 2 h.31. The polyguanidine of claim 28 , wherein Ris a divalent residue selected from the group consisting of optionally substituted benzene claim 28 , divinylbenzene claim 28 , furan claim 28 , pyrrole claim 28 , thiophene claim 28 , pyridine claim 28 , biphenyl claim 28 , fluorene and ethylene.32. The polyguanidine of claim 31 , wherein Ris a divalent residue selected from the group consisting of benzene claim 31 , divinylbenzene claim 31 , pyridine claim 31 , biphenyl and ethylene.33. A method of treating an infection in a human or animal patient claim 22 , the method comprising administering to the human or animal patient the polyguanidine as defined in .34. The method of claim 33 , wherein the infection is a bacterial claim 33 , viral or fungal infection.35. The method of claim ...

COMPOSITIONS AND METHODS FOR THE TREATMENT AND ANALYSIS OF NEUROLOGICAL DISORDERS

Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-β (Aβ) or metal-Aβ species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions. 130-. (canceled)31. A compound comprising:a) a metal chelation component; andb) an amyloid β interaction component.35. The compound of wherein the compound penetrates a blood-brain barrier of a human.36. A method for treating a subject comprising administering the compound of to a subject.37. The method of wherein said subject is a human.38. The method of claim 36 , wherein said subject has a neurological disease or condition.39. The method of wherein said neurological disease or condition has amyloid-β (Aβ) plaques as a pathological marker.40. The method of wherein said neurological disease or condition is Alzheimer's disease.41. The method of wherein said subject has type II diabetes.42. The compound of further comprising a label.43. The compound of wherein said label is a radionuclide or a substitution bearing a radionuclide.44. The compound of wherein said label is a contrast agent.45. A method for detecting a compound in a tissue or subject claim 42 , the method comprising:{'claim-ref': {'@idref': 'CLM-00042', 'claim 42'}, 'exposing a tissue or subject a compound according to ; and detecting the presence of or accumulation of said compound in said tissue or subject.'}46. The method of claim 45 , wherein said tissue comprises neural tissue or pancreatic tissue. Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-β (Aβ) or metal-Aβ species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.More than 36 million people worldwide have ...

INHIBITORS OF HEPATITIS B VIRUS

The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds. 3. The compound according to claim 1 , wherein:A is a 6-membered aromatic or heteroaromatic ring;B is a 6-membered aryl optionally containing one or more N atoms;{'sub': 1-3', '2', '1-6', '3', '2', '3, 'Y is selected from the group consisting of hydrogen, halogen, Calkyl, NH, NH(Calkyl), N(CH), NHC(O)CH, OH and CN or is absent;'}{'sub': 1', '1-6', '1-6', '2', '1-6', '1-6', '1-6', '1-6', '1-6', '1, 'Ris H, linear or branched Calkyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, piperidinyl, pirrolidinyl, oxetanyl, tetrahydrofuranyl, pyridinyl, said Calkyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, piperidinyl, pirrolidinyl, oxetanyl, tetrahydrofuranyl or pyridinyl being optionally substituted with one or more substituents selected from OH, halogen, NH, NH(C═O)OCalkyl, NH(Calkyl), Chydroxyalkyl, 5- or 6-membered heteroaryl, C(═O)Calkyl, C(═O)OCalkyl, OC-6alkyl;'}{'sub': '2', 'Ris H or methyl;'}{'sub': 1', '2', '1-3', '2', '5, 'or Rand Rtaken together form with the N atom to which they are attached a heterocyclic ring selected from piperidine, pirrolidine, morpholine, thiomorpholine and piperazine, said ring being optionally substituted with one or more substituents selected from halogen, Calkyl, OH and CHR;'}{'sub': 3', '4', '1-3, 'Rand Rare each independently H or Calkyl; in particular hydrogen or methyl;'}{'sub': 5', '2', '3', '3', '2', '3', '1-3', '1-3', '1-3, 'Ris selected from the group consisting of OH, NH, NH(CH), N(CH), NHC(O)CH, CN, haloCalkyl, Calkoxy, haloCalkoxy, heterocyclic ring, aryl and heteroaryl;'}{'sub': 1-3', '1-3, 'Ra is selected from the group consisting of hydrogen, halogen, Calkyl, ...

PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT

The present invention relates to an improved process for the preparation of atazanavir bisulfate, an inhibitor of retroviral aspartate protease. The process of the present invention comprises conversion of 1,1-dimethylethyl[(2S,3R)-4-chloro-3-hydroxy-phenylbutan-2-yl]carbamate (Formula II) into 1-[4-(pyridine-2-yl)-phenyl]-4(S)-5 hydroxy-2-N-tert-butoxycarbonylamino-5(S)—N—(N-methoxycarbonyl-(L)-tert-leucyl)amino-6-phenyl-2-azahexane (Formula VII) without isolating intermediate compounds formed therein, followed by its subsequent conversion to atazanavir or its bisulfate salt. 4. The process of claim 3 , wherein the compound of Formula VIII or a salt thereof is further treated with an active ester of N-methoxycarbonyl-(L)-tert-leucine to obtain atazanavir or its bisulfate salt.5. The process of claim 4 , wherein the active ester is obtained by the treatment of N-methoxycarbonyl-(L)-tert-leucine with a compound selected from O-(1 claim 4 ,2-dihydro-2-oxo-1-pyridyl)-N claim 4 ,N claim 4 ,N claim 4 ,N-tetramethyluronium tetrafluoroborate (TPTU) claim 4 , 1-hydroxybenzotriazole (HOBT) claim 4 , N-hydroxysuccinamide or N-ethyl-N′-dimethylaminopropylcarbodiimide (EDC).8. The process of claim 7 , wherein the compound of Formula VIII or a salt thereof is further treated with an active ester of N-methoxycarbonyl-(L)-tert-leucine to obtain atazanavir or its bisulfate salt.9. The process of claim 8 , wherein the active ester is obtained by the treatment of N-methoxycarbonyl-(L)-tert-leucine with a compound selected from O-(1 claim 8 ,2-dihydro-2-oxo-1-pyridyl)-N claim 8 ,N claim 8 ,N claim 8 ,N-tetramethyluronium tetrafluoroborate (TPTU) claim 8 , 1-hydroxybenzotriazole (HOBT) claim 8 , N-hydroxysuccinamide claim 8 , or N-ethyl-N′-dimethylaminopropylcarbodiimide (EDC).11. The process of claim 10 , wherein the treatment of the reaction mixture with an active ester of N-methoxycarbonyl-(L)-tert-leucine is performed in the presence of thionyl chloride or oxalyl chloride.12. The ...

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 1. A radionuclide complex of a compound of formula (I):or a pharmaceutically acceptable salt thereof, wherein L is a leaving group. This application is a Continuation of U.S. patent application Ser. No. 16/511,577, filed Jul. 15, 2019, which is a Continuation of U.S. patent application Ser. No. 15/963,599, filed Apr. 26, 2018, now U.S. Pat. No. 10,398,660 issued on Sep. 3, 2019, which is a Continuation of U.S. patent application Ser. No. 15/518,333, filed Apr. 11, 2017, now U.S. Pat. No. 9,980,930, issued on May 29, 2018 and is a National Stage Application, filed under 35 U.S.C. 371, of International Application No. PCT/AU2015/050640, filed on Oct. 16, 2015, which claims priority to, and the benefit of, AU Application No. 2014904138, filed Oct. 16, 2014. The contents of each of these applications are incorporated by reference in their entirety.The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting radionuclide that is used in medical imaging applications. In particular, it is used in positron emission tomography (PET) for cancer detection and imaging. It has a longer half-life (t=79.3 hours) than other radionuclides used for medical imaging, such as F. For example, F has a tof 110 minutes, which means that its use requires close proximity to a cyclotron facility and rapid and high-yielding synthesis techniques for the preparation of the agents into which it is incorporated. Zr is not plagued by these same problems, which makes Zr particularly attractive for use in ...

METAL-ORGANIC MATERIALS AND METHOD FOR PREPARATION

The present invention provides metal-organic materials, more specifically organometallic polymers, comprising polypyridyl organic ligands such as tetrakis(4-(pyridin-4-ylethynyl)phenyl)methane, tetrakis(4-(2-(pyridin-4-yl)vinyl)phenyl)methane, 1,3,5,7-tetrakis(4-(pyridin-4-ylethynyl)phenyl)adamantane or 1,3,5,7-tetrakis(4-(2-(pyridine-4-yl)vinyl)phenyl) adamantine, and metal ions structurally coordinated with said ligands, and having three-dimensional crystalline micro or sub-micro structure; as well as a method for the preparation thereof. These metal-organic materials are useful as adsorbents in processes for gas adsorption or separation. 2. The metal-organic material according to claim 1 , wherein the metal ion is Ni or Cu and is present as a salt.3. The metal-organic material according to claim 1 , wherein the metal to ligand ratio is 1:2 to 1:10.4. The metal-organic material according to claim 1 , wherein the metal to ligand ratio is 1:2 to 1:4.5. The metal-organic material according to claim 1 , wherein the metal ion is present as a salt of NiBr claim 1 , NiNO claim 1 , or CuNO.6. The metal-organic material according to claim 1 , wherein the material is crystalline.7. The metal-organic material according to claim 6 , wherein the crystalline material is in the shape of an egg claim 6 , barrel claim 6 , or hexagonal prism.8. The metal-organic material according to claim 1 , wherein the material is coated with Au nanoparticles.9. The metal-organic material according to claim 1 , wherein metal ions are Ni and Cu in a ratio of 1:1.10. The metal-organic material according to claim 1 , wherein the metal ions are present as NiBr and NiNOin a 1:1 ratio.12. The metal-organic material according to claim 11 , wherein the metal ion is Ni or Cu and is present as a salt.13. The metal-organic material according to claim 11 , wherein the metal to ligand ratio is 1:2 to 1:10.14. The metal-organic material according to claim 11 , wherein the metal to ligand ratio is 1:2 to 1:4. ...

Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b

Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R 1 , R 2 and R 4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

POLYGUANIDINE POLYMERS AND METHODS OF USE THEREOF

Polyguanidines and methods of use thereof are described. In particular, polyguanidines of formula (I), formula (II), and formula (III) are described. The polyguanidines can be used to treat infection, such as bacterial, viral or fungal infection, and as an ex vivo microbial agent. 2. The polyguanidine of claim 1 , wherein Ris a divalent residue selected from the group consisting of optionally substituted benzene claim 1 , divinylbenzene claim 1 , furan claim 1 , pyrrole claim 1 , thiophene claim 1 , pyridine claim 1 , biphenyl claim 1 , fluorene and ethylene.3. The polyguanidine of claim 2 , wherein Ris a divalent residue selected from the group consisting of benzene claim 2 , divinylbenzene claim 2 , pyridine claim 2 , biphenyl and ethylene.4. A method of treating an infection in a human or animal patient claim 1 , the method comprising administering to the human or animal patient the polyguanidine as defined in .5. The method of claim 4 , wherein the infection is a bacterial claim 4 , viral or fungal infection.6. The method of claim 5 , wherein the polyguanidine is administered topically or systemically.7. The method of claim 6 , wherein the polyguanidine is administered in the form of a drug or a pharmaceutical composition.8. A method of using the polyguanidine as defined in as an ex vivo antimicrobial agent.9. The method of claim 8 , wherein the polyguanidine is an active component of antimicrobial paints claim 8 , coatings claim 8 , foils claim 8 , or membranes.10. A drug or pharmaceutical composition for antagonizing bacterial infections in a human or animal patient comprising a polyguanidine of as an antiinfective.11. The drug or pharmaceutical composition of claim 10 , further comprising at least one pharmaceutically acceptable carrier or excipient and optionally one or more adjuvants and/or one or more further active agents.12. The drug or pharmaceutical composition of claim 11 , comprising at least one further active agent that also shows an antiinfective ...

COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV). 181.-. (canceled)83. The compound of claim 82 , wherein Lis Formula (IIa).84. (canceled)85. (canceled)86. (canceled)88. The compound of claim 82 , wherein Lis Formula (IIb).89. (canceled)90. (canceled)91. (canceled)93. The compound of claim 82 , wherein Lis Formula (IIc).94. (canceled)95. (canceled)96. (canceled)97. (canceled)98. (canceled)99. (canceled)101. The compound of claim 82 , wherein Lis selected from the group consisting of Formula (IId) claim 82 , Formula (IIf) claim 82 , Formula (IIh) and Formula (IIj).102. (canceled)103. (canceled)104. (canceled)105. (canceled)106. (canceled)107. (canceled)108. (canceled)110. The compound of claim 82 , wherein Lis selected from the group consisting of Formula (IIe) and Formula (IIm).111. (canceled)112. (canceled)113. (canceled)114. (canceled)116. The compound of claim 82 , wherein Lis Formula (IIg).117. (canceled)118. (canceled)119. (canceled)120. (canceled)122. The compound of claim 82 , wherein Lis selected from the group consisting of Formula (IIi) claim 82 , Formula (IIk) and Formula (IIl).123. (canceled)124. (canceled)125. (canceled)126. (canceled)128. (canceled)129. (canceled)130. (canceled)131. (canceled)132. (canceled)133. (canceled)134. (canceled)135. (canceled)136. The compound of claim 82 , Ais an optionally substituted aryl.137. (canceled)138. (canceled)139. (canceled)140. The compound of claim 82 , wherein Ais an optionally substituted aryl(Calkyl).141. The compound of claim 82 , wherein Ais an optionally substituted cycloalkyl or an optionally substituted cycloalkenyl.142. The compound of ...

Novel cannabinoid receptor cb2 ligand 4-(aminomethyl)-n, n-dialkylanilines

Disclosed herein are novel cannabionid receptor-2 (CB2) agonists and inverse agonists represented by Formula (I), and method of modulating the activity of CB2 by contacting the CB-2 receptor with a compound of Formula (I). Also, disclosed are methods for treating multiple myeloma or osteoporosis in a mammal in need thereof by modulating the activity of a cannabinoid receptor-2 (CB2).

DERIVATIVES OF N-(ARYLAMINO) SULFONAMIDES AS INHIBITORS OF MEK

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases. 1101-. (canceled)103. A method according to claim 102 , which is for the treatment of an oncologic disease.104. A method according to claim 102 , wherein a compound of formula I or a pharmaceutically acceptable salt thereof is administered.109. A method according to claim 102 , wherein the compound of formula I is administered in combination with an additional therapy claim 102 , which is radiation therapy claim 102 , chemotherapy or a combination of both.110. A method according to claim 102 , further comprising administering at least one additional therapeutic agent.111. A method according to claim 102 , wherein said proliferative disease is cancer.112. A method according to claim 102 , wherein said proliferative disease is cancer claim 102 , which is brain cancer claim 102 , breast cancer claim 102 , lung cancer claim 102 , ovarian cancer claim 102 , pancreatic cancer claim 102 , prostate cancer claim 102 , renal cancer claim 102 , colorectal cancer claim 102 , leukemia claim 102 , myeloid leukemia claim 102 , glioblastoma claim 102 , follicular lymphona claim 102 , pre-B acute leukemia claim 102 , chronic lymphocytic B-leukemia claim 102 , mesothelioma or small cell line cancer.113. A method according to claim 102 , wherein said proliferative disease is cancer claim 102 , which is breast cancer claim 102 , colorectal cancer claim 102 , non-small-cell lung cancer claim 102 , melanoma or pancreatic cancer.114. A method according to claim 102 , wherein said proliferative disease is cancer claim 102 , which is an ovarian claim 102 , thyroid claim 102 , hepatocellular or biliary carcinoma.115. A method according to claim 102 , wherein said proliferative disease is cancer claim 102 , which is acute myeloid leukemia or multiple myeloma.116. A method according to claim 102 , which is for inhibiting tumor size ...

PENTAFLUOROPHENYL SULFONAMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF

The present application relates to sulfonamide containing compounds of Formulae (I) and (II) and compositions containing said compounds effective in the treatment of cell proliferative disorders, in particular cancer, and various methods of use thereof. 2. The compound of claim 1 , wherein Ris selected from Ccycloalkyl and heterocycloalkyl claim 1 , each of which is optionally substituted with one to two of halo claim 1 , CN claim 1 , OH claim 1 , NH claim 1 , ═O claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkenyl claim 1 , NH(Calkyl) claim 1 , N(Calkyl)(Calkyl) claim 1 , OCalkyl claim 1 , OCalkenyl claim 1 , OCalkynyl claim 1 , CalkyleneOCalkyl claim 1 , CalkyleneOCalkenyl claim 1 , CalkyleneOCalkynyl claim 1 , C(O)Calkyl claim 1 , C(O)Calkenyl claim 1 , C(O)Calkynyl claim 1 , C(O)OCalkyl claim 1 , C(O)OCalkenyl claim 1 , C(O)OCalkynyl claim 1 , S(O)Calkyl claim 1 , S(O)Calkenyl claim 1 , S(O)Calkynyl C(O)NHCalkyl claim 1 , C(O)N(Calkyl(Calkyl) and NHC(O)Calkyl).3. The compound of claim 1 , wherein Ris a Ccycloalkyl optionally substituted with one or two substituents independently selected from OCalkyl claim 1 , CalkyleneOCalkyl claim 1 , CalkyleneOCalkynyl claim 1 , C(O)Calkyl claim 1 , C(O)Calkynyl claim 1 , C(O)OCalkyl claim 1 , and C(O)OCalkynyl.4. The compound of claim 3 , wherein Ris unsubstituted cyclopropyl claim 3 , cyclobutyl claim 3 , cyclopentyl or cyclohexyl.5. The compound of claim 3 , wherein Ris unsubstituted cyclopropyl or cyclopropyl substituted with one substituent selected from CalkyleneOCalkyl claim 3 , CalkyleneOCalkynyl claim 3 , C(O)Calkyl claim 3 , C(O)Calkynyl claim 3 , C(O)OCalkyl claim 3 , and C(O)OCalkynyl.6. The compound of claim 1 , wherein Ris selected from heterocycloalkyl claim 1 , aryl and heteroaryl claim 1 , each of which is optionally substituted with one or more of Calkyl claim 1 , Calkenyl claim 1 , Calkynyl halo claim 1 , OH claim 1 , ═O claim 1 , NH claim 1 , NH(Calkyl) claim 1 , N(Calkyl)(Calkyl) claim 1 , OCalkyl claim ...

CHROMOPHORES FOR PHOTOCHROMIC COMPOSITIONS USEFUL FOR THREE DIMENSIONAL DISPLAY APPLICATIONS

Described herein are novel azo-benzene type chromophores. The chromophores are useful in photochromic compositions comprising a polymer matrix and a chromophore, wherein the chromophore is a novel azo-benzene type structure. The photochromic composition is photoresponsive upon irradiation by at least one wavelength of laser light across the visible light spectrum. Photochromic devices which comprise the novel azo-benzene type chromophore compound show significantly higher photoinduced birefringence, higher diffraction efficiency, and brighter images than devices that comprise well known azo-benzene chromophores. The photochromic composition may include a liquid crystal. 2. The chromophore of claim 1 , wherein Y is N.3. The chromophore of claim 1 , wherein R-Rare independently hydrogen or alkyl.4. The chromophore of claim 1 , wherein Z is N or O.5. The chromophore of claim 1 , wherein at least one of X-Xis N.8. A photochromic composition comprising an optically transparent polymer matrix and the chromophore of .9. The photochromic composition of claim 8 , wherein the composition is configured to be photoresponsive upon irradiation by first laser having a first wavelength in the visible light spectrum claim 8 , and wherein the first laser is selected from the group consisting of a blue laser claim 8 , a green laser claim 8 , and a red laser.10. The photochromic composition of claim 8 , wherein two or more chromophores are mixed within the composition.11. The photochromic composition of claim 8 , wherein the chromophore is present in the composition in an amount in the range of about 0.01 wt % to about 30 wt %.12. The photochromic composition of claim 8 , wherein the chromophore is present in the composition in an amount in the range of about 1 wt % to about 15 wt %.14. The photochromic composition of claim 8 , wherein the polymer matrix is formed from polyethylene terephthalate claim 8 , polyacrylate claim 8 , polymethacrylate claim 8 , polyvinyl carbazole claim 8 , ...

SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: 2. The compound of claim 1 , wherein RW— is (R)N— or (R)HN— or (R)— claim 1 , and wherein —WRis —N(R)or —NH(R) or —(R) claim 1 , provided that a nitrogen atom of RW— and/or a nitrogen atom of —WRis linked to the remainder of the molecule.3. The compound of claim 1 , wherein —WRis a fused aryl or a fused heteroaryl group claim 1 , wherein the aryl or heteroaryl group is fused to one or more cyclic hydrocarbon claim 1 , heterocyclic claim 1 , aryl or heteroaryl rings claim 1 , wherein —WRmay be optionally substituted.4. The compound of claim 1 , wherein:{'sup': 1', '1', '1', '1, 'RW— comprises a heteroaryl group, wherein RW— may be optionally substituted;'}{'sup': 1', '1, 'a nitrogen atom of RW— is linked to J; and'}{'sup': 2', '2', '2', '2, '—WRis an aryl or a heteroaryl group, wherein the aryl or the heteroaryl group is substituted at the α and α′ positions, wherein —WRmay optionally be further substituted.'}5. The compound of claim 1 , wherein RW— is RNH— or (R)N— wherein at least one Rcomprises a fused bicyclic group claim 1 , or two Rtogether with the nitrogen atom to which they are attached form a fused bicyclic group claim 1 , wherein RW— may be optionally substituted.8. The compound of claim 7 , wherein:{'sup': '1', 'sub': 1', '6, '(i) Ror A is selected from pyrazole, imidazole, triazole, tetrazole, pyrrole, morpholine, piperazine, 4-methyl piperazine, and fused bicyclics or tricyclics comprising a benzene ring fused with at least one 5-membered heterocycle, such as indole, each of which groups may be optionally substituted at a ring atom with a group selected from halo, isopropyl, morpholinyl, piperidinyl, and piperazinyl, each of which groups may themselves be optionally substituted with C-Calkyl; or'}{'sup': '1', 'sub': 1', '6, '(ii) Ror A is independently selected from pyrazole or triazole, optionally substituted at a ring atom ...

Odorless thiols for permanent waving, straightening and depilatory applications

Described herein is a chemical class of odorless thiols which can serve as reducing agents. This chemical class involves thiols which can be used as reducing agents for permanent styling treatments, depilatory compositions and other applications. The odorless thiols are thiols having a heterocyclic quaternary ammonium salt in their molecule.

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 2. The radionuclide complex of claim 1 , wherein L is OR.3. The radionuclide complex of claim 2 , wherein R is selected from Cto Calkyl claim 2 , Cto Cheteroalkyl claim 2 , Cto Calkene claim 2 , C2 to Cm alkyne and aryl claim 2 , each of which is optionally substituted.4. The radionuclide complex of claim 3 , wherein R is Cto Calkyl claim 3 , preferably Cto Calkyl claim 3 , more preferably methyl or ethyl claim 3 , even more preferably ethyl.5. The radionuclide complex of claim 1 , wherein the leaving group is selected from OCHCH claim 1 , O-p-toluenesulfonate claim 1 , O-methanesulfonate claim 1 , O-trifluoromethanesulfonate claim 1 , O-benzenesulfonate claim 1 , O-m-nitrobenzenesulfonate claim 1 , cyanate claim 1 , azide and halogen.6. The radionuclide complex of claim 1 , wherein the radionuclide is selected from radioisotopes of zirconium claim 1 , gallium claim 1 , lutetium claim 1 , holmium claim 1 , scandium claim 1 , titanium claim 1 , indium and niobium.7. The radionuclide complex of wherein the radionuclide is a radioisotope of zirconium claim 6 , gallium or indium.8. The radionuclide complex of claim 7 , wherein the radionuclide is a radioisotope of zirconium.9. The radionuclide complex of further conjugated to a target molecule to form a radionuclide-labelled conjugate.10. The radionuclide-labelled conjugate of claim 9 , wherein the target molecule is a polypeptide.11. The radionuclide-labelled complex of wherein the complex or conjugate has improved affinity when compared to with DFO-Ph-NCS or a conjugate of DFO-Ph-NCS and the target molecule.12. A method of imaging a patient claim 1 , the method including:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'administering to a patient the radionuclide-labelled conjugate of ; and'}imaging said patient.13. ...

COMPOSITIONS AND METHODS OF TREATMENT FOR NEUROLOGICAL DISORDERS COMPRISING A DEMENTIA

This invention, in at least some embodiments, relates to an inventive molecule, compositions comprising same, and methods of use thereof for treatment of a neurological disorder. 128-. (canceled)3022. The molecule of claim :{'sub': 1', '2, 'wherein for Family A, Ris nitrogen substituted benzyl or H, and Ris H.'}3122. The molecule of claim :wherein for Family A, the molecule is selected from the group consisting of A1-A3 of Appendix I (molecules having catalog numbers F228-0422, F228-0350 or F228-0534);wherein for Family I, the molecule is selected from the group consisting of I1-I5 and I7 of Appendix I (molecules having catalog numbers T636-1937, T636-1114, T636-2387, T636-0134, T636-1210 and T636-2425).3222. A pharmaceutical composition comprising the molecule of claim .3322. A method for treating a mammal in need of treatment thereof , comprising administering to the mammal an inventive molecule of claim , or a pharmaceutical composition comprising the same , for treatment of a neurological disease , wherein said neurological disease includes Alzheimer's disease , a subtype thereof or a related disease.3426. The method of claim , wherein said molecule is selected from the group consisting of:an inventive molecule selected from the group consisting of a molecule given in Appendix I, wherein said molecule is selected from the group consisting of catalogID numbers: T0502-5560; T0508-5190, T202-1455, T202-0973, K851-0113, T5630309, T5672380, T5967389, T5884038, T5231424, T0517-8250, T0511-9200 and T5627721;a molecule as shown in Table 1 herein; anda molecule given in Appendix II, wherein said molecule is selected from the group consisting of catalogID numbers: T6010789, T5993799, T5813085, T6947848, 10517-4117, T5729557, T5705522, Z606-8352, L115-0403, T5712071, T5790476, T5788339, G433-0293, T5719257, T5798761, T5821723, T5787526, T5827594, K405-2595, T5274959, M950-1515, T5450239, G508-0015, T5707230, T5710343, 887-0183, T5453923, 10505-4087, T5673322, T5800607, ...

N-[1-((6-CHLOROPYRIDIN-3-YL)METHYL)PYRIDIN-2(1H)-YLIDENE]-2,2,2- TRIFLUOROACETAMIDE FOR CONTROL OF AGRICULTURAL/HORTICULTURAL PESTS

A compound of formula (Ie′): 124-. (canceled)26. The amine derivative or salt thereof according to claim 25 , wherein Rin formula (Ie′) is a Calkyl group substituted with a halogen atom.27. The amine derivative or salt thereof according to claim 25 , wherein Y in formula (Ie′) is a hydrogen atom or a halogen atom.28. The amine derivative or salt thereof according to claim 25 , wherein Rin formula (Ie′) is a Calkyl group substituted with a halogen atom claim 25 , and Y is a hydrogen atom or a halogen atom.29. The amine derivative or salt thereof according to claim 25 , wherein the compound of formula (Ie′) is a compound selected from the group consisting of: N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[l-((6-chloro-5-fluoropyridin-3-yl)methyl)pyridin-2(1H)-ylidine]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-fluoropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-bromopyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-(1-(6-chloropyridin-3-yl)ethyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2-difluoroacetamide claim 25 , 2-chloro-N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2-difluoroacetamide claim 25 , N-[1-((2-chloropyrimidin-5-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , and N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,3 claim 25 ,3 claim 25 ,3-pentafluoropropanamide.30. The amine derivative or salt thereof according to claim 25 , which has a pest control activity against at least one type of pest selected from the group consisting of lepidopterous pests claim 25 , hemipterous pests claim 25 , thysanopterous pests claim 25 , dipterous pests claim 25 , ...

Noxious organism control agent

The present invention relates to amine derivatives each represented by chemical formula (I) (wherein Ar represents a phenyl group or the like; R 1 represents a hydrogen atom or the like; R 2 represents a C1-6 alkylcarbonyl group or the like; R 3 represents a C1-8 alkylene group or the like; and R 4 represents a hydrogen atom or the like) and a noxious organism control agent comprising at least one of the derivatives. It is found that the amine derivative has an excellent activity for use as a control agent of agricultural and horticultural pests.

3,4-disubstituted-phenylsulphonamides and their therapeutic use

3,4-Disubstituted benzenesulphonamides of general formula (i) in which R4 represents a 5-or 6-membered saturated or unsaturated carbocyclic or heterocyclic ring to which ring is fused an aryl, hetereoaryl, carbocyclic or heterocyclic ring, in which either or both rings may optionally be substituted, and the other substituents are as defined in Claim 1, have therapeutic utility via phosphodiesterase IV inhibition.

Cyclopropylamine derivatives useful as lsd1 inhibitors

The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.

Process for the preparation of hydrazine derivatives useful as intermediates for the preparation of peptide analogues

The invention relates to a novel process for the preparation of compounds of formula (I) wherein R1 is hydrogen or a suitable amino-protecting group, R2 is unsubstituted or substituted alkyl, R3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl, R4, independently of R1, is hydrogen or a suitable amino-protecting group and m is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds. The precursor is an oxo compound, which is in turn prepared by hydrogenation with a suitable complex hydride or with hydrogen in the presence of a suitable catalyst and acyl migration starting from a hydrazone, which is in turn preferably prepared from a nitrile via an imino compound by means of hydrogenation and reaction with a hydrazine derivative, which is prepared from an aldehyde by reaction with a reactive derivative of a carboxylic acid in the presence of a cyanide salt; and the novel intermediates required therefor.

有害生物防除剂

本发明涉及下述化学式（I）所示的胺衍生物（式中Ar表示苯基等，R 1 表示氢原子等，R 2 表示C1～6烷基羰基等，R 3 表示C1～8亚烷基等，R 4 表示氢原子等。）以及包含至少一种以上的该衍生物的有害生物防除剂。发现该胺衍生物作为对农业园艺上的害虫的防除剂而具有优异的活性。

Heterocyclic compound

FIELD: pharmaceutical industry.SUBSTANCE: invention relates to a compound of formula (I)where (1) ring A is represented by the formulawhere the combination of X1, X2and X3(X1, X2, X3) is (carbon atom, carbon atom, carbon atom) or (carbon atom, carbon atom, nitrogen atom); R1represents (1) a fluorine atom, a chlorine atom, a bromine atom, (2) methyl, trifluoromethyl, or (3) a hydroxy group substituted with methyl or trifluoromethyl; R2is (1) a halogen atom, (2) a cyano group, (3) a C1-6alkyl group optionally substituted with 1-3 substituents selected from a halogen atom and a hydroxy group, (4) a C1-6alkoxy group optionally substituted with 1-3 halogen atoms , or (5) a mono- or di-C1-6alkylamino group; and Ring B is optionally further substituted with 1-3 substituents selected from (1) a halogen atom, (2) a C1-6alkyl group optionally substituted with 1-3 hydroxy groups, and (3) a C1-6alkoxy group, or (2) Ring A is represented by the formulawhere the combination of X4and X5(X4, X5) is (carbon atom, carbon atom); ring C is optionally further substituted with 1 to 3 halogen atoms; ring D is a 5-7-membered aromatic heterocycle containing, as ring-forming atoms, in addition to carbon atoms, from 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, or a 5-7-membered non-aromatic heterocycle, containing, as ring-forming atoms, in addition to carbon atoms, from 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom; ring D is optionally further substituted with 1-3 substituents selected from (1) a halogen atom and (2) a hydroxy group; X6represents a hydrogen atom, a fluorine atom or a chlorine atom; X7represents a fluorine atom or a chlorine atom; the combination of X8and X9(X8, X9) is (carbon atom, nitrogen atom), (nitrogen atom, carbon atom) or (nitrogen atom, nitrogen atom); ring E is optionally further substituted with 1-3 substituents selected from (1) a C1-6alkyl group and (2) an amino group; and X10is an amino ...

Patent RU2019106484A3

`”ВУ“” 2019106484`” АЗ Дата публикации: 30.10.2020 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение ж 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2019106484/04(012543) 09.08.2017 РСТ/Р2017/028928 09.08.2017 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 2016-158038 10.08.2016 ]Р 2. 2017-016275 31.01.2017 ]Р Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ГЕТЕРОЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ Заявитель: ТАКЕДА ФАРМАСЬЮТИКАЛ КОМПАНИ ЛИМИТЕД, /]Р 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. п см. Примечания [ ] приняты во внимание следующие пункты: р [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) (070 213/42 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07О 213/42,С07О 213/65, С07Р 213/68, С07Ь 213/73, СО7О 213/75, СО7Р 239/20,С07Б 253/06, С07Р 401/12 , Аб1К 31/437, Аб1К 31/4375, Аб1К 31/44, Аб1ТК 31/4406,Аб1К 31/444, Аб1К 31/4965, Аб1К 31/495, Аб1К 31/497, Аб1К 31/505, Аб1К 31/53, Аб1К 31/53, Аб1Р 35/00 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, ...

Human T2R bitterness receptors and uses thereof

본 발명은, T2R 미각 수용체 패밀리 중 특정 인간 미각 수용체가 예를 들어 커피에 존재하는 특정 쓴맛 화합물에 반응한다는 발견에 관한 것이다. 또한, 본 발명은, 쓴맛 차단제로서 기능을 하는 특정 화합물 및 조성물, 및 예를 들어 커피와 커피맛 식품, 음료 및 의약에서 쓴맛 차단제 또는 풍미 조절제로서의 이의 용도의 발견에 관한 것이다. 또한, 본 발명은 수많은 상이한 인간 T2R에 길항작용을 하는 화합물, 및 분석에서 및 인간 및 동물이 섭취하는 조성물 중 쓴맛 차단제로서의 이의 용도의 발견에 관한 것이다. The present invention relates to the discovery that certain human taste receptors in the T2R taste receptor family respond to certain bitter compounds, for example, present in coffee. The present invention also relates to the discovery of certain compounds and compositions which function as bitter taste blockers and their use as bitter taste blockers or flavor control agents, for example in coffee and coffee flavored foods, drinks and medicines. The invention also relates to compounds which antagonize a number of different human T2Rs and their use in the analysis and in the compositions ingested by humans and animals as bitter taste blockers.

Ингибиторы репликации вируса иммунодефицита человека

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 138 972 A (51) МПК A61K 31/381 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017138972, 22.04.2016 (71) Заявитель(и): ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД (GB) Приоритет(ы): (30) Конвенционный приоритет: 23.04.2015 US 62/151,780 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 23.11.2017 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2016/172424 (27.10.2016) R U (54) Ингибиторы репликации вируса иммунодефицита человека (57) Формула изобретения 1. Соединение формулы I, включая его фармацевтически приемлемые соли: где: каждый из R1a и R1b независимо выбран из водорода, алкила, арила, арилалкила, арилоксиарила, циклоалкила, гетероциклила, гетероциклилалкила и -алкилСО(Rx); где указанный гетероциклил связан с родительской молекулой через атом углерода, и более того где указанные группы R1a и R1b замещены 0-4 группами, независимо выбранными из алкенила, алкокси, алкоксикарбонила, алкила, алкилтиокси, бензилокси, алкинила, Стр.: 1 A 2 0 1 7 1 3 8 9 7 2 A Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ" 2 0 1 7 1 3 8 9 7 2 US 2016/028762 (22.04.2016) R U (43) Дата публикации заявки: 23.05.2019 Бюл. № 15 (72) Автор(ы): БЕНДЕР Джон А. (US), ДЖЕНТЛЗ Роберт Дж. (US), ПЕНДРИ Аннапурна (US), ВАН Алан Сяндун (US), МИНВЭЛЛ Николас А. (US), БЕНО Бретт Р. (US), ФРАЙДЕЛЛ Роберт А. (US), БЕЛЕМА Маконен (US), НГУЕН Ван Н. (US), ЯН Чжун (US), ВАН Гань (US), КУМАРАВЕЛ Селвакумар (IN), ТАНГАТИРУПАТИ Сринивасан (IN), БОРА Раджеш Онкардас (IN), ХОЛЕХАТТИ Шилпа Махешвараппа (IN), МЕТТУ Малликарджуна Рао (IN), ПАНДА Маноранджан (IN) арила, арилалкила, арилокси, карбоновой кислоты, циано, циклоалкила, галогена, галогеналкила, галогеналкокси, гетероциклила, гетероциклилалкила, гидрокси, гидроксиалкила, тиокси, групп -CH2NH2, -алкил-гетероарил, -СО-алкил, CO(Rx), -CON(Ry)2, -NHCON(Ry)2, -NHCO-алкил, -NHСО2алкил, -NHSO2-алкил, -ОСН2-арил, -SO2-алкил, -SO2-N(Ry)2 и - ...

옥심 치환 아미드 화합물 및 유해 생물 방제제

신규 유해 생물 방제제, 특히 살균제 및 살선충제를 제공한다. [식 중, G 1 은 G 1 -1 등으로 나타내는 구조를 나타내고, G 2 는 G 2 -2 등으로 나타내는 구조를 나타내고, W 는 산소 원자 등을 나타내고, X 1 은 할로겐 원자, 메틸, 트리플루오로메틸 등을 나타내고, X 2 , X 3 , X 4 및 X 5 는 각각 독립적으로 수소 원자, 할로겐 원자 등을 나타내고, Y 1 및 Y 3 은 각각 독립적으로 할로겐 원자, 시아노, 메틸, 트리플루오로메틸, C 2 ∼ C 6 알키닐 등을 나타내고, Y 2 및 Y 4 는 각각 독립적으로 수소 원자, 할로겐 원자 등을 나타내고, R 1 은 C 1 ∼ C 6 알킬, C 1 ∼ C 4 할로알킬, R 18 에 의해 치환된 (C 1 ∼ C 4 )알킬, C 3 ∼ C 6 시클로알킬, C 3 ∼ C 6 알케닐 등을 나타내고, R 2 및 R 3 은 각각 독립적으로 수소 원자, 메틸 등을 나타내고, R 4 는 수소 원자 등을 나타내고, R 18 은 C 3 ∼ C 6 시클로알킬, 페닐, (Z) m 에 의해 치환된 페닐 등을 나타내고, Z 는 할로겐 원자 등을 나타내고, m 은 1, 2 또는 3 의 정수를 나타낸다.] 로 나타내는 옥심 치환 아미드 화합물 또는 그 염, 및 그들을 함유하는 유해 생물 방제제.

Pest control agent

Dpp-iv inhibitors

FIELD: chemistry, pharmaceutics. SUBSTANCE: claimed invention relates to novel compounds of general formula (I) Z-C(R 1 R 2 )-C(R 3 NH 2 )-C(R 4 R 5 )-X-N(R 6 R 7 ) (I), or its pharmaceutically acceptable salt which is different because Z represents phenyl; where Z can be substituted with one or more R 8 , where R 8 represents halogen; R 1 , R 4 represent H; R 2 , R 5 represent H; R 3 represents H; X is selected from group consisting of S(O) 2 and C(O); R 6 , R 7 are independently selected from group consisting of H, (C(R 29 R 30 )) m -X 1 -Z 1 and (C(R 31 R 32 )) n -X 2 -X 3 -Z 2 and C 1-4 alkyl, which carries substitution with one or more R 29a , where R 29a is independently selected from group consisting of R 29b and Z 1 , on condition that R 6 and R 7 are selected in such way that R 6 and R 7 were not simultaneously independently selected from group consisting of H, CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 and CH(CH 3 ) 2 ; R 29 R 29b , R 30 , R 31 , R 32 are independently selected from group consisting of H, C 1-6 alkyl and N(R 32a )-C 1-6 alkyl; R 32a represents C 1-6 alkyl; m is 0, 1 or 2; n is 2; X 1 is independently selected from group consisting of covalent bond, -C 1-6 alkyl and -C 1-6 alkyl-N(R 33 )-; X 2 represents -N(R 35 )-; X 3 represents -C(O)-; R 33 represents C 1-6 alkyl; R 35 represents H; Z 1 , Z 2 are independently selected from group consisting of Z 3 and -C(R 37a )Z 3a Z 3b ; R 37a represents H; Z 3 , Z 3a , Z 3b are independently selected from group consisting of T 1 , T 2 , C 1-6 alkyl, C 1-6 alkyl-T 1 and C 1-6 alkyl-T 2 ; T 1 represents phenyl; where T 1 is optionally substituted with one or more R 38 ; R 38 being independently selected from group consisting of halogen, CN, R 39 , C(O)NH 2 , S(O) 2 NH 2 , OT 3 , C(O)N(R 40 )T 3 and T 3 , T 2 is selected from group consisting of C 3-7 cycloalkyl, indanyl, tetralinyl, heterocycle and heterobicycle, T 2 optionally carries substitution with one or more R 41 , where R 41 is independently selected ...

Производные бензолсульфонамида в качестве модуляторов rorc

1. Соединение формулы 1или его фармацевтически приемлемые соли,где А представляет собой группу формулы (а); (b); (с) или (d)В представляет собой группу формулы (е); (f); (g) или (h)C представляет собой группу формулы (i); (j); (k) или (m)m представляет собой 0 или 1;n находится в интервале от 0 до 3;p находится в интервале от 0 до 2;q находится в интервале от 0 до 3;r находится в интервале от 0 до 3;s находится в интервале от 0 до 2;t представляет собой 0 или 1;u находится в интервале от 0 до 3;Rпредставляет собой водород или Салкил;Rпредставляет собой водород или Cалкил;Rпредставляет собой Салкил; Сциклоалкил; Сциклоалкил-Cалкил; гетероциклил; гетероциклил-Салкил; фенил-Салкил или Cалкилсульфонил, где каждая из групп Салкил, Сциклоалкил, Сциклоалкил-Салкил и фенил-Салкил может независимо один или больше раз быть замещена атомом галогена;Rпредставляет собой водород или Cалкил;Rпредставляет собой водород или Cалкил;Rпредставляет собой циано; -(CH)-NRR; -(CH)-S(O)-R; -(CH)-C(O)-NRR;-(CH)-S(O)-NRR; -(CH)-NR-C(O)-R; -(CH)-NR-C(O)-NRRили -(CH)-NR-S(O)-R,где v представляет собой 0 или 1,w находится в интервале от 0 до 2;каждая из групп Rи Rнезависимо представляет собой водород или Cалкил;Rпредставляет собой Салкил; Сциклоалкил или Сциклоалкил-Салкил; иRпредставляет собой водород или Салкил;каждая группа Rнезависимо представляет собой Cалкил; гало; Cалкокси; циано; гало-Салкил; гидрокси-Салкил; гало-Салкокси или Cалкилсульфонил;Rпредставляет собой Cалкил; Сциклоалкил или Сциклоалкил-Cалкил;Rпредставляет собой водород или Cалкил;Rпредставляет собой водород или Салкил;Rпредставляет собой водород; гидрокси; циано; -(CH)-NRR; -(СН)-S(O)-R; -(CH)-C(O)-NRR; -(CH)-S(O)-NRR; -(CH)-NR-C(O)-R; -(CH)-NR-C(O)-NRRили -(CH)-NR-S(O)-R;каждая группа Rнезависимо представляет собой Cалкил; гало; Cалкокси; циано; гало-Салкил; гало-Салкокси или Салкилсульфонил;каждая группа Rнезависимо представляет собой Cалкил; гало; Cалкокси; циано; га РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК A61K 31/18 ( ...

헤테로고리 화합물

GCN2 억제 작용을 가질 수 있고, 암 등의 GCN2 관련 질환의 예방 또는 치료에 유용할 것으로 기대되는 헤테로고리 화합물이 제공된다. 하기 화학식 (I)으로 표현되는 화합물: 여기에서, 각각의 기호는 본 명세서에 기재된 바와 같거나, 이들의 염이다.

인간 면역결핍 바이러스 복제 억제제

약제학적으로 허용되는 염을 포함하는, 하기 화학식(I)의 화합물, 및 인간 면역결핍 바이러스 (HIV) 감염증을 치료하기 위한 조성물 및 방법이 기술된다:

Oxime-substituted amide compound and pest control agent

신규 유해 생물 방제제, 특히 살균제 및 살선충제를 제공한다. [식 중, G 1 은 G 1 -1 등으로 나타내는 구조를 나타내고, G 2 는 G 2 -2 등으로 나타내는 구조를 나타내고, W 는 산소 원자 등을 나타내고, X 1 은 할로겐 원자, 메틸, 트리플루오로메틸 등을 나타내고, X 2 , X 3 , X 4 및 X 5 는 각각 독립적으로 수소 원자, 할로겐 원자 등을 나타내고, Y 1 및 Y 3 은 각각 독립적으로 할로겐 원자, 시아노, 메틸, 트리플루오로메틸, C 2 ∼ C 6 알키닐 등을 나타내고, Y 2 및 Y 4 는 각각 독립적으로 수소 원자, 할로겐 원자 등을 나타내고, R 1 은 C 1 ∼ C 6 알킬, C 1 ∼ C 4 할로알킬, R 18 에 의해 치환된 (C 1 ∼ C 4 )알킬, C 3 ∼ C 6 시클로알킬, C 3 ∼ C 6 알케닐 등을 나타내고, R 2 및 R 3 은 각각 독립적으로 수소 원자, 메틸 등을 나타내고, R 4 는 수소 원자 등을 나타내고, R 18 은 C 3 ∼ C 6 시클로알킬, 페닐, (Z) m 에 의해 치환된 페닐 등을 나타내고, Z 는 할로겐 원자 등을 나타내고, m 은 1, 2 또는 3 의 정수를 나타낸다.] 로 나타내는 옥심 치환 아미드 화합물 또는 그 염, 및 그들을 함유하는 유해 생물 방제제. New pesticides, especially fungicides and nematocides. [Wherein, G 1 represents a structure represented by such as G 1 -1, G 2 represents a structure represented by G, such as 2 -2, W represents an, oxygen atom, X 1 represents a halogen atom, methyl, tri represents methyl such as fluoro, X 2, X 3, X 4 and X 5 each independently represent a hydrogen atom, a halogen atom, Y 1 And Y 3 each independently represents a halogen atom, cyano, methyl, trifluoromethyl, C 2 -C 6 alkynyl, etc. Y 2 and Y 4 each independently represent a hydrogen atom, a halogen atom, etc., and R 1 represents C 1 -C 6 alkyl, C 1 -C 4 haloalkyl, (C 1 -C 4 ) alkyl substituted by R 18 , C 3 -C 6 cycloalkyl, C 3 -C 6 alkenyl, and the like , R 2 and R 3 are each independently a hydrogen atom or a methyl group, R 4 is a hydrogen atom or the like, R 18 is C 3 -C 6 cycloalkyl, phenyl, phenyl substituted with (Z) m , , Z represents a halogen atom or the like, and m represents an integer of 1, 2 or 3]. Water or a salt thereof, and a pesticide containing them.

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Compounds inhibiting (blocking) bitter taste, methods for use and production thereof

FIELD: chemistry.SUBSTANCE: invention relates to a compound of general formula(I) or pharmaceutically acceptable salts thereof, where Alk is an C-Calkyl group; G is C=O and Q is CRRor NR, where Rand R, being identical or different, independently denote H, C-Calkyl, optionally substituted with a substitute selected from a group comprising carboxy, phenoxy, benzyloxy, C-Calkoxy or hydroxy; C-CcycloalkylC-Calkyl; phenylC-Calkyl, optionally substituted with a halogen; phenylamidoC-Calkyl; phenylC-CalkylamidoC-Calkyl, optionally substituted with a C-Calkoxy group; or Rand R, together with a carbon atom with which they are bonded form a C=O or C-Calkenyl group, optionally substituted with a phenyl; Mis CR, where Ris H; Mis CR, where Ris H; Ris H, C-Calkyl, substituted with a phenoxy group; C-CcycloalkylC-Calkyl; arylC-Calkyl, optionally substituted with 1 or 2 substitutes selected from a group comprising C-Calkyl, C-Calkoxy, C-Calkoxycarbonyl, carboxyl, N-methylamido, hydroxy, C-CalkoxyC-Calkoxy, C-Calkylthio, C-Calkylsulphanyl, cyano, halogen, perfluoroC-Calkyl, nitro, formyl, hydroxyC-Calkyl and amino, wherein the aryl moiety is a phenyl or naphthyl; and heteroarylC-Calkyl, where the heteroaryl moiety is pyridinyl, optionally substituted with 1 or 2 groups selected from C-Calkoxy or hydroxyC-Calkyl, pyrazolyl or isoxazolyl, substitute with 1 or 2 C-Calkyl groups; Rand Ris C-Calkyl. The invention also relates to specific compounds, a method of reducing or weakening bitter taste, a composition of a food/non-food product or beverage or drug for reducing or lightening bitter taste and a method of producing a compound of formula (I).EFFECT: obtaining novel compounds which are useful as bitter taste inhibitors or taste modulators.37 cl, 6 dwg, 12 tbl, 186 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 413/06 C07D 413/14 C07D 407/14 C07D 409/14 C07D 417/14 C07C 311/16 ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 311/12 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C 311/15 C07C 335/12 C07D 213/36 (12) ...

Nitrogen heteroaromatic containing azobenzene compound and composition for green hologram recording comprising thereof

본 발명은 함질소 헤테로방향족 포함 아조벤젠 화합물, 이를 포함하는 홀로그램 기록용 조성물, 홀로그램 기록용 매체, 이를 사용한 홀로그램 기록 재료 및 홀로그램 기록 또는 재기록 방법에 관한 것으로써, 본 발명의 아조벤젠 단량체 화합물은 녹색 파장에서 등흡수점이 존재하고 이로부터 광 이성질화가 일어나며, 적은 양의 광조사에 의해서도 굴절율 변화를 크게 할 수 있는 고복굴절율 부분을 포함하고 있어 아조벤젠 단량체 화합물을 포함하는 고분자는 녹색 레이저 조사에 의한 홀로그램 기록/재기록 소재로 유용하게 사용될 수 있다. The present invention relates to a nitrogen-containing heteroaromatic-containing azobenzene compound, a hologram recording composition comprising the same, a hologram recording medium, a hologram recording material using the same, and a hologram recording or rewriting method, wherein the azobenzene monomer compound of the present invention is produced at a green wavelength There is an isosorption point and photoisomerization occurs therefrom, and it contains a high birefringence part that can increase the refractive index change even with a small amount of light irradiation. It can be usefully used as a rewritable material.

Azapeptide derivatives

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to novel derivatives of atazanavir sulfate - HIV protease inhibitor. EFFECT: invention also relates to pharmaceutical compositions which possess antiviral activity with respect to HIV. 19 cl, 5 dwg, 11 tbl, 20 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 448 958 (13) C2 (51) МПК ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ C07D C07F C07K A61K A61K A61K A61P 213/42 (2006.01) 9/58 (2006.01) 5/10 (2006.01) 31/4418 (2006.01) 31/675 (2006.01) 38/07 (2006.01) 31/18 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010100821/04, 12.06.2008 (24) Дата начала отсчета срока действия патента: 12.06.2008 (72) Автор(ы): ХАРБЕСОН Скотт Л. (US), ТУНГ Роджер Д. (US) R U (73) Патентообладатель(и): КОНСЕРТ ФАРМАСЬЮТИКАЛЗ, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: 12.06.2007 US 60/934,201 29.02.2008 US 61/067,627 (43) Дата публикации заявки: 20.07.2011 Бюл. № 20 2 4 4 8 9 5 8 2 4 4 8 9 5 8 R U (56) Список документов, цитированных в отчете о поиске: RU 2004106787 A, 10.12.2004. WO 2006014282 A2, 09.02.2006. XU ZHONGMIN et al. "Process Research and Development for an Efficient Synthesis of the HIV Protease Inhibitor BMS-232632" ORGANIC PROCESS RESEARCH AND DEVELOPMENT, 2002, vol.6, no.3, 2002, pages 323-328. ZHANG HUIPING et al. "A facile and efficient synthesis of d3-labelled Reyataz" JOURNAL (см. прод.) C 2 C 2 (45) Опубликовано: 27.04.2012 Бюл. № 12 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 12.01.2010 (86) Заявка PCT: US 2008/007331 (12.06.2008) (87) Публикация заявки РСТ: WO 2008/156632 (24.12.2008) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной (54) ПРОИЗВОДНЫЕ АЗАПЕПТИДОВ (57) Реферат: Изобретение относится к новым производным сульфата атазанавира ингибитора ВИЧ протеазы. Данное изобретение также относится к фармацевтическим композициям, обладающим противовирусной активностью в отношении ...

Preparation method and application of metal organic cage-shaped compound for preparing aniline by catalytic reduction of nitrobenzene

本发明涉及精细化工技术领域，一种用于催化还原硝基苯制苯胺的金属有机笼状化合物的制备方法及其应用，其中制备方法，是以过渡金属盐中的Co 2+ 作为节点，以L作为配体反应制得金属有机笼状化合物，其合成路线如下：Co 2+ +L→Co‑L；所述配体L选自H 4 TPO，所述过渡金属盐选自高氯酸钴、硝酸钴、四氟硼酸钴或三氟甲磺酸钴中的一种；采用本发明方法制备的金属有机笼状化合物原料价格低廉，产率高，得到的化合物化学性质稳定，易于投入实际应用中，作为一种催化剂在光照条件下还原硝基苯的轮转次数可以达到200000。

Compounds that inhibit (block) bitter taste in compositions and use thereof

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

2-cyanobenzene sulfonamides as pesticides

2-Cyanobenzene sulfonamide compounds (I) and their N-oxides or salts, are new. 2-Cyanobenzene sulfonamide compounds of formula (I) and their N-oxides or salts, are new. A : e.g. 1-6C-alkandiyl, 3-6C-cycloalkyldiyl or 2-6C-alkendiyl; B 1>e.g. (het)aryl, 1-6C-arylalkyl or 1-6C-hetarylalkyl; Q : optionally saturated 5-7-membered heterocyclic ring or 9-10-membered annelated heterobicyclic ring system; R 1>e.g. H, halo, 1-6C-alkyl or 1-6C-haloalkyl; and R 2>-R 4>e.g. (het)aryl, H, halo, CN or NO 2. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. [Image] ACTIVITY : Pesticide; Fungicide; Insecticide; Agaracide; Anthelmintic; Nematocide; Herbicide; Plant Growth Regulant; Antimicrobial; Antibacterial; Virucide; Arthropodicide. MECHANISM OF ACTION : None given.

Pesticidal methods using heterocyclic compounds and derivatives for combating animal pests

The present invention relates to pesticidal methods for the use and application of substituted heterocyclic compounds of formula (I) and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal heterocyclic compounds of formula (I) or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The heterocyclic compounds of the present invention are defined by the following general formula (I) wherein X, T, R 1 , R 2 , R 3 and Het are defined as in the description.

Alpha unsaturated amines, their production and use.

Novel triazolinthione derivatives

The present invention relates to novel triazolinthione derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.

SELECTIVE HYDROXAMATE INHIBITORS MMP

1. Соединение формулы (I): ! ! где R1 представляет собой циано, (С1-С7)алкил, амино, R4-O-, (С1-С7)алкил-NHC(O)-, R5-C(O)NH-, R6C(O)-, R9-C(O)-O- или R10-O-C(O)-, где ! R4, R6, R9 и R10 независимо представляют собой водород, (С1-С7)алкил, моно- или ди-(С1-С7)алкиламино или арил, каждый из которых необязательно замещен от одного до пяти раз заместителями, выбранными из группы, состоящей из (С1-С7) алкила, галогена, гидроксила, (С1-С7) алкокси и арила; ! R5 представляет собой водород, (С1-С7)алкил, (R7)(R8)N- или (С1-С7) алкокси; ! R7 и R8 независимо представляют собой водород, (С1-С7)алкил или арил-(С1-С7)алкил; ! R2 представляет собой водород или (С1-С7)алкил, который необязательно замещен от одного до трех раз заместителями, выбранными из группы, состоящей из (С1-С7)алкила, гидрокси, арила, гетероциклила, гетероарила, (С1-С7)алкил-O-С(O)-, ди-(С1-С7)алкиламино-С(O)-, где каждый арил, гетероциклил и гетероарил далее необязательно замещен (С1-С7)алкилом; или ! R3 представляет собой (С1-С7)алкил или циклоалкил; ! его фармацевтически приемлемая соль; или его оптический изомер; или смесь оптических изомеров. ! 2. Соединение по п.1, где ! R1 представляет собой (С1-С7) алкил, R4-O-, R5-C(O)NH- или R9-C(O)-O-, где R4 представляет собой (С1-С7) алкил, необязательно замещенный от одного до трех раз галогеном, R5 представляет собой водород, (С1-С7) алкокси или моно-(С1-С7)-алкиламино, и R9 представляет собой моно-(С1-С7)-алкиламино; ! R2 представляет собой (С1-С7) алкил, необязательно замещенный (С1-С7)алкил-О-С(О)-, ди-(С1-С7)алкиламино или гидрокси; или ! R2 представляет собой арил-(С1-С7)алкил-, гетероарил-(С1-С7)алкил-, гетероциклил-(С1-С7)алкил, где указанный гетероциклил необязательно замещен (С1-С7)алкилом; и ! R3 представляет собой (С1-С7) алкил; ! или его фармаце (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2008 142 598 (13) A (51) МПК C07C 311/19 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) ...

Nitrogen-containing heterocyclic derivatives, pharmaceutical composition based on thereof and anticancer agent

Изобретение относится к азотсодержащим гетероциклическим производным формулы (I) A-B-D-E (I), где А означает 5- или 6-членный гетероарил, содержащий в цикле один или два атома азота; В означает этенилен; D означает фенилен; Е означает группу -N(COR)-SO 2 -G, где G означает фенил; R означает 5- или 6-членный гетероарил или гетероарилметил, содержащие в цикле один или два атома азота, или группу -(CH 2 ) n -N(R 5 )R 6 , где n означает целое число от 1 до 5; R 5 и R 6 одинаковые или разные: водород, С 1 -С 6 алкил, гидроксиалкил, аминоалкил, или R 5 и R 6 вместе с атомом азота могут образовывать 5-7-членную циклическую аминогруппу – N(R 5 )R 6 , которая кроме атома азота может включать атом кислорода, серы или азота в качестве образующего цикл члена, или их N-оксидам. Соединения формулы (I) обладают противораковой активностью и могут найти применение в медицине. 3 с. и 7 з.п. ф-лы, 1 табл. ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) (13) 2 248 969 C2 C 07 D 213/38, 213/89, 401/12, 401/14, 403/12, 403/14, 413/12, A 61 K 31/44, 31/4439, 31/444, 31/4545, 31/496, 31/5377, ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) A 61 P 35/00 ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2002118708/04, 13.12.2000 (24) Äàòà íà÷àëà äåéñòâè ïàòåíòà: 13.12.2000 (72) Àâòîð(û): ÑÓÇÓÊÈ Òîñèþêè (JP), ÀÎÊÈ Òîìèåñè (JP) (30) Ïðèîðèòåò: 14.12.1999 JP 11/354101 04.07.2000 JP 2000/202393 (73) Ïàòåíòîîáëàäàòåëü(ëè): ÍÈÏÏÎÍ ÑÈÍßÊÓ ÊÎ., ËÒÄ. (JP) R U (43) Äàòà ïóáëèêàöèè çà âêè: 10.04.2004 (45) Îïóáëèêîâàíî: 27.03.2005 Áþë. ¹ 9 2 2 4 8 9 6 9 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: RU 2021989 C1, 30.10.1994. WO 95/27699 A1, 19.10.1995. US 5529999 A, 25.06.1996. US 5721246 A, 24.02.1998. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 15.07.2002 2 2 4 8 9 6 9 R U (87) Ïóáëèêàöè PCT: WO 01/44195 (21.06.2001) C 2 C 2 (86) Çà âêà PCT: JP 00/08781 (13.12.2000) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà ...

Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK

This invention concerns N—(2-arylamino) aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

Arylsulfonamido-substituted hydroxamic acids

Compounds of formula I wherein R, R₁, R₂ and Ar are as defined in the description, have valuable pharmaceutical properties and are effective especially as matrix metalloproteinase inhibitors, for example for the treatment of arthritis. They are prepared in a manner known per se.

Derivatives of N-(arylamino)sulfonamides as inhibitors of MEK

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

Hydroxamic acid derivative and mmp inhibitor containing the same as active ingredient

Arylsulfonamido-substituted hydroxamic acids

The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.

Process employing controlled crystallization in forming crystals of a pharmaceutical

A process is provided which employs reactive controlled crystallization to produce drug substance having desirable crystal properties which process involves providing reactants A and B in liquid or solution form and adding reactant B to reactant A using a cubic or incremental addition technique to control extent of reaction and thus crystallization kinetics, including supersaturation and nucleation, to produce crystals of drug substance which are generally larger, better quality and with few fines and narrow particle size distribution than normally obtainable employing prior art crystallization techniques. In addition, crystals of drug substance produced by the above process is also provided.

Sulfonamide-substituted 5-membered fused ring compounds, their use as pharmaceuticals and pharmaceutical formulations containing them

method for production of polyguanidines

a invenção se relaciona a um método para preparação de produtos de policondensação de guanidina, aminoguanidina ou diaminoguanidina g com um ou mais derivados de benzil ou alil ba de acordo com o seguinte esquema de reação no qual cada x representa independentemente um grupo de partida; cada r1 representa independentemente, ou um sistema de anel aromático com pelo menos um anel aromático, opcionalmente contendo um ou mais hetero átomos selecionados de o, n e s e, opcionalmente, sendo substituído com um ou dois grupos vinil aos quais o(s) grupo(s) -ch2-x é/são ligado(s), ou representa etileno; gua representa uma guanidindiil, aminoguanidindiil ou resíduo de diaminoguanidindiil; y representa h-gua, e z representa h; ou y e z juntos representam uma ligação química para obter uma estrutura cíclica; no qual pelo menos um derivado de benzil ou alil ba é submetido a uma reação de policondensação com guanidina excessiva, aminoguanidina ou diaminoguanidina g após eliminação de hx.

Phytopathogenic fungicide, derivative of 2-pyridylmethylamine, fungicide composition, method for control of phytopathogenic fungi

FIELD: organic chemistry, fungicides. SUBSTANCE: invention describes fungicide comprising compound of the formula (I): wherein A 1 means 2-pyridyl with up to 2 substituents that can be similar or different and taken among halogen atom, alkyl consisting of 1-5 carbon atoms and substituted with halogen atom, group -OSO 2 R 5a wherein R 5a is alkyl consisting of 1-5 carbon atoms, cyano-group, -COOR 5a ; A means phenyl optionally substituted with up to 5 similar or different substituents taken among the group including halogen atom, cyano-, hydroxy-, nitro-group, radicals E, OE, SE wherein E is alkyl consisting of 1-5 carbon atoms, phenyl or pyrrolyl being each among them can be substituted with halogen atom or cyano-group, 2-phthalimido- group, n-COOR 5a , amino-group substituted with two alkyl groups consisting of 1-5 carbon atoms; L means groups comprising -(C=O)-, -(C= S)-, -(SO 2 )-; R 1 means hydrogen atom, alkyl consisting of 1-5 carbon atoms optionally substituted with cyano-group or phenyl, -COOR 5a ; R 2 means hydrogen atom, alkyl consisting of 1-5 carbon atoms, or its salt. Invention describes derivative of 2-pyridylmethylamine of the formula (I) or its salt wherein R 1 and R 2 mean hydrogen atom; A 1 , A 2 , L have values indicated above; fungicide composition and method for control of phytopathogenic fungi using above indicated compounds. Invention provides high fungicide activity of claimed compounds. EFFECT: enhanced fungicide activity of compounds. 4 cl, 4 tbl, 8 ex ЭДС сс ПЧ сэ (19) РОССИЙСКОЕ — АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ ФЕДЕРАЦИИ ВЦ 2 224 746 (51) МПК? (13) С2 213/85, 401/12, А 01 М 43/40 К ПАТЕНТУ РОССИЙСКОЙ С 070 213/26, 213/61, 213/65, (21), (22) Заявка: 2000124062104 , 16.02.1999 (24) Дата начала действия патента: 16.02.1999 (30) Приоритет: 19.02.1998 СВ — 9803413.5 30.06.1998 СВ —9813998.3 11.08.1998 СВ —9817353.7 (43) Дата публикации заявки: 27.08.2002 (46) Дата публикации: 27.02.2004 (56) Ссылки: $У 1316557 ...

Process for preparation of new amine-derivatives

Amide derivatives

Selective inhibitors interfering with fibroblast growth factor receptor and frs2 interaction for the prevention and treatment of cancer

The invention relates to medicine and includes the use of inhibitors which selectively interfere with the interaction between a fibroblast growth factor receptor and FRS2, and with the interaction with other components of the FRS2 complex. Use of the selective inhibitors described in the present invention leads to a proven increase in anti-tumor efficacy relative to other inhibitors and monoclonal antibodies, a decrease in the toxicity of treatment, and the possibility of achieving complete blockage using a low agent concentration and of conducting long-term treatment. The advantage of the invention includes the development of a novel class of medicinal agents for treating malignant neoplasms and other diseases.

Method for producing polyguanidine

2-pyridinylethylbenzamide derivatives

一种通式(I)的化合物。一种制备该化合物的方法。一种包含通式(I)的化合物的杀真菌组合物。一种通过施用通式(I)的化合物或包含该化合物的组合物来治疗植物的方法。

Alpha-unsaturated amines, their production and use

本发明是关于式I化合物及其盐中的新化合物及其制法；这些化合物在农业上有杀虫/杀螨作用。式I中X 1 、X 2 中一个是吸电基团，另一个是H或吸电基团；R 1 为通过N相连的基团；R 2 为H或通过C、N或O相连的基团；n为0，1或2；A为杂环或环烃基。这些化合物的制法例如有使式II化合物与Y-W 2 反应等等，其中当W 1 为基团(1)时，W 2 为R 1 ，而当W 1 为R 1 时，W 2 为基团(1)。

Novel imaging composition and uses thereof

Sulfamoylbenzamide derivatives as antiviral agents against hbv infection

本发明涉及一种药物组合物，包括用作前基因组RNA衣壳化抑制剂的氨磺酰苯甲酰胺衍生物，用于治疗乙型肝炎病毒（HBV）感染。