ES2907461T3 - Compuestos antihelmínticos, composiciones y procedimientos de uso de los mismos - Google Patents
Compuestos antihelmínticos, composiciones y procedimientos de uso de los mismos Download PDFInfo
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- ES2907461T3 ES2907461T3 ES16702865T ES16702865T ES2907461T3 ES 2907461 T3 ES2907461 T3 ES 2907461T3 ES 16702865 T ES16702865 T ES 16702865T ES 16702865 T ES16702865 T ES 16702865T ES 2907461 T3 ES2907461 T3 ES 2907461T3
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- diyl
- alkyl
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- compounds
- amino
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 259
- 239000000203 mixture Substances 0.000 title claims description 158
- 230000000507 anthelmentic effect Effects 0.000 title claims description 101
- 238000000034 method Methods 0.000 title description 26
- 150000003839 salts Chemical class 0.000 claims abstract description 20
- 241001465754 Metazoa Species 0.000 claims description 61
- 206010061217 Infestation Diseases 0.000 claims description 23
- 238000011282 treatment Methods 0.000 claims description 12
- 208000030852 Parasitic disease Diseases 0.000 claims description 11
- 239000003096 antiparasitic agent Substances 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 8
- 229940125687 antiparasitic agent Drugs 0.000 claims description 4
- IUSARDYWEPUTPN-OZBXUNDUSA-N (2r)-n-[(2s,3r)-4-[[(4s)-6-(2,2-dimethylpropyl)spiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-3-hydroxy-1-[3-(1,3-thiazol-2-yl)phenyl]butan-2-yl]-2-methoxypropanamide Chemical compound C([C@H](NC(=O)[C@@H](C)OC)[C@H](O)CN[C@@H]1C2=CC(CC(C)(C)C)=CN=C2OC2(CCC2)C1)C(C=1)=CC=CC=1C1=NC=CS1 IUSARDYWEPUTPN-OZBXUNDUSA-N 0.000 claims description 2
- 229940125807 compound 37 Drugs 0.000 claims description 2
- ABJSOROVZZKJGI-OCYUSGCXSA-N (1r,2r,4r)-2-(4-bromophenyl)-n-[(4-chlorophenyl)-(2-fluoropyridin-4-yl)methyl]-4-morpholin-4-ylcyclohexane-1-carboxamide Chemical compound C1=NC(F)=CC(C(NC(=O)[C@H]2[C@@H](C[C@@H](CC2)N2CCOCC2)C=2C=CC(Br)=CC=2)C=2C=CC(Cl)=CC=2)=C1 ABJSOROVZZKJGI-OCYUSGCXSA-N 0.000 claims 1
- GLGNXYJARSMNGJ-VKTIVEEGSA-N (1s,2s,3r,4r)-3-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3h-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound CCN1C(=O)CCCC2=C(OC)C(NC=3N=C(C(=CN=3)Cl)N[C@H]3[C@H]([C@@]4([H])C[C@@]3(C=C4)[H])C(N)=O)=CC=C21 GLGNXYJARSMNGJ-VKTIVEEGSA-N 0.000 claims 1
- QFLWZFQWSBQYPS-AWRAUJHKSA-N (3S)-3-[[(2S)-2-[[(2S)-2-[5-[(3aS,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-[1-bis(4-chlorophenoxy)phosphorylbutylamino]-4-oxobutanoic acid Chemical compound CCCC(NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CCCCC1SC[C@@H]2NC(=O)N[C@H]12)C(C)C)P(=O)(Oc1ccc(Cl)cc1)Oc1ccc(Cl)cc1 QFLWZFQWSBQYPS-AWRAUJHKSA-N 0.000 claims 1
- TVTJUIAKQFIXCE-HUKYDQBMSA-N 2-amino-9-[(2R,3S,4S,5R)-4-fluoro-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-ynyl-1H-purine-6,8-dione Chemical compound NC=1NC(C=2N(C(N(C=2N=1)[C@@H]1O[C@@H]([C@H]([C@H]1O)F)CO)=O)CC#C)=O TVTJUIAKQFIXCE-HUKYDQBMSA-N 0.000 claims 1
- LNUFLCYMSVYYNW-ZPJMAFJPSA-N [(2r,3r,4s,5r,6r)-2-[(2r,3r,4s,5r,6r)-6-[(2r,3r,4s,5r,6r)-6-[(2r,3r,4s,5r,6r)-6-[[(3s,5s,8r,9s,10s,13r,14s,17r)-10,13-dimethyl-17-[(2r)-6-methylheptan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-yl]oxy]-4,5-disulfo Chemical compound O([C@@H]1[C@@H](COS(O)(=O)=O)O[C@@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1[C@@H](COS(O)(=O)=O)O[C@@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1[C@@H](COS(O)(=O)=O)O[C@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1C[C@@H]2CC[C@H]3[C@@H]4CC[C@@H]([C@]4(CC[C@@H]3[C@@]2(C)CC1)C)[C@H](C)CCCC(C)C)[C@H]1O[C@H](COS(O)(=O)=O)[C@@H](OS(O)(=O)=O)[C@H](OS(O)(=O)=O)[C@H]1OS(O)(=O)=O LNUFLCYMSVYYNW-ZPJMAFJPSA-N 0.000 claims 1
- XRWSZZJLZRKHHD-WVWIJVSJSA-N asunaprevir Chemical compound O=C([C@@H]1C[C@H](CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C)OC1=NC=C(C2=CC=C(Cl)C=C21)OC)N[C@]1(C(=O)NS(=O)(=O)C2CC2)C[C@H]1C=C XRWSZZJLZRKHHD-WVWIJVSJSA-N 0.000 claims 1
- KGNDCEVUMONOKF-UGPLYTSKSA-N benzyl n-[(2r)-1-[(2s,4r)-2-[[(2s)-6-amino-1-(1,3-benzoxazol-2-yl)-1,1-dihydroxyhexan-2-yl]carbamoyl]-4-[(4-methylphenyl)methoxy]pyrrolidin-1-yl]-1-oxo-4-phenylbutan-2-yl]carbamate Chemical compound C1=CC(C)=CC=C1CO[C@H]1CN(C(=O)[C@@H](CCC=2C=CC=CC=2)NC(=O)OCC=2C=CC=CC=2)[C@H](C(=O)N[C@@H](CCCCN)C(O)(O)C=2OC3=CC=CC=C3N=2)C1 KGNDCEVUMONOKF-UGPLYTSKSA-N 0.000 claims 1
- 229940125758 compound 15 Drugs 0.000 claims 1
- 229940125833 compound 23 Drugs 0.000 claims 1
- 229940125961 compound 24 Drugs 0.000 claims 1
- 229940125851 compound 27 Drugs 0.000 claims 1
- -1 3-pentenyl Chemical group 0.000 description 543
- 125000000217 alkyl group Chemical group 0.000 description 149
- 125000001188 haloalkyl group Chemical group 0.000 description 103
- 229910052736 halogen Inorganic materials 0.000 description 94
- 150000002367 halogens Chemical class 0.000 description 93
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 90
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 88
- 125000003282 alkyl amino group Chemical group 0.000 description 87
- 125000004663 dialkyl amino group Chemical group 0.000 description 84
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- 125000004103 aminoalkyl group Chemical group 0.000 description 77
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 77
- 125000003118 aryl group Chemical group 0.000 description 73
- 239000000243 solution Substances 0.000 description 66
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 64
- 125000004438 haloalkoxy group Chemical group 0.000 description 61
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- 230000015572 biosynthetic process Effects 0.000 description 53
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 53
- 238000009472 formulation Methods 0.000 description 51
- 125000001072 heteroaryl group Chemical group 0.000 description 50
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 49
- 125000000753 cycloalkyl group Chemical group 0.000 description 45
- 125000003342 alkenyl group Chemical group 0.000 description 43
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 43
- 125000000304 alkynyl group Chemical group 0.000 description 42
- 125000004440 haloalkylsulfinyl group Chemical group 0.000 description 42
- 238000003786 synthesis reaction Methods 0.000 description 41
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 40
- 125000004995 haloalkylthio group Chemical group 0.000 description 39
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 34
- 125000000392 cycloalkenyl group Chemical group 0.000 description 34
- 125000000623 heterocyclic group Chemical group 0.000 description 34
- 239000007787 solid Substances 0.000 description 34
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 33
- 125000004414 alkyl thio group Chemical group 0.000 description 33
- 125000004955 1,4-cyclohexylene group Chemical group [H]C1([H])C([H])([H])C([H])([*:1])C([H])([H])C([H])([H])C1([H])[*:2] 0.000 description 31
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 30
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- 238000005160 1H NMR spectroscopy Methods 0.000 description 22
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- 239000002904 solvent Substances 0.000 description 22
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 21
- 125000005140 aralkylsulfonyl group Chemical group 0.000 description 21
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- 125000005143 heteroarylsulfonyl group Chemical group 0.000 description 14
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 13
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 13
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- BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 description 1
- 229960001600 xylazine Drugs 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
- BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 description 1
- 229960000317 yohimbine Drugs 0.000 description 1
- AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 0.000 description 1
- 229960004764 zafirlukast Drugs 0.000 description 1
- 239000004246 zinc acetate Substances 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
- UBQNRHZMVUUOMG-UHFFFAOYSA-N zonisamide Chemical compound C1=CC=C2C(CS(=O)(=O)N)=NOC2=C1 UBQNRHZMVUUOMG-UHFFFAOYSA-N 0.000 description 1
- 229960002911 zonisamide Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/14—Ectoparasiticides, e.g. scabicides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562105463P | 2015-01-20 | 2015-01-20 | |
| PCT/US2016/014148 WO2016118638A1 (en) | 2015-01-20 | 2016-01-20 | Anthelmintic compounds, compositions and method of using thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2907461T3 true ES2907461T3 (es) | 2022-04-25 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES16702865T Active ES2907461T3 (es) | 2015-01-20 | 2016-01-20 | Compuestos antihelmínticos, composiciones y procedimientos de uso de los mismos |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10597364B2 (https=) |
| EP (1) | EP3247701B1 (https=) |
| JP (1) | JP6771469B2 (https=) |
| CN (1) | CN107257793A (https=) |
| AU (3) | AU2016209321B2 (https=) |
| BR (1) | BR112017015273A2 (https=) |
| CA (1) | CA2973873A1 (https=) |
| ES (1) | ES2907461T3 (https=) |
| MX (1) | MX379304B (https=) |
| NZ (1) | NZ734082A (https=) |
| WO (1) | WO2016118638A1 (https=) |
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| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| MX385718B (es) | 2016-06-13 | 2025-03-18 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4). |
| US10710980B2 (en) | 2016-07-20 | 2020-07-14 | Novartis Ag | Aminopyridine derivatives and their use as selective ALK-2 inhibitors |
| PT3600309T (pt) | 2017-03-28 | 2022-10-03 | Gilead Sciences Inc | Combinações terapêuticas para o tratamento de doenças hepáticas |
| JP7312749B2 (ja) | 2017-08-04 | 2023-07-21 | スカイホーク・セラピューティクス・インコーポレーテッド | スプライシングをモジュレートする方法および組成物 |
| TWI793151B (zh) | 2017-08-23 | 2023-02-21 | 瑞士商諾華公司 | 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途 |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| DK3820573T3 (da) | 2018-07-10 | 2023-10-23 | Novartis Ag | 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidin-2,6-dion-derivativer og anvendelse deraf ved behandling af ikaros family zinc finger 2 (ikzf2)-afhængige sygdomme |
| AR116524A1 (es) * | 2018-10-04 | 2021-05-19 | Elanco Tiergesundheit Ag | Potenciación de tratamiento de helmintos |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| GB201820626D0 (en) * | 2018-12-18 | 2019-01-30 | Univ Of Canterbury | Conjugates |
| EP3911647B1 (en) | 2019-01-15 | 2023-12-13 | Gilead Sciences, Inc. | Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same |
| SG11202107614PA (en) | 2019-01-18 | 2021-08-30 | Astrazeneca Ab | Pcsk9 inhibitors and methods of use thereof |
| AU2020209216A1 (en) | 2019-01-18 | 2021-08-26 | Astrazeneca Ab | PCSK9 inhibitors and methods of use thereof |
| WO2020163405A1 (en) | 2019-02-05 | 2020-08-13 | Skyhawk Therapeutics, Inc. | Methods and compositions for modulating splicing |
| JP7551629B2 (ja) | 2019-02-05 | 2024-09-17 | スカイホーク・セラピューティクス・インコーポレーテッド | スプライシングを調節するための方法および組成物 |
| JP7603594B2 (ja) | 2019-02-06 | 2024-12-20 | スカイホーク・セラピューティクス・インコーポレーテッド | スプライシングを調節するための方法および組成物 |
| JP7603595B2 (ja) | 2019-02-06 | 2024-12-20 | スカイホーク・セラピューティクス・インコーポレーテッド | スプライシングを調節するための方法および組成物 |
| CA3233305A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| CA3133100A1 (en) * | 2019-03-19 | 2020-09-24 | Boehringer Ingelheim Animal Health USA Inc. | Anthelmintic aza-benzothiophene and aza-benzofuran compounds |
| UY38687A (es) | 2019-05-17 | 2023-05-15 | Novartis Ag | Inhibidores del inflamasoma nlrp3, composiciones, combinaciones de los mismos y métodos para su uso |
| US11129829B2 (en) | 2019-06-17 | 2021-09-28 | Skyhawk Therapeutics, Inc. | Methods for modulating splicing |
| CA3157525A1 (en) | 2019-10-25 | 2021-04-29 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| CN115038443A (zh) | 2019-11-22 | 2022-09-09 | 因西特公司 | 包含alk2抑制剂和jak2抑制剂的组合疗法 |
| WO2021154796A1 (en) | 2020-01-29 | 2021-08-05 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| BR112022020291A2 (pt) | 2020-04-07 | 2022-12-06 | Mitobridge Inc | Inibidores de cd38 |
| EP4149941B1 (en) | 2020-05-15 | 2025-09-03 | Algen Biotechnologies, Inc. | Certain chemical compositions and methods of use thereof |
| JP2023530316A (ja) | 2020-06-16 | 2023-07-14 | インサイト・コーポレイション | 貧血の治療のためのａｌｋ２阻害剤 |
| EP4247804A1 (en) | 2020-11-20 | 2023-09-27 | Gilead Sciences, Inc. | Polyheterocyclic glp-1 r modulating compounds |
| WO2022192430A1 (en) | 2021-03-11 | 2022-09-15 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| EP4304711A1 (en) | 2021-03-11 | 2024-01-17 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| US11932630B2 (en) | 2021-04-16 | 2024-03-19 | Novartis Ag | Heteroaryl aminopropanol derivatives |
| PH12023552860A1 (en) | 2021-04-21 | 2024-05-20 | Gilead Sciences Inc | Carboxy-benzimidazole glp-1r modulating compounds |
| UY40374A (es) | 2022-08-03 | 2024-02-15 | Novartis Ag | Inhibidores de inflamasoma nlrp3 |
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| DE4208254A1 (de) | 1992-03-14 | 1993-09-16 | Hoechst Ag | Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid |
| AU1631699A (en) | 1997-12-18 | 1999-07-05 | E.I. Du Pont De Nemours And Company | Cyclohexylamine arthropodicides and fungicides |
| AU2001233044A1 (en) | 2000-01-28 | 2001-08-07 | Akkadix Corporation | Methods for killing nematodes and nematode eggs using bis-amino-1,2,4-thiadiazoles |
| JPWO2002100833A1 (ja) | 2001-06-12 | 2004-09-24 | 住友製薬株式会社 | Ｒｈｏキナーゼ阻害剤 |
| EP1689722A2 (en) * | 2003-10-10 | 2006-08-16 | Bayer Pharmaceuticals Corporation | 4-aminopyrimidine derivatives for treatment of hyperproliferative disorders |
| EP1751136B1 (en) * | 2004-05-07 | 2014-07-02 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
| DE102005032838A1 (de) * | 2005-07-14 | 2007-02-08 | Merck Patent Gmbh | Mischung von Onium-Alkylsulfonaten und Onium-Alkylsulfiten |
| WO2007063839A1 (ja) * | 2005-11-30 | 2007-06-07 | Shionogi & Co., Ltd. | シクロヘキサン誘導体 |
| TW200938203A (en) | 2007-12-17 | 2009-09-16 | Intervet Int Bv | Anthelmintic agents and their use |
| TW201041868A (en) | 2009-03-20 | 2010-12-01 | Intervet Int Bv | Anthelmintic agents and their use |
| TW201111358A (en) | 2009-06-18 | 2011-04-01 | Intervet Int Bv | Anthelmintic agents and their use |
| CN102686579A (zh) * | 2009-10-09 | 2012-09-19 | Irm责任有限公司 | 作为gpr119活性调节剂的化合物和组合物 |
| AU2011253058A1 (en) * | 2010-05-13 | 2012-12-06 | Amgen Inc. | Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors |
| CA2798325A1 (en) * | 2010-05-13 | 2011-11-17 | Amgen Inc. | Heteroaryloxyheterocyclyl compounds as pde10 inhibitors |
| EP2468096A1 (en) | 2010-12-21 | 2012-06-27 | Intervet International BV | Anthelmintic combinations |
| US8530461B2 (en) * | 2011-12-29 | 2013-09-10 | Boehringer Ingelheim International Gmbh | Azetidine derivatives |
| JP6233855B2 (ja) * | 2012-08-08 | 2017-11-22 | ノバルティス・ティーアゲズントハイト・アクチェンゲゼルシャフトＮｏｖａｒｔｉｓ Ｔｉｅｒｇｅｓｕｎｄｈｅｉｔ Ａｇ | 殺虫剤としての置換されたアジン類 |
| NZ723198A (en) * | 2012-11-20 | 2018-11-30 | Boehringer Ingelheim Animal Health Usa Inc | Anthelmintic compounds and compositions and methods of using thereof |
| SI3527563T1 (sl) * | 2013-03-12 | 2022-01-31 | Vertex Pharmaceuticals Incorporated | Inhibitorji DNA-PK |
| EP3071559B1 (en) | 2013-11-18 | 2018-01-10 | Elanco Tiergesundheit AG | (hetero)arylamides for controlling endoparasites |
| ES2842592T3 (es) | 2014-05-19 | 2021-07-14 | Boehringer Ingelheim Animal Health Usa Inc | Compuestos antihelmínticos |
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2016
- 2016-01-20 BR BR112017015273-8A patent/BR112017015273A2/pt active Search and Examination
- 2016-01-20 ES ES16702865T patent/ES2907461T3/es active Active
- 2016-01-20 EP EP16702865.3A patent/EP3247701B1/en active Active
- 2016-01-20 MX MX2017009408A patent/MX379304B/es unknown
- 2016-01-20 CA CA2973873A patent/CA2973873A1/en not_active Abandoned
- 2016-01-20 US US15/544,837 patent/US10597364B2/en active Active
- 2016-01-20 JP JP2017538327A patent/JP6771469B2/ja not_active Expired - Fee Related
- 2016-01-20 NZ NZ734082A patent/NZ734082A/en not_active IP Right Cessation
- 2016-01-20 CN CN201680010899.2A patent/CN107257793A/zh active Pending
- 2016-01-20 WO PCT/US2016/014148 patent/WO2016118638A1/en not_active Ceased
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2019
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2020
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Also Published As
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|---|---|
| AU2016209321B2 (en) | 2019-05-09 |
| CN107257793A (zh) | 2017-10-17 |
| US10597364B2 (en) | 2020-03-24 |
| AU2020204400A1 (en) | 2020-07-30 |
| AU2016209321A1 (en) | 2017-08-17 |
| JP6771469B2 (ja) | 2020-10-21 |
| EP3247701B1 (en) | 2021-09-22 |
| JP2018502877A (ja) | 2018-02-01 |
| MX2017009408A (es) | 2017-10-02 |
| MX379304B (es) | 2025-03-11 |
| AU2019202773B2 (en) | 2020-07-02 |
| CA2973873A1 (en) | 2016-07-28 |
| WO2016118638A1 (en) | 2016-07-28 |
| NZ734082A (en) | 2019-01-25 |
| AU2019202773A1 (en) | 2019-05-16 |
| US20180009754A1 (en) | 2018-01-11 |
| BR112017015273A2 (pt) | 2018-01-09 |
| EP3247701A1 (en) | 2017-11-29 |
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