JP2017525677A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017525677A5 JP2017525677A5 JP2017501012A JP2017501012A JP2017525677A5 JP 2017525677 A5 JP2017525677 A5 JP 2017525677A5 JP 2017501012 A JP2017501012 A JP 2017501012A JP 2017501012 A JP2017501012 A JP 2017501012A JP 2017525677 A5 JP2017525677 A5 JP 2017525677A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- haloalkyl
- acceptable salt
- pharmaceutically acceptable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 198
- 150000001875 compounds Chemical class 0.000 claims description 146
- 125000000623 heterocyclic group Chemical group 0.000 claims description 116
- 125000001424 substituent group Chemical group 0.000 claims description 109
- 150000003839 salts Chemical class 0.000 claims description 94
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 86
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims description 81
- 229910052739 hydrogen Inorganic materials 0.000 claims description 80
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 74
- 229910052799 carbon Inorganic materials 0.000 claims description 73
- 125000003545 alkoxy group Chemical group 0.000 claims description 72
- 239000001257 hydrogen Substances 0.000 claims description 72
- 125000003282 alkyl amino group Chemical group 0.000 claims description 50
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 50
- 229910052760 oxygen Inorganic materials 0.000 claims description 48
- 208000002193 Pain Diseases 0.000 claims description 43
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 39
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 38
- 150000002431 hydrogen Chemical class 0.000 claims description 37
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 36
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 35
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 35
- 125000001188 haloalkyl group Chemical group 0.000 claims description 33
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 32
- 125000003342 alkenyl group Chemical group 0.000 claims description 28
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 26
- 125000005842 heteroatom Chemical group 0.000 claims description 26
- 229910052717 sulfur Inorganic materials 0.000 claims description 26
- 125000002947 alkylene group Chemical group 0.000 claims description 25
- 125000004450 alkenylene group Chemical group 0.000 claims description 22
- 125000004419 alkynylene group Chemical group 0.000 claims description 22
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 22
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 21
- 125000002837 carbocyclic group Chemical group 0.000 claims description 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 14
- 241000124008 Mammalia Species 0.000 claims description 13
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 12
- 125000004414 alkyl thio group Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims description 8
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 8
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 8
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 125000005843 halogen group Chemical group 0.000 claims description 8
- 125000004043 oxo group Chemical group O=* 0.000 claims description 8
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- -1 methoxyethyl Chemical group 0.000 claims description 7
- 208000020016 psychiatric disease Diseases 0.000 claims description 7
- 208000023504 respiratory system disease Diseases 0.000 claims description 7
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 6
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims description 6
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims description 6
- 208000005298 acute pain Diseases 0.000 claims description 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 6
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 claims description 6
- 150000002500 ions Chemical class 0.000 claims description 6
- 125000001624 naphthyl group Chemical group 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 230000000069 prophylactic effect Effects 0.000 claims description 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 6
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 6
- 230000001225 therapeutic effect Effects 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 208000000094 Chronic Pain Diseases 0.000 claims description 4
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims description 4
- 208000003251 Pruritus Diseases 0.000 claims description 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical group C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
- 108010052164 Sodium Channels Proteins 0.000 claims description 4
- 102000018674 Sodium Channels Human genes 0.000 claims description 4
- ORILYTVJVMAKLC-UHFFFAOYSA-N adamantane Chemical compound C1C(C2)CC3CC1CC2C3 ORILYTVJVMAKLC-UHFFFAOYSA-N 0.000 claims description 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 claims description 4
- SHOMMGQAMRXRRK-UHFFFAOYSA-N bicyclo[3.1.1]heptane Chemical compound C1C2CC1CCC2 SHOMMGQAMRXRRK-UHFFFAOYSA-N 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 230000004907 flux Effects 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 201000006417 multiple sclerosis Diseases 0.000 claims description 4
- WPHGSKGZRAQSGP-UHFFFAOYSA-N norcarane Chemical compound C1CCCC2CC21 WPHGSKGZRAQSGP-UHFFFAOYSA-N 0.000 claims description 4
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 4
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims description 3
- 125000002393 azetidinyl group Chemical group 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 claims description 2
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical compound C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 claims description 2
- ZNGWEEUXTBNKFR-UHFFFAOYSA-N 1,4-oxazepane Chemical compound C1CNCCOC1 ZNGWEEUXTBNKFR-UHFFFAOYSA-N 0.000 claims description 2
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims description 2
- DGGKXQQCVPAUEA-UHFFFAOYSA-N 8-azabicyclo[3.2.1]octane Chemical compound C1CCC2CCC1N2 DGGKXQQCVPAUEA-UHFFFAOYSA-N 0.000 claims description 2
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- 206010058019 Cancer Pain Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 206010010904 Convulsion Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- PMPVIKIVABFJJI-UHFFFAOYSA-N Cyclobutane Chemical compound C1CCC1 PMPVIKIVABFJJI-UHFFFAOYSA-N 0.000 claims description 2
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims description 2
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- 206010019233 Headaches Diseases 0.000 claims description 2
- 101000620451 Homo sapiens Leucine-rich glioma-inactivated protein 1 Proteins 0.000 claims description 2
- 206010020844 Hyperthermia malignant Diseases 0.000 claims description 2
- WRYCSMQKUKOKBP-UHFFFAOYSA-N Imidazolidine Chemical compound C1CNCN1 WRYCSMQKUKOKBP-UHFFFAOYSA-N 0.000 claims description 2
- 206010065390 Inflammatory pain Diseases 0.000 claims description 2
- 208000007914 Labor Pain Diseases 0.000 claims description 2
- 208000035945 Labour pain Diseases 0.000 claims description 2
- 102100022275 Leucine-rich glioma-inactivated protein 1 Human genes 0.000 claims description 2
- 208000026709 Liddle syndrome Diseases 0.000 claims description 2
- 208000018717 Malignant hyperthermia of anesthesia Diseases 0.000 claims description 2
- 208000019695 Migraine disease Diseases 0.000 claims description 2
- 206010028372 Muscular weakness Diseases 0.000 claims description 2
- 206010061533 Myotonia Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000000693 Neurogenic Urinary Bladder Diseases 0.000 claims description 2
- 206010029279 Neurogenic bladder Diseases 0.000 claims description 2
- WYNCHZVNFNFDNH-UHFFFAOYSA-N Oxazolidine Chemical compound C1COCN1 WYNCHZVNFNFDNH-UHFFFAOYSA-N 0.000 claims description 2
- 208000012075 Paroxysmal dystonia Diseases 0.000 claims description 2
- 208000010886 Peripheral nerve injury Diseases 0.000 claims description 2
- 208000004983 Phantom Limb Diseases 0.000 claims description 2
- 206010056238 Phantom pain Diseases 0.000 claims description 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Chemical group C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims description 2
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 2
- 208000004550 Postoperative Pain Diseases 0.000 claims description 2
- 206010037113 Pseudoaldosteronism Diseases 0.000 claims description 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 2
- 208000005793 Restless legs syndrome Diseases 0.000 claims description 2
- 206010039020 Rhabdomyolysis Diseases 0.000 claims description 2
- 206010040744 Sinus headache Diseases 0.000 claims description 2
- 208000001871 Tachycardia Diseases 0.000 claims description 2
- 206010043269 Tension headache Diseases 0.000 claims description 2
- 208000008548 Tension-Type Headache Diseases 0.000 claims description 2
- 206010043994 Tonic convulsion Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 230000036506 anxiety Effects 0.000 claims description 2
- 206010003119 arrhythmia Diseases 0.000 claims description 2
- 230000006793 arrhythmia Effects 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- JSMRMEYFZHIPJV-UHFFFAOYSA-N bicyclo[2.1.1]hexane Chemical compound C1C2CC1CC2 JSMRMEYFZHIPJV-UHFFFAOYSA-N 0.000 claims description 2
- GPRLTFBKWDERLU-UHFFFAOYSA-N bicyclo[2.2.2]octane Chemical compound C1CC2CCC1CC2 GPRLTFBKWDERLU-UHFFFAOYSA-N 0.000 claims description 2
- JAPMJSVZDUYFKL-UHFFFAOYSA-N bicyclo[3.1.0]hexane Chemical compound C1CCC2CC21 JAPMJSVZDUYFKL-UHFFFAOYSA-N 0.000 claims description 2
- LPCWKMYWISGVSK-UHFFFAOYSA-N bicyclo[3.2.1]octane Chemical compound C1C2CCC1CCC2 LPCWKMYWISGVSK-UHFFFAOYSA-N 0.000 claims description 2
- WNTGVOIBBXFMLR-UHFFFAOYSA-N bicyclo[3.3.1]nonane Chemical compound C1CCC2CCCC1C2 WNTGVOIBBXFMLR-UHFFFAOYSA-N 0.000 claims description 2
- QVAUSBVLMVBCPN-UHFFFAOYSA-N bicyclo[4.1.1]octane Chemical compound C1C2CC1CCCC2 QVAUSBVLMVBCPN-UHFFFAOYSA-N 0.000 claims description 2
- 208000028683 bipolar I disease Diseases 0.000 claims description 2
- 208000025307 bipolar depression Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 230000035606 childbirth Effects 0.000 claims description 2
- TXWRERCHRDBNLG-UHFFFAOYSA-N cubane Chemical compound C12C3C4C1C1C4C3C12 TXWRERCHRDBNLG-UHFFFAOYSA-N 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 208000037765 diseases and disorders Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 238000002651 drug therapy Methods 0.000 claims description 2
- 208000010118 dystonia Diseases 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 2
- 208000003532 hypothyroidism Diseases 0.000 claims description 2
- 230000002989 hypothyroidism Effects 0.000 claims description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 2
- 230000000302 ischemic effect Effects 0.000 claims description 2
- 201000007004 malignant hyperthermia Diseases 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 2
- 206010027599 migraine Diseases 0.000 claims description 2
- 230000036473 myasthenia Effects 0.000 claims description 2
- 208000004296 neuralgia Diseases 0.000 claims description 2
- 208000021722 neuropathic pain Diseases 0.000 claims description 2
- 201000001119 neuropathy Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 230000004112 neuroprotection Effects 0.000 claims description 2
- UMRZSTCPUPJPOJ-KNVOCYPGSA-N norbornane Chemical compound C1C[C@H]2CC[C@@H]1C2 UMRZSTCPUPJPOJ-KNVOCYPGSA-N 0.000 claims description 2
- 125000005593 norbornanyl group Chemical group 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 208000019865 paroxysmal extreme pain disease Diseases 0.000 claims description 2
- 230000002085 persistent effect Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- FOEYMRPOKBCNCR-UHFFFAOYSA-N spiro[2.5]octane Chemical compound C1CC11CCCCC1 FOEYMRPOKBCNCR-UHFFFAOYSA-N 0.000 claims description 2
- CTDQAGUNKPRERK-UHFFFAOYSA-N spirodecane Chemical compound C1CCCC21CCCCC2 CTDQAGUNKPRERK-UHFFFAOYSA-N 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims description 2
- 230000008542 thermal sensitivity Effects 0.000 claims description 2
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims description 2
- 208000004371 toothache Diseases 0.000 claims description 2
- 239000003053 toxin Substances 0.000 claims description 2
- 231100000765 toxin Toxicity 0.000 claims description 2
- 230000000472 traumatic effect Effects 0.000 claims description 2
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 2
- 208000003663 ventricular fibrillation Diseases 0.000 claims description 2
- 208000009935 visceral pain Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 230000001419 dependent effect Effects 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 230000001537 neural effect Effects 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 125000006621 (C3-C8) cycloalkyl-(C1-C6) alkyl group Chemical group 0.000 description 2
- 125000001054 5 membered carbocyclic group Chemical group 0.000 description 2
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 206010049447 Tachyarrhythmia Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462021587P | 2014-07-07 | 2014-07-07 | |
| US62/021,587 | 2014-07-07 | ||
| PCT/US2015/039413 WO2016007534A1 (en) | 2014-07-07 | 2015-07-07 | Therapeutic compounds and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017525677A JP2017525677A (ja) | 2017-09-07 |
| JP2017525677A5 true JP2017525677A5 (enExample) | 2018-08-16 |
Family
ID=53761514
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017501012A Pending JP2017525677A (ja) | 2014-07-07 | 2015-07-07 | 治療用化合物及びその使用方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (4) | US10005724B2 (enExample) |
| EP (1) | EP3166939B1 (enExample) |
| JP (1) | JP2017525677A (enExample) |
| CN (1) | CN106715418A (enExample) |
| WO (1) | WO2016007534A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3166939B1 (en) | 2014-07-07 | 2019-06-05 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| WO2016191312A1 (en) * | 2015-05-22 | 2016-12-01 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| JP6469238B2 (ja) | 2015-09-18 | 2019-02-13 | 科研製薬株式会社 | ビアリール誘導体及びそれを含有する医薬 |
| CN108495851A (zh) | 2015-11-25 | 2018-09-04 | 基因泰克公司 | 取代的苯甲酰胺及其使用方法 |
| TW201726637A (zh) | 2015-12-18 | 2017-08-01 | 默沙東藥廠 | 對電位閘控鈉通道具選擇活性之羥基烷基胺-及羥基環烷基胺-取代之二胺-芳基磺胺化合物 |
| EP3854782A1 (en) | 2016-03-30 | 2021-07-28 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| KR102366077B1 (ko) * | 2016-05-20 | 2022-02-21 | 제논 파마슈티칼스 인크. | 벤젠술폰아미드 화합물 및 치료제로서의 그의 용도 |
| WO2018175707A1 (en) | 2017-03-24 | 2018-09-27 | Genentech, Inc. | 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors |
| SG11202001684PA (en) | 2017-10-06 | 2020-03-30 | Forma Therapeutics Inc | Inhibiting ubiquitin specific peptidase 30 |
| EP3759098A1 (en) | 2018-02-26 | 2021-01-06 | Genentech, Inc. | Pyridine-sulfonamide compounds and their use against pain and related conditions |
| EP3774801A1 (en) | 2018-03-30 | 2021-02-17 | F. Hoffmann-La Roche AG | Fused ring hydro-pyrido compounds as sodium channel inhibitors |
| ES2988920T3 (es) | 2018-05-17 | 2024-11-22 | Forma Therapeutics Inc | Compuestos bicíclicos fusionados útiles como inhibidores de la peptidasa 30 específica de ubiquitina |
| TW202003490A (zh) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療性化合物及其使用方法 |
| AU2019301628C1 (en) | 2018-07-09 | 2025-02-06 | Lieber Institute, Inc. | Pyridine carboxamide compounds for inhibiting NaV1.8 |
| SG11202100137TA (en) | 2018-07-09 | 2021-02-25 | Lieber Institute Inc | PYRIDAZINE COMPOUNDS FOR INHIBITING Nav1.8 |
| PL3860989T3 (pl) | 2018-10-05 | 2023-07-10 | Forma Therapeutics, Inc. | Sprzężone piroliny, które działają jako inhibitory proteazy 30 swoistej dla ubikwityny (usp30) |
| CN112955437A (zh) * | 2018-11-05 | 2021-06-11 | 默克专利有限公司 | 可用于有机电子器件中的化合物 |
| CN115215787A (zh) * | 2021-04-19 | 2022-10-21 | 中国科学院上海药物研究所 | 生长抑素受体5拮抗剂及其用途 |
Family Cites Families (117)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3705185A (en) | 1969-04-14 | 1972-12-05 | Minnesota Mining & Mfg | N-aroyl sulfonamides |
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| GB8524157D0 (en) | 1984-10-19 | 1985-11-06 | Ici America Inc | Heterocyclic amides |
| US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
| DK24089D0 (da) | 1989-01-20 | 1989-01-20 | Hans Bundgaard | Novel prodrug derivatives of biologically active agents containing hydroxyl groups or nh-acidic groups |
| GB8911854D0 (en) | 1989-05-23 | 1989-07-12 | Ici Plc | Heterocyclic compounds |
| US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| IL101860A0 (en) | 1991-05-31 | 1992-12-30 | Ici Plc | Heterocyclic derivatives |
| EP0652775B1 (en) | 1992-07-27 | 2000-04-19 | THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by the SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES | Targeting of liposomes to the blood-brain barrier |
| DE69332691T2 (de) | 1992-11-23 | 2003-12-18 | Aventis Pharmaceuticals Inc., Cincinnati | Substituierte 3-(aminoalkylamino)-1,2-benzisoxazole und verwandte verbindungen |
| US5573653A (en) | 1994-07-11 | 1996-11-12 | Sandoz Ltd. | Electrochemical process for thiocyanating aminobenzene compounds |
| AU688102B2 (en) | 1994-08-30 | 1998-03-05 | Sankyo Company Limited | Isoxazoles |
| US5753653A (en) | 1995-12-08 | 1998-05-19 | Agouron Pharmaceuticals, Inc. | Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses |
| GB9828442D0 (en) | 1998-12-24 | 1999-02-17 | Karobio Ab | Novel thyroid receptor ligands and method II |
| US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
| WO2002017930A2 (en) | 2000-08-30 | 2002-03-07 | The Board Of Trustees Of The Leland Stanford Junior University | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
| DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
| AU2002322720B2 (en) | 2001-07-25 | 2008-11-13 | Raptor Pharmaceutical Inc. | Compositions and methods for modulating blood-brain barrier transport |
| KR100789567B1 (ko) | 2001-11-06 | 2007-12-28 | 동화약품공업주식회사 | 3-아미도-1,2-벤조이소옥사졸 유도체, 그 염, 제조방법 및 용도 |
| DE10201550A1 (de) | 2002-01-17 | 2003-07-31 | Merck Patent Gmbh | Phenoxy-Piperidine |
| US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| US7332486B2 (en) | 2002-08-08 | 2008-02-19 | Memory Pharmaceuticals Corp. | Phosphodiesterase 4 inhibitors |
| AU2003302676A1 (en) | 2002-12-03 | 2004-06-23 | Blanchette Rockefeller Neurosciences Institute | Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier |
| MY141521A (en) | 2002-12-12 | 2010-05-14 | Hoffmann La Roche | 5-substituted-six-membered heteroaromatic glucokinase activators |
| EA200501462A1 (ru) | 2003-04-15 | 2006-04-28 | Пфайзер Инк. | Альфа-замещенные карбоновые кислоты в качестве модуляторов ppar |
| ZA200601942B (en) | 2003-08-08 | 2007-05-30 | Vertex Pharma | Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain |
| TW200524888A (en) | 2003-08-08 | 2005-08-01 | Vertex Pharma | Compositions useful as inhibitors of voltage-gated ion channels |
| EP1663239A4 (en) | 2003-09-10 | 2008-07-23 | Cedars Sinai Medical Center | KALIUM CHANNEL-MEDIATED FEEDING OF MEDICINES BY THE BLOOD BRAIN BARRIER |
| WO2005032488A2 (en) | 2003-10-03 | 2005-04-14 | Portola Pharmaceuticals, Inc. | 2,4-dioxo-3-quinazolinylaryl sulfonylureas |
| US7081539B2 (en) | 2004-03-25 | 2006-07-25 | Dainippon Sumitomo Pharma Co., Ltd. | One-pot process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide |
| AU2005267883A1 (en) | 2004-07-30 | 2006-02-09 | Merck & Co., Inc. | Indanone potentiators of metabotropic glutamate receptors |
| ES2343640T3 (es) | 2004-08-12 | 2010-08-05 | Amgen Inc. | Bisaril-sulfonamidas. |
| NZ554211A (en) | 2004-09-29 | 2010-10-29 | Portola Pharm Inc | Substituted 2H-1,3-Benzoxazin-4(3H)-ones |
| JP2008189549A (ja) | 2005-05-12 | 2008-08-21 | Astellas Pharma Inc | カルボン酸誘導体またはその塩 |
| DE102005038947A1 (de) | 2005-05-18 | 2006-11-30 | Grünenthal GmbH | Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln |
| US7632837B2 (en) | 2005-06-17 | 2009-12-15 | Bristol-Myers Squibb Company | Bicyclic heterocycles as cannabinoid-1 receptor modulators |
| CN101277939A (zh) | 2005-09-09 | 2008-10-01 | 布里斯托尔-迈尔斯斯奎布公司 | 无环ikur抑制剂 |
| CN101287702A (zh) | 2005-10-19 | 2008-10-15 | 弗·哈夫曼-拉罗切有限公司 | N-苯基苯乙酰胺非核苷逆转录酶抑制剂 |
| WO2007062078A2 (en) | 2005-11-23 | 2007-05-31 | Ligand Pharmaceuticals Inc. | Thrombopoietin activity modulating compounds and methods |
| AR058296A1 (es) | 2005-12-09 | 2008-01-30 | Kalypsys Inc | Inhibidores de histona desacetilasa y composicion farmaceutica |
| MX2008013194A (es) | 2006-04-11 | 2008-12-01 | Vertex Pharma | Composiciones utiles como inhibidores de canales de sodio regulados por voltaje. |
| ATE542818T1 (de) | 2006-10-11 | 2012-02-15 | Amgen Inc | Imidazo- und triazolopyridinverbindungen und verfahren zu deren anwendung |
| JP2010516812A (ja) | 2007-01-30 | 2010-05-20 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | 有糸分裂キナーゼの調節剤 |
| JP2010518026A (ja) | 2007-02-05 | 2010-05-27 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | ナトリウムチャネルが介在する疾患または状態の治療に有用なピリドピリミジノン化合物 |
| ATE461177T1 (de) | 2007-03-23 | 2010-04-15 | Icagen Inc | Ionenkanal-hemmer |
| NZ581309A (en) | 2007-05-25 | 2012-02-24 | Vertex Pharma | Ion channel modulators and methods of use |
| EP2154130A4 (en) | 2007-06-07 | 2011-09-07 | Astellas Pharma Inc | pyridone |
| US20090012103A1 (en) | 2007-07-05 | 2009-01-08 | Matthew Abelman | Substituted heterocyclic compounds |
| TW200911766A (en) | 2007-07-13 | 2009-03-16 | Astrazeneca Ab | New compounds |
| EP2173743A2 (en) | 2007-07-13 | 2010-04-14 | Icagen, Inc. | Sodium channel inhibitors |
| JPWO2009022731A1 (ja) | 2007-08-10 | 2010-11-18 | 日本ケミファ株式会社 | P2x4受容体拮抗剤 |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| US8642660B2 (en) | 2007-12-21 | 2014-02-04 | The University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| EP2305641A4 (en) | 2008-06-23 | 2012-08-22 | Astellas Pharma Inc | SULPHONAMIDE COMPOUND OR SALT THEREOF |
| WO2010022055A2 (en) | 2008-08-20 | 2010-02-25 | Amgen Inc. | Inhibitors of voltage-gated sodium channels |
| HUE025013T2 (hu) | 2009-01-12 | 2016-04-28 | Pfizer Ltd | Szulfonamid-származékok |
| PT2464645T (pt) | 2009-07-27 | 2017-10-11 | Gilead Sciences Inc | Compostos heterocíclicos fusionados como moduladores do canal de iões |
| US8809380B2 (en) | 2009-08-04 | 2014-08-19 | Raqualia Pharma Inc. | Picolinamide derivatives as TTX-S blockers |
| RU2609021C2 (ru) | 2009-09-25 | 2017-01-30 | Астеллас Фарма Инк. | Замещенные соединения амида |
| WO2011059042A1 (ja) | 2009-11-12 | 2011-05-19 | 武田薬品工業株式会社 | 芳香環化合物 |
| WO2011063001A1 (en) | 2009-11-18 | 2011-05-26 | Concert Pharmaceuticals, Inc. | Niacin prodrugs and deuterated versions thereof |
| TW201139406A (en) | 2010-01-14 | 2011-11-16 | Glaxo Group Ltd | Voltage-gated sodium channel blockers |
| HUE029012T2 (en) | 2010-02-12 | 2017-02-28 | Nivalis Therapeutics Inc | New S-nitrosoglutathion reductase inhibitors |
| WO2011153588A1 (en) | 2010-06-10 | 2011-12-15 | Biota Scientific Management Pty Ltd | Viral polymerase inhibitors |
| EP2588186A1 (en) | 2010-06-30 | 2013-05-08 | Cardiac Pacemakers, Inc. | Lead having coil electrode with preferential bending region |
| US9279003B2 (en) | 2010-07-07 | 2016-03-08 | Purdue Pharma L.P. | Analogs of sodium channel peptide toxin |
| JP5872552B2 (ja) * | 2010-07-09 | 2016-03-01 | ファイザー・リミテッドPfizer Limited | 化学化合物 |
| CA2804593C (en) | 2010-07-09 | 2015-11-24 | Pfizer Limited | Biphenyloxybenzensulphonamide derivatives useful as sodium channel inhibitors |
| JP5860045B2 (ja) | 2010-07-09 | 2016-02-16 | ファイザー・リミテッドPfizer Limited | 化合物 |
| CA2801032A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | N-sulfonylbenzamide derivatives useful as voltage gated sodium channel inhibitors |
| WO2012007883A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | Sulfonamide derivatives as nav1.7 inhibitors for the treatment of pain |
| CA2804716A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | Chemical compounds |
| ES2526541T3 (es) | 2010-07-12 | 2015-01-13 | Pfizer Limited | N-sulfonilbenzamidas como inhibidores de canales de sodio dependientes de voltaje |
| JP2013531030A (ja) | 2010-07-12 | 2013-08-01 | ファイザー・リミテッド | 電位開口型ナトリウムチャネルの阻害剤としてのn−スルホニルベンズアミド |
| JP2013531687A (ja) * | 2010-07-16 | 2013-08-08 | パーデュー、ファーマ、リミテッド、パートナーシップ | ナトリウムチャネル遮断剤としてのピリジン化合物 |
| CA2812081A1 (en) | 2010-09-13 | 2012-03-22 | Novartis Ag | Triazine-oxadiazoles |
| WO2012039657A1 (en) | 2010-09-22 | 2012-03-29 | Astrazeneca Ab | Novel chromane compound for the treatment of pain disorders |
| JP2014500303A (ja) | 2010-12-22 | 2014-01-09 | パーデュー、ファーマ、リミテッド、パートナーシップ | ナトリウムチャネル遮断剤としての置換ピリジン |
| WO2012095781A1 (en) | 2011-01-13 | 2012-07-19 | Pfizer Limited | Indazole derivatives as sodium channel inhibitors |
| BR112013019211A2 (pt) | 2011-02-02 | 2021-07-06 | Vertex Pharma | amidas de piperidina espirocíclicas de pirrolopirazina como moduladores de canais de íon |
| AU2012296529A1 (en) | 2011-08-17 | 2014-02-20 | Amgen Inc. | Heteroaryl sodium channel inhibitors |
| JP2014528486A (ja) | 2011-10-13 | 2014-10-27 | ケース ウエスタン リザーブ ユニバーシティ | Rxrアゴニスト化合物および方法 |
| MX2014005068A (es) | 2011-10-28 | 2014-07-30 | Merck Sharp & Dohme | Compuestos de benzoxazolinona con actividad selectiva en canales de sodio activados por voltaje. |
| ES2586213T3 (es) | 2011-10-31 | 2016-10-13 | Xenon Pharmaceuticals Inc. | Compuestos de bencenosulfonamida y su uso como agentes terapéuticos |
| JP6014155B2 (ja) | 2011-10-31 | 2016-10-25 | ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. | ビアリールエーテルスルホンアミドおよび治療剤としてのそれらの使用 |
| WO2013072758A1 (en) | 2011-11-15 | 2013-05-23 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| EP2788332A1 (en) | 2011-12-07 | 2014-10-15 | Amgen, Inc. | Bicyclic aryl and heteroaryl sodium channel inhibitors |
| ES2593533T3 (es) | 2011-12-15 | 2016-12-09 | Pfizer Limited | Derivados de sulfonamida |
| US8859559B2 (en) * | 2011-12-20 | 2014-10-14 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
| WO2013102826A1 (en) | 2012-01-04 | 2013-07-11 | Pfizer Limited | N-aminosulfonyl benzamides |
| JP2015083542A (ja) | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | 3位置換プロリン誘導体 |
| US8889741B2 (en) | 2012-02-09 | 2014-11-18 | Daiichi Sankyo Company, Limited | Cycloalkane derivatives |
| US9346798B2 (en) | 2012-02-13 | 2016-05-24 | Amgen Inc. | Dihydrobenzoxazine and tetrahydroquinoxaline sodium channel inhibitors |
| WO2013134518A1 (en) | 2012-03-09 | 2013-09-12 | Amgen Inc. | Sulfamide sodium channel inhibitors |
| WO2013146969A1 (ja) | 2012-03-29 | 2013-10-03 | 第一三共株式会社 | 新規二置換シクロヘキサン誘導体 |
| BR112014026399B1 (pt) * | 2012-04-25 | 2022-11-01 | Raqualia Pharma Inc | Composto de fórmula (ii), composição farmacêutica, uso e processo para preparar uma composição farmacêutica |
| BR112014029161A2 (pt) | 2012-05-22 | 2017-06-27 | Genentech Inc | benzamidas n-substituídas e seu uso no tratamento de dor |
| BR112015000187A2 (pt) | 2012-07-06 | 2017-06-27 | Genentech Inc | benzamidas substituídas com n e métodos de uso das mesmas |
| EP2876105A4 (en) | 2012-07-19 | 2016-01-13 | Sumitomo Dainippon Pharma Co Ltd | 1- (CYCLOALKYL-CARBONYL) PROLIN DERIVATIVE |
| US9624208B2 (en) | 2012-10-26 | 2017-04-18 | Merck Sharp & Dohme Corp. | Benzoxazolinone compounds with selective activity in voltage-gated sodium channels |
| US9388179B2 (en) | 2012-10-26 | 2016-07-12 | Merck Sharp & Dohme Corp. | N-substituted indazole sulfonamide compounds with selective activity in voltage-gated sodium channels |
| JP2014118368A (ja) * | 2012-12-14 | 2014-06-30 | Taisho Pharmaceutical Co Ltd | アザスピロアルカン化合物を有効成分として含有する血糖低下作用薬 |
| WO2014096941A1 (en) | 2012-12-20 | 2014-06-26 | Purdue Pharma L.P. | Cyclic sulfonamides as sodium channel blockers |
| ES2857687T3 (es) | 2013-01-31 | 2021-09-29 | Vertex Pharma | Piridona amidas como moduladores de los canales de sodio |
| US20140296266A1 (en) | 2013-03-01 | 2014-10-02 | Gilead Sciences, Inc. | Therapeutic compounds |
| BR112015022488A2 (pt) | 2013-03-14 | 2017-07-18 | Genentech Inc | triazolopiridinas substituídas e métodos de uso das mesmas |
| BR112015022096A8 (pt) | 2013-03-15 | 2019-11-26 | Chromocell Corp | compostos moduladores de canal de sódio, composição que os compreende e uso dos mesmos |
| BR112015023397A2 (pt) | 2013-03-15 | 2017-07-18 | Genentech Inc | benzoxazois substituídos e métodos de uso dos mesmos |
| WO2015051043A1 (en) | 2013-10-01 | 2015-04-09 | Amgen Inc. | Biaryl acyl-sulfonamide compounds as sodium channel inhibitors |
| CR20160296A (es) | 2013-11-27 | 2016-09-20 | Genentech Inc | Benzamidas sustituidas y métodos para usarlas |
| EP3166939B1 (en) | 2014-07-07 | 2019-06-05 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
-
2015
- 2015-07-07 EP EP15744417.5A patent/EP3166939B1/en active Active
- 2015-07-07 JP JP2017501012A patent/JP2017525677A/ja active Pending
- 2015-07-07 WO PCT/US2015/039413 patent/WO2016007534A1/en not_active Ceased
- 2015-07-07 US US15/321,335 patent/US10005724B2/en active Active
- 2015-07-07 CN CN201580047074.3A patent/CN106715418A/zh active Pending
-
2018
- 2018-05-24 US US15/988,956 patent/US10125098B2/en not_active Expired - Fee Related
- 2018-10-02 US US16/150,070 patent/US10526285B2/en not_active Expired - Fee Related
-
2019
- 2019-12-03 US US16/702,286 patent/US11149002B2/en not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2015143906A (ru) | Замещенные триазолопиридины и способы их применения | |
| CN103402977B (zh) | 巨大戟二萜醇-3-酰化物iii和巨大戟二萜醇-3-氨基甲酸酯 | |
| JP6353460B2 (ja) | Hbv感染に対する抗ウイルス剤としての官能化ベンズアミド誘導体 | |
| RU2015143834A (ru) | Замещенные бензоксазолы и способы их применения | |
| JP2015523369A5 (enExample) | ||
| RU2007141633A (ru) | Спирогетероциклические соединения и их применение в качестве терапевтических средств | |
| ES2987563T3 (es) | Moduladores del receptor de glucocorticoides ciclohexenilo pirimidina | |
| KR20150036223A (ko) | 질소함유 헤테로고리 유도체 및 그의 약물에서의 용도 | |
| US20190224198A1 (en) | Cap-dependent endonuclease inhibitors | |
| EP2635587A1 (en) | Novel 6-arylamino pyridone carboxamide as mek inhibitors | |
| WO2014204263A1 (en) | Substituted pyridinone compounds as mek inhibitors | |
| HRP20170695T1 (hr) | Fenil-3-aza-biciklo[3.1.0]heks-3-il-metanoni i njihova uporaba u obliku lijeka | |
| JP7201688B2 (ja) | 置換テトラヒドロピランジヒドロチエノピリミジンおよびホスホジエステラーゼ阻害剤としてのそれらの使用 | |
| CN115745979A (zh) | 一种蛋白靶向降解化合物及其用途 | |
| KR20240055751A (ko) | Bcl-2 패밀리 단백질을 분해하는 화합물 및 이의 의약에서의 응용 | |
| RU2762279C2 (ru) | Замещенные пиразолоазепин-4-оны и их применение в качестве ингибиторов фосфодиэстеразы | |
| US11572347B2 (en) | Orally available sEH/PDE4 dual inhibitors | |
| RU2768746C2 (ru) | Замещенные пиразолоазепин-4-оны и их применение в качестве ингибиторов фосфодиэстеразы | |
| JP2025502293A (ja) | チューブリン-srcデュアルターゲット阻害剤としてのジアリール系化合物 | |
| JP2021530532A (ja) | Trk阻害剤としてのイミダゾ[1,2−b]ピリダジン誘導体 | |
| AU2022346718A1 (en) | Fused heterocyclic rings as ripk1 inhibitors | |
| EP3858812B1 (en) | Mdm2 inhibitor, preparation method therefor, pharmaceutical composition thereof, and use thereof | |
| EP3344625A1 (en) | Thiazolo(3,2-a) pyrimidinone and other heterobicyclic pyrimidinone compounds for use in medical therapy | |
| US20230365521A1 (en) | Compounds for increasing the nicotinamide adenine dinucleotide in a subject and methods of use thereof | |
| WO2023136589A1 (en) | Fused heteroaryl hydroxamates as sting agonists |