JP2019502686A5 - - Google Patents
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- JP2019502686A5 JP2019502686A5 JP2018531178A JP2018531178A JP2019502686A5 JP 2019502686 A5 JP2019502686 A5 JP 2019502686A5 JP 2018531178 A JP2018531178 A JP 2018531178A JP 2018531178 A JP2018531178 A JP 2018531178A JP 2019502686 A5 JP2019502686 A5 JP 2019502686A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- ring
- membered heterocyclic
- phenyl
- membered
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 188
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 183
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 182
- 229910052736 halogen Inorganic materials 0.000 claims description 126
- 150000002367 halogens Chemical class 0.000 claims description 126
- 125000004043 oxo group Chemical group O=* 0.000 claims description 100
- 229910052760 oxygen Inorganic materials 0.000 claims description 100
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 96
- 125000005842 heteroatom Chemical group 0.000 claims description 96
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 92
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 89
- 229910052739 hydrogen Inorganic materials 0.000 claims description 80
- 239000001257 hydrogen Substances 0.000 claims description 80
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims description 69
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims description 58
- 229910052717 sulfur Inorganic materials 0.000 claims description 55
- 125000002619 bicyclic group Chemical group 0.000 claims description 54
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 53
- 150000002431 hydrogen Chemical class 0.000 claims description 47
- 229910052757 nitrogen Inorganic materials 0.000 claims description 44
- 206010030136 Oesophageal achalasia Diseases 0.000 claims description 43
- 208000000289 Esophageal Achalasia Diseases 0.000 claims description 42
- 201000000621 achalasia Diseases 0.000 claims description 42
- 125000001072 heteroaryl group Chemical group 0.000 claims description 41
- 125000002723 alicyclic group Chemical group 0.000 claims description 36
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 35
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 claims description 33
- 210000005070 sphincter Anatomy 0.000 claims description 27
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 25
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 23
- 125000004429 atom Chemical group 0.000 claims description 22
- 229910052799 carbon Inorganic materials 0.000 claims description 21
- 239000003814 drug Substances 0.000 claims description 20
- 210000000111 lower esophageal sphincter Anatomy 0.000 claims description 19
- 229940124597 therapeutic agent Drugs 0.000 claims description 19
- 230000002496 gastric effect Effects 0.000 claims description 18
- 125000001931 aliphatic group Chemical group 0.000 claims description 17
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 16
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 16
- 125000003003 spiro group Chemical group 0.000 claims description 16
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 15
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 13
- 125000006413 ring segment Chemical group 0.000 claims description 12
- 208000035475 disorder Diseases 0.000 claims description 11
- 125000001153 fluoro group Chemical group F* 0.000 claims description 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 10
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 206010020772 Hypertension Diseases 0.000 claims description 7
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 7
- 230000001631 hypertensive effect Effects 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 239000002840 nitric oxide donor Substances 0.000 claims description 6
- 230000001148 spastic effect Effects 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 206010001935 American trypanosomiasis Diseases 0.000 claims description 4
- -1 C 1-4 haloal Kokishi Chemical group 0.000 claims description 4
- 208000024699 Chagas disease Diseases 0.000 claims description 4
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical group O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims description 4
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 4
- 241000223109 Trypanosoma cruzi Species 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 229960001597 nifedipine Drugs 0.000 claims description 4
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical group COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 claims description 4
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 3
- 125000004122 cyclic group Chemical group 0.000 claims description 3
- 125000001188 haloalkyl group Chemical group 0.000 claims description 3
- 229940125526 sGC activator Drugs 0.000 claims description 3
- 239000000021 stimulant Substances 0.000 claims description 3
- 229940127280 BAY 41-2272 Drugs 0.000 claims description 2
- ATOAHNRJAXSBOR-UHFFFAOYSA-N BAY 41-2272 Chemical compound NC1=NC(C=2C3=CC=CN=C3N(CC=3C(=CC=CC=3)F)N=2)=NC=C1C1CC1 ATOAHNRJAXSBOR-UHFFFAOYSA-N 0.000 claims description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 206010019196 Head injury Diseases 0.000 claims description 2
- 229910002651 NO3 Inorganic materials 0.000 claims description 2
- 208000028373 Neck injury Diseases 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 208000025966 Neurological disease Diseases 0.000 claims description 2
- IOVCWXUNBOPUCH-UHFFFAOYSA-M Nitrite anion Chemical compound [O-]N=O IOVCWXUNBOPUCH-UHFFFAOYSA-M 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims description 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims description 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims description 2
- 108010057266 Type A Botulinum Toxins Proteins 0.000 claims description 2
- 229940089093 botox Drugs 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 239000000480 calcium channel blocker Substances 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 208000014674 injury Diseases 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 230000000626 neurodegenerative effect Effects 0.000 claims description 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N nitrate group Chemical group [N+](=O)([O-])[O-] NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims description 2
- FBUKVWPVBMHYJY-UHFFFAOYSA-N nonanoic acid Chemical compound CCCCCCCCC(O)=O FBUKVWPVBMHYJY-UHFFFAOYSA-N 0.000 claims description 2
- 208000012111 paraneoplastic syndrome Diseases 0.000 claims description 2
- 230000037361 pathway Effects 0.000 claims description 2
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims description 2
- 238000009097 single-agent therapy Methods 0.000 claims description 2
- ICRHORQIUXBEPA-UHFFFAOYSA-N thionitrous acid Chemical compound SN=O ICRHORQIUXBEPA-UHFFFAOYSA-N 0.000 claims description 2
- 229930192474 thiophene Natural products 0.000 claims description 2
- 230000008733 trauma Effects 0.000 claims description 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 28
- 239000000203 mixture Substances 0.000 claims 24
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 22
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000000034 method Methods 0.000 description 37
- 125000001424 substituent group Chemical group 0.000 description 12
- 125000004432 carbon atom Chemical group C* 0.000 description 8
- 210000005072 internal anal sphincter Anatomy 0.000 description 6
- 208000005392 Spasm Diseases 0.000 description 5
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 3
- 210000001187 pylorus Anatomy 0.000 description 3
- 125000001963 4 membered heterocyclic group Chemical group 0.000 description 2
- 230000004064 dysfunction Effects 0.000 description 2
- 239000011737 fluorine Substances 0.000 description 2
- 235000019000 fluorine Nutrition 0.000 description 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- VAIBMQLMFYXTLJ-UHFFFAOYSA-N 2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]-5-pyridin-4-ylpyrimidin-4-amine Chemical compound NC1=NC(C=2C3=CC=CN=C3N(CC=3C(=CC=CC=3)F)N=2)=NC=C1C1=CC=NC=C1 VAIBMQLMFYXTLJ-UHFFFAOYSA-N 0.000 description 1
- PQHLRGARXNPFCF-UHFFFAOYSA-N 5-chloro-2-[(5-chlorothiophen-2-yl)sulfonylamino]-n-(4-morpholin-4-ylsulfonylphenyl)benzamide Chemical group S1C(Cl)=CC=C1S(=O)(=O)NC1=CC=C(Cl)C=C1C(=O)NC1=CC=C(S(=O)(=O)N2CCOCC2)C=C1 PQHLRGARXNPFCF-UHFFFAOYSA-N 0.000 description 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical group [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 1
- 208000016534 Idiopathic achalasia Diseases 0.000 description 1
- YWQFJNWMWZMXRW-FQEVSTJZSA-N NC([C@@](CNc(nc(-c1n[n](Cc(cccc2)c2F)c(-c2n[o]cc2)c1)nc1)c1F)(C(F)(F)F)O)=O Chemical compound NC([C@@](CNc(nc(-c1n[n](Cc(cccc2)c2F)c(-c2n[o]cc2)c1)nc1)c1F)(C(F)(F)F)O)=O YWQFJNWMWZMXRW-FQEVSTJZSA-N 0.000 description 1
- 229910003827 NRaRb Inorganic materials 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 229950007878 ataciguat Drugs 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229950002128 cinaciguat Drugs 0.000 description 1
- WPYWMXNXEZFMAK-UHFFFAOYSA-N cinaciguat Chemical compound C=1C=C(C(O)=O)C=CC=1CN(CCCCC(=O)O)CCC1=CC=CC=C1OCC(C=C1)=CC=C1CCC1=CC=CC=C1 WPYWMXNXEZFMAK-UHFFFAOYSA-N 0.000 description 1
- 230000036461 convulsion Effects 0.000 description 1
- 229950006400 etriciguat Drugs 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- WXXSNCNJFUAIDG-UHFFFAOYSA-N riociguat Chemical group N1=C(N)C(N(C)C(=O)OC)=C(N)N=C1C(C1=CC=CN=C11)=NN1CC1=CC=CC=C1F WXXSNCNJFUAIDG-UHFFFAOYSA-N 0.000 description 1
- 229960000529 riociguat Drugs 0.000 description 1
- 210000004514 sphincter of oddi Anatomy 0.000 description 1
- QZFHIXARHDBPBY-UHFFFAOYSA-N vericiguat Chemical compound N1=C(N)C(NC(=O)OC)=C(N)N=C1C(C1=CC(F)=CN=C11)=NN1CC1=CC=CC=C1F QZFHIXARHDBPBY-UHFFFAOYSA-N 0.000 description 1
- 229950005018 vericiguat Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562266988P | 2015-12-14 | 2015-12-14 | |
| US62/266,988 | 2015-12-14 | ||
| PCT/US2016/066357 WO2017106175A2 (en) | 2015-12-14 | 2016-12-13 | USE OF sGC STIMULATORS FOR THE TREATMENT OF GASTROINTESTINAL SPHINCTER DYSFUNCTION |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019502686A JP2019502686A (ja) | 2019-01-31 |
| JP2019502686A5 true JP2019502686A5 (https=) | 2020-01-30 |
Family
ID=58737844
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018531178A Pending JP2019502686A (ja) | 2015-12-14 | 2016-12-13 | 消化管括約筋機能障害の治療へのｓＧＣ刺激薬の使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20180344735A1 (https=) |
| EP (1) | EP3389655A2 (https=) |
| JP (1) | JP2019502686A (https=) |
| KR (1) | KR20180094965A (https=) |
| CN (1) | CN108463224A (https=) |
| AU (1) | AU2016371762A1 (https=) |
| CA (1) | CA3006764A1 (https=) |
| EA (1) | EA201891416A1 (https=) |
| IL (1) | IL259639A (https=) |
| MX (1) | MX2018007152A (https=) |
| WO (1) | WO2017106175A2 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3194386A2 (en) * | 2014-09-17 | 2017-07-26 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
| CN110267949A (zh) * | 2016-11-08 | 2019-09-20 | 塞科里昂医疗股份有限公司 | sGC刺激剂 |
| ES2972711T3 (es) | 2016-11-08 | 2024-06-14 | Tisento Therapeutics Inc | Tratamiento de enfermedades del CNS con estimuladores de la GCs |
| EP3554488A2 (en) * | 2016-12-13 | 2019-10-23 | Cyclerion Therapeutics, Inc. | Use of sgc stimulators for the treatment of esophageal motility disorders |
| KR20250141845A (ko) * | 2018-07-11 | 2025-09-29 | 티센토 쎄라퓨틱스 인크. | 미토콘드리아 장애의 치료를 위한 sGC 자극제의 용도 |
| WO2022265984A1 (en) * | 2021-06-14 | 2022-12-22 | Curtails Llc | Use of nep inhibitors for the treatment of gastrointestinal sphincter disorders |
| WO2023202642A1 (zh) * | 2022-04-20 | 2023-10-26 | 上海挚盟医药科技有限公司 | Rho相关蛋白激酶抑制剂及其制备和应用 |
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-
2016
- 2016-12-13 US US16/061,992 patent/US20180344735A1/en not_active Abandoned
- 2016-12-13 EA EA201891416A patent/EA201891416A1/ru unknown
- 2016-12-13 WO PCT/US2016/066357 patent/WO2017106175A2/en not_active Ceased
- 2016-12-13 CA CA3006764A patent/CA3006764A1/en not_active Abandoned
- 2016-12-13 AU AU2016371762A patent/AU2016371762A1/en not_active Abandoned
- 2016-12-13 CN CN201680078621.9A patent/CN108463224A/zh active Pending
- 2016-12-13 KR KR1020187019784A patent/KR20180094965A/ko not_active Withdrawn
- 2016-12-13 JP JP2018531178A patent/JP2019502686A/ja active Pending
- 2016-12-13 EP EP16867373.9A patent/EP3389655A2/en not_active Withdrawn
- 2016-12-13 MX MX2018007152A patent/MX2018007152A/es unknown
-
2018
- 2018-05-28 IL IL259639A patent/IL259639A/en unknown
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