JP2019502686A5 - - Google Patents
Download PDFInfo
- Publication number
- 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.)
- Pending
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3389655A2 (enExample) |
| JP (1) | JP2019502686A (enExample) |
| KR (1) | KR20180094965A (enExample) |
| CN (1) | CN108463224A (enExample) |
| AU (1) | AU2016371762A1 (enExample) |
| CA (1) | CA3006764A1 (enExample) |
| EA (1) | EA201891416A1 (enExample) |
| IL (1) | IL259639A (enExample) |
| MX (1) | MX2018007152A (enExample) |
| WO (1) | WO2017106175A2 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10844064B2 (en) * | 2014-09-17 | 2020-11-24 | Cyclerion Therapeutics, Inc. | sGC stimulators |
| WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
| AU2017356887B2 (en) * | 2016-11-08 | 2022-06-30 | Cyclerion Therapeutics, Inc. | sGC stimulators |
| EP3538096B1 (en) * | 2016-11-08 | 2024-02-28 | Tisento Therapeutics Inc. | Treatment of cns diseases with sgc stimulators |
| WO2018111795A2 (en) * | 2016-12-13 | 2018-06-21 | Ironwood Pharmaceuticals, Inc. | Use of sgc stimulators for the treatment of esophageal motility disorders |
| US12220414B2 (en) * | 2018-07-11 | 2025-02-11 | Tisento Therapeutics Inc. | Use of sGC stimulators for the treatment of mitochondrial disorders |
| WO2022265984A1 (en) * | 2021-06-14 | 2022-12-22 | Curtails Llc | Use of nep inhibitors for the treatment of gastrointestinal sphincter disorders |
| JP2025515296A (ja) * | 2022-04-20 | 2025-05-14 | シャンハイ ジムン バイオファーマ，インコーポレーテッド | Ｒｈｏ関連プロテインキナーゼ阻害剤ならびにその調製および応用 |
Family Cites Families (111)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| GB8928043D0 (en) * | 1989-12-12 | 1990-02-14 | Pfizer Ltd | Muscarinic receptor antagonists |
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
| JP2928079B2 (ja) | 1994-02-14 | 1999-07-28 | 永信薬品工業股▲ふん▼有限公司 | １−（置換ベンジル）−３−（置換アリール）縮合ピラゾール類、その製造法及びその用途 |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| DE19642255A1 (de) | 1996-10-14 | 1998-04-16 | Bayer Ag | Verwendung von 1-Benzyl-3-(substituierten-hetaryl) -kondensierten Pyrazol-Derivaten |
| ATE431347T1 (de) | 1996-10-14 | 2009-05-15 | Bayer Healthcare Ag | Neue heterocyclylmethyl-substituierte pyrazolderivate und ihre verwendung in der behandlung von herz-kreislauf-erkrankungen |
| DE19649460A1 (de) | 1996-11-26 | 1998-05-28 | Bayer Ag | Neue substituierte Pyrazolderivate |
| DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| US6451805B1 (en) | 1997-11-14 | 2002-09-17 | Bayer Aktiengesellschaft | Substituted pyrazole derivatives for the treatment of cardiocirculatory diseases |
| CZ302691B6 (cs) | 1998-07-08 | 2011-09-07 | Sanofi - Aventis Deutschland GmbH | N-Arylamidová sloucenina, zpusob její prípravy, farmaceutický prostredek tuto slouceninu obsahující, tato sloucenina pro použití jako aktivátor a pro použití k terapii nebo profylaxi |
| DE19830430A1 (de) | 1998-07-08 | 2000-01-13 | Hoechst Marion Roussel De Gmbh | Schwefelsubstituierte Sulfonylamino-carbonsäure-N-arylamide, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| DE19834044A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Neue substituierte Pyrazolderivate |
| DE19834045A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | (4-Amino-5-ethylpyrimidin-2-yl)-1-(2-fluorbenzyl)-1H-pyrazolo[3,4-b]pyridin |
| DE19834047A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Substituierte Pyrazolderivate |
| DE19846514A1 (de) | 1998-10-09 | 2000-04-20 | Bayer Ag | Neue Heterocyclyl-methyl-substituierte Pyrazole |
| GB9824310D0 (en) | 1998-11-05 | 1998-12-30 | Univ London | Activators of soluble guanylate cyclase |
| DE19920352A1 (de) | 1999-05-04 | 2000-11-09 | Bayer Ag | Substituiertes Pyrazolderivat |
| DE19942809A1 (de) | 1999-09-08 | 2001-03-15 | Bayer Ag | Verfahren zur Herstellung substituierter Pyrimidinderivate |
| DE19943635A1 (de) | 1999-09-13 | 2001-03-15 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| DE19962926A1 (de) | 1999-12-24 | 2001-06-28 | Bayer Ag | Verfahren zur Co-Mahlung von Stoffen und Lactose mittels Strahlmühlen |
| DE10021069A1 (de) | 2000-04-28 | 2001-10-31 | Bayer Ag | Substituiertes Pyrazolderivat |
| DE10054278A1 (de) | 2000-11-02 | 2002-05-08 | Bayer Ag | Verwendung von Stimulatoren der löslichen Guanylatcyclase zur Behandlung von Osteoporose |
| AR031176A1 (es) | 2000-11-22 | 2003-09-10 | Bayer Ag | Nuevos derivados de pirazolpiridina sustituidos con piridina |
| DE10057754A1 (de) | 2000-11-22 | 2002-05-23 | Bayer Ag | Neue Sulfonamid-substituierte Pyrazolopyridinderivate |
| AU2002221827A1 (en) | 2000-11-22 | 2002-06-03 | Bayer Aktiengesellschaft | Novel lactame-substituted pyrazolopyridine derivatives |
| DE10057751A1 (de) | 2000-11-22 | 2002-05-23 | Bayer Ag | Neue Carbamat-substituierte Pyrazolopyridinderivate |
| BR0206980A (pt) * | 2001-02-05 | 2004-07-06 | Michael Albert Kamm | Uso de um modulador do tÈnus do músculo liso |
| DE10122894A1 (de) | 2001-05-11 | 2002-11-14 | Bayer Ag | Neue Sulfonat-substituierte Pyrazolopyridinderivate |
| DE10132416A1 (de) | 2001-07-04 | 2003-01-16 | Bayer Ag | Neue Morpholin-überbrückte Pyrazolopyridinderivate |
| GB0207104D0 (en) * | 2002-03-26 | 2002-05-08 | Pfizer Ltd | Stable hydrate of a muscarinic receptor antagonist |
| DE10216145A1 (de) | 2002-04-12 | 2003-10-23 | Bayer Ag | Verwendung von Stimulatoren der löslichen Guanylatcyclase zur Behandlung von Glaukom |
| DE10220570A1 (de) | 2002-05-08 | 2003-11-20 | Bayer Ag | Carbamat-substituierte Pyrazolopyridine |
| DE10222550A1 (de) | 2002-05-17 | 2003-11-27 | Bayer Ag | Substituierte Benzyl-pyrazolopyridine |
| DE10232571A1 (de) | 2002-07-18 | 2004-02-05 | Bayer Ag | 4-Aminosubstituierte Pyrimidinderivate |
| DE10232572A1 (de) | 2002-07-18 | 2004-02-05 | Bayer Ag | Neue 2,5-disubstituierte Pyrimidinderivate |
| DE10242941A1 (de) | 2002-09-16 | 2004-03-18 | Bayer Ag | Substituiertes Pyrazolderivat |
| DE10244810A1 (de) | 2002-09-26 | 2004-04-08 | Bayer Ag | Neue Morpholin-überbrückte Indazolderivate |
| DE102006020327A1 (de) | 2006-04-27 | 2007-12-27 | Bayer Healthcare Ag | Heterocyclisch substituierte, anellierte Pyrazol-Derivate und ihre Verwendung |
| DE102006021733A1 (de) | 2006-05-09 | 2007-11-22 | Bayer Healthcare Ag | 3-Tetrazolylindazole und 3-Tetrazolylpyrazolopyridine sowie ihre Verwendung |
| DE102006043443A1 (de) | 2006-09-15 | 2008-03-27 | Bayer Healthcare Ag | Neue aza-bicyclische Verbindungen und ihre Verwendung |
| DE102006054757A1 (de) | 2006-11-21 | 2008-05-29 | Bayer Healthcare Ag | Neue aza-bicyclische Verbindungen und ihre Verwendung |
| CN101939053A (zh) | 2007-09-06 | 2011-01-05 | 默沙东公司 | 可溶性的鸟苷酸环化酶活化剂 |
| US8397065B2 (en) | 2007-10-17 | 2013-03-12 | Telcordia Technologies, Inc. | Secure content based routing in mobile ad hoc networks |
| CA2711134A1 (en) | 2008-01-24 | 2009-07-30 | Merck Sharp & Dohme Corp. | Angiotensin ii receptor antagonists |
| CA2743864A1 (en) | 2008-11-25 | 2010-06-10 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| DE102008063992A1 (de) | 2008-12-19 | 2010-09-02 | Lerner, Zinoviy, Dipl.-Ing. | Neue aliphatisch substituierte Pyrazolopyridine und ihre Verwendung |
| DE102009004245A1 (de) | 2009-01-09 | 2010-07-15 | Bayer Schering Pharma Aktiengesellschaft | Neue anellierte, Heteroatom-verbrückte Pyrazol- und Imidazol-Derivate und ihre Verwendung |
| CA2753434C (en) | 2009-02-26 | 2014-07-15 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| RU2430726C2 (ru) * | 2009-09-28 | 2011-10-10 | Иван Сергеевич Рагинов | Способ лечения ахалазии пищевода |
| UY33041A (es) | 2009-11-27 | 2011-06-30 | Bayer Schering Pharma Aktienegesellschaft | Procedimiento para la preparaciòn de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificaciòn para el uso como principio activo farmacèutico |
| DK3415515T3 (da) | 2009-11-27 | 2020-03-16 | Adverio Pharma Gmbh | Fremgangsmåde til fremstilling af methyl-{4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamat |
| EP2513101A1 (de) | 2009-12-14 | 2012-10-24 | Bayer Intellectual Property GmbH | Neue solvate von methyl{4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamat |
| US20130178475A1 (en) | 2010-03-17 | 2013-07-11 | Ironwood Pharmaceuticals, Inc. | sGC STIMULATORS |
| US9284301B2 (en) | 2010-03-25 | 2016-03-15 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| ES2549979T3 (es) | 2010-05-26 | 2015-11-03 | Adverio Pharma Gmbh | El uso de estimuladores de la sGC, activadores de la sGC, solos y en combinaciones con inhibidores de la PDE5 para el tratamiento de esclerosis sistémica (EcS) |
| DE102010021637A1 (de) | 2010-05-26 | 2011-12-01 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung |
| UA107112C2 (uk) | 2010-05-27 | 2014-11-25 | Мерк Шарп Енд Доме Корп. | Активатори розчинної гуанілатциклази |
| TWI532737B (zh) | 2010-06-30 | 2016-05-11 | 艾諾屋製藥公司 | 可溶性鳥苷酸環化酶（ｓＧＣ）刺激物 |
| EP2590979A1 (de) | 2010-07-09 | 2013-05-15 | Bayer Intellectual Property GmbH | Annellierte pyrimidine und triazine und ihre verwendung zur behandlung bzw. prophylaxe von herz-kreislauf-erkrankungen |
| JP5940062B2 (ja) | 2010-07-09 | 2016-06-29 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 環縮合４−アミノピリミジンおよび可溶性グアニル酸シクラーゼの刺激剤としてのその使用 |
| DE102010031667A1 (de) | 2010-07-22 | 2012-01-26 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Methyl-pyrimidin-5-ylcarbamate und ihre Verwendung |
| DE102010031665A1 (de) | 2010-07-22 | 2012-01-26 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Oxazolidinone und Oxazinanone und ihre Verwendung |
| DE102010040233A1 (de) | 2010-09-03 | 2012-03-08 | Bayer Schering Pharma Aktiengesellschaft | Bicyclische Aza-Heterocyclen und ihre Verwendung |
| WO2012058132A1 (en) | 2010-10-28 | 2012-05-03 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| DE102010043379A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung |
| JP5878546B2 (ja) | 2010-11-09 | 2016-03-08 | アイアンウッド ファーマシューティカルズ インコーポレイテッド | ｓＧＣ刺激剤 |
| US20140171434A1 (en) | 2011-01-11 | 2014-06-19 | Bayer Pharma Aktiengessellschaft | Substituted imidazopyridines and imidazopyridazines and the use thereof |
| WO2012143510A1 (de) | 2011-04-21 | 2012-10-26 | Bayer Intellectual Property Gmbh | Fluoralkyl-substituierte pyrazolopyridine und ihre verwendung |
| DE102011075398A1 (de) | 2011-05-06 | 2012-11-08 | Bayer Pharma Aktiengesellschaft | Substituierte Imidazopyridazine und ihre Verwendung |
| EP2716642B1 (en) | 2011-05-30 | 2016-07-20 | Astellas Pharma Inc. | Imidazopyridine compound |
| CN103906752B (zh) | 2011-07-06 | 2016-08-24 | 拜耳知识产权有限责任公司 | 杂芳基取代的吡唑并吡啶及其用作可溶性鸟苷酸环化酶刺激剂的用途 |
| BR112014005110A2 (pt) | 2011-09-02 | 2017-04-18 | Bayer Ip Gmbh | pirimidinas aneladas substituídas e utilização das mesmas |
| HUE053745T2 (hu) | 2011-11-25 | 2021-07-28 | Adverio Pharma Gmbh | Helyettesített 5-fluor-1H-pirazolopiridin kristályos formában |
| CN102491974B (zh) | 2011-12-12 | 2013-08-07 | 南京药石药物研发有限公司 | 1-（2-氟苄基）-1H-吡唑并[3，4-b]吡啶-3-甲脒盐酸盐的合成方法 |
| CA2861804C (en) | 2011-12-27 | 2021-10-26 | Ironwood Pharmaceuticals, Inc. | 2-benzyl,3(pyrimidin-2-yl)substituted pyrazoles useful as sgc stimulators |
| DE102012200352A1 (de) | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte, annellierte Imidazole und Pyrazole und ihre Verwendung |
| DE102012200360A1 (de) | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte Triazine und ihre Verwendung |
| DE102012200349A1 (de) | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte annellierte Pyrimidine und Triazine und ihre Verwendung |
| JP6140738B2 (ja) | 2012-03-06 | 2017-05-31 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 置換アザ二環およびその使用 |
| WO2014047111A1 (en) | 2012-09-18 | 2014-03-27 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| EP2897953B8 (en) | 2012-09-19 | 2019-06-26 | Cyclerion Therapeutics, Inc. | Sgc stimulators |
| US8796305B2 (en) | 2012-11-05 | 2014-08-05 | Bayer Pharma Aktiengesellschaft | Carboxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use |
| US9126998B2 (en) | 2012-11-05 | 2015-09-08 | Bayer Pharma AG | Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use |
| US9624214B2 (en) | 2012-11-05 | 2017-04-18 | Bayer Pharma Aktiengesellschaft | Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use |
| US8778964B2 (en) | 2012-11-05 | 2014-07-15 | Bayer Pharma Aktiengesellschaft | Hydroxy-substituted imidazo[1,2-a]-pyridinecarboxamides and their use |
| EP2927231B1 (en) | 2012-11-30 | 2017-09-20 | Astellas Pharma Inc. | Imidazopyridine compounds |
| CA2901636A1 (en) | 2013-02-21 | 2014-08-28 | Adverio Pharma Gmbh | Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate |
| HK1220974A1 (zh) | 2013-03-01 | 2017-05-19 | Bayer Pharma Aktiengesellschaft | 三氟甲基取代的稠合嘧啶类及其用途 |
| WO2014131741A1 (de) | 2013-03-01 | 2014-09-04 | Bayer Pharma Aktiengesellschaft | Benzyl-substituierte pyrazolopyridine und ihre verwendung |
| ES2911276T3 (es) | 2013-03-15 | 2022-05-18 | Cyclerion Therapeutics Inc | Estimuladores de sGC |
| US9776997B2 (en) | 2013-06-04 | 2017-10-03 | Bayer Pharma Aktiengesellschaft | 3-aryl-substituted imidazo[1,2-A]pyridines and their use |
| CA2920565A1 (en) | 2013-08-08 | 2015-02-12 | Bayer Pharma Aktiengesellschaft | Substituted pyrazolo[1,5-a]pyridine-3-carboxamides and use thereof |
| WO2015082411A1 (de) | 2013-12-05 | 2015-06-11 | Bayer Pharma Aktiengesellschaft | Aryl- und hetaryl-substituierte imidazo[1,2-a]pyridin-3-carboxamide und ihre verwendung |
| JP2016540017A (ja) | 2013-12-11 | 2016-12-22 | アイアンウッド ファーマシューティカルズ インコーポレイテッド | ｓＧＣ刺激物質 |
| EP3079700B1 (en) | 2013-12-11 | 2020-11-25 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| WO2015088885A1 (en) | 2013-12-11 | 2015-06-18 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| WO2015106268A1 (en) * | 2014-01-13 | 2015-07-16 | Ironwood Pharmaceuticals, Inc. | USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS |
| CN106459090A (zh) | 2014-02-19 | 2017-02-22 | 拜耳制药股份公司 | 3‑(嘧啶‑2‑基)咪唑并[1,2‑a]吡啶 |
| WO2015140199A1 (de) | 2014-03-21 | 2015-09-24 | Bayer Pharma Aktiengesellschaft | Cyano-substituierte imidazo[1,2-a]pyridincarboxamide und ihre verwendung |
| JP2017508811A (ja) | 2014-03-21 | 2017-03-30 | バイエル・ファルマ・アクティエンゲゼルシャフト | 置換イミダゾ［１，２−ａ］ピリジンカルボキサミドおよびその使用 |
| WO2015150366A1 (de) | 2014-04-03 | 2015-10-08 | Bayer Pharma Aktiengesellschaft | Cyclisch substituierte phenolether-derivate und ihre verwendung |
| CN106458938A (zh) | 2014-04-03 | 2017-02-22 | 拜耳制药股份公司 | 手性2,5‑二取代的环戊烷甲酸衍生物及其用途 |
| WO2015150364A1 (de) | 2014-04-03 | 2015-10-08 | Bayer Pharma Aktiengesellschaft | Substituierte benzotriazinonbutansäuren und ihre verwendung |
| US20170114049A1 (en) | 2014-04-03 | 2017-04-27 | Bayer Pharma Aktiengesellschaft | 2,5-disubstituted cyclopentane carboxylic acids for the treatment of respiratory tract diseases |
| WO2015150363A1 (de) | 2014-04-03 | 2015-10-08 | Bayer Pharma Aktiengesellschaft | 2,5-disubstituierte cyclopentancarbonsäuren und ihre verwendung |
| WO2016044445A2 (en) | 2014-09-17 | 2016-03-24 | Ironwood Pharmaceuticals, Inc. | sGC STIMULATORS |
| CN107223125B (zh) | 2014-09-17 | 2019-09-27 | 赛科理音医疗有限公司 | sGC刺激剂 |
| US10844064B2 (en) | 2014-09-17 | 2020-11-24 | Cyclerion Therapeutics, Inc. | sGC stimulators |
| EP3194382B1 (en) | 2014-09-17 | 2021-09-08 | Cyclerion Therapeutics, Inc. | Pyrazole derivatives as sgc stimulators |
-
2016
- 2016-12-13 KR KR1020187019784A patent/KR20180094965A/ko not_active Withdrawn
- 2016-12-13 CA CA3006764A patent/CA3006764A1/en not_active Abandoned
- 2016-12-13 WO PCT/US2016/066357 patent/WO2017106175A2/en not_active Ceased
- 2016-12-13 AU AU2016371762A patent/AU2016371762A1/en not_active Abandoned
- 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 EA EA201891416A patent/EA201891416A1/ru unknown
- 2016-12-13 US US16/061,992 patent/US20180344735A1/en not_active Abandoned
- 2016-12-13 MX MX2018007152A patent/MX2018007152A/es unknown
- 2016-12-13 CN CN201680078621.9A patent/CN108463224A/zh active Pending
-
2018
- 2018-05-28 IL IL259639A patent/IL259639A/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2023506410A5 (enExample) | ||
| JP2017531019A5 (enExample) | ||
| RU2014105624A (ru) | Соединения индазола, способ их применения и фармацевтическая композиция | |
| JP2019520417A5 (enExample) | ||
| WO2020131631A1 (en) | Bicyclic derivatives | |
| JP2008509187A5 (enExample) | ||
| EA031655B1 (ru) | Бензимидазол-2-амины в качестве ингибиторов midhi | |
| IL273169B1 (en) | New combination of active agents for the treatment of progressive fibrosing interstitial lung diseases (pf-ild) | |
| RU2005137276A (ru) | Замещенные дигидрохиназолины с противовирусными свойствами | |
| RU2008142841A (ru) | СОЕДИНЕНИЯ ИМИДАЗО-[1, 2-b]-ПИРИДАЗИНА (ВАРИАНТЫ), СПОСОБ ПОЛУЧЕНИЯ СОЕДИНЕНИЙ ИМИДАЗО-[1, 2-b]-ПИРИДАЗИНА (ВАРИАНТЫ), ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ЛЕКАРСТВЕННОЕ СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ И/ИЛИ ПРЕДУПРЕЖДЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С МОДУЛЯЦИЕЙ ГАМКА РЕЦЕПТОРОВ | |
| RU2011121567A (ru) | Изоиндолиновые соединения для применения при лечении рака | |
| JP2019507185A5 (enExample) | ||
| JP2010500376A5 (enExample) | ||
| JP2022500425A5 (enExample) | ||
| RU2009132188A (ru) | Режим дозирования ингибиторов комт | |
| JP2021530513A5 (enExample) | ||
| JP2019520344A5 (enExample) | ||
| JP2024520654A5 (enExample) | ||
| PE20220964A1 (es) | Derivados de n-metil, n-(6-(metoxi)piridazin-3-il) amina como moduladores de autotaxina (atx) para el tratamiento de enfermedades inflamatorias de las vias respiratorias o fibroticas | |
| JP2021518379A5 (enExample) | ||
| JP2006512366A5 (enExample) | ||
| RU2007106930A (ru) | Производные хиназолина | |
| JP2022549601A5 (enExample) | ||
| JP2005514370A5 (enExample) | ||
| JP2021505537A5 (enExample) |