JP2013526598A5 - - Google Patents
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- Publication number
- JP2013526598A5 JP2013526598A5 JP2013511644A JP2013511644A JP2013526598A5 JP 2013526598 A5 JP2013526598 A5 JP 2013526598A5 JP 2013511644 A JP2013511644 A JP 2013511644A JP 2013511644 A JP2013511644 A JP 2013511644A JP 2013526598 A5 JP2013526598 A5 JP 2013526598A5
- Authority
- JP
- Japan
- Prior art keywords
- ssc
- systemic
- scleroderma
- systemic scleroderma
- fibrosis
- 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.)
- Granted
Links
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 68
- 206010042953 Systemic sclerosis Diseases 0.000 claims 68
- 206010016654 Fibrosis Diseases 0.000 claims 18
- 230000004761 fibrosis Effects 0.000 claims 18
- 239000003814 drug Substances 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 6
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 238000011282 treatment Methods 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 206010039710 Scleroderma Diseases 0.000 claims 4
- 230000000968 intestinal effect Effects 0.000 claims 4
- 208000011379 keloid formation Diseases 0.000 claims 4
- 230000000069 prophylactic effect Effects 0.000 claims 4
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims 4
- -1 4-methylpiperazine- 1-yl Chemical group 0.000 claims 3
- SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 claims 3
- 210000004072 lung Anatomy 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 238000011321 prophylaxis Methods 0.000 claims 3
- 230000002792 vascular Effects 0.000 claims 3
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical compound O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 claims 2
- 206010048768 Dermatosis Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000003449 preventive effect Effects 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 201000002793 renal fibrosis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229960003310 sildenafil Drugs 0.000 claims 2
- 208000017520 skin disease Diseases 0.000 claims 2
- WOXKDUGGOYFFRN-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 WOXKDUGGOYFFRN-IIBYNOLFSA-N 0.000 claims 2
- 229960002381 vardenafil Drugs 0.000 claims 2
- 210000001835 viscera Anatomy 0.000 claims 2
- 230000009278 visceral effect Effects 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- PNDCCASNKRUOMF-AXUFZUPDSA-N CO[C@H]1[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1CO[C@@H](O[C@@H]2[C@@H](O)[C@H](O)CO[C@H]2N2[C@@H](CC(N)=O)C(=O)\C(=C(/O)\C=C\C=C\C=C\C=C\C=C(/Cl)\C=C\C=C(/Cl)[C@H]3O[C@H](C)C[C@@H]3Cl)C2=O)[C@@H](O)[C@@H]1O Chemical compound CO[C@H]1[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1CO[C@@H](O[C@@H]2[C@@H](O)[C@H](O)CO[C@H]2N2[C@@H](CC(N)=O)C(=O)\C(=C(/O)\C=C\C=C\C=C\C=C\C=C(/Cl)\C=C\C=C(/Cl)[C@H]3O[C@H](C)C[C@@H]3Cl)C2=O)[C@@H](O)[C@@H]1O PNDCCASNKRUOMF-AXUFZUPDSA-N 0.000 claims 1
- YNPNZTXNASCQKK-UHFFFAOYSA-N Phenanthrene Natural products C1=CC=C2C3=CC=CC=C3C=CC2=C1 YNPNZTXNASCQKK-UHFFFAOYSA-N 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- DGEZNRSVGBDHLK-UHFFFAOYSA-N [1,10]phenanthroline Chemical compound C1=CN=C2C3=NC=CC=C3C=CC2=C1 DGEZNRSVGBDHLK-UHFFFAOYSA-N 0.000 claims 1
- 229960000307 avanafil Drugs 0.000 claims 1
- WEAJZXNPAWBCOA-INIZCTEOSA-N avanafil Chemical compound C1=C(Cl)C(OC)=CC=C1CNC1=NC(N2[C@@H](CCC2)CO)=NC=C1C(=O)NCC1=NC=CC=N1 WEAJZXNPAWBCOA-INIZCTEOSA-N 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- MIJFNYMSCFYZNY-UHFFFAOYSA-N mirodenafil Chemical compound C1=C(C=2NC=3C(CCC)=CN(CC)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)N1CCN(CCO)CC1 MIJFNYMSCFYZNY-UHFFFAOYSA-N 0.000 claims 1
- 229950002245 mirodenafil Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 229960000835 tadalafil Drugs 0.000 claims 1
- 229960000438 udenafil Drugs 0.000 claims 1
- IYFNEFQTYQPVOC-UHFFFAOYSA-N udenafil Chemical compound C1=C(C=2NC=3C(CCC)=NN(C)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)NCCC1CCCN1C IYFNEFQTYQPVOC-UHFFFAOYSA-N 0.000 claims 1
- 229940075420 xanthine Drugs 0.000 claims 1
- HEBVOFQYGAFWQK-UHFFFAOYSA-M CC(C1)OC(C)CN1S(c(cc1)ccc1NC(c(cc(cc1)Cl)c1[N-]S(c1c(C)[o]nc1C)(=O)=O)=O)(=O)=O Chemical compound CC(C1)OC(C)CN1S(c(cc1)ccc1NC(c(cc(cc1)Cl)c1[N-]S(c1c(C)[o]nc1C)(=O)=O)=O)(=O)=O HEBVOFQYGAFWQK-UHFFFAOYSA-M 0.000 description 1
- YNDMDCJWXXDPFE-UHFFFAOYSA-N Cc1c(COc2ccccc2-c2nc(-[n]3ncc(C(O)=O)c3C(F)(F)F)ccc2)ccc(-c(cc2)ccc2OC(F)(F)F)c1 Chemical compound Cc1c(COc2ccccc2-c2nc(-[n]3ncc(C(O)=O)c3C(F)(F)F)ccc2)ccc(-c(cc2)ccc2OC(F)(F)F)c1 YNDMDCJWXXDPFE-UHFFFAOYSA-N 0.000 description 1
- PLCADJYGXJZMIW-UHFFFAOYSA-M O=C(c(cc(cc1)Cl)c1[N-]S(c([s]1)ccc1Cl)(=O)=O)Nc(cc1)ccc1S(N1CCOCC1)(=O)=O Chemical compound O=C(c(cc(cc1)Cl)c1[N-]S(c([s]1)ccc1Cl)(=O)=O)Nc(cc1)ccc1S(N1CCOCC1)(=O)=O PLCADJYGXJZMIW-UHFFFAOYSA-M 0.000 description 1
- OQBDWBYZWRWNMG-UHFFFAOYSA-N OC(c1c(C(F)(F)F)[n](-c2cccc(-c(cc(cc3)Cl)c3OCc3ccc(C(CC4)CCC4C(F)(F)F)cc3)n2)nc1)=O Chemical compound OC(c1c(C(F)(F)F)[n](-c2cccc(-c(cc(cc3)Cl)c3OCc3ccc(C(CC4)CCC4C(F)(F)F)cc3)n2)nc1)=O OQBDWBYZWRWNMG-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102010021637.2 | 2010-05-26 | ||
| DE102010021637A DE102010021637A1 (de) | 2010-05-26 | 2010-05-26 | Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung |
| EP10170413 | 2010-07-22 | ||
| EP10170413.8 | 2010-07-22 | ||
| PCT/EP2011/058433 WO2011147810A1 (en) | 2010-05-26 | 2011-05-24 | THE USE OF sGC STIMULATORS, sGC ACTIVATORS, ALONE AND COMBINATIONS WITH PDE5 INHIBITORS FOR THE TREATMENT OF SYSTEMIC SCLEROSIS (SSc). |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013526598A JP2013526598A (ja) | 2013-06-24 |
| JP2013526598A5 true JP2013526598A5 (enExample) | 2014-07-10 |
| JP5883852B2 JP5883852B2 (ja) | 2016-03-15 |
Family
ID=45003356
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013511644A Expired - Fee Related JP5883852B2 (ja) | 2010-05-26 | 2011-05-24 | 全身性強皮症（ＳＳｃ）を処置するためのｓＧＣ刺激剤、ｓＧＣアクチベーター単独およびＰＤＥ５阻害剤との組み合わせ剤の使用 |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US10189856B2 (enExample) |
| EP (1) | EP2576548B1 (enExample) |
| JP (1) | JP5883852B2 (enExample) |
| KR (1) | KR101881174B1 (enExample) |
| CN (1) | CN103038232B (enExample) |
| AU (1) | AU2011257336B2 (enExample) |
| CA (2) | CA2955143C (enExample) |
| CL (1) | CL2012003281A1 (enExample) |
| CR (1) | CR20120597A (enExample) |
| CY (1) | CY1116703T1 (enExample) |
| DK (1) | DK2576548T3 (enExample) |
| EA (1) | EA030735B9 (enExample) |
| ES (1) | ES2549979T3 (enExample) |
| HR (1) | HRP20150987T1 (enExample) |
| HU (1) | HUE025162T2 (enExample) |
| IL (1) | IL223128A (enExample) |
| MA (1) | MA34249B1 (enExample) |
| ME (1) | ME02207B (enExample) |
| MX (1) | MX2012013574A (enExample) |
| MY (1) | MY170094A (enExample) |
| NZ (1) | NZ603799A (enExample) |
| PH (1) | PH12012502322A1 (enExample) |
| PL (1) | PL2576548T3 (enExample) |
| PT (1) | PT2576548E (enExample) |
| RS (1) | RS54261B1 (enExample) |
| SG (1) | SG185690A1 (enExample) |
| SI (1) | SI2576548T1 (enExample) |
| TN (1) | TN2012000550A1 (enExample) |
| UA (1) | UA116521C2 (enExample) |
| WO (1) | WO2011147810A1 (enExample) |
| ZA (1) | ZA201208824B (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| EP2594270A3 (en) * | 2011-11-18 | 2013-07-31 | BIP Patents | The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc) |
| 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 |
| 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 |
| MX338887B (es) | 2012-09-07 | 2016-05-04 | Boehringer Ingelheim Int | Alcoxipirazoles como activadores de guanilato ciclasa soluble. |
| EP2897953B8 (en) | 2012-09-19 | 2019-06-26 | Cyclerion Therapeutics, Inc. | Sgc stimulators |
| 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 |
| EP2968330B1 (en) | 2013-03-15 | 2021-09-29 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| WO2015011086A1 (en) | 2013-07-25 | 2015-01-29 | Bayer Pharma Aktiengesellschaft | Sgc stimulators or sgc activators and pde5 inhibitors in combination with additional treatment for the therapy of cystic fibrosis |
| EP3059224B1 (en) | 2013-10-15 | 2019-03-20 | TOA Eiyo Ltd. | 4-aminomethylbenzoic acid derivative |
| WO2015106268A1 (en) | 2014-01-13 | 2015-07-16 | Ironwood Pharmaceuticals, Inc. | USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS |
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| TW201625584A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| AU2015292833B2 (en) | 2014-07-22 | 2019-11-28 | Boehringer Ingelheim International Gmbh | Heterocyclic carboxylic acids as activators of soluble guanylate cyclase |
| TN2017000465A1 (en) * | 2015-05-06 | 2019-04-12 | Bayer Pharma AG | The use of sgc stimulators, sgc activators, alone and combinations with pde5 inhibitors for the treatment of digital ulcers (du) concomitant to systemic sclerosis (ssc) |
| LT3325013T (lt) * | 2015-07-23 | 2020-11-10 | Bayer Pharma Aktiengesellschaft | Tirpios guanilatciklazės (sgc) stimuliatoriai/aktyvatoriai derinyje su nep inhibitoriumi ir (arba) angiotenzino aii antagonistu ir jų naudojimas |
| CN108367165B (zh) * | 2015-10-07 | 2022-03-04 | 艾葳生物科技有限公司 | 治疗皮肤纤维化病症的组合物和方法 |
| KR20180094965A (ko) | 2015-12-14 | 2018-08-24 | 아이언우드 파마슈티컬스, 인코포레이티드 | 위장 괄약근 기능장애의 치료를 위한 sGC 자극제의 용도 |
| CN108473470A (zh) | 2015-12-18 | 2018-08-31 | 诺华股份有限公司 | 作为可溶性鸟苷酸环化酶激活剂的茚满衍生物及其用途 |
| US11357777B2 (en) | 2016-02-01 | 2022-06-14 | Cyclerion Therapeutics, Inc. | Use of sGC stimulators for the treatment of nonalcoholic steatohepatitis (NASH) |
| WO2018111795A2 (en) | 2016-12-13 | 2018-06-21 | Ironwood Pharmaceuticals, Inc. | Use of sgc stimulators for the treatment of esophageal motility disorders |
| US20190388407A1 (en) | 2017-02-12 | 2019-12-26 | Aiviva Biopharma, Inc. | Multikinase inhibitors of vegf and tfg beta and uses thereof |
| KR102615821B1 (ko) | 2017-04-11 | 2023-12-21 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 불소-치환된 인다졸 화합물 및 이의 용도 |
| CN108690016B (zh) * | 2017-04-11 | 2022-08-12 | 广东东阳光药业有限公司 | 吡唑并吡啶类化合物及其用途 |
| US11508483B2 (en) | 2018-05-30 | 2022-11-22 | Adverio Pharma Gmbh | Method of identifying a subgroup of patients suffering from dcSSc which benefits from a treatment with sGC stimulators and sGC activators in a higher degree than a control group |
| US12220414B2 (en) | 2018-07-11 | 2025-02-11 | Tisento Therapeutics Inc. | Use of sGC stimulators for the treatment of mitochondrial disorders |
| JP2021534153A (ja) | 2018-08-15 | 2021-12-09 | アイビバ バイオファーマ インコーポレイテッド | Ｖｅｇｆおよびｔｇｆベータのマルチキナーゼ阻害剤およびその使用 |
| CN111638329B (zh) * | 2020-06-09 | 2021-06-01 | 南方医科大学 | 一种用于检测布鲁氏菌病elispot检测试剂盒及其应用 |
| EP3925953A1 (en) * | 2020-06-16 | 2021-12-22 | Adverio Pharma GmbH | Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate |
| CN115160312B (zh) * | 2022-06-29 | 2023-12-26 | 常州制药厂有限公司 | 一种维立西呱关键中间体及其制备方法 |
| KR20250088783A (ko) | 2022-11-04 | 2025-06-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 전신 경화증을 치료하기 위한 가용성 구아닐레이트 사이클라제 활성제 |
| KR102831482B1 (ko) * | 2022-11-04 | 2025-07-07 | 한국타이어앤테크놀로지 주식회사 | 차량용 타이어의 젖은 노면 제동성능 측정방법 |
| CN117462685A (zh) * | 2023-04-14 | 2024-01-30 | 北京悦康科创医药科技股份有限公司 | Pde5抑制剂或其组合物在制备用于治疗泌尿系统疾病药物中的用途 |
| CN117567461A (zh) * | 2023-10-13 | 2024-02-20 | 佛山奕安赛医药科技有限公司 | 一种维利西呱中间体的制备方法 |
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