JP2015527394A5 - - Google Patents
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- Publication number
- JP2015527394A5 JP2015527394A5 JP2015531142A JP2015531142A JP2015527394A5 JP 2015527394 A5 JP2015527394 A5 JP 2015527394A5 JP 2015531142 A JP2015531142 A JP 2015531142A JP 2015531142 A JP2015531142 A JP 2015531142A JP 2015527394 A5 JP2015527394 A5 JP 2015527394A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound according
- pharmaceutically acceptable
- acceptable salt
- compound
- 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
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- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 22
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- -1 2-oxabicyclo [3.2.0] heptanyl Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 230000003176 fibrotic effect Effects 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000004106 butoxy group Chemical group [*]OC([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 208000020629 overactive bladder Diseases 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen 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
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261697899P | 2012-09-07 | 2012-09-07 | |
| US61/697,899 | 2012-09-07 | ||
| PCT/US2013/057826 WO2014039434A1 (en) | 2012-09-07 | 2013-09-03 | Alkoxy pyrazoles as soluble guanylate cyclase activators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015527394A JP2015527394A (ja) | 2015-09-17 |
| JP2015527394A5 true JP2015527394A5 (https=) | 2016-02-12 |
| JP5970134B2 JP5970134B2 (ja) | 2016-08-17 |
Family
ID=49170904
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015531142A Active JP5970134B2 (ja) | 2012-09-07 | 2013-09-03 | 可溶性グアニル酸シクラーゼ活性化因子としてのアルコキシピラゾール |
Country Status (37)
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20191755T1 (hr) * | 2012-09-07 | 2019-12-27 | Boehringer Ingelheim International Gmbh | Alkoksipirazoli kao aktivatori topljive gvanilat ciklaze |
| 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 |
| PL3172202T3 (pl) * | 2014-07-22 | 2020-07-13 | Boehringer Ingelheim International Gmbh | Heterocykliczne kwasy karboksylowe jako aktywatory rozpuszczalnej cyklazy guanylanowej |
| CA3008776A1 (en) | 2015-12-18 | 2017-06-22 | Novartis Ag | Indane derivatives and the use thereof as soluble guanylate cyclase activators |
| CN109890379A (zh) | 2016-10-11 | 2019-06-14 | 拜耳制药股份公司 | 包含sGC活化剂和盐皮质激素受体拮抗剂的组合产品 |
| WO2019081456A1 (en) | 2017-10-24 | 2019-05-02 | Bayer Aktiengesellschaft | USE OF SGC ACTIVATORS AND STIMULATORS COMPRISING A BETA2 SUBUNIT |
| EP3498298A1 (en) | 2017-12-15 | 2019-06-19 | Bayer AG | The use of sgc stimulators and sgc activators alone or in combination with pde5 inhibitors for the treatment of bone disorders including osteogenesis imperfecta (oi) |
| EP3787610A1 (en) | 2018-04-30 | 2021-03-10 | Bayer Aktiengesellschaft | The use of sgc activators and sgc stimulators for the treatment of cognitive impairment |
| EP3793553A1 (en) | 2018-05-15 | 2021-03-24 | Bayer Aktiengesellschaft | 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization |
| EP3574905A1 (en) | 2018-05-30 | 2019-12-04 | 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 |
| WO2020011804A1 (en) * | 2018-07-12 | 2020-01-16 | Boehringer Ingelheim International Gmbh | Alkoxy pyrazoles as soluble guanylate cyclase activators |
| US20220128561A1 (en) | 2019-01-17 | 2022-04-28 | Bayer Aktiengesellschaft | Methods to determine whether a subject is suitable of being treated with an agonist of soluble gyanylyl cyclase (sgc) |
| EP3976591B1 (en) * | 2019-10-18 | 2023-04-19 | FMC Corporation | Methods for the preparation of 5-bromo-2-(3-chloro-pyridin-2-yl)-2h-pyrazole-3-carboxylic acid |
| CN112079712B (zh) * | 2020-09-18 | 2022-12-13 | 江苏美迪克化学品有限公司 | 一种对乙烯基水杨酸的制备方法 |
| EP4011873A1 (en) | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| AR124297A1 (es) * | 2020-12-10 | 2023-03-15 | Bayer Ag | Ácidos pirazol piperidin carboxílicos sustituidos |
| GB202102895D0 (en) | 2021-03-01 | 2021-04-14 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| EP4496571A1 (en) * | 2022-03-21 | 2025-01-29 | Boehringer Ingelheim International GmbH | Soluble guanylate cyclase activators for treating portal hypertension |
| EP4536205A1 (en) | 2022-06-09 | 2025-04-16 | Bayer Aktiengesellschaft | Soluble guanylate cyclase activators for use in the treatment of heart failure with preserved ejection fraction in women |
| CN120225203A (zh) | 2022-11-04 | 2025-06-27 | 勃林格殷格翰国际有限公司 | 用于治疗系统性硬化症的可溶性鸟苷酸环化酶活化剂 |
| WO2024123847A1 (en) | 2022-12-09 | 2024-06-13 | Boehringer Ingelheim International Gmbh | Solid forms of a sgc activator |
| CN121620369A (zh) | 2023-08-16 | 2026-03-06 | 勃林格殷格翰国际有限公司 | 用于治疗临床显著门静脉高压和失代偿期肝硬化的可溶性鸟苷酸环化酶激活剂 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9824310D0 (en) * | 1998-11-05 | 1998-12-30 | Univ London | Activators of soluble guanylate cyclase |
| US20040067938A1 (en) | 2000-09-29 | 2004-04-08 | Penglie Zhang | Quaternary amines and related inhibitors of factor xa |
| AR031176A1 (es) | 2000-11-22 | 2003-09-10 | Bayer Ag | Nuevos derivados de pirazolpiridina sustituidos con piridina |
| WO2002043201A1 (en) | 2000-11-22 | 2002-05-30 | Visx, Incorporated | Temperature actuated positioning device for non-linear optical elements |
| GB0212785D0 (en) | 2002-05-31 | 2002-07-10 | Glaxo Group Ltd | Compounds |
| ZA200504898B (en) * | 2002-12-20 | 2006-11-29 | Pharmacia Corp | Acyclic pyrazole compounds |
| AU2006272088A1 (en) | 2005-07-18 | 2007-01-25 | Bayer Schering Pharma Aktiengesellschaft | Novel use of activators and stimulators of soluble guanylate cyclase for the prevention or treatment of renal disorders |
| US20080045560A1 (en) | 2006-08-15 | 2008-02-21 | Wyeth | Pyrrolidine and related derivatives useful as PR modulators |
| AU2008250643A1 (en) | 2007-05-12 | 2008-11-20 | Bayer Schering Pharma Aktiengesellschaft | sGC stimulators, sGC activators and combinations for the treatment of urological disorders |
| BRPI0816382A2 (pt) * | 2007-09-06 | 2015-02-24 | Merck Sharp & Dohme | Composto, composição, e, métodos para ativar a guanilato ciclase solúvel e para tratar ou previnir doenças |
| WO2009043495A1 (en) * | 2007-10-05 | 2009-04-09 | Sanofi-Aventis Deutschland Gmbh | Use of sulfonyl-substituted 2-sulfonylaminobenzoic acid n-phenylamides in the treatment of pain |
| WO2009068652A1 (en) | 2007-11-30 | 2009-06-04 | Smithkline Beecham Corporation | 2, 6-disubstituted pyridines and 2, 4-disubstituted pyrimidines as soluble guanylate cyclase activators |
| TW200938529A (en) * | 2007-12-03 | 2009-09-16 | Smithkline Beecham Corp | Compounds |
| CA2720343A1 (en) | 2008-04-04 | 2009-10-08 | Takeda Pharmaceutical Company Limited | Heterocyclic derivative and use thereof |
| WO2010015653A1 (en) | 2008-08-07 | 2010-02-11 | Smithkline Beecham Corporation | Pyrimidine derivatives as activators of soluble guanylate cyclase |
| WO2010015652A2 (en) | 2008-08-07 | 2010-02-11 | Smithkline Beecham Corporation | Thiazole compounds as activators of soluble guanylate cyclase |
| AU2009322836B2 (en) | 2008-11-25 | 2013-04-04 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| JP5780430B2 (ja) | 2009-01-17 | 2015-09-16 | アドヴェリオ・ファーマ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 勃起不全の処置用のＰＤＥ５阻害剤と組み合わせたｓＧＣ刺激剤またはｓＧＣ活性化剤 |
| KR20110133034A (ko) | 2009-02-26 | 2011-12-09 | 머크 샤프 앤드 돔 코포레이션 | 가용성 구아닐레이트 시클라제 활성화제 |
| CN102770133A (zh) * | 2010-02-05 | 2012-11-07 | 拜耳知识产权有限责任公司 | 用于治疗囊性纤维化的单独和与PDE5抑制剂组合的sGC刺激剂或sGC激活剂 |
| WO2011095553A1 (en) | 2010-02-05 | 2011-08-11 | Bayer Schering Pharma Aktiengesellschaft | Sgc stimulators or sgc activators in combination with pde5 inhbitors for the treatment of erectile dysfunction |
| HRP20150987T1 (hr) * | 2010-05-26 | 2015-10-23 | Adverio Pharma Gmbh | UPORABA sGC STIMULATORA, sGC AKTIVATORA, SAMOSTALNO I U KOMBINACIJAMA S INHIBITORIMA PDE5 ZA LIJEÄŚENJE SISTEMSKE SKLEROZE (SSc) |
| EP2687210A1 (de) | 2010-06-25 | 2014-01-22 | Bayer Intellectual Property GmbH | Verwendung von Stimulatoren und Aktivatoren der löslichen Guanylatzyklase zur Behandlung von Sichelzellanämie und Konservierung von Blutersatzstoffen |
| EP2632551B1 (en) | 2010-10-28 | 2016-07-06 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| JP5715713B2 (ja) | 2011-03-10 | 2015-05-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 可溶性グアニル酸シクラーゼ活性化因子 |
| US8815857B2 (en) | 2011-08-12 | 2014-08-26 | Boehringer Ingelheim International Gmbh | Soluble guanylate cyclase activators |
| 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) |
| HRP20191755T1 (hr) * | 2012-09-07 | 2019-12-27 | Boehringer Ingelheim International Gmbh | Alkoksipirazoli kao aktivatori topljive gvanilat ciklaze |
-
2013
- 2013-09-03 HR HRP20191755TT patent/HRP20191755T1/hr unknown
- 2013-09-03 PT PT137626669T patent/PT2892891T/pt unknown
- 2013-09-03 MD MDA20150019A patent/MD4425C1/ro active IP Right Grant
- 2013-09-03 GE GEAP201313783A patent/GEP20176631B/en unknown
- 2013-09-03 NZ NZ703989A patent/NZ703989A/en unknown
- 2013-09-03 AU AU2013312931A patent/AU2013312931B2/en active Active
- 2013-09-03 LT LTEP13762666.9T patent/LT2892891T/lt unknown
- 2013-09-03 WO PCT/US2013/057826 patent/WO2014039434A1/en not_active Ceased
- 2013-09-03 US US14/016,452 patent/US8906904B2/en not_active Ceased
- 2013-09-03 MA MA37891A patent/MA37891B1/fr unknown
- 2013-09-03 JP JP2015531142A patent/JP5970134B2/ja active Active
- 2013-09-03 CN CN201380046266.3A patent/CN104619695B/zh active Active
- 2013-09-03 UA UAA201503030A patent/UA115881C2/uk unknown
- 2013-09-03 SG SG11201500861QA patent/SG11201500861QA/en unknown
- 2013-09-03 DK DK13762666.9T patent/DK2892891T3/da active
- 2013-09-03 ES ES13762666T patent/ES2748798T3/es active Active
- 2013-09-03 PL PL13762666T patent/PL2892891T3/pl unknown
- 2013-09-03 RS RSP20191306 patent/RS59394B1/sr unknown
- 2013-09-03 PE PE2015000295A patent/PE20151001A1/es active IP Right Grant
- 2013-09-03 CA CA2880494A patent/CA2880494C/en active Active
- 2013-09-03 EP EP13762666.9A patent/EP2892891B1/en active Active
- 2013-09-03 EA EA201500298A patent/EA027244B1/ru not_active IP Right Cessation
- 2013-09-03 BR BR112015004529-4A patent/BR112015004529B1/pt active IP Right Grant
- 2013-09-03 SG SG10201510668UA patent/SG10201510668UA/en unknown
- 2013-09-03 KR KR1020157005961A patent/KR101692707B1/ko active Active
- 2013-09-03 HU HUE13762666A patent/HUE046996T2/hu unknown
- 2013-09-03 AP AP2015008231A patent/AP2015008231A0/xx unknown
- 2013-09-03 MX MX2015002807A patent/MX338887B/es active IP Right Grant
- 2013-09-03 SI SI201331583T patent/SI2892891T1/sl unknown
- 2013-09-06 AR ARP130103197A patent/AR092869A1/es active IP Right Grant
- 2013-09-06 TW TW102132286A patent/TWI586661B/zh active
- 2013-09-06 UY UY0001035012A patent/UY35012A/es active IP Right Grant
-
2015
- 2015-01-29 IL IL236987A patent/IL236987A/en active IP Right Grant
- 2015-02-03 CL CL2015000255A patent/CL2015000255A1/es unknown
- 2015-02-18 TN TNP2015000054A patent/TN2015000054A1/fr unknown
- 2015-03-03 PH PH12015500457A patent/PH12015500457B1/en unknown
- 2015-03-06 CL CL2015000562A patent/CL2015000562A1/es unknown
- 2015-04-02 EC ECIEPI201512804A patent/ECSP15012804A/es unknown
-
2016
- 2016-10-31 US US15/338,605 patent/USRE46886E1/en active Active
-
2019
- 2019-10-22 CY CY20191101099T patent/CY1122610T1/el unknown
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