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 |
|---|---|---|---|---|
| ES2748798T3 (es) * | 2012-09-07 | 2020-03-18 | Boehringer Ingelheim Int | Alcoxi pirazoles como activadores de la guanilato ciclasa soluble |
| 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 |
| EP3172202B1 (en) * | 2014-07-22 | 2020-01-29 | Boehringer Ingelheim International GmbH | Heterocyclic carboxylic acids as activators of soluble guanylate cyclase |
| JP2018537488A (ja) | 2015-12-18 | 2018-12-20 | ノバルティス アーゲー | インダン誘導体、ならびに可溶性グアニル酸シクラーゼ活性化剤としてのその使用 |
| CA3039735A1 (en) | 2016-10-11 | 2018-04-19 | Bayer Pharma Aktiengesellschaft | Combination containing sgc activators and mineralocorticoid receptor antagonists |
| 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) |
| JP7314173B2 (ja) | 2018-04-30 | 2023-07-25 | バイエル アクチェンゲゼルシャフト | 認知障害の治療のためのｓＧＣ活性化薬及びｓＧＣ刺激薬の使用 |
| CA3100096A1 (en) | 2018-05-15 | 2019-11-21 | 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 |
| EP3820470B1 (en) | 2018-07-12 | 2024-09-11 | Boehringer Ingelheim International GmbH | Alkoxy pyrazoles as soluble guanylate cyclase activators for use in treating portal hypertension |
| EP3911675A1 (en) | 2019-01-17 | 2021-11-24 | Bayer Aktiengesellschaft | Methods to determine whether a subject is suitable of being treated with an agonist of soluble guanylyl cyclase (sgc) |
| MX2022004631A (es) * | 2019-10-18 | 2022-05-24 | Fmc Corp | Metodos para la preparacion del acido 5-bromo-2-(3-cloropiridin-2- il)-2h-pirazol-3-carboxilico. |
| 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 |
| EP4259617B1 (en) * | 2020-12-10 | 2024-10-23 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| EP4011873A1 (en) | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| GB202102895D0 (en) | 2021-03-01 | 2021-04-14 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| CN118900690A (zh) | 2022-03-21 | 2024-11-05 | 勃林格殷格翰国际有限公司 | 用于治疗门脉高压的可溶性鸟苷酸环化酶活化剂 |
| 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 |
| WO2024097316A1 (en) | 2022-11-04 | 2024-05-10 | Boehringer Ingelheim International Gmbh | Soluble guanylate cyclase activators for treating systemic sclerosis |
| US20240199590A1 (en) * | 2022-12-09 | 2024-06-20 | Boehringer Ingelheim International Gmbh | Solid forms of a sgc activator |
| WO2025036839A1 (en) | 2023-08-16 | 2025-02-20 | Boehringer Ingelheim International Gmbh | Soluble guanylate cyclase activators for treating clinically significant portal hypertension and decompensated cirrhosis |
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 |
| WO2002026712A2 (en) | 2000-09-29 | 2002-04-04 | Millennium Pharmaceuticals, Inc. | Quaternary amines and related inhibitors of factor xa |
| AU2002228819A1 (en) | 2000-11-22 | 2002-06-03 | Visx Incorporated | Temperature actuated positioning device for non-linear optical elements |
| AR031176A1 (es) | 2000-11-22 | 2003-09-10 | Bayer Ag | Nuevos derivados de pirazolpiridina sustituidos con piridina |
| GB0212785D0 (en) | 2002-05-31 | 2002-07-10 | Glaxo Group Ltd | Compounds |
| CN1747949A (zh) | 2002-12-20 | 2006-03-15 | 法马西亚公司 | 无环吡唑化合物 |
| BRPI0614001A2 (pt) | 2005-07-18 | 2011-03-01 | Bayer Healthcare Ag | uso de ativadores e estimuladores de guanilato ciclase solúvel para a prevenção ou tratamento de distúrbios renais |
| US20080045560A1 (en) | 2006-08-15 | 2008-02-21 | Wyeth | Pyrrolidine and related derivatives useful as PR modulators |
| WO2008138483A1 (en) * | 2007-05-12 | 2008-11-20 | Bayer Schering Pharma Aktiengesellschaft | sGC STIMULATORS, sGC ACTIVATORS AND COMBINATIONS FOR THE TREATMENT OF UROLOGICAL DISORDERS |
| KR20100059952A (ko) * | 2007-09-06 | 2010-06-04 | 머크 샤프 앤드 돔 코포레이션 | 가용성 구아닐레이트 사이클라제 활성제 |
| CN101815514B (zh) * | 2007-10-05 | 2012-05-09 | 塞诺菲-安万特德国有限公司 | 磺酰基取代的2-磺酰基氨基苯甲酸n-苯基酰胺在治疗疼痛中的应用 |
| 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 |
| PE20091258A1 (es) * | 2007-12-03 | 2009-09-12 | Smithkline Beecham Corp | Derivados de piridina como activadores de la guanilato ciclasa soluble |
| CN102056907B (zh) * | 2008-04-04 | 2014-12-31 | 武田药品工业株式会社 | 杂环衍生物及其用途 |
| WO2010015652A2 (en) | 2008-08-07 | 2010-02-11 | Smithkline Beecham Corporation | Thiazole compounds as activators of soluble guanylate cyclase |
| WO2010015653A1 (en) * | 2008-08-07 | 2010-02-11 | Smithkline Beecham Corporation | Pyrimidine derivatives as activators of soluble guanylate cyclase |
| AU2009322836B2 (en) | 2008-11-25 | 2013-04-04 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| EP2387404B1 (en) * | 2009-01-17 | 2014-06-25 | Bayer Intellectual Property GmbH | Sgc stimulators and activators in combination with pde5 inhbitors for the treatment of erectile dysfunction |
| CN102414194A (zh) | 2009-02-26 | 2012-04-11 | 默沙东公司 | 可溶性鸟苷酸环化酶激活剂 |
| 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 |
| SI2531187T1 (sl) * | 2010-02-05 | 2016-01-29 | Adverio Pharma Gmbh | Stimulatorji sGC ali aktivatorji sGC sami in v kombinaciji z inhibitorji PDE5 za zdravljenje cistične fibroze |
| SI2576548T1 (sl) * | 2010-05-26 | 2015-11-30 | Adverio Pharma Gmbh | Uporaba sGC stimulatorjev, sGC aktivatorjev, samih in v kombinacijah s PDE5 inhibitorji za zdravljenje sistemske skleroze |
| 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 |
| JP5826393B2 (ja) | 2011-08-12 | 2015-12-02 | 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 |
| 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) |
| ES2748798T3 (es) * | 2012-09-07 | 2020-03-18 | Boehringer Ingelheim Int | Alcoxi pirazoles como activadores de la guanilato ciclasa soluble |
-
2013
- 2013-09-03 ES ES13762666T patent/ES2748798T3/es active Active
- 2013-09-03 DK DK13762666.9T patent/DK2892891T3/da active
- 2013-09-03 MD MDA20150019A patent/MD4425C1/ro active IP Right Grant
- 2013-09-03 PL PL13762666T patent/PL2892891T3/pl unknown
- 2013-09-03 HU HUE13762666A patent/HUE046996T2/hu unknown
- 2013-09-03 BR BR112015004529-4A patent/BR112015004529B1/pt active IP Right Grant
- 2013-09-03 GE GEAP201313783A patent/GEP20176631B/en unknown
- 2013-09-03 KR KR1020157005961A patent/KR101692707B1/ko active Active
- 2013-09-03 EA EA201500298A patent/EA027244B1/ru not_active IP Right Cessation
- 2013-09-03 AU AU2013312931A patent/AU2013312931B2/en active Active
- 2013-09-03 MA MA37891A patent/MA37891B1/fr unknown
- 2013-09-03 SG SG10201510668UA patent/SG10201510668UA/en unknown
- 2013-09-03 RS RSP20191306 patent/RS59394B1/sr unknown
- 2013-09-03 SI SI201331583T patent/SI2892891T1/sl unknown
- 2013-09-03 WO PCT/US2013/057826 patent/WO2014039434A1/en not_active Ceased
- 2013-09-03 AP AP2015008231A patent/AP2015008231A0/xx unknown
- 2013-09-03 EP EP13762666.9A patent/EP2892891B1/en active Active
- 2013-09-03 PT PT137626669T patent/PT2892891T/pt 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 US US14/016,452 patent/US8906904B2/en not_active Ceased
- 2013-09-03 SG SG11201500861QA patent/SG11201500861QA/en unknown
- 2013-09-03 CN CN201380046266.3A patent/CN104619695B/zh active Active
- 2013-09-03 JP JP2015531142A patent/JP5970134B2/ja active Active
- 2013-09-03 NZ NZ703989A patent/NZ703989A/en unknown
- 2013-09-03 HR HRP20191755TT patent/HRP20191755T1/hr unknown
- 2013-09-03 UA UAA201503030A patent/UA115881C2/uk unknown
- 2013-09-03 LT LTEP13762666.9T patent/LT2892891T/lt unknown
- 2013-09-03 MX MX2015002807A patent/MX338887B/es active IP Right Grant
- 2013-09-06 UY UY0001035012A patent/UY35012A/es active IP Right Grant
- 2013-09-06 AR ARP130103197A patent/AR092869A1/es active IP Right Grant
- 2013-09-06 TW TW102132286A patent/TWI586661B/zh active
-
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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