SG11201805272XA - 4-amino-2-(1h-pyrazolo[3,4-b]pyridin-3-yl)-6-oxo-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidine derivatives and the respective (1h-indazol-3-yl) derivatives as cgmp modulators for treating cardiovascular diseases - Google Patents
4-amino-2-(1h-pyrazolo[3,4-b]pyridin-3-yl)-6-oxo-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidine derivatives and the respective (1h-indazol-3-yl) derivatives as cgmp modulators for treating cardiovascular diseasesInfo
- Publication number
- SG11201805272XA SG11201805272XA SG11201805272XA SG11201805272XA SG11201805272XA SG 11201805272X A SG11201805272X A SG 11201805272XA SG 11201805272X A SG11201805272X A SG 11201805272XA SG 11201805272X A SG11201805272X A SG 11201805272XA SG 11201805272X A SG11201805272X A SG 11201805272XA
- Authority
- SG
- Singapore
- Prior art keywords
- new jersey
- rahway
- international
- east lincoln
- road
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 29 June 2017 (29.06.2017) WIPOIPCT (10) International Publication Number WO 2017/112617 A1 (51) International Patent Classification: C07D 487/04 (2006.01) A61P 9/10 (2006.01) A61K31/519 (2006.01) A61P 9/12 (2006.01) A61P 9/00 (2006.01) A61P 9/04 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2016/067654 20 December 2016 (20.12.2016) English (30) Priority Data: PCT/CN2015/098251 22 December 2015 (22.12.2015) English CN (71) Applicant (for all designated States except US): MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (72) Inventors; and (71) Applicants (for NZ, US only)-. BERGER, Raphelle [FR/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). CHEN, Yi-Heng [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). LI, Guoqing [US/US]; 2000 Galloping Hill Road, Kenil- worth, New Jersey 07033 (US). GARFUNKLE, Joie [US/US]; 600 Coporate Drive, Lebanon, New Jersey 08833 (US). LI, Hong [CN/US]; 126 East Lincoln Aven ue, Rahway, New Jersey 07065-0907 (US). MIAO, Shouwu [CN/US]; 295 Prestwick Way, Edison, New Jer sey 08820 (US). RAGHAVAN, Subharekha [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). SMITH, Cameron, J. [US/US]; 9004 Snowford Court, Montgomery Village, Maryland 20886-4017 (US). STELMACH, John [US/US]; 228 Seneca Place, West- field, New Jersey 07090 (US). WHITEHEAD, Alan [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). ZHANG, Rui [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). ZHANG, Yong [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). FU, Jianmin [US/CN]; 6 Tai-He Road, BDA, Beijing 100176 (CN). JI, Gang [CN/CN]; 6 Tai-He Road, BDA, Beijing 100176 (CN). JIANG, Falong [CN/CN]; 6 Tai-He Road, BDA, beijing 100176 (CN). (74) Common Representative: MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, [Continued on next page] (54) Title: 4-AMINO-2-(lH-PYRAZOLO[3,4-B]PYRIDIN-3-YL)-6-OXO-6,7-DIHYDRO-5H-PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AND THE RESPECTIVE (1H-INDAZOL-3-YL) DERIVATIVES AS CGMP MODULATORS FOR TREATING CARDIOVASCULAR DISEASES l> CJ o CJ o & (R (I) (57) : The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the sub scripts m, p, and q are as described herein. The com pounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate ("cGMP"), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance, such as cardiovascular disease, endothelial dysfunction, dia stolic dysfunction, atherosclerosis, hypertension, heart failure, pulmonary hypertension (WHO groups I, II, III, IV), angina pectoris, thrombosis, restenosis, myocardial infarction, stroke, cardiac insufficiency, fibrosis, pulmonary hypertonia, erectile dysfunction, asthma, acute respiratory distress syndrome (ARDS), chronic kidney disease, cystic fibrosis, sickle cell an emia, scleroderma, Raynaud's Syndrome, diabetes, diabetic retinopathy, cirrhosis of the liver, chronic ob structive pulmonary disease (COPD), acute lung in jury, pulmonary fibrosis or interstitial lung disease. The invention also provides pharmaceutical composi tions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The inven tion also relates to the compounds or their pharma ceutically acceptable salts for use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose. wo 2017/112617 AI i inn nil ii mil mi mil in mi i ii 111 mi mi mi mi mi mi mini mi 111 mi HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3))
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2015/098251 WO2017107052A1 (en) | 2015-12-22 | 2015-12-22 | Soluble guanylate cyclase stimulators |
| PCT/US2016/067654 WO2017112617A1 (en) | 2015-12-22 | 2016-12-20 | 4-amino-2-(1h-pyrazolo[3,4-b]pyridin-3-yl)-6-oxo-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidine derivatives and the respective (1h-indazol-3-yl) derivatives as cgmp modulators for treating cardiovascular diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201805272XA true SG11201805272XA (en) | 2018-07-30 |
Family
ID=57758775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201805272XA SG11201805272XA (en) | 2015-12-22 | 2016-12-20 | 4-amino-2-(1h-pyrazolo[3,4-b]pyridin-3-yl)-6-oxo-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidine derivatives and the respective (1h-indazol-3-yl) derivatives as cgmp modulators for treating cardiovascular diseases |
Country Status (39)
| Country | Link |
|---|---|
| US (2) | US10030027B2 (en) |
| EP (1) | EP3394067B1 (en) |
| JP (1) | JP6454448B2 (en) |
| KR (1) | KR102191312B1 (en) |
| CN (1) | CN108738320B (en) |
| AR (1) | AR107154A1 (en) |
| AU (1) | AU2016377364B2 (en) |
| BR (1) | BR112018012579B8 (en) |
| CA (1) | CA3009193C (en) |
| CL (1) | CL2018001671A1 (en) |
| CO (1) | CO2018006300A2 (en) |
| CR (1) | CR20180330A (en) |
| CY (1) | CY1123173T1 (en) |
| DK (1) | DK3394067T3 (en) |
| DO (1) | DOP2018000153A (en) |
| EA (1) | EA036445B1 (en) |
| EC (1) | ECSP18054606A (en) |
| ES (1) | ES2794654T3 (en) |
| HK (1) | HK1255028A1 (en) |
| HR (1) | HRP20200857T1 (en) |
| HU (1) | HUE049941T2 (en) |
| IL (1) | IL260020B (en) |
| LT (1) | LT3394067T (en) |
| ME (1) | ME03748B (en) |
| MX (2) | MX2018007728A (en) |
| MY (1) | MY194021A (en) |
| NI (1) | NI201800069A (en) |
| PE (1) | PE20181802A1 (en) |
| PH (1) | PH12018501342A1 (en) |
| PL (1) | PL3394067T3 (en) |
| PT (1) | PT3394067T (en) |
| RS (1) | RS60344B1 (en) |
| SG (1) | SG11201805272XA (en) |
| SI (1) | SI3394067T1 (en) |
| SV (1) | SV2018005715A (en) |
| TN (1) | TN2018000219A1 (en) |
| TW (1) | TWI724079B (en) |
| UA (1) | UA122264C2 (en) |
| WO (2) | WO2017107052A1 (en) |
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