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1. (WO2017112617) 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
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/112617 International Application No.: PCT/US2016/067654
Publication Date: 29.06.2017 International Filing Date: 20.12.2016
IPC:
C07D 487/04 (2006.01) ,A61K 31/519 (2006.01) ,A61P 9/00 (2006.01) ,A61P 9/10 (2006.01) ,A61P 9/12 (2006.01) ,A61P 9/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
12
Antihypertensives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
04
Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
Applicants:
MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue Rahway, New Jersey 07065-0907, US (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JP, KE, KG, KH, KM, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
BERGER, Raphelle [FR/US]; US (NZ, US)
CHEN, Yi-Heng [US/US]; US (NZ, US)
LI, Guoqing [US/US]; US (NZ, US)
GARFUNKLE, Joie [US/US]; US (NZ, US)
LI, Hong [CN/US]; US (NZ, US)
MIAO, Shouwu [CN/US]; US (NZ, US)
RAGHAVAN, Subharekha [US/US]; US (NZ, US)
SMITH, Cameron, J. [US/US]; US (NZ, US)
STELMACH, John [US/US]; US (NZ, US)
WHITEHEAD, Alan [US/US]; US (NZ, US)
ZHANG, Rui [US/US]; US (NZ, US)
ZHANG, Yong [US/US]; US (NZ, US)
FU, Jianmin [US/CN]; CN (NZ, US)
JI, Gang [CN/CN]; CN (NZ, US)
JIANG, Falong [CN/CN]; CN (NZ, US)
Inventors:
BERGER, Raphelle; US
CHEN, Yi-Heng; US
LI, Guoqing; US
GARFUNKLE, Joie; US
LI, Hong; US
MIAO, Shouwu; US
RAGHAVAN, Subharekha; US
SMITH, Cameron, J.; US
STELMACH, John; US
WHITEHEAD, Alan; US
ZHANG, Rui; US
ZHANG, Yong; US
FU, Jianmin; CN
JI, Gang; CN
JIANG, Falong; CN
Common
Representative:
MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue Rahway, New Jersey 07065-0907, US
Priority Data:
PCT/CN2015/09825122.12.2015CN
Title (EN) 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
(FR) DÉRIVÉS DE 4-AMINO-2-(1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL)-6-OXO-6,7-DIHYDRO-5H-PYRROLO[2,3-D]PYRIMIDINE ET DÉRIVÉS RESPECTIFS DE (1H-INDAZOL-3-YL) EN TANT QUE MODULATEURS CGMP POUR LE TRAITEMENT DE MALADIES CARDIOVASCULAIRES
Abstract:
(EN) The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds 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, diastolic 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 anemia, scleroderma, Raynaud's Syndrome, diabetes, diabetic retinopathy, cirrhosis of the liver, chronic obstructive pulmonary disease (COPD), acute lung injury, pulmonary fibrosis or interstitial lung disease. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to the compounds or their pharmaceutically acceptable salts for use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
(FR) L'invention concerne des composés de formule (I) ou les sels pharmaceutiquement acceptables de ceux-ci, dans lesquels X, Y, Z, R1, R2, R4, Ra et les indices m, p, et q sont tels que décrits ici. Les composés ou leurs sels pharmaceutiquement acceptables peuvent moduler la production de guanosine monophosphate cyclique ("cGMP") par le corps, et sont généralement appropriés pour la thérapie et la prophylaxie de maladies qui sont associées à un équilibre cGMP perturbé, telles que les maladies cardiovasculaires, le dysfonctionnement endothélial, le dysfonctionnement diastolique, l'athérosclérose, l'hypertension, l'insuffisance cardiaque, l'hypertension pulmonaire (WHO groupes I, II, III,IV), l'angine de poitrine, la thrombose, la resténose, l'infarctus du myocarde, l'accident vasculaire cérébral, l'insuffisance cardiaque, la fibrose, l'hypertonie pulmonaire, le dysfonctionnement érectile, l'asthme, le syndrome de détresse respiratoire aiguë (ARDS), une maladie rénale chronique, la mucoviscidose, la drépanocytose, la sclérodermie, le syndrome de Raynaud, le diabète, la rétinopathie diabétique, la cirrhose du foie, la bronchopneumopathie chronique obstructive (BPCO), une lésion pulmonaire aiguë, la fibrose pulmonaire ou une maladie pulmonaire interstitielle. L'invention concerne également des compositions pharmaceutiques qui comprennent des composés de formule (I) ou des sels pharmaceutiquement acceptables de ceux-ci. L'invention concerne également les composés ou leurs sels pharmaceutiquement acceptables pour une utilisation dans la thérapie et la prophylaxie des maladies susmentionnées et pour la préparation de produits pharmaceutiques à cette fin.
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Designated States: 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, 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
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
UAa201808060AU2016377364IN201847022924CA3009193MYPI 2018001031IL260020
SG11201805272XKR1020180095904ID2018/09731EP3394067MX2018007728CN108738320
DOP2018000153BR112018012579EA201891303CR20180330PH1/2018/501342