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1. (WO2017156009) CRYSTALLINE(2S,4R)-5-(5'-CHLORO-2'-FLUORO-[1,1'-BIPHENYL]-4-YL)-2-(ETHOXYMETHYL)-4-(3-HYDROXYISOXAZOLE-5-CARBOXAMIDO)-2-METHYLPENTANOIC ACID AND USES THEREOF
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Pub. No.: WO/2017/156009 International Application No.: PCT/US2017/021172
Publication Date: 14.09.2017 International Filing Date: 07.03.2017
Chapter 2 Demand Filed: 26.10.2017
IPC:
C07D 261/18 (2006.01) ,A61K 31/42 (2006.01) ,A61P 9/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
261
Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02
not condensed with other rings
06
having two or more double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
18
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42
Oxazoles
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
Applicants:
THERAVANCE BIOPHARMA R&D IP, LLC [US/US]; 901 Gateway Boulevard South San Francisco, California 94080, US
Inventors:
HUGHES, Adam D.; US
FLEURY, Melissa; US
RAPTA, Miroslav; US
THALLADI, Venkat R.; US
FASS, Gene Timothy; US
SIMEONE, Michael; US
BALDWIN, R. Michael; US
BOURDET, David L.; US
Agent:
HAGENAH, Jeffrey A.; US
PETKA, Wendy Ann; US
SAXON, Roberta P.; US
Priority Data:
62/305,39308.03.2016US
62/346,33606.06.2016US
Title (EN) CRYSTALLINE(2S,4R)-5-(5'-CHLORO-2'-FLUORO-[1,1'-BIPHENYL]-4-YL)-2-(ETHOXYMETHYL)-4-(3-HYDROXYISOXAZOLE-5-CARBOXAMIDO)-2-METHYLPENTANOIC ACID AND USES THEREOF
(FR) ACIDE (2S,4R)-5-(5'-CHLORO-2'-FLUORO-[1,1'-BIPHÉNYL]-4-YL)-2-(ÉTHOXYMÉTHYL)-4-(3-HYDROXYISOXAZOLE-5-CARBOXAMIDO)-2-MÉTHYL-PENTANOÏQUE CRISTALLIN ET UTILISATIONS CORRESPONDANTES
Abstract:
(EN) In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I') forms.
(FR) L’invention concerne, selon un aspect, une forme cristalline de la structure, ou un sel pharmaceutiquement acceptable correspondant, présentant une activité d'inhibition de la néprilysine. Selon un autre aspect, l'invention concerne des compositions pharmaceutiques comprenant cette forme cristalline ; des procédés d'utilisation de cette forme cristalline et de sa forme soluble (I) ; et des procédés de préparation de formes soluble (I) et cristalline (I').
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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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)