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1. SG11201908517X - PYRIMIDINYL-PYRIDYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF TREATING IRE1-RELATED DISEASES AND DISORDERS

Office Singapore
Application Number 11201908517X
Application Date 16.03.2018
Publication Number 11201908517X
Publication Date 30.10.2019
Publication Kind A1
IPC
C07D 403/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 403/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14containing three or more hetero rings
A61K 31/4545
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/445
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
A61K 31/506
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/506
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 401/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 405/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
Applicants GENENTECH, INC.
Inventors BRAUN, Marie-Gabrielle
GIBBONS, Paul
LEE, Wendy
LY, Cuong
RUDOLPH, Joachim
SCHWARZ, Jacob
ASHKENAZI, Avi
FU, Leo
LAI, Tommy
WANG, Fei
BEVERIDGE, Ramsay
ZHAO, Liang
Priority Data PCT/CN2017/077059 17.03.2017 CN
Title
(EN) PYRIMIDINYL-PYRIDYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF TREATING IRE1-RELATED DISEASES AND DISORDERS
Abstract
(EN)
DISEASES AND DISORDERS cc kr) ,•\"% h N SD (R 6 ), 0 1-1 O C RA N H R 7 1 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 20 September 2018 (20.09.2018) WIPO I PCT oimitia °nolo OilIIIII0111IIIIIOH o imio oimIE (10) International Publication Number WO 2018/166528 Al (51) International Patent Classification: CO7D 403/04 (2006.01) A61K 31/445 (2006.01) CO7D 403/14 (2006.01) A61K 31/506 (2006.01) A61K 31/4545 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/CN2018/079292 (22) International Filing Date: 16 March 2018 (16.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: PCT/CN2017/077059 17 March 2017 (17.03.2017) CN (71) Applicants: GENENTECH, INC. [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). THE RE- GENTS OF THE UNIVERSITY OF CALIFORNIA [US/US]; 1111 Franklin Street, Twelfth Floor, Oakland, California 94607 (US). = (72) Inventors; and (71) Applicants (for MN only): BRAUN, Marie-Gabrielle [FR/US]; 1 DNA Way, South San Francisco, California 94080 (US). GIBBONS, Paul [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). LEE, Wendy [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). LY, Cuong [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). RUDOLPH, Joachim [DE/US]; 1 DNA Way, South San Francisco, California 94080 (US). SCHWARZ, Jacob [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). ASHKE- NAZI, Avi [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). FU, Leo [CN/CN]; 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131 (CN). LAI, Tommy [CN/CN]; 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131 (CN). WANG, Fei [CN/CN]; 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131 (CN). BEVERIDGE, Ramsay [CA/CA]; 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1 (CA). ZHAO, Liang [CA/CA]; 2525 Av- enue Marie-Curie, Montreal, Quebec H4S 2E1 (CA). (74) Agent: WU, FENG & ZHANG; 3 FL, Building 2, Yard 3, Fengxiuzhonglu Road, Haidian District, Beijing 100094 (CN). (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, HN, HR, HU, ID, IL, IN, IR, IS, JO, 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). Published: — with international search report (Art. 21(3)) (54) Title: PYRIMIDINYL-PYRIDYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF TREATING IRE1-RELATED (57) Abstract: Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formu- la (I) or (I') structure : or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula (I) or (I') compounds, as well as methods of using such IRE1 modulators, alone and in combina- tion with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.