SG11201903187WA - Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors - Google Patents

Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors

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Publication number
SG11201903187WA
SG11201903187WA SG11201903187WA SG11201903187WA SG11201903187WA SG 11201903187W A SG11201903187W A SG 11201903187WA SG 11201903187W A SG11201903187W A SG 11201903187WA SG 11201903187W A SG11201903187W A SG 11201903187WA SG 11201903187W A SG11201903187W A SG 11201903187WA
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SG
Singapore
Prior art keywords
boulder
colorado
walnut
array
street
Prior art date
Application number
SG11201903187WA
Inventor
Steven W Andrews
Sean Aronow
James F Blake
Barbara J Brandhuber
James Collier
Adam Cook
Julia Haas
Yutong Jiang
Gabrielle R Kolakowski
Elizabeth A Mcfaddin
Megan L Mckenney
Oren T Mcnulty
Andrew T Metcalf
David A Moreno
Ginelle A Ramann
Tony P Tang
Li Ren
Shane M Walls
Original Assignee
Array Biopharma Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of SG11201903187WA publication Critical patent/SG11201903187WA/en

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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD HIM 0 11101 HOE HI 1 0 101110 Ell 010 HE 100 MO MIS Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/071454 Al 19 April 2018 (19.04.2018) WIP0 1 PCT (51) International Patent Classification: nut Street, Boulder, Colorado 80301 (US). MORENO, CO7D 471/04 (2006.01) A61P 35/00 (2006.01) David A. [US/US]; c/o Array BioPharma Inc., 3200 Walnut A61K 31/437 (2006.01) Street, Boulder, Colorado 80301 (US). RAMANN, Ginelle (21) International Application Number: A. [US/US]; c/o Array BioPharma, Inc., 3200 Walnut St., PCT/US2017/055993 Boulder, Colorado 80301 (US). TANG, Tony P. [US/US]; c/o Array BioPharma Inc., 3200 Walnut Street, Boulder, (22) International Filing Date: Colorado 80301 (US). REN, Li [US/US]; c/o Array Bio- 10 October 2017 (10.10.2017) Pharma Inc., 3200 Walnut Street, Boulder, Colorado 80301 (US). WALLS, Shane M. [US/US]; c/o Array BioPharma, (25) Filing Language: English Inc., 3200 Walnut St., Boulder, Colorado 80301 (US). (26) Publication Language: English (74) Agent: FOLLETT, Angela D. et al.; Fish & Richardson (30) Priority Data: P.C., P.O. Box 1022, Minneapolis, Minnesota 55440-1022 62/406,275 10 October 2016 (10.10.2016) US (US). 62/447,849 18 January 2017 (18.01.2017) US (81) Designated States (unless otherwise indicated, for every 62/491,180 27 April 2017 (27.04.2017) US kind of national protection available): AE, AG, AL, AM, 62/531,690 12 July 2017 (12.07.2017) US AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, 62/566,030 29 September 2017 (29.09.2017) US CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, (72) Inventors; and DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (71) Applicants: ANDREWS, Steven W. [US/US]; c/o Array HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, BioPharma Inc., 3200 Walnut Street, Boulder, Colorado KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 80301 (US). ARONOW, Sean [US/US]; c/o Array Bio- MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, Pharma, Inc., 3200 Walnut St., Boulder, Colorado 80301 OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (US). BLAKE, James F. [US/US]; c/o Array BioPhar- SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, ma Inc., 3200 Walnut Street, Boulder, Colorado 80301 TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (US). BRANDHUBER, Barbara J. [US/US]; c/o Array (84) Designated States (unless otherwise indicated, for every BioPharma Inc., 3200 Walnut Street, Boulder, Colorado kind of regional protection available): ARIPO (BW, GH, 80301 (US). COLLIER, James [US/US]; c/o Array Bio GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, Pharma, Inc., 3200 Walnut St., Boulder, Colorado 80301 UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (US). COOK, Adam [US/US]; c/o Array BioPharma Inc., 3200 Walnut Street, Boulder, Colorado 80301 (US). HAAS, 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, Julia [[JS/US]; c/o Array BioPharma Inc., 3200 Wal- MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, nut Street, Boulder, Colorado 80301 (US). JIANG, Yu- TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, tong [US/US]; c/o Array BioPharma Inc., 3200 Walnut KM, ML, MR, NE, SN, TD, TG). Street, Boulder, Colorado 80301 (US). KOLAKOWSKI, Gabrielle R. [US/US]; c/o Array BioPharma Inc., 3200 Published: Walnut Street, Boulder, Colorado 80301 (US). MCFAD- — DIN, Elizabeth A. [US/US]; c/o Array BioPharma, Inc., with international search report (Art. 21(3)) — with sequence listing part of description (Rule 5.2(a)) 3200 Walnut St., Boulder, Colorado 80301 (US). MCKEN- NEY, Megan L. [US/US]; c/o Array BioPharma, Inc., 3200 Walnut St., Boulder, Colorado 80301 (US). MCNULTY, Oren T. [US/US]; c/o Array BioPharma, Inc., 3200 Wal- nut St., Boulder, Colorado 80301 (US). METCALF, An- drew T. [US/US]; c/o Array BioPharma Inc., 3200 Wal- (54) Title: SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS (57) : Provided herein are compounds of the Formula I: (I) or pharmaceu- lin N i (Ra)„ tically acceptable salt or solvate thereof, wherein A, B, X 1 , X, X, X 2 3 4 , Ring D, E, 11' Il 1 X3=X2 R a , R b , n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which IN 0 p --.... / D ~X 4 _X~ d ca is rd n o b e e e tr rs . ated with a RET kinase inhibitor, including RET-associated diseases and X4-x1 B - O Il (Rb),„ © N I C
SG11201903187WA 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors SG11201903187WA (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662406275P 2016-10-10 2016-10-10
US201762447849P 2017-01-18 2017-01-18
US201762491180P 2017-04-27 2017-04-27
US201762531690P 2017-07-12 2017-07-12
US201762566030P 2017-09-29 2017-09-29
PCT/US2017/055993 WO2018071454A1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors

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SG11201903187WA true SG11201903187WA (en) 2019-05-30

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EP (2) EP4144735A1 (en)
JP (1) JP7075399B2 (en)
KR (1) KR102287752B1 (en)
CN (1) CN110177786B (en)
AU (1) AU2017342027B2 (en)
BR (1) BR112019007143A2 (en)
CA (1) CA3039912A1 (en)
CL (1) CL2019000942A1 (en)
CO (1) CO2019004649A2 (en)
CR (1) CR20190224A (en)
DK (1) DK3523302T3 (en)
DO (1) DOP2019000091A (en)
EC (1) ECSP19033052A (en)
ES (1) ES2926136T3 (en)
HR (1) HRP20221154T1 (en)
HU (1) HUE060089T2 (en)
IL (1) IL265918B (en)
JO (1) JOP20190077A1 (en)
LT (1) LT3523302T (en)
MD (1) MD3523302T2 (en)
MX (1) MX2019004204A (en)
PE (1) PE20191613A1 (en)
PH (1) PH12019500776A1 (en)
PL (1) PL3523302T3 (en)
PT (1) PT3523302T (en)
RS (1) RS63510B1 (en)
SA (1) SA519401544B1 (en)
SG (1) SG11201903187WA (en)
SI (1) SI3523302T1 (en)
TN (1) TN2019000107A1 (en)
TW (1) TWI752098B (en)
UA (1) UA125032C2 (en)
WO (1) WO2018071454A1 (en)

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