SG11201908619TA - Pd-1/pd-l1 inhibitors - Google Patents

Pd-1/pd-l1 inhibitors

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Publication number
SG11201908619TA
SG11201908619TA SG11201908619TA SG11201908619TA SG 11201908619T A SG11201908619T A SG 11201908619TA SG 11201908619T A SG11201908619T A SG 11201908619TA SG 11201908619T A SG11201908619T A SG 11201908619TA
Authority
SG
Singapore
Prior art keywords
california
foster city
gilead sciences
lakeside
co7d
Prior art date
Application number
Inventor
Evangelos Aktoudianakis
Todd Appleby
Aesop Cho
Zhimin Du
Michael Graupe
Juan A Guerrero
Salman Y Jabri
Lateshkumar Thakorlal Lad
Tello Paulo A Machicao
Jonathan William Medley
Samuel E Metobo
Prasenjit Kumar Mukherjee
Devan Naduthambi
Gregory Notte
Eric Q Parkhill
Barton W Phillips
Scott Preston Simonovich
Neil H Squires
Chandrasekar Venkataramani
Peiyuan Wang
William J Watkins
Jie Xu
Kin Shing Yang
Christopher Allen Ziebenhaus
Original Assignee
Gilead Sciences 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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of SG11201908619TA publication Critical patent/SG11201908619TA/en

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    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 containing two hetero rings
    • C07D401/12Heterocyclic 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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
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    • C07D295/088Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 25 October 2018 (25.10.2018) WIPO I PCT omit IIl °nolo oimIE (10) International Publication Number WO 2018/195321 Al (51) International Patent Classification: C07D 405/14 (2006.01) CO7D 519/00 (2006.01) A61K 31/497 (2006.01) A61P 35/00 (2006.01) CO7D 403/14 (2006.01) CO7D 401/14 (2006.01) CO7D 241/18 (2006.01) CO7D 401/04 (2006.01) CO7D 241/20 (2006.01) CO7D 498/04 (2006.01) CO7D 487/08 (2006.01) CO7D 213/61 (2006.01) CO7D 487/10 (2006.01) CO7D 213/64 (2006.01) CO7D 491/107 (2006.01) (21) International Application Number: PCT/US2018/028382 (22) International Filing Date: 19 April 2018 (19.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/488,017 20 April 2017 (20.04.2017) US 62/507,678 17 May 2017 (17.05.2017) US (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 Lakeside Drive, Foster City, California 94404 (US). (72) Inventors: AKTOUDIANAKIS, Evangelos; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). APPLEBY, Todd; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). CHO, Aesop; c/o Gilead Sciences, Inc., 333 Lakeside Dri- ve, Foster City, California 94404 (US). DU, Zhimin; c/ o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). GRAUPE, Michael; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). GUERRERO, Juan A.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). JABRI, Salman Y.; 870 Harrison St., Unit 404, San Francisco, California 94107 (US). LAD, Lateshku- mar Thakorlal; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). MACHICAO TELLO, Paulo A.; c/o Gilead Sciences, Inc., 333 Lake- side Drive, Foster City, California 94404 (US). MEDLEY, Jonathan William; c/o Gilead Sciences, Inc., 333 Lake- side Drive, Foster City, California 94404 (US). METO- BO, Samuel E.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). MUKHERJEE, Declarations under Rule 4.17: Prasenjit Kumar; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). NADUTHAM- 1-1 BI, Devan; c/o Gilead Sciences, Inc., 333 Lakeside Dri- ve, Foster City, California 94404 (US). NOTTE, Grego- ry; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). PARKHILL, Eric Q.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Cal- (54) Title: PD-1/PD-L1 INHIBITORS ifornia 94404 (US). PHILLIPS, Barton W.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). SIMONOVICH, Scott Preston; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Califor- nia 94404 (US). SQUIRES, Neil H.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). VENKATARAMANI, Chandrasekar; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). WANG, Peiyuan; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). WATKINS, William J.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). XU, Jie; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). YANG, Kin Shing; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Califor- nia 94404 (US). ZIEBENHAUS, Christopher Allen; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Cal- ifornia 94404 (US). (74) Agent: TANNER, Lorna L. et al.; SHEPPARD MULLIN RICHTER & HAMPTON, 379 Lytton Avenue, Palo Alto, California 94301-1479 (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, 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). as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) 1-1 © (57) : Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents N and compositions of said compounds for the treatment of cancer are disclosed. O [Continued on next page] WO 2018/195321 Al IIMEDIMOM0101011EFIEDERIMEIIIMOVOIllii0VOIMIE Published: with international search report (Art. 21(3)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h))
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