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21. 发明公开

EP3204008A4 USE OF BIOMARKERS FOR PREDICTING CLINICAL SENSITIVITY TO CANCER TREATMENT 审中-公开
公开(公告)号：EP3204008A4
公开(公告)日：2018-03-07
申请号：EP15848775
申请日：2015-10-06
申请人： CELGENE CORP
发明人： LOPEZ-GIRONA ANTONIA , CATHERS BRIAN E , LU GANG , JACKSON PILGRIM , HANDA HIROSHI
IPC分类号： A61K31/454 , C07D401/04 , G01N33/574
CPC分类号： A61K31/454 , G01N33/57426 , G01N33/57484 , G01N2800/52
摘要： A method of identifying a subject having cancer who is likely to be responsive to a treatment compound, comprising administering the treatment compound to a subject having cancer; obtaining a sample from the subject; determining the level of a biomarker in the sample from the subject; and diagnosing the subject as being likely to be responsive to the treatment compound if the level of the biomarker in the sample of the subject changes as compared to a reference level of the biomarker; wherein the treatment compound is a compound of Formula (I):

22. 发明专利

AU2020372333A1 Methods for treating a hematological cancer and the use of companion biomarkers for 2-(2,6-Dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione 未知
公开(公告)号：AU2020372333A1
公开(公告)日：2022-04-28
申请号：AU2020372333
申请日：2020-10-20
申请人： CELGENE CORP
发明人： ANTON MARIA SORAYA CARRANCIO , FONTANILLO CELIA FONTANILLO , KASIBHATLA SHAILAJA , LOPEZ-GIRONA ANTONIA , LU GANG , WANG KAI
IPC分类号： C07D403/14 , A61P35/00 , C07D407/14
摘要： A method of identifying a subject having a hematological cancer who is likely to be responsive to a treatment compound, comprising administering the treatment compound to the subject having the hematological cancer; obtaining a sample from the subject; determining the level of a biomarker in the sample from the subject; and diagnosing the subject as being likely to be responsive to the treatment compound if the level of the biomarker in the sample of the subject changes as compared to a reference level of the biomarker; wherein the treatment compound is Compound 1, Compound 2, or Compound 3.

23. 发明专利

SG11202111232RA METHODS OF TREATING NON-HODGKIN LYMPHOMA USING 2-(2,6-DIOXOPIPERIDIN-3-YL)-4-((2-FLUORO-4-((3-MORPHOLINOAZETIDIN-1-YL)METHYL)BENZYL)AMINO)ISOINDOLINE-1,3-DIONE 未知
公开(公告)号：SG11202111232RA
公开(公告)日：2021-11-29
申请号：SG11202111232R
申请日：2020-04-09
申请人： CELGENE CORP
发明人： ANTON MARIA , BUCHHOLZ TONIA , LOPEZ-GIRONA ANTONIA , NARLA RAMA , POURDEHNAD MICHAEL
IPC分类号： A61K31/5377 , A61K39/395 , A61P35/00
摘要： Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with rituximab, for treating, preventing or managing non-Hodgkin lymphoma.

24. 发明专利

ES2872967T3 Métodos para determinar la eficacia de fármacos usando IKZF3 (AIOLOS) 未知
公开(公告)号：ES2872967T3
公开(公告)日：2021-11-03
申请号：ES18201542
申请日：2013-06-28
申请人： CELGENE CORP
发明人： SCHAFER PETER H , CHOPRA RAJESH , CORRAL LAURA , WANG MARIA YINGLIN , JACKSON PILGRIM , LOPEZ-GIRONA ANTONIA
IPC分类号： G01N33/50
摘要： Un método para determinar si un compuesto es capaz de alterar la respuesta inmune en un sujeto, que comprende: (a) poner en contacto una primera célula del sujeto con el compuesto in vitro; (b) obtener una primeras muestra de la primera célula de la etapa (a); (c) determinar el nivel de IKZF3 (Aiolos) en la primera muestra; y (d) comparar el nivel de IKZF3 (Aiolos) de la etapa (c) con el nivel de IKZF3 (Aiolos) obtenido de una muestra de referencia, en donde una disminución en el nivel en comparación con la referencia es indicativa de la eficacia del compuesto para alterar la respuesta inmune en el sujeto.

25. 发明专利

NZ765933A Antiproliferative compounds and methods of use thereof 未知
公开(公告)号：NZ765933A
公开(公告)日：2021-10-29
申请号：NZ76593315
申请日：2015-07-10
申请人： CELGENE CORP
发明人： MULLER GEORGE W , MAN HON-WAH , LOPEZ-GIRONA ANTONIA , MACBETH KYLE , HANSEN JOSHUA , CORREA MATTHEW , RAHEJA RAJ , KHALIL EHAB , CATHERS BRIAN E , POURDEHNAD MICHAEL
IPC分类号： C07D401/14 , A61K31/454 , A61P35/00 , C07D401/04
摘要： Compounds of formula (I) for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed. In Formula (I) R1 is optionally substituted cycloalkyi, aryl, heteroaryl or heterocyclyl; and R2 and R3 are each halo.

26. 发明专利

NZ728127A Antiproliferative compounds and methods of use thereof 未知
公开(公告)号：NZ728127A
公开(公告)日：2021-08-27
申请号：NZ72812715
申请日：2015-07-10
申请人： CELGENE CORP
发明人： MULLER GEORGE W , MAN HON-WAH , LOPEZ-GIRONA ANTONIA , MACBETH KYLE , HANSEN JOSHUA , CORREA MATTHEW , RAHEJA RAJ , KHALIL EHAB , CATHERS BRIAN E , POURDEHNAD MICHAEL
IPC分类号： C07D401/14 , A61K31/454 , A61P35/00 , C07D401/04
摘要： Compounds of formula (I) for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed. In Formula (I) R1 is optionally substituted cycloalkyi, aryl, heteroaryl or heterocyclyl; and R2 and R3 are each halo.

27. 发明专利

ES2843973T3 Composiciones y métodos para inducir cambios conformacionales en cereblon y otras ubiquitina ligasas E3 未知
公开(公告)号：ES2843973T3
公开(公告)日：2021-07-21
申请号：ES15811480
申请日：2015-06-26
申请人： CELGENE CORP
发明人： CHAMBERLAIN PHILIP PAUL , CATHERS BRIAN , LOPEZ-GIRONA ANTONIA
IPC分类号： A61K38/00 , A61K31/454 , A61K31/517 , A61P35/00 , A61P43/00 , C12Q1/37 , G01N23/20 , G16B15/00
摘要： Un método para identificar un compuesto de ensayo que induce un cambio conformacional en cereblon (CRBN) o altera de otra forma las propiedades de una superficie de CRBN, que comprende (a) (i) obtener una primera estructura de cristal de CRBN y un compuesto de referencia, y (ii) determinar una estructura tridimensional del primer cristal por difracción de rayos x para obtener un primer conjunto de coordenadas atómicas; (b) (i) obtener un segundo cristal que comprende CRBN y el compuesto de ensayo, y (ii) determinar una estructura tridimensional del segundo cristal por difracción de rayos x para obtener un segundo conjunto de coordenadas atómicas; y (c) comparar dicho primer conjunto de coordenadas atómicas con dicho segundo conjunto de coordenadas atómicas; en donde una diferencia en las coordenadas atómicas es indicativa de un compuesto que induce un cambio conformacional o alteración en CRBN; y en donde dicho cambio conformacional o alteración tiene un efecto en W380, W386 y/o W400 de CRBN; tiene un efecto en E377 de CRBN; o tiene un efecto en V388 de CRBN.

28. 发明专利

AU2017205170B2 Methods for treating cancer and the use of biomarkers as a predictor of clinical sensitivity to therapies 未知
公开(公告)号：AU2017205170B2
公开(公告)日：2021-06-24
申请号：AU2017205170
申请日：2017-01-06
申请人： CELGENE CORP
发明人： FILVAROFF ELLEN , LOPEZ-GIRONA ANTONIA , LU GANG
IPC分类号： C07D401/04 , A61K31/454 , C07D417/14
摘要： A method of identifying a subject having cancer who is likely to be responsive to a treatment compound, comprising administering the treatment compound to the subject having the cancer; obtaining a sample from the subject; determining the level of a biomarker in the sample from the subject; and diagnosing the subject as being likely to be responsive to the treatment compound if the level of the biomarker in the sample of the subject changes as compared to a reference level of the biomarker; wherein the treatment compound is a compound of Formula I:

29. 发明专利

PL3166937T3 ZWIĄZKI ANTYPROLIFERACYJNE I SPOSOBY ICH ZASTOSOWANIA 未知
公开(公告)号：PL3166937T3
公开(公告)日：2020-02-28
申请号：PL15739485
申请日：2015-07-10
申请人： CELGENE CORP
发明人： HANSEN JOSHUA , CORREA MATTHEW DANIEL , RAHEJA RAJ , LOPEZ-GIRONA ANTONIA , MAN HON-WAH , MULLER GEORGE W , KHALIL EHAB M , MACBETH KYLE , CATHERS BRIAN E , POURDEHNAD MICHAEL
IPC分类号： C07D401/14 , A61K31/454 , A61P35/00 , C07D401/04

30. 发明专利

SG11202000143PA ANTIPROLIFERATIVE COMPOUNDS AND METHODS OF USE THEREOF 未知
公开(公告)号：SG11202000143PA
公开(公告)日：2020-02-27
申请号：SG11202000143P
申请日：2018-07-09
申请人： CELGENE CORP
发明人： ALEXANDER MATTHEW , ARTMAN GERALD , BRAY GORDON , CARMICHAEL JAMES , CARRANCIO SORAYA , CATHERS BRIAN E , CORREA MATTHEW , HANSEN JOSHUA , HAVENS COURTNEY , KERCHER TIMOTHY , LOPEZ-GIRONA ANTONIA , LU XIAOLING , MAN HON-WAH , NAGY MARK , NARLA RAMA , PICCOTTI JOSEPH , PIERCE DANIEL , TAVARES-GRECO PAULA , WHITEFIELD BRANDON , WONG LILLY , ZOU NANFEI
IPC分类号： A61K31/496 , A61K31/573 , A61K38/05 , A61P35/00 , C07D241/02
摘要： INTERNATIONAL APPLICATION (19) World Intellectual Property Organization International Bureau PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) vitivio VIII oviolo ~~~~ I D oimIE (43) International Publication Date 17 January 2019 (17.01.2019) (10) International Publication Number WO 2019/014100 Al WIPO I PCT Cmpd No. Total AUC Compd A 1232 Compd 1 1547.5 Figure 1B MICHAEL, James [GB/GB]; 11 Cherry Tree Lane, Ed- walton, Nottingham NG12 4AL (GB). CARRANCIO, So- raya [ES/US]; 5205 Fiore Terrace, Apt. B419, San Diego, CA 92122 (US). CATHERS, Brian E. [US/US]; 10040 Branford Road, San Diego, CA 92129 (US). CORREA, Matthew, D. [US/US]; 9025 Three Seasons Road, San Diego, CA 92126 (US). HANSEN, Joshua [US/US]; 5633 Bellevue Avenue, La Jolla, CA 92037 (US). HAVENS, Courtney, G. [US/US]; 3504 Felton Street, San Diego, CA 92104 (US). KERCHER, Timothy, S. [US/US]; 11283 Paul Barwick Court, San Diego, CA 92126 (US). LOPEZ- GIRONA, Antonia [US/US]; 8959 January Place, San Diego, CA 92122 (US). LU, Xiaoling [CN/US]; 3 Run- nymede Court, Whippany, NJ 07981 (US). MAN, Hon- Wah [US/US]; 27 Grant Way, Princeton, NJ 08540 (US). NAGY, Mark, A. [US/US]; 345 Willowspring Drive N., Encinitas, CA 92024 (US). NARLA, Rama, K. [US/US]; 5157 Great Meadow Drive, San Diego, CA 92130 (US). PICCOTTI, Joseph, R. [US/US]; 742 Rihely Place, Encinitas, CA 92024 (US). PIERCE, Daniel, W. [US/US]; 3406 Lodge Drive, Belmont, CA 94002 (US). TAVARES- GRECO, Paula, A. [BR/US]; 300 Parsippany Road, Par- sippany, NJ 07054 (US). WHITEFIELD, Brandon, W. [US/US]; 6406 Friars Road, #335, San Diego, CA 92108 (US). WONG, Lilly, L. [US/US]; 871 Viva Court, Solana (51) International Patent Classification: A61K 31/496 (2006.01) A61K 31/573 (2006.01) CO7D 241/02 (2006.01) A61P 35/00 (2006.01) A61K 38/05 (2006.01) (21) International Application Number: PCT/US2018/041230 (22) International Filing Date: 09 July 2018 (09.07.2018) English English (25) Filing Language: (26) Publication Language: (30) Priority Data: 62/530,778 10 July 2017 (10.07.2017) US 62/593,185 30 November 2017 (30.11.2017) US 62/675,581 23 May 2018 (23.05.2018) US (71) Applicant: CELGENE CORPORATION [US/US]; 86 Morris Avenue, Summit, NJ 07901 (US). (72) Inventors; and (71) Applicants: ALEXANDER, Matthew, D. [US/US]; 12488 Carmel Cape, San Diego, CA 92130 (US). ART- MAN, Gerald, D., III [US/US]; 8 Halls Mill Road, As- bury, NJ 08802 (US). BRAY, Gordon, L. [US/US]; 301 Main Street, Unit 8C, San Francisco, CA 94105 (US). CAR- (54) Title: ANTIPROLIFERATWE COMPOUNDS AND METHODS OF USE THEREOF (57) : Provided herein is 4-(4-(44(2-(2,6-dioxopiperidin-3-y1)-1-oxoisoin- -• Compound A dolin-4-yfloxy)methypbenzyppiperazin- 1 -y1)-3-fluorobenzonitrile, or an enantiomer, a 600 mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, and —v— Compound 1 methods for treating, preventing or managing multiple myeloma using such compounds. Also provided are pharmaceutical compositions comprising the compounds, and methods of use of the compositions. 1 2 log[cpd], nM Figure 1A A - I Compound A Compound 1 W O 20 19/0 14100 Al [Continued on next page] WO 2019/014100 Al MIDEDIMOMOIDEIROMOIONIMMEIEDIONHEMOM1011 Beach, CA 92075 (US). ZOU, Nanfei [US/US]; 66 Wood- land Avenue, Fanwood, New Jersey 07023 (US). (74) Agent: BRUNER, Michael, J. et al.; Jones Day, 250 Vesey Street, New York, NY 10281-1047 (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). Published: — with international search report (Art. 21(3))

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