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1. 发明专利

IL265625D0 Activatable anti-ctla-4 antibodies and uses thereof 未知
公开(公告)号：IL265625D0
公开(公告)日：2019-05-30
申请号：IL26562519
申请日：2019-03-26
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC , TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
IPC分类号： C07K20060101
摘要： Provided herein are activatable anti-human CTLA-4 antibodies comprising a heavy chain comprising a VH domain and a light chain comprising a masking moiety (MM), a cleavable moiety (CM), and a VL domain. Such activatable anti-human CTLA-4 antibodies have CTLA-4 binding activity in the tumor microenvironment, where the masking moiety is removed by proteolytic cleavage of the cleavable moiety by tumor-specific proteases, but exhibit greatly reduced binding to CTLA-4 outside the tumor. In this way, the activatable anti-human CTLA-4 antibodies of the present invention retain anti-tumor activity while reducing the side effects associated with anti-CTLA-4 activity outside the tumor.

2. 发明专利

PE20191131A1 ANTICUERPOS ANTI ANTIGENO 4 DEL LINFOCITO T CITOTOXICO (CTLA-4) ACTIVABLES Y SUS USOS 未知
公开(公告)号：PE20191131A1
公开(公告)日：2019-09-02
申请号：PE2019000902
申请日：2017-11-02
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C07K19/00
摘要： SE REFIERE A UN ANTICUERPO ANTI-CTLA-4 HUMANO ACTIVABLE QUE COMPRENDE: I) UNA CADENA PESADA QUE COMPRENDE UN DOMINIO VARIABLE DE LA CADENA PESADA (VH) QUE COMPRENDE CDRH1 DE SEC ID NO: 557; CDRH2 DE SEC ID NO: 558; Y CDRH3 DE SEC ID NO: 559; Y II) UNA CADENA LIVIANA QUE COMPRENDE a) UN DOMINIO VARIABLE DE CADENA LIVIANA (VL) QUE COMPRENDE CDRL1 DE SEC ID NO: 560; CDRL2 DE SEC ID NO: 561; Y CDRL3 DE SEC ID NO: 562; b) UN RESTO ESCINDIBLE (CM); Y c) UN RESTO ENMASCARADOR (MM); DONDE DICHO ANTICUERPO ADEMAS COMPRENDE UN SEGUNDO PEPTIDO LIGADOR (LP2); UN AGENTE TOXICO Y UN RESTO DETECTABLE QUE ES UN AGENTE DE DIAGNOSTICO. TAMBIEN SE REFIERE A UN METODO PARA PRODUCIR UN ANTICUERPO ANTI-CTLA-4 HUMANO ACTIVABLE Y A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE DICHO ANTICUERPO, SIENDO UTIL EN EL TRATAMIENTO DEL CANCER DE VEJIGA, CANCER DE HUESO, MAMA, CUELLO UTERINO

3. 发明专利

SG11201902857SA ACTIVATABLE ANTI-CTLA-4 ANTIBODIES AND USES THEREOF 未知
公开(公告)号：SG11201902857SA
公开(公告)日：2019-05-30
申请号：SG11201902857S
申请日：2017-11-02
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C07K19/00
摘要： 40 60 Days Post Implantation 'gr ' E 2500- 10/10 TF nE 2500 E 2000- E 2000 E 1500- E 1500 7 , 1000- 0 1000 500- 0 E 500 0 0 20 40 60 Days Post Implantation 8/10 TF 20 40 60 Days Post Implantation rTe E E 0 0 2500 2000 1500 1000 500 0 FIG. 9D YV23 2001 9/10 TF 20 40 60 Days Post Implantation FIG. 9E YV24 2001 2500 2000 1500 1000 500 0 FIG. 9F YV39 2001 2500 2000 1500 1000 500 0 Fsi E E E E C . 7 2500 E 2000 E 1500 0 1000 8 500 E 0 7/10 TF 20 40 60 Days Post Implantation E ‘ E ) o 0 E I- 10/101T 20 40 60 Days Post Implantation (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (43) International Publication Date 1111111111110110101011111011110 100111MIONOITEREMOVIO# (10) International Publication Number WO 2018/085555 A8 11 May 2018 (11.05.2018) WIPO I PCT (51) International Patent Classification: CO7K 16/28 (2006.01) A61K 39/395 (2006.01) C07K 19/00 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/US2017/059740 (22) International Filing Date: 02 November 2017 (02.11.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/417,212 03 November 2016 (03.11.2016) US (71) Applicants: BRISTOL-MYERS SQUIBB COMPANY [US/US]; Rt. 206 & Province Line Road, Princeton, New Jersey 08543 (US). CYTOMX THERAPEUTICS, INC. [US/US]; 151 Oyster Point Boulevard, Suite 400, South San Francisco, California 94080 (US). (72) Inventors: TIPTON, Kimberly Ann; c/o CytomX Thera- peutics, Inc., 151 Oyster Point Boulevard, Suite 400, South San Francisco, California 94080 (US). WEST, James William; c/o CytomX Therapeutics, Inc., 151 Oyster Point Boulevard, Suite 400, South San Francisco, California 94080 (US). DESHPANDE, Shrikant; c/o Bristol-Myers Squibb Company, 700 Bay Road, Redwood City, California 94063 (US). ENGELHARDT, John J.; c/o Bristol-Myers Squibb Company, 700 Bay Road, Redwood City, California 94063 (US). (74) Agent: CALVO, Paul A. et al.; Sterne, Kessler, Goldstein & Fox P.L.L.C., 1100 New York Avenue, NW, Washing- ton, District of Columbia 20005 (US). (54) Title: ACTIVATABLE ANTI-CTLA-4 ANTIBODIES AND USES THEREOF FIG. 9A Control mg2a FIG. 9B !pi mg2a (YV1) FIG. 9C YV04 2001 (57) : Provided herein are activatable anti-human CTLA-4 antibodies comprising a heavy chain comprising a VH domain and a light chain comprising a masking moiety (MM), a cleavable moiety (CM), and a VL domain. Such activatable anti-human CTLA-4 00 antibodies have CTLA-4 binding activity in the tumor microenvironment, where the masking moiety is removed by proteolytic cleavage O of the cleavable moiety by tumor-specific proteases, but exhibit greatly reduced binding to CTLA-4 outside the tumor. In this way, the 00 activatable anti-human CTLA-4 antibodies of the present invention retain anti-tumor activity while reducing the side effects associated O with anti-CTLA-4 activity outside the tumor. O [Continued on next page] WO 2018/085555 A8 MIDEDIM01101 DIDIRE10111011111111111HHH11111111101111111111 (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). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) 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)) with sequence listing part of description (Rule 5.2(a)) (48) Date of publication of this corrected version: 31 May 2018 (31.05.2018) (15) Information about Correction: see Notice of 31 May 2018 (31.05.2018)

4. 发明专利

CL2019001226A1 Anticuerpos anti antígeno 4 del linfocito t citotóxico (ctla-4) activables y sus usos. 未知
公开(公告)号：CL2019001226A1
公开(公告)日：2019-09-13
申请号：CL2019001226
申请日：2019-05-03
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
IPC分类号： A61K39/395 , A61P35/00 , C07K16/28 , C07K19/00
摘要： EN LA PRESENTE SE PROPORCIONAN ANTICUERPOS ANTI-CTLA-4 HUMANO ACTIVABLES QUE COMPRENDEN UNA CADENA PESADA QUE COMPRENDE UN DOMINIO VH Y UNA CADENA LIVIANA QUE COMPRENDE UN RESTO ENMASCARADOR (MM). UN RESTO ESCINDIBLE (CM), Y UN DOMINIO VL. TALES ANTICUERPOS ANTI-CTLA-4 HUMANO ACTIVABLES TIENEN ACTIVIDAD DE UNIÓN A CTLA-4 EN EL MICROAMBIENTE TUMORAL, CARACTERIZADO PORQUE EL RESTO ENMASCARADOR SE ELIMINA POR ESCISIÓN PROTEOLÍTICA DEL RESTO ESCINDIBLE POR PROTEASAS ESPECÍFICAS DEL TUMOR, PERO EXHIBEN UNA UNIÓN MUY REDUCIDA A CTLA-4 FUERA DEL TUMOR. DE ESTA MANERA, LOS ANTICUERPOS ANTI-CTLA-4 HUMANO ACTIVABLES DE LA PRESENTE INVENCIÓN RETIENEN ACTIVIDAD ANTITUMORAL MIENTRAS QUE REDUCEN LOS EFECTOS SECUNDARIOS ASOCIADOS CON ACTIVIDAD ANTI-CTLA-4 FUERA DEL TUMOR.

5. 发明专利

CO2019004469A2 Anticuerpos anti antígeno 4 del linfocito t citotóxico (ctla-4) activables y sus usos 未知
公开(公告)号：CO2019004469A2
公开(公告)日：2019-05-10
申请号：CO2019004469
申请日：2019-04-30
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C07K19/00
摘要： En la presente se proporcionan anticuerpos anti-CTLA-4 humano activables que comprenden una cadena pesada que comprende un dominio VH y una cadena liviana que comprende un resto enmascarador (MM), un resto escindible (CM), y un dominio VL. Tales anticuerpos anti-CTLA-4 humano activables tienen actividad de unión a CTLA-4 en el microambiente tumoral, caracterizado porque el resto enmascarador se elimina por escisión proteolítica del resto escindible por proteasas específicas del tumor, pero exhiben una unión muy reducida a CTLA-4 fuera del tumor. De esta manera, los anticuerpos anti-CTLA-4 humano activables de la presente invención retienen actividad antitumoral mientras que reducen los efectos secundarios asociados con actividad anti-CTLA-4 fuera del tumor.

6. 发明专利

CA3042679A1 ACTIVATABLE ANTI-CTLA-4 ANTIBODIES AND USES THEREOF 未知
公开(公告)号：CA3042679A1
公开(公告)日：2018-05-11
申请号：CA3042679
申请日：2017-11-02
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C07K19/00
摘要： Provided herein are activatable anti-human CTLA-4 antibodies comprising a heavy chain comprising a VH domain and a light chain comprising a masking moiety (MM), a cleavable moiety (CM), and a VL domain. Such activatable anti-human CTLA-4 antibodies have CTLA-4 binding activity in the tumor microenvironment, where the masking moiety is removed by proteolytic cleavage of the cleavable moiety by tumor-specific proteases, but exhibit greatly reduced binding to CTLA-4 outside the tumor. In this way, the activatable anti-human CTLA-4 antibodies of the present invention retain anti-tumor activity while reducing the side effects associated with anti-CTLA-4 activity outside the tumor.

7. 发明专利

AU2017355446A1 Activatable anti-CTLA-4 antibodies and uses thereof 未知
公开(公告)号：AU2017355446A1
公开(公告)日：2019-05-02
申请号：AU2017355446
申请日：2017-11-02
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , DESHPANDE SHRIKANT , ENGELHARDT JOHN J
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C07K19/00
摘要： Provided herein are activatable anti-human CTLA-4 antibodies comprising a heavy chain comprising a VH domain and a light chain comprising a masking moiety (MM), a cleavable moiety (CM), and a VL domain. Such activatable anti-human CTLA-4 antibodies have CTLA-4 binding activity in the tumor microenvironment, where the masking moiety is removed by proteolytic cleavage of the cleavable moiety by tumor-specific proteases, but exhibit greatly reduced binding to CTLA-4 outside the tumor. In this way, the activatable anti-human CTLA-4 antibodies of the present invention retain anti-tumor activity while reducing the side effects associated with anti-CTLA-4 activity outside the tumor.

8. 发明专利

AR110678A1 ANTICUERPOS ANTI-CTLA-4 ACTIVABLES Y SUS USOS 未知
公开(公告)号：AR110678A1
公开(公告)日：2019-04-24
申请号：ARP170103060
申请日：2017-11-03
申请人： SQUIBB BRISTOL MYERS CO , CYTOMX THERAPEUTICS INC
发明人： ENGLEHARDT JOHN J , DESHPANDE SHRIKANT , WEST JAMES WILLIAM , TIPTON KIMBERLY ANN
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C07K16/24 , C07K19/00 , C12N15/13 , C12P21/02
摘要： Anticuerpos anti-CTLA-4 (antígeno 4 de linfocitos T citotóxicos) humano activables que comprenden una cadena pesada que comprende un dominio VH y una cadena liviana que comprende un resto enmascarador (MM), un resto escindible (CM), y un dominio VL. Tales anticuerpos anti-CTLA-4 humano activables tienen actividad de unión a CTLA-4 en el microambiente tumoral, donde el resto enmascarador se elimina por escisión proteolítica del resto escindible por proteasas especificas del tumor, pero exhiben una unión muy reducida a CTLA-4 fuera del tumor. De esta manera, los anticuerpos anti-CTLA-4 humano activables retienen actividad antitumoral mientras que reducen los efectos secundarios asociados con actividad anti-CTLA-4 fuera del tumor. Composición farmacéutica; molécula de ácido nucleico; vector; método.

9. 发明公开

KR20180040138A 항PD-1 항체, 활성화 가능한 항PD-1 항체, 및 이들의 사용 방법 审中-公开
公开(公告)号：KR20180040138A
公开(公告)日：2018-04-19
申请号：KR20187003863
申请日：2016-07-13
申请人： CYTOMX THERAPEUTICS INC
发明人： TIPTON KIMBERLY ANN , WEST JAMES WILLIAM , CHAN CHANTY MARIATEGUE
IPC分类号： C07K16/28 , A61K39/00 , A61K47/68 , C07K16/30
CPC分类号： C07K16/2818 , A61K39/3955 , A61K47/6849 , A61K2039/505 , A61K2039/507 , A61K2039/545 , C07K16/30 , C07K16/3015 , C07K16/3023 , C07K16/303 , C07K16/3038 , C07K16/3046 , C07K16/3053 , C07K16/3069 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/569 , C07K2317/622 , C07K2317/76 , C07K2317/92 , C07K2319/50
摘要： 본발명은일반적으로프로그램화된세포사멸단백질 1(PD-1)에특이적으로결합하는항체, PD-1에특이적으로결합하는활성화가능한항체및 상기항PD-1 항체및 항PD-1 활성화가능한항체의제조방법및 다양한치료학적, 진단학적및 예방학적적응증에서의사용방법에관한것이다.

10. 发明申请

WO2014026136A3 PROTEASE-RESISTANT SYSTEMS FOR POLYPEPTIDE DISPLAY AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译：多肽显示抗蛋白酶体系及其制备及其使用方法
公开(公告)号：WO2014026136A3
公开(公告)日：2014-05-08
申请号：PCT/US2013054378
申请日：2013-08-09
申请人： CYTOMX THERAPEUTICS INC
发明人： LA PORTE SHERRY , WEST JAMES WILLIAM , MOORE STEPHEN JAMES
IPC分类号： C12N1/21
CPC分类号： C12N15/1037 , C07K14/001 , C07K14/705 , C07K16/18 , C07K16/2809 , C07K16/2866 , C07K2317/622 , C07K2319/02 , C07K2319/03 , C07K2319/21 , C12N15/1044 , C12Q1/37 , C40B40/02 , G01N33/6845
摘要： The present invention generally relates to bacterial polypeptide display systems, libraries using these bacterial display systems, and methods of making and using these systems, including methods for improved display of polypeptides on the extracellular surface of bacteria using circularly permuted transmembrane bacterial polypeptides that have been modified to increase resistance to protease degradation and to enhance polypeptide display characteristics.
摘要翻译：本发明一般涉及细菌多肽展示系统，使用这些细菌显示系统的文库，以及制备和使用这些系统的方法，包括使用已经修饰的环状置换的跨膜细菌多肽来改善细菌细胞外表面多肽的显示方法以增加对蛋白酶降解的抗性并增强多肽显示特征。

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