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1. 发明专利

SG11201910182RA STABLE FORMULATIONS OF PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF USE THEREOF 未知
公开(公告)号：SG11201910182RA
公开(公告)日：2019-11-28
申请号：SG11201910182R
申请日：2018-05-01
申请人： MERCK SHARP & DOHME
发明人： SHARMA MANOJ , BENJAMIN WENDY , MITTAL SARITA , BASARKAR ASHWIN , NARASIMHAN CHAKRAVARTHY NACHU , KASHI RAMESH , SHAMEEM MOHAMMED , BHATTACHARYA SOUMENDU , FORREST WILLIAM , KRISHNAMACHARI YOGITA
IPC分类号： A61K9/00 , A61K9/08 , A61K9/19 , A61K39/00 , A61K39/395 , A61K47/26 , C07K16/18
摘要： INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization IiiimmomiolollmonolooloionmllooluioluovoimIE International Bureau (10) International Publication Number WO 2018/204368 Al (43) International Publication Date 08 November 2018 (08.11.2018) WIPO I PCT (51) International Patent Classification: A61K 9/00 (2006.01) A61K 39/395 (2006.01) A61K 9/08 (2006.01) A61K 47/26 (2006.01) A61K 9/19 (2006.01) C07K 16/18 (2006.01) A61K 39/00 (2006.01) (21) International Application Number: PCT/US2018/030459 (22) International Filing Date: 01 May 2018 (01.05.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/500,238 02 May 2017 (02.05.2017) US (71) Applicant (for all designated States except US): MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (72) Inventors; and (71) Applicants (for US only): SHARMA, Manoj, K. [US/US]; 7 Fraser Street, Littleton, Massachusetts 01460 (US). BEN- JAMIN, Wendy [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). MITTAL, Sarita [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jer- sey 07033 (US). BASARKAR, Ashwin [IN/US]; 2304 Sunnyview Oval, Keasbey, New Jersey 08832 (US). NARASIMHAN, Chakravarthy Nachu [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). KASHI, Ramesh, K. [US/US]; 5 Hickory Lane, War- ren, New Jersey 07059 (US). SHAMEEM, Mohammed [US/US]; 4 Surim Court, Nanuet, New York 10954 (US). (72) Inventors; and (71) Applicants (for NZ, US only): BHATTACHARYA, Soumendu [US/US]; 2000 Galloping Hill Road, Kenil- worth, New Jersey 07033 (US). FORREST, William, P, Jr. [US/US]; 126 East Lincoln Avenue, Rahway, New Jer- sey 07065-0907 (US). (54) Title: STABLE FORMULATIONS OF PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF USE THEREOF Pre — Pea k 1+ 2 12 10 8 — 6 — 4- 2 Oxidation by HP—HIC =T=0 • . 4 weeks 8 weeks co 00 O C 0 H1 H2 H3 H4 H5 H6 H7 H8 H9 H10 H11 H12 H13 H14 Formulation FIG.7 (57) : The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. In some embodiments the formulations of the invention comprise between 5-200 mg/mL anti- PD-1 antibody, or antigen binding fragment thereof. The invention further provides methods for treating various cancers with stable formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by intravenous or subcutaneous administration. [Continued on next page] WO 2018/204368 Al MIDEDIMIIII11111111111111111111111111111111111111111111111011110111110111111111111 (74) Common Representative: MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (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). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(11)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a))

2. 发明专利

AU2018263862A1 Stable formulations of programmed death receptor 1 (PD-1) antibodies and methods of use thereof 未知
公开(公告)号：AU2018263862A1
公开(公告)日：2019-11-21
申请号：AU2018263862
申请日：2018-05-01
申请人： MERCK SHARP & DOHME
发明人： SHARMA MANOJ K , BENJAMIN WENDY , MITTAL SARITA , BASARKAR ASHWIN , NARASIMHAN CHAKRAVARTHY NACHU , KASHI RAMESH S , SHAMEEM MOHAMMED , BHATTACHARYA SOUMENDU , FORREST JR WILLIAM P , KRISHNAMACHARI YOGITA
IPC分类号： C07K16/18 , A61K9/00 , A61K9/08 , A61K9/19 , A61K39/00 , A61K39/395 , A61K47/26
摘要： The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. In some embodiments the formulations of the invention comprise between 5-200 mg/mL anti- PD-1 antibody, or antigen binding fragment thereof. The invention further provides methods for treating various cancers with stable formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by intravenous or subcutaneous administration.

3. 发明专利

SG184760A1 FORMULATION CONTAINING CYCLIN-DEPENDENT KINASE INHIBITING COMPOUND AND METHOD OF TREATING TUMORS USING THE SAME 未知
公开(公告)号：SG184760A1
公开(公告)日：2012-10-30
申请号：SG2012068458
申请日：2008-09-16
申请人： MERCK SHARP & DOHME
发明人： ANTOCHSHUK VALENTYN , BANNERJI RAJAT , DABBARA ANITA , KIRSCHMEIER PAUL , PARRY DAVID A , SHAMEEM MOHAMMED , STATKEVICH PAUL , YAO SIU-LONG
摘要： FORMULATION CONTAINING CYCLIN-DEPENDENT KINASE INHIBITING COMPOUND AND METHOD OF TREATING TUMORS USING THE SAMEThis application discloses a novel formulation containing a 3-amino-4-substitutedpyrazole derivative which has cyclin-dependent kinase inhibiting properties, and a method of treating tumors using the novel formulation.Figure 1.

4. 发明公开

EP2512489A4 FORMULATIONS OF ACADESINE 审中-公开
标题翻译：美洲洋麻黄素
公开(公告)号：EP2512489A4
公开(公告)日：2014-04-02
申请号：EP10838147
申请日：2010-12-09
申请人： MERCK SHARP & DOHME
发明人： ANTOCHSHUK VALENTYN , BHALLA AMARDEEP SINGH BHUPENDER , SHAMEEM MOHAMMED
IPC分类号： A61K31/7056 , A61K9/00 , A61K47/02 , A61K47/18
CPC分类号： A61K31/7056 , A61K9/0019 , A61K9/08 , A61K47/02 , A61K47/10 , A61K47/18

5. 发明专利

CL2019003142A1 Formulaciones estables de anticuerpos contra el receptor de muerte programada 1 (pd-1) y métodos para su uso. 未知
公开(公告)号：CL2019003142A1
公开(公告)日：2020-07-10
申请号：CL2019003142
申请日：2019-10-30
申请人： MERCK SHARP & DOHME
发明人： SHARMA MANOJ K , BENJAMIN WENDY , MITTAL SARITA , BASARKAR ASHWIN , NARASIMHAN CHAKRAVARTHY NACHU , KASHI RAMESH S , SHAMEEM MOHAMMED , BHATTACHARYA SOUMENDU , FORREST WILLIAM P JR , KRISHNAMACHARI YOGITA
IPC分类号： A61K39/00 , A61K9/00 , A61K9/08 , A61K9/19 , A61K39/395 , A61K47/26 , C07K16/18
摘要： La invención se refiere a formulaciones estables de anticuerpos contra el receptor de muerte programada humano PD-1, o fragmentos de fijación al antígeno de este. En algunas formas de realización, las formulaciones de la invención comprenden entre 5 y 200 mg/ml de anticuerpo anti-PD-1, o un fragmento de fijación al antígeno de este. La invención además proporciona métodos para tratar distintos tipos de cáncer con formulaciones estables de la invención. En algunas formas de realización de los métodos de la invención, las formulaciones se administran a un sujeto mediante administración intravenosa o subcutánea.

6. 发明专利

PE20200513A1 FORMULACIONES ESTABLES DE ANTICUERPOS CONTRA EL RECEPTOR DE MUERTE PROGRAMADA 1 (PD-1) Y METODOS PARA SU USO 未知
公开(公告)号：PE20200513A1
公开(公告)日：2020-03-05
申请号：PE2019002280
申请日：2018-05-01
申请人： MERCK SHARP & DOHME
发明人： SHARMA MANOJ K , BENJAMIN WENDY , MITTAL SARITA , BASARKAR ASHWIN , NARASIMHAN CHAKRAVARTHY NACHU , KASHI RAMESH S , SHAMEEM MOHAMMED , BHATTACHARYA SOUMENDU , FORREST JR WILLIAM P , KRISHNAMACHARI YOGITA
IPC分类号： A61K9/00 , A61K9/08 , A61K9/19 , A61K39/00 , A61K39/395 , A61K47/26 , C07K16/18
摘要： Referido a una formulacion de anticuerpo anti-PD 1 humano, que comprende: (a) alrededor de 5 a 200 mg/ml de un anticuerpo anti-PD-1 humano, o un fragmento de union al antigeno del mismo; (b) alrededor de 5 a 20 mM de amortiguador; (c) un estabilizante seleccionado entre: (1) alrededor de 6-8% p/v sacarosa, trehalosa, entre otros; (2) alrededor de 3-5% p/v manitol, sorbitol, entre otros; y alrededor de 1.8-2.2% p/v de glicina, o sal de esta farmaceuticamente aceptable; (d) alrededor de 0.01% a 0.10% de tensioactivo no ionico; y (e) alrededor de 1 a 20 mM de antioxidante; y en donde su pH esta entre 5.0 y 6.0. Esta formulacion estable, de solucion reconstituida, especificamente pembrolizumab, es util para el tratamiento de diversos tipos de cancer o infecciones cronicas, en donde su administracion es por via intravenosa o subcutanea.

7. 发明专利

CO2019012151A2 Formulaciones estables de anticuerpos contra el receptor de muerte programada 1 (pd-1) y métodos para su uso 未知
公开(公告)号：CO2019012151A2
公开(公告)日：2020-02-07
申请号：CO2019012151
申请日：2019-10-30
申请人： MERCK SHARP & DOHME
发明人： BHATTACHARYA SOUMENDU , NARASIMHAN CHAKRAVARTHY NACHU , SHARMA MANOJ K , BENJAMIN WENDY , MITTAL SARITA , BASARKAR ASHWIN , KASHI RAMESH S , SHAMEEM MOHAMMED , FORREST WILLIAM P JR , KRISHNAMACHARI YOGITA
IPC分类号： A61K9/00 , A61K9/08 , A61K9/19 , A61K39/00 , A61K39/395 , A61K47/26 , C07K16/18
摘要： La invención se refiere a formulaciones estables de anticuerpos contra el receptor de muerte programada humano PD-1, o fragmentos de fijación al antígeno de este. En algunas formas de realización, las formulaciones de la invención comprenden entre 5 y 200 mg/ml de anticuerpo anti-PD-1, o un fragmento de fijación al antígeno de este. La invención además proporciona métodos para tratar distintos tipos de cáncer con formulaciones estables de la invención. En algunas formas de realización de los métodos de la invención, las formulaciones se administran a un sujeto mediante administración intravenosa o subcutánea.

8. 发明专利

CA3062160A1 STABLE FORMULATIONS OF PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF USE THEREOF 未知
公开(公告)号：CA3062160A1
公开(公告)日：2018-11-08
申请号：CA3062160
申请日：2018-05-01
申请人： MERCK SHARP & DOHME
发明人： SHARMA MANOJ K , BENJAMIN WENDY , MITTAL SARITA , BASARKAR ASHWIN , NARASIMHAN CHAKRAVARTHY NACHU , KASHI RAMESH S , SHAMEEM MOHAMMED , BHATTACHARYA SOUMENDU , FORREST WILLIAM P , KRISHNAMACHARI YOGITA
IPC分类号： A61K47/26 , A61K39/395 , A61K47/18 , A61K47/20 , A61K47/22 , A61P31/00 , A61P35/00
摘要： The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. In some embodiments the formulations of the invention comprise between 5-200 mg/mL anti- PD-1 antibody, or antigen binding fragment thereof. The invention further provides methods for treating various cancers with stable formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by intravenous or subcutaneous administration.

10. 发明专利

AU2005272862B2 Stable pegylated interferon formulation 未知
公开(公告)号：AU2005272862B2
公开(公告)日：2011-03-10
申请号：AU2005272862
申请日：2005-08-11
申请人： MERCK SHARP & DOHME
发明人： SHAMEEM MOHAMMED , DABBARA ANITA
IPC分类号： A61K9/19 , A61K38/21 , A61K47/26 , A61K47/48 , A61P31/12 , A61P35/00
摘要： The present invention relates to lyophilized formulations of pegylated interferon which are prepared using trehalose as a cryoprotectant. The formulations have a low moisture content, which helps stabilize the pegylated interferon during storage of the formulations at room temperature. In addition, methods for preparing these formulations are provided.

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