IP Library Granted Patent US 10,646,584
Granted Patent B2
US 10,646,584 · App. 16/412,138 · Granted May 12, 2020

Pyrrolobenzodiazepines and conjugates thereof

Inventor: Philip Wilson Howard (Cambridge, GB)
Assignee: MEDIMMUNE LIMITED
A61K47/6855A61K45/06A61K47/65A61K47/6803C07D487/04C07D519/00Y02P20/582
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Quick Facts
Patent No.
US 10,646,584
App. No.
16/412,138
Granted
May 12, 2020
Kind
B2
Abstract

A compound which is either A: or B: and salts and solvates thereof, as well as their conjugates with a cell-binding agent.

Claims (103)

1. A method of providing compound RelB to a target proliferative cell population in a subject:

which comprises contacting a target proliferative cell population with a conjugate of formula ConjB:

wherein “CBA” represents a cell binding agent.

2. The method according to claim 1 , wherein the cell binding agent is an antibody or an active fragment thereof.

3. The method according to claim 2 , wherein the antibody or antibody fragment is an antibody or antibody fragment for a tumor-associated antigen.

4. The method of claim 2 , wherein the antibody or antibody fragment is an antibody which binds to one or more tumor-associated antigens or cell-surface receptors selected from (1)-(88):

(1) BMPR1B;

(2) E16;

(3) STEAP1;

(4) 0772P;

(5) MPF;

(6) Napi3b;

(7) Sema 5b;

(8) PSCA hlg;

(9) ETBR;

(10) MSG783;

(11) STEAP2;

(12) TrpM4;

(13) CRIPTO;

(14) CD21;

(15) CD79b;

(16) FcRH2;

(17) HER2;

(18) NCA;

(19) MDP;

(20) IL20R-alpha;

(21) Brevican;

(22) EphB2R;

(23) ASLG659;

(24) PSCA;

(25) GEDA;

(26) BAFF-R;

(27) CD22;

(28) CD79a;

(29) CXCR5;

(30) HLA-DOB;

(31) P2X5;

(32) CD72;

(33) LY64;

(34) FcRH1;

(35) IRTA2;

(36) TENB2;

(37) PSMA—FOLH1;

(38) SST;

(38.1) SSTR2;

(38.2) SSTR5;

(38.3) SSTR1;

(38.4)SSTR3;

(38.5) SSTR4;

(39) ITGAV;

(40) ITGB6;

(41) CEACAM5;

(42) MET;

(43) MUC1;

(44) CA9;

(45) EGFRvIII;

(46) CD33;

(47) CD19;

(48) IL2RA;

(49) AXL;

(50) CD30-TNFRSF8;

(51) BCMA-TNFRSF17;

(52) CT Ags—CTA;

(53) CD174 (Lewis Y)-FUT3;

(54) CLEC14A;

(55) GRP78—HSPA5;

(56) CD70;

(57) Stem Cell specific antigens;

(58) ASG-5;

(59) ENPP3;

(60) PRR4;

(61) GCC—GUCY2C;

(62) Liv-1—SLC39A6;

(63) 5T4;

(64) CD56—NCMA1;

(65) CanAg;

(66) FOLR1;

(67) GPNMB;

(68) TIM-1—HAVCR1;

(69) RG-1/Prostate tumor target Mindin—Mindin/RG-1;

(70) B7-H4—VTCN1;

(71) PTK7;

(72) CD37;

(73) CD138—SDC1;

(74) CD74;

(75) Claudins—CLs;

(76) EGFR;

(77) Her3;

(78) RON-MST1R;

(79) EPHA2;

(80) CD20—MS4A1;

(81) Tenascin C—TNC;

(82) FAP;

(83) DKK-1;

(84) CD52;

(85) CS1-SLAMF7;

(86) Endoglin-ENG;

(87) Annexin A1—ANXA1;

(88) V-CAM (CD106)-VCAM1.

5. The method of claim 2 , wherein the antibody or antibody fragment is a cysteine-engineered antibody.

6. The method of claim 2 , wherein the drug loading (p) of drugs (D) to antibody (Ab) is an integer from 1 to about 8.

7. The method of claim 6 , wherein p is 1, 2, 3, or 4.

8. The method of claim 1 , wherein the target proliferative cell population is a tumor cell population.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2019
From: SPIROGEN SÀRL
To: MEDIMMUNE LIMITED
Reel/Frame 049208/0850 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 15, 2019
From: HOWARD, PHILIP WILSON
To: SPIROGEN LIMITED
Reel/Frame 049188/0378 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 15, 2019
From: SPIROGEN LIMITED
To: SPIROGEN DEVELOPMENTS SÀRL
Reel/Frame 049188/0394 →
MERGER Recorded May 15, 2019
From: SPIROGEN DEVELOPMENTS SÀRL
To: SPIROGEN SÀRL
Reel/Frame 049188/0402 →
Continuity (4)
Continuation 15847308 · Dec 19, 2017
Continuation 14051743 · Oct 11, 2013
Provisional Application 61712928 · Oct 12, 2012
Related Publication 20190388554A1 · Dec 26, 2019