HRP20170334T1 - Spojevi enedina, njihovi konjugati, primjene i metode - Google Patents

Spojevi enedina, njihovi konjugati, primjene i metode Download PDF

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HRP20170334T1
HRP20170334T1 HRP20170334TT HRP20170334T HRP20170334T1 HR P20170334 T1 HRP20170334 T1 HR P20170334T1 HR P20170334T T HRP20170334T T HR P20170334TT HR P20170334 T HRP20170334 T HR P20170334T HR P20170334 T1 HRP20170334 T1 HR P20170334T1
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Naidu S. Chowdari
Sanjeev Gangwar
Bilal Sufi
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Bristol-Myers Squibb Company
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/439—Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans

Claims (13)

1. Spoj koji ima strukturu predstavljenu formulom (I) [image] gdje R0 je NHR1a, NHC(=O)OR1b, NHC(=O)NHR1b, OC(=O)NHR1b, (CH2)1-4NHR1a, F, Cl, Br, OR1a, ili SR1b; R1a je H, C1-C6 alkil, (CH2)nNH2, C(=O)(CH2)nNH2, C(=O)CHR8NH2, ili C(=O)R9NH2; R1b je H, C1-C6 alkil, (CH2)nNH2, [image] R2 je H, R10, C(=O)R10, ili C(=O)OR10; R3 je H ili nesupstituirani ili supstituirani C1-C6 alkil; R4 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R5 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R6 je H ili nesupstituirani ili supstituirani C1-C6 alkil; ili R5 i R6 se kombiniraju da formiraju =O; R7 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b; OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R8 je ostatak bočnog lanca α-amino kiseline odabrane od grupe koja se sastoji od alanin, arginin, asparagin, asparaginska kiselina, γ-karboksiglutaminska kiselina, citrulin, cistein, glutaminska kiselina, glutamin, glicin, histidin, izoleucin, leucin, lizin, metionin, norleucin, norvalin, ornitin, fenilalanin, serin, treonin, triptofan, tirozin, i valin; R9 je nesupstituiran ili supstituiran arilen, nesupstituiran ili supstituiran heteroarilen, nesupstituiran ili supstituiran alkilarilen, nesupstituiran ili supstituiran cikloalkilen ili nesupstituiran ili supstituiran heterocikloalkilen; svako R10 je nezavisno nesupstituiran ili supstituiran C1-C6 alkil, nesupstituiran ili supstituiran cikloalkil, nesupstituiran ili supstituiran heterocikloalkil, nesupstituiran ili supstituiran arilalkil, nesupstituiran ili supstituiran aril; ili nesupstituiran ili supstituiran heteroaril; gdje supstituenti supstituiranih dijelova su nezavisno jedan od drugog odabrani od alkil, alkenil, alkinil, aril, heteroaril, cikloalifatik, heterocikloalifatik, halo, haloalkil, hidroksil, hidroksialkil, cijano, nitro, alkoksi, -O(hidroksialkil), -O(haloalkil), -O(cikloalkil), -O(heterocikloalkil), -O(aril), alkiltio, ariltio, =O, =NH, =N(alkil), =NOH, =NO(alkil), -C(=O)(alkil), -C(=O)H, -CO2H, -C(=O)NHOH, -C(=O)O(alkil), -C(=O)O(hidroksialkil), -C(=O)NH2, -C(=O)NH(alkil), -C(=O)N(alkil)2, -OC(=O)(alkil), -OC(=O)(hidroksialkil), -OC(=O)O(alkil), -OC(=O)O(hidroksialkil), -OC(=O)NH2, -OC(=O)NH(alkil), -OC(=O)N(alkil)2, azido, -NH2, -NH(alkil), -N(alkil)2, -NH(aril), -NH(hidroksialkil), -NHC(=O)(alkil), -NHC(=O)H, -NHC(=O)NH2, -NHC(=O)NH(alkil), -NHC(=O)N(alkil)2, -NHC(=NH)NH2, -OSO2(alkil), -SH, -S(alkil), -S(aril), -S(cikloalkil), -S(=O)alkil, -SO2(alkil), -SO2NH2, -SO2NH(alkil), i -SO2N(alkil)2; i n je 2, 3, 4, 5, ili 6; ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu sa patentnim zahtjevom 1, koje ima strukturu predstavljenu formulom (Ia): [image]
3. Spoj u skladu sa patentnim zahtjevom 1, koje ima strukturu predstavljenu formulom (Ib): [image]
4. Spoj u skladu sa patentnim zahtjevom 3, gdje R1a je odabrano od grupe koja se sastoji od H, Me, [image] [image] i [image]
5. Konjugat, koji ima strukturu predstavljenu formulom (III) [D(XD)aC(XZ]b]mZ (III) gdje Z je ciljajući dio; XD je prvi dio koji razdvaja; XZ je drugi dio koji razdvaja; C je odvojiva grupa; indeksi a i b su nezavisno 0 ili 1; indeks m je l, 2, 3, 4, 5, 6, 7, 8, 9, ili 10; i D je odabrano iz grupe koja se sastoji od [image] [image] [image] [image] [image] ili [image] gdje R2 je H, R10, C(=O)R10, ili C(=O)OR10; R3 je H ili nesupstituiran ili supstituiran C1-C6 alkil; R4 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R5 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R6 je H ili nesupstituiran ili supstituiran C1-C6 alkil; ili R5 i R6 kombiniraju se da formiraju =O; R7 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R8 je bočni lanac ostatka α-amino kiseline odabran od grupe koja se sastoji od alanin, arginin, asparagin, asparaginska kiselina, γ-karboksiglutaminska kiselina, citrulin, cistein, glutaminska kiselina, glutamin, glicin, histidin, izoleucin, leucin, lizin, metionin, norleucin, norvalin, ornitin, fenilalanin, serin, treonin, triptofan, tirozin, i valin; R9 je nesupstituiran ili supstituiran arilen, nesupstituiran ili supstituiran heteroarilen, nesupstituiran ili supstituiran alkilarilen, nesupstituiran ili supstituiran cikloalkilen ili nesupstituiran ili supstituiran heterocikloalkilen; svako R10 je nezavisno nesupstituiran ili supstituiran C1-C6 alkil, nesupstituiran ili supstituiran cikloalkil, nesupstituiran ili supstituiran heterocikloalkil, nesupstituiran ili supstituiran arilalkil, nesupstituiran ili supstituiran aril; ili nesupstituiran ili supstituiran heteroaril; R12 je C1-C6 alkil; gdje supstituenti supstituiranih dijelova su nezavisno jedan od drugog odabrani od alkil, alkenil, alkinil, aril, heteroaril, cikloalifatik, heterocikloalifatik, halo, haloalkil, hidroksil, hidroksialkil, cijano, nitro, alkoksi, -O(hidroksialkil), -O(haloalkil), -O(cikloalkil), -O(heterocikloalkil), -O(aril), alkiltio, ariltio, =O, =NH, =N(alkil), =NOH, =NO(alkil), -C(=O)(alkil), -C(=O)H, -CO2H, -C(=O)NHOH, -C(=O)O(alkil), -C(=O)O(hidroksialkil), -C(=O)NH2, -C(=O)NH(alkil), -C(=O)N(alkil)2, -OC(=O)(alkil), -OC(=O)(hidroksialkil), -OC(=O)O(alkil), -OC(=O)O(hidroksialkil), -OC(=O)NH2, -OC(=O)NH(alkil), -OC(=O)N(alkil)2, azido, -NH2, -NH(alkil), -N(alkil)2, -NH(aril), -NH(hidroksialkil), -NHC(=O)(alkil), -NHC(=O)H, -NHC(=O)NH2, -NHC(=O)NH(alkil), -NHC(=O)N(alkil)2, -NHC(=NH)NH2, -OSO2(alkil), -SH, -S(alkil), -S(aril), -S(cikloalkil), -S(=O)alkil, -SO2(alkil), -SO2NH2, -SO2NH(alkil), i -SO2N(alkil)2; i n je 2, 3,4, 5, ili 6.
6. Kompozicija koja ima strukturu u skladu sa formulom (IV) D-(XD)aC(XZ)b-R31 (IV) gdje R31 je reaktivna funkcionalna grupa; XD je prvi dio koji razdvaja; XZ je drugi dio koji razdvaja; C je odvojiva grupa; indeksi a i b su nezavisno 0 ili 1; indeks m je l, 2, 3, 4, 5, 6, 7, 8, 9, ili 10; i D je odabrano od grupe koja se sastoji od [image] [image] [image] [image] [image] ili [image] gdje R2 je H, R10, C(=O)R10, ili C(=O)OR10; R3 je H ili nesupstituirani ili supstituirani C1-C6 alkil; R4 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R5 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R6 je H ili nesupstituiran ili supstituiran C1-C6 alkil; ili R5 i R6 koji se kombiniraju da formiraju =O; R7 je OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(=O)OR10, OC(=O)NHR1b, OC(=O)R10, SC(=O)R10, ili NHC(=O)R10; R8 je ostatak bočnog lanca α-amino kiseline odabrane od grupe koja se sastoji od alanin, arginin, asparagin, asparaginska kiselina, γ-karboksiglutaminska kiselina, citrulin, cistein, glutaminska kiselina, glutamin, glicin, histidin, izoleucin, leucin, lizin, metionin, norleucin, norvalin, ornitin, fenilalanin, serin, treonin, triptofan, tirozin, i valin; R9 je nesupstituiran ili supstituiran arilen, nesupstituiran ili supstituiran heteroarilen, nesupstituiran ili supstituiran alkilarilen, nesupstituiran ili supstituiran cikloalkilen ili nesupstituiran ili supstituiran heterocikloalkilen; svaki R10 je nezavisno nesupstituiran ili supstituiran C1-C6 alkil, nesupstituiran ili supstituiran cikloalkil, nesupstituiran ili supstituiran heterocikloalkil, nesupstituiran ili supstituiran arilalkil, nesupstituiran ili supstituiran aril; ili nesupstituiran ili supstituiran heteroaril; R12 je C1-C6 alkil; gdje su susptituenti supstituiranih dijelova nezavisno jedan od drugog izabrani od alkil, alkenil, alkinil, aril, heteroaril, cikloalifatik, heterocikloalifatik, halo, haloalkil, hidroksil, hidroksialkil, cijano, nitro, alkoksi, -O(hidroksialkil), -O(haloalkil), -O(cikloalkil), -O(heterocikloalkil), -O(aril), alkiltio, ariltio, =O, =NH, =N(alkil), =NOH, =NO(alkil), -C(=O)(alkil), -C(=O)H, -CO2H, -C(=O)NHOH, -C(=O)O(alkil), -C(=O)O(hidroksialkil), -C(=O)NH2, -C(=O)NH(alkil), -C(=O)N(alkil)2, -OC(=O)(alkil), -OC(=O)(hidroksialkil), -OC(=O)O(alkil), -OC(=O)O(hidroksialkil), -OC(=O)NH2, -OC(=O)NH(alkil), -OC(=O)N(alkil)2, azido, -NH2, -NH(alkil), -N(alkil)2, -NH(aril), -NH(hidroksialkil), -NHC(=O)(alkil), -NHC(=O)H, -NHC(=O)NH2, -NHC(=O)NH(alkil), -NHC(=O)N(alkil)2, -NHC(=NH)NH2, -OSO2(alkil), -SH, -S(alkil), -S(aril), -S(cikloalkil), -S(=O)alkil, -SO2(alkil), -SO2NH2, -SO2NH(alkil), i -SO2N(alkil)2; i n je 2, 3, 4, 5, ili 6.
7. Kompozicija prema patentnom zahtjevu 6, gdje R31 je -NH2, -OH, -CO2H, -SH, maleimido, ciklooktin, azido, hidroksilamino, ili N-hidroksisukcinimido.
8. Kompozicija prema bilo kojem od patentnih zahtjeva 1 do 4 ili konjugat prema patentnom zahtjevu 5 za primjenu u metodi za liječenje raka kod subjekta koji je obolio od takvog raka.
9. Kompozicija prema bilo kojem od patentnih zahtjeva 1 do 4 za primjenu u metodi za liječenje raka prema patentnom zahtjevu 8, gdje je spoj konjugiran za ciljajući dio koji je antitijelo.
10. Kompozicija prema bilo kojem od patentnih zahtjeva 1 do 4 za primjenu u metodi za liječenje raka prema patentnom zahtjevu 9, gdje se antitijelo vezuje za antigen koji je prekomjerno eksprimiran ili jedinstveno eksprimiran pomoću raka.
11. Kompozicija prema bilo kojem od patentnih zahtjeva 1 do 4 ili konjugat prema patentnom zahtjevu 5 za primjenu u metodi za liječenje raka prema patentnom zahtjevu 8, gdje je rak odabran iz grupe koja se sastoji od leukemije, raka bubrega, raka jajnika, raka pluća, raka debelog crijeva, raka dojke, i raka prostate.
12. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 4 i farmaceutski prihvatljiv nosač.
13. Farmaceutska kompozicija koja sadrži konjugat prema patentnom zahtjevu 5 i farmaceutski prihvatljiv nosač.
HRP20170334TT 2012-02-13 2017-03-01 Spojevi enedina, njihovi konjugati, primjene i metode HRP20170334T1 (hr)

Applications Claiming Priority (4)

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US201261598143P 2012-02-13 2012-02-13
US201261653785P 2012-05-31 2012-05-31
PCT/US2013/025247 WO2013122823A1 (en) 2012-02-13 2013-02-08 Enediyne compounds, conjugates thereof, and uses and methods therefor
EP13704871.6A EP2814829B1 (en) 2012-02-13 2013-02-08 Enediyne compounds, conjugates thereof, and uses and methods therefor

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Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
MX368016B (es) * 2013-08-14 2019-09-13 Univ Rice William M Derivados de uncialamicina, métodos de sintesis y su uso como agentes antitumor.
EP3647322B1 (en) 2014-03-20 2021-10-20 Bristol-Myers Squibb Company Stabilized fibronectin based scaffold molecules
SI3221363T1 (sl) 2014-11-21 2020-09-30 Bristol-Myers Squibb Company Protitelesa proti CD73 in njihova uporaba
LT3221346T (lt) 2014-11-21 2020-11-10 Bristol-Myers Squibb Company Antikūnai, apimantys modifikuotas sunkiosios grandinės pastoviąsias sritis
EP3224277B1 (en) 2014-11-25 2020-08-26 Bristol-Myers Squibb Company Novel pd-l1 binding polypeptides for imaging
US10336766B2 (en) * 2015-01-08 2019-07-02 The Scripps Research Institute Anticancer drug candidates
ES2736106T3 (es) 2015-03-10 2019-12-26 Bristol Myers Squibb Co Anticuerpos que se pueden conjugar mediante la transglutaminasa y conjugados producidos a partir de ellos
HUE061253T2 (hu) 2015-05-29 2023-06-28 Bristol Myers Squibb Co Antitestek OX40 ellen és azok felhasználásai
CN108884147B (zh) 2015-09-23 2024-02-27 百时美施贵宝公司 结合磷脂酰肌醇蛋白聚糖3的基于纤连蛋白的支架分子
CN107043406B (zh) 2015-11-03 2021-08-17 财团法人工业技术研究院 化合物、连接子-药物、及配体-药物耦合体
CA3008678A1 (en) 2015-12-21 2017-06-29 Bristol-Myers Squibb Company Variant antibodies for site-specific conjugation
IL295230A (en) 2016-03-04 2022-10-01 Bristol Myers Squibb Co Combination therapy with anti-cd73 antibodies
CN106267188A (zh) * 2016-08-15 2017-01-04 深圳大学 小分子免疫激动剂偶联pd‑1抗体的新型抗体及其在抗肿瘤中的应用
WO2018048975A1 (en) 2016-09-09 2018-03-15 Bristol-Myers Squibb Company Use of an anti-pd-1 antibody in combination with an anti-mesothelin antibody in cancer treatment
WO2018218056A1 (en) 2017-05-25 2018-11-29 Birstol-Myers Squibb Company Antibodies comprising modified heavy constant regions
EP3720504A1 (en) * 2017-12-06 2020-10-14 Synaffix B.V. Enediyne conjugates
CN110183659B (zh) * 2018-02-21 2022-04-26 香港科技大学 含有杂环的聚合物、其制备方法及其应用
JP2022513653A (ja) 2018-11-28 2022-02-09 ブリストル－マイヤーズ スクイブ カンパニー 修飾された重鎖定常領域を含む抗体
FI3886914T3 (fi) 2018-11-30 2023-05-26 Bristol Myers Squibb Co Glutamiinin sisältävän kevytketjun c-terminaalisen jatkeen käsittävä vasta-aine, sen konjugaatteja, ja menetelmiä ja käyttöjä
KR20210102334A (ko) 2018-12-12 2021-08-19 브리스톨-마이어스 스큅 컴퍼니 트랜스글루타미나제 접합을 위해 변형된 항체, 그의 접합체, 및 방법 및 용도
CN114174305A (zh) * 2019-05-22 2022-03-11 德克萨斯大学***董事会 用于治疗癌症的官能化的金卡宾萘醌络合物
WO2021055306A1 (en) 2019-09-16 2021-03-25 Bristol-Myers Squibb Company Dual capture method for analysis of antibody-drug conjugates
BR112023026735A2 (pt) 2021-06-28 2024-03-12 Byondis Bv Conjugado, composto de conector-fármaco, uso de um composto de conector-fármaco, e, composição farmacêutica

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1981001145A1 (en) 1979-10-18 1981-04-30 Univ Illinois Hydrolytic enzyme-activatible pro-drugs
US4475196A (en) 1981-03-06 1984-10-02 Zor Clair G Instrument for locating faults in aircraft passenger reading light and attendant call control system
US4447233A (en) 1981-04-10 1984-05-08 Parker-Hannifin Corporation Medication infusion pump
US4631190A (en) 1981-06-26 1986-12-23 Shen Wei C Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US5144011A (en) 1981-06-26 1992-09-01 Boston University Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US4439196A (en) 1982-03-18 1984-03-27 Merck & Co., Inc. Osmotic drug delivery system
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US4447224A (en) 1982-09-20 1984-05-08 Infusaid Corporation Variable flow implantable infusion apparatus
US4487603A (en) 1982-11-26 1984-12-11 Cordis Corporation Implantable microinfusion pump system
US4486194A (en) 1983-06-08 1984-12-04 James Ferrara Therapeutic device for administering medicaments through the skin
US4698420A (en) 1985-02-25 1987-10-06 Xoma Corporation Antibody hybrid molecules and process for their preparation
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US5374548A (en) 1986-05-02 1994-12-20 Genentech, Inc. Methods and compositions for the attachment of proteins to liposomes using a glycophospholipid anchor
MX9203291A (es) 1985-06-26 1992-08-01 Liposome Co Inc Metodo para acoplamiento de liposomas.
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US5108921A (en) 1989-04-03 1992-04-28 Purdue Research Foundation Method for enhanced transmembrane transport of exogenous molecules
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5281710A (en) * 1990-08-01 1994-01-25 The Scripps Research Institute Dynemicin analogs: synthesis, methods of preparation and use
US5162330A (en) * 1990-11-05 1992-11-10 Bristol-Myers Squibb Co. Dynemicin c antibiotic, its triacetyl derivative and pharmaceutical composition containing same
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
US6955811B2 (en) 1997-11-07 2005-10-18 Trillium Therapeutics Inc. Methods of inhibiting immune response suppression by administering antibodies to OX-2
KR100996759B1 (ko) 1999-08-24 2010-11-25 메다렉스, 인코포레이티드 인간 씨티엘에이-4 항체 및 그의 용도
CN101671335A (zh) 2001-05-31 2010-03-17 梅达莱克斯公司 细胞毒素、其有用的前体药物、连接基团和稳定剂
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
IL162835A0 (en) 2002-01-09 2005-11-20 Medarex Inc Human monoclonal antibodies against cd30
JP4753867B2 (ja) 2003-04-15 2011-08-24 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー ヒトｉｌ−１８を含むコンジュゲートおよびその置換変異体
TWI353992B (en) 2003-07-22 2011-12-11 Schering Ag Rg1 antibodies and uses thereof
WO2005051976A2 (en) 2003-11-20 2005-06-09 Ansata Therapeutics, Inc. Protein and peptide ligation processes and one-step purification processes
US8170637B2 (en) * 2008-05-06 2012-05-01 Neurosky, Inc. Dry electrode device and method of assembly
WO2005082023A2 (en) 2004-02-23 2005-09-09 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
US7691962B2 (en) 2004-05-19 2010-04-06 Medarex, Inc. Chemical linkers and conjugates thereof
NZ550934A (en) 2004-05-19 2010-05-28 Medarex Inc Chemical linkers and conjugates thereof
US7521541B2 (en) 2004-09-23 2009-04-21 Genetech Inc. Cysteine engineered antibodies and conjugates
US7714016B2 (en) 2005-04-08 2010-05-11 Medarex, Inc. Cytotoxic compounds and conjugates with cleavable substrates
EP2161336B2 (en) 2005-05-09 2017-03-29 ONO Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1(PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics
CA2611814A1 (en) 2005-06-20 2007-01-04 Medarex, Inc. Cd19 antibodies and their uses
US20080279868A1 (en) 2005-09-26 2008-11-13 Medarex, Inc. Antibody-Drug Conjugates and Methods of Use
EA016186B1 (ru) 2005-09-26 2012-03-30 Медарекс, Инк. Человеческие моноклональные антитела к cd70 и их применение
WO2007038868A2 (en) * 2005-10-03 2007-04-12 The University Of British Columbia Novel enediyne compound and uses thereof
CN101365679B (zh) 2005-10-26 2012-11-14 梅达莱克斯公司 制备cc-1065类似物的方法和化合物
WO2007059404A2 (en) 2005-11-10 2007-05-24 Medarex, Inc. Duocarmycin derivatives as novel cytotoxic compounds and conjugates
JP5714212B2 (ja) 2005-12-08 2015-05-07 メダレックス・リミテッド・ライアビリティ・カンパニーＭｅｄａｒｅｘ， Ｌ．Ｌ．Ｃ． Ｏ８ｅに対するヒトモノクローナル抗体
EA017812B1 (ru) 2005-12-08 2013-03-29 Медарекс, Инк. Выделенное моноклональное антитело или его антигенсвязывающий участок, которые связываются с протеинтирозинкиназой 7 ( ptk7) человека, и их применение
KR100869414B1 (ko) 2005-12-13 2008-11-21 야마하 가부시키가이샤 건반식 음판 타악기용의 음판 및 그 제조방법, 음판타악기의 음원 유닛 및 건반식 타악기
ATE542888T1 (de) 2006-09-08 2012-02-15 Ambrx Inc Standortspezifische inkorporation nicht natürlicher aminosäuren in wirbeltierzellen
ES2678060T3 (es) 2006-12-01 2018-08-08 E. R. Squibb & Sons, L.L.C. Anticuerpos, en particular, anticuerpos humanos, que se unen a CD22 y usos de los mismos
UY30776A1 (es) 2006-12-21 2008-07-03 Medarex Inc Anticuerpos cd44
TWI412367B (zh) 2006-12-28 2013-10-21 Medarex Llc 化學鏈接劑與可裂解基質以及其之綴合物
CL2008000510A1 (es) 2007-02-21 2008-08-22 Medarex Inc Compuestos conjugados farmaco-ligandos, que se unen a citotoxinas potentes; composicion farmaceutica; y uso para retardar o detener el crecimiento de un tumor en un mamifero.
US8865875B2 (en) 2007-08-22 2014-10-21 Medarex, L.L.C. Site-specific attachment of drugs or other agents to engineered antibodies with C-terminal extensions
BRPI0816014A8 (pt) 2007-10-01 2018-06-19 Bristol Myers Squibb Co anticorpo humano monoclonal isolado, composição, conjugado anticorpo-molécula parceiro, mólecula isolada de ácido nucléico, vetor de expressão, célula hospedeira, método para preparar um anticorpo anti-mesotelina, método de inibição do crescimento de uma célula tumoral expressando a mesotelina, método de tratamento do câncer em um indivíduo, anticorpo anti-mesotelina isolado, e método de inibir o crescimento de uma célula expressando a mesotelina
US8940501B2 (en) 2009-01-30 2015-01-27 Whitehead Institute For Biomedical Research Methods for ligation and uses thereof

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