AR078131A1 - Conjugados su preparacion y su aplicacion terapeutica - Google Patents
Conjugados su preparacion y su aplicacion terapeuticaInfo
- Publication number
- AR078131A1 AR078131A1 ARP100102290A ARP100102290A AR078131A1 AR 078131 A1 AR078131 A1 AR 078131A1 AR P100102290 A ARP100102290 A AR P100102290A AR P100102290 A ARP100102290 A AR P100102290A AR 078131 A1 AR078131 A1 AR 078131A1
- Authority
- AR
- Argentina
- Prior art keywords
- gcr1
- cr15r16
- cr13r14
- group
- piperidinyl
- Prior art date
Links
- 230000001225 therapeutic effect Effects 0.000 title 1
- 101150039048 GCR1 gene Proteins 0.000 abstract 56
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- PSNOPSMXOBPNNV-VVCTWANISA-N cryptophycin 1 Chemical class C1=C(Cl)C(OC)=CC=C1C[C@@H]1C(=O)NC[C@@H](C)C(=O)O[C@@H](CC(C)C)C(=O)O[C@H]([C@H](C)[C@@H]2[C@H](O2)C=2C=CC=CC=2)C/C=C/C(=O)N1 PSNOPSMXOBPNNV-VVCTWANISA-N 0.000 abstract 6
- 239000003795 chemical substances by application Substances 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 150000001413 amino acids Chemical class 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- -1 -OH Chemical group 0.000 abstract 1
- 102100031172 C-C chemokine receptor type 1 Human genes 0.000 abstract 1
- 101710149814 C-C chemokine receptor type 1 Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 239000007864 aqueous solution Substances 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000002118 epoxides Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 abstract 1
- 239000000243 solution Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/08—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and more than one oxygen atom
-
- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
- C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
- C07D245/06—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems condensed with one six-membered ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Un derivado de criptoficina de la formula (2) en la que R1 representa un átomo de halogeno y R2 representa un grupo -OH, un grupo acilo derivado de un aminoácido AA o un grupo alcanoiloxi C1-4; o bien R1 y R2 forman conjuntamente un motivo epoxido; AA indica un aminoácido natural o no natural; R3 representa un grupo alquilo C1-6; R4 y R5 representan los dos H o forman conjuntamente un doble enlace CH=CH entre C13 y C14; R6 y R7 representan independientemente uno de otro H o un grupo alquilo C1-6; R8 y R9 representan independientemente uno de otro H o un grupo alquilo C1-6; R10 representa al menos un sustituyente del nucleo fenilo elegido entre: H, un grupo OH, alcoxi C1-4, un átomo de halogeno o bien un grupo -NH2, -NHalquilo(C1-6) o -N(alquilo(C1-6))2; R11 representa al menos un sustituyente del nucleo fenilo elegido entre H o un grupo alquilo C1-4; L representa un conector en posicion orto (o), meta (rn) o para (p), con preferencia para, del nucleo fenilo portador del motivo GCR1 elegido entre: -G'X(CR13R14)t(OCH2CH2)y(CR15R16)u Q GCR1; -G'X(CR13R14)t(OCH2CH2)y-Y'-(CR15R16)u Q GCR1; -G'X(CR13R14)t(CR17=CR18)(CR15R16)u(OCH2CH2)y Q GCR1; -G'X(CR13R14)t(OCH2CH2)y(CR17=CR18)(CR15R16)u Q GCR1; -G'X(CR13R14)t-fenil-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-furil-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-oxazolil-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-tiazolil-(CR15R16)u Y' Q GCR1; -G'X (CR13R14)t-tienil-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-imidazolil-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-piperazinil-CO(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-piperidinil-metil-NR12-CO(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-piperidinil-(CR15R16)u Y' Q GCR1; -G'X (CR13R14)t-piperidinil-NR12-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-triazoIil-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-triazolil-(CR15R16)u Y' Q GCR1; -G'X(CR13R14)t-fenil(CR15R16)u Q GCR1; -G'X(CR13R14)t-furil-(CR15R16)u Q GCR1; -G'X (CR13R14)t-oxazolil-(CR15R16)u Q GCR1; -G'X(CR13R14)t-tiazolil-(CR15R16)u Q GCR1; -G'X(CR13R14)t-tienil-(CR15R16)u Q GCR1; -G'X (CR13R14)t-imidazolil-(CR15R16)u Q GCR1; -G'X(CR13R14)t-piperazinil-(CR15R16)u Q GCR1; -G'X(CR13R14)t-piperidinil-(CR15R16)u Q GCR1; -G'X (CR13R14)t-piperidinil-metil-NR12-(CR15R16)u Q GCR1; -G'X(CR13R14)t-piperidinil-NR12-(CR15R16)u Q GCR1; -G' X(CR13R14)t-triazolil-(CR15R16)u Q GCR1; o -Gö Y (CR13R14)t(OCH2CH2)y(CR15R16)u Q GCR1; -Gö Y (CR13R14)t(OCH2CH2)y-Y'-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t(CR17=CR18)(CR15R16)u(OCH2CH2)y Q GCR1; -Gö Y (CR13R14)t(OCH2CH2)(CR17=CR18)(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-fenil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-furil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-oxazolil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-tiazolil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-tienil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-imidazolil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-piperazinil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-piperidinil-metil-NR12-CO(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-piperidinil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-piperidinil-NR12-(CR15R16)u Y' Q GCR1; -Gö Y (CR15R14)t-triazolil-(CR15R16)u Y' Q GCR1; -Gö Y (CR13R14)t-fenil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-furil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-oxazolil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-tiazolil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-tienil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-imidazolil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-piperazinil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-piperazinil-(CR15R16)u Q CCR1; -Gö Y (CR13R14)t-piperidinil-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-piperidinil-metil-NR12-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-piperidinil-NR12-(CR15R16)u Q GCR1; -Gö Y (CR13R14)t-triazolil-(CR15R16)u Q GCR1; formulas en las que: G' representa un grupo -CH=CH- o -(CH2)n-; Gö representa un grupo -(CH2)n-; n representa un numero entero que va de 1 a 6; X representa un enlace simple o un grupo -CO-, -COO-, o -CONR12-, estando el grupo CO unido a G'; Y representa un grupo -O-, -OCO, -OCOO, -OCONR12-, -NR12-, -NR12CO-, -NR12CONR'12-, -NR12COO-, o -S(O)q-, estando el átomo O o el grupo NR12 unidos a Gö; q representa un numero entero que puede valer 0, 1 o 2; Y', representa un grupo -O-, -OCO, -OCOO, -OCONR12-, -NR12-, -NR12CO-, -NR12CONR'12-, -NR12COO-; -S(O)q-, -CO-, -COO-, o -CONR12-; R12, R'12, R13, R14, R15, R16, R17 y R18 representan independientemente uno de otro H o un grupo alquilo C1-6; t, u e y representan numeros enteros que pueden ir cada uno de 0 a 20 y tales que t+u+y sea superior o igual a 1; en el caso del conector de la formula -Gö Y (CR13R14)t(OCH2CH2)y-Y'-(CR15R16)u Q GCR1, si y vale 0 y cuando Q representa un enlace simple, entonces u no puede valer 0; Q representa un enlace simple, un grupo alquileno C1-10 o un grupo (OCH2CH2)i, representando i un numero entero que va de 1 a 20, más particularmente de 1 a 10, más particularmente aun de 1 a 8, o de 1 a 6 y aun más particularmente de 2 a 5; GCR1 representa -SZa, -C(=O)-ZbRb, formulas (3) o (4) con R12 representando H o alquilo C1-6, más particularmente el grupo metilo; o bien L se elige entre las formulas (5) formulas en las que el resto (1) representa uno de los 9 grupos de formulas (6) o n representa un numero entero que va de 1 a 6; ALK representa un grupo alquileno C1-12; R12 y R'12 representan independientemente uno de otro H o un grupo alquilo C1-6, más particularmente el grupo metilo; i representa un numero entero que va de 1 a 20, más particularmente de 1 a 10, más particularmente aun de 1 a 8, o de 1 a 6 y aun más particularmente de 2 a 5; 5 o bien L es un conector de la formula (7) en la que (AA)w, representa una cadena de w aminoácidos AA unidos entre sí por enlaces peptídicos; w representa un numero entero que va de 1 a 12, con preferencia de 1 a 6; n representa un numero entero que va de 1 a 6; D representa uno de los D1 a D3 para los que R12 representa H o un grupo alquilo C1-6; R19, R20, R21, R22 representan independientemente uno de otro H, un átomo de halogeno, -OH, -CN o un grupo alquilo C1-4; T unido a (CH2)n representa NR12 u O; V1 representa O, S, NR12; V2 representa CR22 o N; V3, V4, V5 se eligen independientemente uno de otro entre CR22 o N; Za representa H o el grupo -SRa, con Ra representando un grupo alquilo C1-6, cicloalquilo C3-7, arilo, heteroarilo o heterocicloalquilo C3-7; Zb representa un enlace simple, -O- o -NH-, con Rb representando H o un grupo alquilo C1-6, cicloalquilo C3-7, arilo, heteroarilo o heterocicloalquilo C3-7. Reivindicacion 17: Un procedimiento de preparacion de un agente de seleccion de la diana al que está unido al menos un derivado de criptoficina, denominado conjugado, que consiste en: (i) poner en contacto y dejar reaccionar una solucion acuosa de un agente de seleccion de la diana eventualmente tamponada y una solucion del derivado de criptoficina tal como se ha definido en una de las reivindicaciones 1 a 16; (ii) después separar opcionalmente el conjugado formado en la etapa (i) del derivado de criptoficina y/o del agente de seleccion de la diana que no haya reaccionado y/o de los agregados que se hayan formado. Reivindicacion 26: La utilizacion de un derivado de criptoficina de la formula (3) en la que G representa un grupo -CH=CH2 o -(CH2)nY, que se situa en posicion orto (o), meta (m) o para (p) del nucleo fenilo portador del motivo CR1, con preferencia en posicion para; Y representa -OH; -CI; N3 -NH2 -SH; -COOH; -NR12-CH2-C:::CH en el que R12 representa H o un grupo alquilo C1-6, más particularmente el grupo metilo; -OGP en el que GP indica un grupo saliente; -OC(=O)-O-(4-nitrofenilo); -maleimido, o de la formula (8) teniendo los grupos R1 a R11, los mismos significados que en las reivindicaciones 1, 11 o 12 y siendo n un numero entero que va de 1 a 6, para la preparacion de un agente de seleccion de la diana al que está unido al menos uno de dichos derivados de criptoficina.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0903170A FR2947269B1 (fr) | 2009-06-29 | 2009-06-29 | Nouveaux composes anticancereux |
| FR0905651A FR2947271B1 (fr) | 2009-06-29 | 2009-11-25 | Nouveaux composes anticancereux |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078131A1 true AR078131A1 (es) | 2011-10-19 |
Family
ID=41611078
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102290A AR078131A1 (es) | 2009-06-29 | 2010-06-28 | Conjugados su preparacion y su aplicacion terapeutica |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US8952147B2 (es) |
| EP (1) | EP2448929A1 (es) |
| JP (1) | JP5746692B2 (es) |
| KR (1) | KR101770584B1 (es) |
| CN (1) | CN102482238B (es) |
| AR (1) | AR078131A1 (es) |
| BR (1) | BRPI1015131A2 (es) |
| CA (1) | CA2766762C (es) |
| CL (1) | CL2011003229A1 (es) |
| CO (1) | CO6430462A2 (es) |
| CR (1) | CR20110670A (es) |
| DO (1) | DOP2011000376A (es) |
| EA (1) | EA024627B1 (es) |
| EC (1) | ECSP11011553A (es) |
| FR (2) | FR2947269B1 (es) |
| HN (1) | HN2011003414A (es) |
| IL (1) | IL217208A (es) |
| MA (1) | MA33465B1 (es) |
| MX (1) | MX2011013764A (es) |
| MY (1) | MY156684A (es) |
| NI (1) | NI201100219A (es) |
| NZ (1) | NZ597136A (es) |
| PE (1) | PE20121031A1 (es) |
| SG (2) | SG10201607595WA (es) |
| SV (1) | SV2011004086A (es) |
| TN (1) | TN2011000636A1 (es) |
| TW (1) | TW201110986A (es) |
| UY (1) | UY32745A (es) |
| WO (1) | WO2011001052A1 (es) |
| ZA (1) | ZA201109537B (es) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1928503T1 (sl) | 2005-08-24 | 2012-11-30 | Immunogen Inc | Postopek za pripravo konjugatov majtansinoid protitelo |
| TR201907573T4 (tr) | 2009-06-03 | 2019-06-21 | Immunogen Inc | Konjugasyon yöntemleri̇ |
| AR077280A1 (es) | 2009-06-29 | 2011-08-17 | Incyte Corp | Pirimidinonas como inhibidores de pi3k, y composiciones farmaceuticas que los comprenden |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| AR081823A1 (es) | 2010-04-14 | 2012-10-24 | Incyte Corp | DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| KR20220009505A (ko) | 2011-03-29 | 2022-01-24 | 이뮤노젠 아이엔씨 | 일-단계 방법에 의한 메이탄시노이드 항체 접합체의 제조 |
| DK2751109T3 (en) | 2011-09-02 | 2017-01-23 | Incyte Holdings Corp | HETEROCYCLYLAMINES AS PI3K INHIBITORS |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| US10035817B2 (en) | 2012-10-04 | 2018-07-31 | Immunogen, Inc. | Method of purifying cell-binding agent-cytotoxic agent conjugates with a PVDF membrane |
| US9359400B2 (en) | 2013-07-11 | 2016-06-07 | Novartis Ag | Site-specific chemoenzymatic protein modifications |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| SG11201701455SA (en) * | 2014-09-03 | 2017-03-30 | Immunogen Inc | Cytotoxic benzodiazepine derivatives |
| GB201416960D0 (en) | 2014-09-25 | 2014-11-12 | Antikor Biopharma Ltd | Biological materials and uses thereof |
| TWI748941B (zh) | 2015-02-27 | 2021-12-11 | 美商英塞特公司 | Ｐｉ３ｋ抑制劑之鹽及製備方法 |
| EP3069734A1 (en) | 2015-03-17 | 2016-09-21 | Exiris S.r.l. | Cryptophycin-based antibody-drug conjugates with novel self-immolative linkers |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| CN107029242A (zh) | 2015-11-03 | 2017-08-11 | 财团法人工业技术研究院 | 抗体药物复合物及其制造方法 |
| TWI714661B (zh) * | 2015-11-05 | 2021-01-01 | 法商賽諾菲公司 | 新穎念珠藻素化合物及接合物、其製備與其治療用途 |
| WO2017136769A1 (en) * | 2016-02-04 | 2017-08-10 | Eisai R&D Management Co., Ltd. | Peptide drug conjugates |
| WO2018178277A1 (en) | 2017-03-29 | 2018-10-04 | Avicenna Oncology Gmbh | New targeted cytotoxic isocombretaquinoline derivatives and conjugates thereof |
| EP3621658A1 (en) * | 2017-05-10 | 2020-03-18 | Sanofi | Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation |
| WO2019030284A1 (en) | 2017-08-09 | 2019-02-14 | Helmholtz-Zentrum für Infektionsforschung GmbH | NOVEL TARGETED CYTOTOXIC RATJADONE DERIVATIVES AND CONJUGATES THEREOF |
| SG11202005678UA (en) * | 2017-12-22 | 2020-07-29 | Univ Cornell | 18f-labeled peptide ligands useful in pet and cerenkov luminescene imaging |
| SG11202100934PA (en) | 2018-08-02 | 2021-02-25 | Dyne Therapeutics Inc | Muscle targeting complexes and uses thereof for treating dystrophinopathies |
| US12018087B2 (en) | 2018-08-02 | 2024-06-25 | Dyne Therapeutics, Inc. | Muscle-targeting complexes comprising an anti-transferrin receptor antibody linked to an oligonucleotide and methods of delivering oligonucleotide to a subject |
| WO2020028864A1 (en) | 2018-08-02 | 2020-02-06 | Dyne Therapeutics, Inc. | Muscle targeting complexes and uses thereof for treating facioscapulohumeral muscular dystrophy |
| US11168141B2 (en) | 2018-08-02 | 2021-11-09 | Dyne Therapeutics, Inc. | Muscle targeting complexes and uses thereof for treating dystrophinopathies |
| US11911484B2 (en) | 2018-08-02 | 2024-02-27 | Dyne Therapeutics, Inc. | Muscle targeting complexes and uses thereof for treating myotonic dystrophy |
| FR3085952B1 (fr) | 2018-09-17 | 2020-10-30 | Centre Nat Rech Scient | Conjugue anticorps-medicament comprenant des derives de quinoline |
| EP4038085A1 (en) | 2019-09-30 | 2022-08-10 | The Regents of The University of Michigan | Biocatalytic synthesis of cryptophycin anticancer agents |
| EP4046996A1 (en) | 2021-02-19 | 2022-08-24 | Universität Bielefeld | Cryptophycin compounds and conjugates thereof |
| US11969475B2 (en) | 2021-07-09 | 2024-04-30 | Dyne Therapeutics, Inc. | Muscle targeting complexes and uses thereof for treating facioscapulohumeral muscular dystrophy |
| US11672872B2 (en) | 2021-07-09 | 2023-06-13 | Dyne Therapeutics, Inc. | Anti-transferrin receptor antibody and uses thereof |
| US11633498B2 (en) | 2021-07-09 | 2023-04-25 | Dyne Therapeutics, Inc. | Muscle targeting complexes and uses thereof for treating myotonic dystrophy |
| US11638761B2 (en) | 2021-07-09 | 2023-05-02 | Dyne Therapeutics, Inc. | Muscle targeting complexes and uses thereof for treating Facioscapulohumeral muscular dystrophy |
| US11771776B2 (en) | 2021-07-09 | 2023-10-03 | Dyne Therapeutics, Inc. | Muscle targeting complexes and uses thereof for treating dystrophinopathies |
| WO2023057564A1 (en) | 2021-10-07 | 2023-04-13 | Sanofi | IMIDAZO[4,5-c]QUINOLINE-4-AMINE COMPOUNDS AND CONJUGATES THEREOF, THEIR PREPARATION, AND THEIR THERAPEUTIC APPLICATIONS |
| US11931421B2 (en) | 2022-04-15 | 2024-03-19 | Dyne Therapeutics, Inc. | Muscle targeting complexes and formulations for treating myotonic dystrophy |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2719170A (en) | 1954-07-28 | 1955-09-27 | Du Pont | Alkyl omega-carboxyalkyl disulfides and their lower alkyl esters |
| US4981979A (en) | 1987-09-10 | 1991-01-01 | Neorx Corporation | Immunoconjugates joined by thioether bonds having reduced toxicity and improved selectivity |
| JPH04502469A (ja) | 1988-12-22 | 1992-05-07 | ゾマ コーポレイション | ヒンダードカップリング剤および方法 |
| US5208020A (en) | 1989-10-25 | 1993-05-04 | Immunogen Inc. | Cytotoxic agents comprising maytansinoids and their therapeutic use |
| CA2056039A1 (en) | 1991-01-22 | 1992-07-23 | Philip L. Fuchs | Carbacyclin analogs |
| NZ305571A (en) | 1995-03-07 | 1999-02-25 | Univ Hawaii | Cryptophycin derivatives, use in pharmaceutical compositions to inhibit mammalian cell proloferation and treat neoplasia |
| IL128610A (en) * | 1996-08-30 | 2004-07-25 | Lilly Co Eli | Cryptophycin compound and its use as a medicament for treating neoplasm |
| WO2000023429A2 (en) | 1998-10-16 | 2000-04-27 | Eli Lilly And Company | Stereoselective process for producing cryptophycins |
| AU1930100A (en) | 1998-12-07 | 2000-06-26 | Eli Lilly And Company | Crotylboration process to produce cryptophycin compounds |
| JP2005511627A (ja) * | 2001-11-20 | 2005-04-28 | シアトル ジェネティクス，インコーポレーテッド | 抗ｃｄ３０抗体を使用する免疫学的疾患の治療 |
| US20040249130A1 (en) * | 2002-06-18 | 2004-12-09 | Martin Stanton | Aptamer-toxin molecules and methods for using same |
| AU2003259163B2 (en) | 2002-08-16 | 2008-07-03 | Immunogen, Inc. | Cross-linkers with high reactivity and solubility and their use in the preparation of conjugates for targeted delivery of small molecule drugs |
| US7230101B1 (en) | 2002-08-28 | 2007-06-12 | Gpc Biotech, Inc. | Synthesis of methotrexate-containing heterodimeric molecules |
| EA010570B1 (ru) | 2002-11-07 | 2008-10-30 | Иммьюноджен, Инк. | Антитело к cd33 и способы его применения |
| WO2004103272A2 (en) | 2003-05-20 | 2004-12-02 | Immunogen, Inc. | Improved cytotoxic agents comprising new maytansinoids |
| ATE496944T1 (de) | 2003-07-21 | 2011-02-15 | Immunogen Inc | Ca6-antigenspezifisches zytotoxisches konjugat und verfahren zu dessen anwendung |
| US20050175619A1 (en) | 2004-02-05 | 2005-08-11 | Robert Duffy | Methods of producing antibody conjugates |
| US7375078B2 (en) | 2004-02-23 | 2008-05-20 | Genentech, Inc. | Heterocyclic self-immolative linkers and conjugates |
| AR048098A1 (es) | 2004-03-15 | 2006-03-29 | Wyeth Corp | Conjugados de caliqueamicina |
| TW200630106A (en) | 2004-10-08 | 2006-09-01 | Wyeth Corp | Immunotherapy of autoimmune disorders |
| EP1669358A1 (en) | 2004-12-07 | 2006-06-14 | Aventis Pharma S.A. | Cytotoxic agents comprising new taxanes |
| BRPI0515745A (pt) * | 2004-12-09 | 2008-08-05 | Centocor Inc | imunoconjugados de antiintegrina, métodos e usos |
| US7385028B2 (en) | 2004-12-22 | 2008-06-10 | Ambrx, Inc | Derivatization of non-natural amino acids and polypeptides |
| JP2008536485A (ja) * | 2005-03-07 | 2008-09-11 | アーケミックス コーポレイション | Ｐｓｍａに対する安定化したアプタマーおよび前立腺癌治療薬としてのそれらの使用 |
| US7714016B2 (en) | 2005-04-08 | 2010-05-11 | Medarex, Inc. | Cytotoxic compounds and conjugates with cleavable substrates |
| RS52060B (en) | 2006-01-25 | 2012-04-30 | Sanofi | CYTOTOXIC AGENTS CONTAINING NEW TOMAIMYCIN DERIVATIVES |
| EP1832577A1 (en) | 2006-03-07 | 2007-09-12 | Sanofi-Aventis | Improved prodrugs of CC-1065 analogs |
| EP2010475A2 (en) | 2006-04-27 | 2009-01-07 | Intezyne Technologies Incorporated | Heterofunctional poly(ethylene glycol) containing acid-labile amino protecting groups and uses thereof |
| EP1864682A1 (en) | 2006-06-09 | 2007-12-12 | Sanofi-Aventis | Leptomycin derivatives |
| ES2673822T3 (es) | 2006-07-18 | 2018-06-25 | Sanofi | Anticuerpo antagonista contra EphA2 para el tratamiento de cáncer |
| EP1914242A1 (en) | 2006-10-19 | 2008-04-23 | Sanofi-Aventis | Novel anti-CD38 antibodies for the treatment of cancer |
| CN104383553A (zh) * | 2007-06-25 | 2015-03-04 | 恩多塞特公司 | 含有亲水性间隔区接头的共轭物 |
| PT2019104E (pt) | 2007-07-19 | 2013-12-03 | Sanofi Sa | Agentes citotóxicos compreendendo novos derivados de tomaimicina e sua utilização terapêutica |
| EP2185188B1 (en) | 2007-08-22 | 2014-08-06 | Medarex, L.L.C. | Site-specific attachment of drugs or other agents to engineered antibodies with c-terminal extensions |
| EP2276509B1 (en) | 2008-04-11 | 2016-06-15 | Seattle Genetics, Inc. | Detection and tratment of pancreatic, ovarian and other cancers |
| KR101764081B1 (ko) | 2008-04-30 | 2017-08-01 | 이뮤노젠 아이엔씨 | 가교제 및 그 용도 |
| SG189817A1 (en) | 2008-04-30 | 2013-05-31 | Immunogen Inc | Potent conjugates and hydrophilic linkers |
| WO2010014812A2 (en) | 2008-07-30 | 2010-02-04 | The Research Foundation Of State University Of New York | Peptide compositions and methods of use |
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