AR045342A1 - Inhibidores de quinesina mitotica - Google Patents
Inhibidores de quinesina mitoticaInfo
- Publication number
- AR045342A1 AR045342A1 ARP040102815A ARP040102815A AR045342A1 AR 045342 A1 AR045342 A1 AR 045342A1 AR P040102815 A ARP040102815 A AR P040102815A AR P040102815 A ARP040102815 A AR P040102815A AR 045342 A1 AR045342 A1 AR 045342A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- heterocyclyl
- cycloalkyl
- optionally substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 230000000394 mitotic effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 15
- 125000001424 substituent group Chemical group 0.000 abstract 15
- 125000003118 aryl group Chemical group 0.000 abstract 12
- 125000000623 heterocyclic group Chemical group 0.000 abstract 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 125000000304 alkynyl group Chemical group 0.000 abstract 11
- 125000003342 alkenyl group Chemical group 0.000 abstract 8
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 125000002950 monocyclic group Chemical group 0.000 abstract 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- RSEBUVRVKCANEP-UHFFFAOYSA-N 2-pyrroline Chemical class C1CC=CN1 RSEBUVRVKCANEP-UHFFFAOYSA-N 0.000 abstract 1
- 102000010638 Kinesin Human genes 0.000 abstract 1
- 108010063296 Kinesin Proteins 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- -1 maryl Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Ceramic Engineering (AREA)
- Manufacturing & Machinery (AREA)
- Structural Engineering (AREA)
- Materials Engineering (AREA)
- Health & Medical Sciences (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
La presente se refiere a compuestos de dihidropirrol que son útiles para tratar enfermedades proliferativas celulares, para tratar trastornos asociados a la actividad quinesina KSP. Reivindicación 1: Un compuesto de fórmula (1) o una sal o estereoisómero farmacéuticamente aceptable del mismo, en la que: a es 0 o 1; b es 0 o 1; m es 0, 1 o 2; n es 0, 1, 2, o 3; r es 0 o 1; s es 0 o 1; s es 0 o 1; t es 0, 1 o 2; R1 y R2 se seleccionan independientemente de H, alquilo C1-6, arilo, heterociclilo y cicloalquilo C3-6, opcionalmente sustituido con 1 2 o 3 sustituyentes seleccionados de R7; R3 se selecciona de: 1) H, 2) alquilo C1-10; 3) alquil C1-10-O-Rd; 4) alquenil C2-10-O-Rd; 5) alquinil C2-10-O-Rd; 6) (alquilen C1-69n-cicloalquil C3-8-O-Rd; 7) alquil C1-10-(C=O)b-NRcRc´; 8) alquenil C2-10-(C=O)b-NRcRc´; 9) alquinil C2-10-(C=O)b-NRcRc´; 10) (alquilen C1-6)n-cicloalquil C3-8-(C=O)b-NRcRc´; 11) alquil C1-10-S(O),-Rd; 12) alquenil C2-10-S(O)m-Rd; 13) alquinil C2-10-S(O)m-Rd; 14) (alquilen C1-6)n-cicloalquil C3-8-S(O)m-Rd; estando opcionalmente sustituidos dichos alquilo, alquenilo, alquinilo y cicloalquilo con uno o más sustituyentes seleccionados de R6; R4 se selecciona independientemente de: 1) (C=O)aOb-alquilo C1-10; 2) (C=O)aObarilo; 3) CO2H; 4) halo, 5) CN, 6) OH, 7) Ob-perfluoroalquilo C1-6; 8) Oa(C=O)nNR8R9; 9) S(O)mRa, 10) S(O)2NR8R9, estando opcionalmente sustituidos dichos alquilo, arilo, alquenilo, alquinilo, heterociclilo y cicloalquilo con 1, 2 o 3 sustituyentes seleccionados de R7; R5 se selecciona de: 1) H, 2) (C=O)aOb-alquilo C1-10; 3) (C=O)aOb-arilo, 4) CO2H, 5) halo, 6) CN, 7) OH, 8) Ob-perfluoroalquilo C1-6, 9) Oa(C=O)bNR8R9; 10) S(O)mRa; 11) S(O)2NR8R9, y 12) -OPO(OH)2; estando opcionalmente sustituidos dichos alquilo, marilo, alquenilo, alquinilo, heterociclilo y cicloalquilo con 1, 2 o 3 sustituyentes seleccionados de R7; R6 se selecciona independientemente de: 1) (C=O)aOb-alquilo C1-10; 2) (C=O)aOb-arilo; 3) alquenilo C2-10; 4) alquinilo C2-10; 5) (C=O)aOb-heterociclilo, 6) CO2H, 7) halo, 8) CN, 9) OH, 10) Ob-perfluoroalquilo C1-6; 11) Oa(C=O)bNR8R9; 12) A(O)mRa, 13) S(O)2NR8R9, 14) oxo, 15) CHO, 16) (N=O)R8R9, 17) (C=O)aOb-cicloalquilo C3-8, y 18) -OPO(OH)2; estando opcionalmente sustituidos dichos alquilo, arilo, alquenilo, alquinilo, heterociclilo y cicloalquilo con 1, 2 o 3 sustituyentes seleccionados de R7; R7 se selecciona de: 1) (C=O)rOs-alquilo C1-10, 2) Or-perfluoroalquilo C1-3, 3) oxo, 4) OH, 5) halo, 6) CN, 7) alquenilo C2-10, 8) alquinilo C2-10, 9) (C=O)rOs-cicloalquilo C3-6, 10) (C=O)rOs-alquilen C0-6-arilo, 11) (C=O)rOs-alquilen C0-6-heterociclilo, 12) (C=O)rOs-alquilen C0-6-N(Rb)2, 13) C(O)Ra, 14) alquilen C0-6-CO2Ra, 15) C(O)H, 16) alquilen C0-6-CO2H, y 17) (C=O)rN(Rb)2, 18) S(O)mRa, 19) S(O)2N(Rb)2; y 20) -OPO(OH)2; estando opcionalmente sustituidos dichos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, alquileno y heterociclilo con hasta 3 sustituyentes seleccionados de Rb, OH, alcoxi C1-6, halógeno, CO2H, CN, O(C=O)alquilo C1-6, oxo, NO2 y N(Rb)2; R8 y R9 se seleccionan independientemente de: 1) H; 2) (C=O)Ob-alquilo C1-10, 3) (C=O)Ob-cicloalquilo C3-8, 4) (C=O)Ob-arilo, 5) (C=O)Ob-heterociclilo, 6) alquilo C1-10, 7) arilo, 8) alquenilo C2-10, 9) alquinilo C2-10, 10) heterociclilo, 11) cicloalquilo C3-8, 12) SO2Ra, y 13) (C=O)NRb2, estando opcionalmente sustituidos dichos alquilo, cicloalquilo, arilo, heterociclilo, alquenilo y alquinilo con 1, 2 o 3 sustituyentes seleccionados de R7, o R8 y R9 pueden tomarse conjuntamente con el átomo de N al que están unidos para formar un heterociclo monocíclico o bicíclico con 3-7 miembros en cada anillo y que contiene opcionalmente, además del N, 1 o 2 heteroátomos adicionales seleccionados de N, O y S, estando opcionalmente sustituido dicho heterociclo monocíclico o bicíclico con 1, 2 o 3 sustituyentes seleccionados de R7; R10 se selecciona de: F y -CH2F; R13 se selecciona de: H y -CH2F, a condición de que si t es 1, R13 sea H; Rox está ausente o es oxo; Ra se selecciona independientemente de: alquilo c1-6, cicloalquilo C3-6, arilo o heterociclilo, opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados de R7; Rb se selecciona independientemente de: H, alquilo c1-6, arilo, heterociclilo, cicloalquilo C3-6, (C=O)O-alquilo C1-6, (C=O)alquilo C1-6, (C=O)arilo, (C=O)heterociclilo, (C=O)NReRe´ o S(O)2Ra, opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados de R7; Rc y Rc´ se seleccionan independientemente de H, alquilo C1-6, arilo, NH2, OH, ORa, -alquil(C1-6)-OH, -alquil(C1-6)-O-alquilo C1-6, (C=O)O-alquilo C1-6, (C=O)alquilo C1-6, (C=O)arilo, (C=O)heterociclilo, (C=O)NReRe´, S(O)2Ra y -alquil (C1-6)-N(Rb)2, estando opcionalmente sustituido el alquilo con 1, 2 o 3 sustituyentes seleccionados de R7; o Rc y Rc´ pueden tomarse conjuntamente con el N al que están unidos para formar un heterociclo monocíclico o bicíclico de 3-7 miembros en cada anillo y que contiene opcionalmente, además del N, 1 o 2 heteroátomos adicionales seleccionados de N, O y S, estando opcionalmente sustituido dicho heterociclo monocíclico o bicíclico con 1, 2 o 3 sustituyentes seleccionados de R7; Rd se selecciona de H, alquilo C1-6, -alquil(C2-6)-OH, -alquil(C1-6)-O-alquilo C1-6 y -alquil(C1-6)-N(Rb)2, en los que el alquilo está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de R7; Re y Re´ se seleccionan independientemente de: H, alquilo C1-6, arilo, heterociclilo y cicloalquilo C3-6, opcionalmente sustituidos con 1 , 2 o 3 sustituyentes seleccionados de R7;: o Re y Re´ pueden tomarse conjuntamente con el N al que están unidos para formar un heterociclo monocíclico o bicíclico de 3-7 miembros en cada anillo y que contiene opcionalmente, además del N, 1 o 2 heteroátomos adicionales seleccionados de N. O y S, estando opcionalmente sustituido dicho heterociclo monocíclico o bicíclico con 1, 2 o 3 sustituyentes seleccionados de R7.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49563703P | 2003-08-15 | 2003-08-15 | |
| US51268003P | 2003-10-20 | 2003-10-20 | |
| US56358604P | 2004-04-19 | 2004-04-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045342A1 true AR045342A1 (es) | 2005-10-26 |
Family
ID=34222358
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040102815A AR045342A1 (es) | 2003-08-15 | 2004-08-06 | Inhibidores de quinesina mitotica |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20050038074A1 (es) |
| KR (1) | KR20060058716A (es) |
| AR (1) | AR045342A1 (es) |
| BR (1) | BRPI0413580A (es) |
| CO (1) | CO5650252A2 (es) |
| EC (1) | ECSP066362A (es) |
| IL (1) | IL173513A0 (es) |
| IS (1) | IS8276A (es) |
| MA (1) | MA27986A1 (es) |
| NO (1) | NO20061194L (es) |
| PE (1) | PE20050730A1 (es) |
| TW (1) | TW200510380A (es) |
| WO (1) | WO2005019205A1 (es) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003276005B2 (en) | 2002-06-14 | 2009-01-15 | Merck Sharp & Dohme Corp. | Mitotic kinesin inhibitors |
| IL165624A0 (en) | 2002-06-14 | 2006-01-15 | Merck & Co Inc | Mitotic kinesin inhibitors |
| US7638549B2 (en) | 2003-08-15 | 2009-12-29 | Merck & Co. Inc. | Mitotic kinesin inhibitors |
| CA2533889A1 (en) | 2003-08-15 | 2005-03-03 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| US7465746B2 (en) * | 2003-08-15 | 2008-12-16 | Merck & Co., Inc. | Fluorinated 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP |
| EP1740537A2 (en) * | 2004-04-19 | 2007-01-10 | Merck & Co., Inc. | A process for the preparation of 2,2-disubstituted pyrroles |
| ATE550019T1 (de) | 2005-05-17 | 2012-04-15 | Merck Sharp & Dohme | Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs |
| US7723330B2 (en) | 2006-03-07 | 2010-05-25 | Array Biopharma Inc. | Heterobicyclic pyrazole compounds and methods of use |
| WO2009052288A1 (en) | 2007-10-19 | 2009-04-23 | Schering Corporation | Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting ksp kinesin activity |
| EP2413932A4 (en) | 2009-04-01 | 2012-09-19 | Merck Sharp & Dohme | HAMMER OF ACT ACTIVITY |
| CA2777043C (en) | 2009-10-14 | 2015-12-15 | Schering Corporation | Substituted piperidines that increase p53 activity and the uses thereof |
| EP2584903B1 (en) | 2010-06-24 | 2018-10-24 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| CN103068980B (zh) | 2010-08-02 | 2017-04-05 | 瑟纳治疗公司 | 使用短干扰核酸（siNA）的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1（CTNNB1）基因表达的抑制 |
| RU2745848C2 (ru) | 2010-08-17 | 2021-04-01 | Сирна Терапьютикс, Инк. | ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК) |
| EP2613782B1 (en) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| WO2012058210A1 (en) | 2010-10-29 | 2012-05-03 | Merck Sharp & Dohme Corp. | RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA) |
| WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| EP2770987B1 (en) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| EP3919620A1 (en) | 2012-05-02 | 2021-12-08 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) compositions |
| CA2882950A1 (en) | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| SMT201700595T1 (it) | 2012-11-28 | 2018-03-08 | Merck Sharp & Dohme | Composizioni e metodi per trattare il cancro |
| WO2014100065A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| WO2015034925A1 (en) | 2013-09-03 | 2015-03-12 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| JOP20190055A1 (ar) | 2016-09-26 | 2019-03-24 | Merck Sharp & Dohme | أجسام مضادة ضد cd27 |
| US10975084B2 (en) | 2016-10-12 | 2021-04-13 | Merck Sharp & Dohme Corp. | KDM5 inhibitors |
| JP7160833B2 (ja) | 2017-04-13 | 2022-10-25 | サイロパ ビー．ブイ． | 抗ｓｉｒｐアルファ抗体 |
| EP3706742B1 (en) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2019094312A1 (en) | 2017-11-08 | 2019-05-16 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2019148412A1 (en) | 2018-02-01 | 2019-08-08 | Merck Sharp & Dohme Corp. | Anti-pd-1/lag3 bispecific antibodies |
| WO2020033282A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2020033285A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| CA3108388A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| EP3833667B1 (en) | 2018-08-07 | 2024-03-13 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| CA3107770C (en) | 2018-08-16 | 2023-09-05 | Emd Millipore Corporation | Closed bioprocessing device |
| EP4076459B1 (en) | 2019-12-17 | 2026-04-29 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| ES3074517T3 (en) | 2019-12-17 | 2026-07-21 | Merck Sharp & Dohme Llc | 4-(3,4-dihydroisoquinolin-2(1h)-yl)-3-hydroxypiperidine derivatives as prmt5 inhibitors for the treatment of cancer and sickle cell disease |
| EP4076460B1 (en) | 2019-12-17 | 2026-01-21 | Merck Sharp & Dohme LLC | 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidine derivatives as prmt5 inhibitors for the treatment of cancer |
| ES3022307T3 (en) | 2019-12-17 | 2025-05-28 | Merck Sharp & Dohme Llc | Prmt5 inhibitors |
| DE212025000115U1 (de) | 2024-07-30 | 2026-06-18 | Sairopa B.V. | Anti-SIRP Alpha-Antikörperformulierungen und ihre Verwendung |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6057342A (en) * | 1996-08-16 | 2000-05-02 | Dupont Pharmaceutical Co. | Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof |
| US6440686B1 (en) * | 2000-06-15 | 2002-08-27 | Cytokinetics, Inc. | Methods for screening and therapeutic applications of kinesin modulators |
| CA2467916A1 (en) * | 2001-12-06 | 2003-06-19 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| AU2003276005B2 (en) * | 2002-06-14 | 2009-01-15 | Merck Sharp & Dohme Corp. | Mitotic kinesin inhibitors |
| IL165624A0 (en) * | 2002-06-14 | 2006-01-15 | Merck & Co Inc | Mitotic kinesin inhibitors |
| US7235580B2 (en) * | 2002-10-18 | 2007-06-26 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
-
2004
- 2004-08-06 AR ARP040102815A patent/AR045342A1/es not_active Application Discontinuation
- 2004-08-06 PE PE2004000762A patent/PE20050730A1/es not_active Application Discontinuation
- 2004-08-11 WO PCT/US2004/025980 patent/WO2005019205A1/en not_active Ceased
- 2004-08-11 US US10/916,096 patent/US20050038074A1/en not_active Abandoned
- 2004-08-11 KR KR1020067003087A patent/KR20060058716A/ko not_active Ceased
- 2004-08-11 BR BRPI0413580-6A patent/BRPI0413580A/pt not_active Application Discontinuation
- 2004-08-13 TW TW093124289A patent/TW200510380A/zh unknown
-
2006
- 2006-01-31 IS IS8276A patent/IS8276A/is unknown
- 2006-02-02 IL IL173513A patent/IL173513A0/en unknown
- 2006-02-08 MA MA28785A patent/MA27986A1/fr unknown
- 2006-02-10 CO CO06013574A patent/CO5650252A2/es not_active Application Discontinuation
- 2006-02-13 EC EC2006006362A patent/ECSP066362A/es unknown
- 2006-03-14 NO NO20061194A patent/NO20061194L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0413580A (pt) | 2006-10-17 |
| US20050038074A1 (en) | 2005-02-17 |
| ECSP066362A (es) | 2006-10-31 |
| CO5650252A2 (es) | 2006-06-30 |
| MA27986A1 (fr) | 2006-07-03 |
| PE20050730A1 (es) | 2005-09-20 |
| KR20060058716A (ko) | 2006-05-30 |
| IS8276A (is) | 2006-01-31 |
| NO20061194L (no) | 2006-05-05 |
| WO2005019205A1 (en) | 2005-03-03 |
| TW200510380A (en) | 2005-03-16 |
| IL173513A0 (en) | 2006-07-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR064010A1 (es) | Inhibidores de la actividad de la akt | |
| AR061804A1 (es) | Inhibidores de tirosina quinasa | |
| PE20250021A1 (es) | Cicloalquil 3-oxopiperazin carboxamidas y cicloheteroalquil 3-oxopiperazin carboxamidas como inhibidores de nav1.8 | |
| CO5261601A1 (es) | Indolilquinolinonas utiles como inhibidores de la tirosinoquinasa | |
| AR056536A1 (es) | Compuestos de 2-amino-5- [4-(difluormetoxi)fenil]-5-fenilimidazolona como inhibidores de la beta secretasa (bace) | |
| AR117163A2 (es) | Composiciones parasiticidas que comprenden un agente activo de isoxazolina, sus métodos y usos | |
| AR067948A1 (es) | Metodo para preparar derivados de 5-haloalquil-4,5-dihidroisoxazol | |
| AR044152A1 (es) | Derivados de alquilarilo, metodo de preparacion y uso para el tratamiento de la obesidad | |
| AR074052A1 (es) | Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk cinasa | |
| AR072952A1 (es) | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso | |
| AR058546A1 (es) | Derivados de 2- adamantilurea como inhibidores selectivos de 11 beta - hsd1 | |
| PE20090435A1 (es) | Inhibidores de tetrahidropiranocromeno de gamma secretasa | |
| PE20080841A1 (es) | Derivados de quinazolinona e isoquinolinona y su uso para el tratamiento o prevencion de trastornos relacionados con el estres o la depresion | |
| AR065814A1 (es) | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. | |
| CO6140030A2 (es) | Derivados de 4-bencilftalazinona 2-sustituidos como antagonistas de histamina h1 y h3 | |
| PE20011047A1 (es) | Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas | |
| AR051326A1 (es) | Pirazolobenzodiazepinas disustituidas | |
| ATE450532T1 (de) | Pyridinyl- oder pyrimidinylthiazole mit proteinkinasehemmender wirkung | |
| AR109677A1 (es) | Derivados heterocíclicos bicíclicos fusionados como plaguicidas | |
| PE20121282A1 (es) | Antagonistas de espiro-oxindol de mdm2 | |
| PE20061106A1 (es) | Derivados de 2-(4-oxo-4h-quinazolin-3-il)acetamida | |
| PE20061305A1 (es) | Compuestos derivados de fenilacetamidas como inhibidores de proteincinasas | |
| AR071300A1 (es) | Compuestos; composiciones farmaceuticas en base al compuesto y uso del mismo para la manufactura de un medicamento | |
| AR065811A1 (es) | Derivados de 2-amino-4h-imidazol-4-ona,composiciones farmaceuticas que los contienen y usos para el tratamiento de la enfermedad de alzheimer y otros trastornos neurodegenerativos. | |
| AR084152A1 (es) | Compuestos de triazolopirimidina como inhibidores de pde10a, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades del snc |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |