AR114159A2 - Pirrolidina-2-carboxamidas sustituidas - Google Patents
Pirrolidina-2-carboxamidas sustituidasInfo
- Publication number
- AR114159A2 AR114159A2 ARP180103640A ARP180103640A AR114159A2 AR 114159 A2 AR114159 A2 AR 114159A2 AR P180103640 A ARP180103640 A AR P180103640A AR P180103640 A ARP180103640 A AR P180103640A AR 114159 A2 AR114159 A2 AR 114159A2
- Authority
- AR
- Argentina
- Prior art keywords
- ch2ch2o
- substituted
- unsubstituted
- so2r
- cor
- Prior art date
Links
- 150000003857 carboxamides Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 125000003342 alkenyl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000002148 esters Chemical class 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 229910006069 SO3H Inorganic materials 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- -1 nitro, ethynyl Chemical group 0.000 abstract 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 1
- 229920002554 vinyl polymer Polymers 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- 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
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Se proporcionan compuestos de la fórmula (1) en la que X, Y, R¹, R², R³, R⁴, R⁵, R⁶ y R⁷ tienen los significados aquí descritos y los enantiómeros y sales y ésteres farmacéuticamente aceptables de los mismos. Estos compuestos son útiles como agentes anticancerosos. Reivindicación 1: Los compuestos de la fórmula (1) en la que X se elige entre el grupo formado por H, F, Cl, Br, I, ciano, nitro, etinilo, ciclopropilo, metilo, etilo, isopropilo, vinilo y metoxi; Y es de uno a cuatro restos elegidos con independencia entre el grupo formado por H, F, Cl, Br, I, CN, OH, nitro, alquilo inferior, cicloalquilo, alcoxi inferior, alquenilo inferior, cicloalquenilo, alquinilo inferior, arilo, heteroarilo, heterociclo, COOR, OCOR, CONRR, NRCOR, NRSO₂R, SO₂NRR y NRR, en los que R y R se eligen con independencia entre H, alquilo inferior sustituido o sin sustituir, cicloalquilo inferior sustituido o sin sustituir, alquenilo inferior sustituido o sin sustituir, cicloalquenilo inferior sustituido o sin sustituir, arilo sustituido o sin sustituir, heteroarilo sustituido o sin sustituir y heterociclo sustituido o sin sustituir; y en el caso de que R y R puedan unirse de modo independiente para formar una estructura cíclica elegida entre cicloalquilo sustituido o sin sustituir, cicloalquenilo sustituido o sin sustituir, heteroarilo sustituido o sin sustituir y heterociclo sustituido o sin sustituir, uno de R¹ y R² se elige entre el grupo formado por alquilo inferior, alquilo inferior sustituido, alquenilo inferior, alquenilo inferior sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclo, heterociclo sustituido, cicloalquilo, cicloalquilo sustituido, cicloalquenilo y cicloalquenilo sustituido y el otro es hidrógeno o alquilo inferior; R³ es H o alquilo inferior; uno de R⁴ y R⁵ se elige entre el grupo formado por alquilo inferior, alquilo inferior sustituido, alquenilo inferior, alquenilo inferior sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclo, heterociclo sustituido, cicloalquilo, cicloalquilo sustituido, cicloalquenilo y cicloalquenilo sustituido y el otro es hidrógeno; R⁶ y R⁷ se eligen entre el grupo formado por (CH₂)ₙ-R, (CH₂)ₙ-NRR, (CH₂)ₙ-NRCOR, (CH₂)ₙ-NRSO₂R, (CH₂)ₙ-COOH, (CH₂)ₙ-COOR, (CH₂)ₙ-CONRR, (CH₂)ₙ-OR, (CH₂)ₙ-SR, (CH₂)ₙ-SOR, (CH₂)ₙ-SO₂R, (CH₂)ₙ-COR, (CH₂)ₙ-SO₃H, (CH₂)ₙ-SONRR, (CH₂)ₙ-SO₂NRR, (CH₂CH₂O)ₘ-(CH₂)ₙ-R, (CH₂CH₂O)ₘ-(CH₂)ₙ-OH, (CH₂CH₂O)ₘ-(CH₂)ₙ-OR, (CH₂CH₂O)ₘ-(CH₂)ₙ-NRR, (CH₂CH₂O)ₘ-(CH₂)ₙ-NRCOR, (CH₂CH₂O)ₘ-(CH₂)ₙ-NRSO₂R, (CH₂CH₂O)ₘ-(CH₂)ₙ-COOH, (CH₂CH₂O)ₘ-(CH₂)ₙ-COOR, (CH₂CH₂O)ₘ-(CH₂)ₙ-CONRR, (CH₂CH₂O)ₘ-(CH₂)ₙ-SO₂R, (CH₂CH₂O)ₘ(CH₂)ₙ-COR, (CH₂CH₂O)ₘ-(CH₂)ₙ-SONRR, (CH₂CH₂O)ₘ-(CH₂)ₙ-SO₂NRR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-R, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-OH, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-OR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-NRR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-NRCOR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-NRSO₂R, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-COOH, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-COOR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-CONRR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-SO₂R, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-COR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-SONRR, (CH₂)ₚ-(CH₂CH₂O)ₘ-(CH₂)ₙ-SO₂NRR, -COR, -SOR y SO₂R, en los que R y R tienen los significados definidos anteriormente; m, n y p son con independencia un número de 0 a 6; y las sales y ésteres farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12/702,402 US8354444B2 (en) | 2008-09-18 | 2010-02-09 | Substituted pyrrolidine-2-carboxamides |
Publications (1)
Publication Number | Publication Date |
---|---|
AR114159A2 true AR114159A2 (es) | 2020-07-29 |
Family
ID=43608850
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110100393A AR080143A1 (es) | 2010-02-09 | 2011-02-07 | Pirrolidina-2-carboxamidas sustituidas, composicion farmaceutica que las contiene y su uso en el tratamiento de tastornos oncologicos |
ARP180103640A AR114159A2 (es) | 2010-02-09 | 2018-12-13 | Pirrolidina-2-carboxamidas sustituidas |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110100393A AR080143A1 (es) | 2010-02-09 | 2011-02-07 | Pirrolidina-2-carboxamidas sustituidas, composicion farmaceutica que las contiene y su uso en el tratamiento de tastornos oncologicos |
Country Status (32)
Country | Link |
---|---|
US (1) | US8354444B2 (es) |
EP (1) | EP2534132B1 (es) |
JP (1) | JP5612710B2 (es) |
KR (1) | KR101461298B1 (es) |
CN (1) | CN102753522B (es) |
AR (2) | AR080143A1 (es) |
AU (1) | AU2011214506C1 (es) |
BR (1) | BR112012019672B1 (es) |
CA (1) | CA2788236C (es) |
CL (1) | CL2012002189A1 (es) |
CR (1) | CR20120410A (es) |
CY (1) | CY1119049T1 (es) |
DK (1) | DK2534132T3 (es) |
EC (1) | ECSP12012083A (es) |
ES (1) | ES2629439T3 (es) |
HK (1) | HK1171452A1 (es) |
HR (1) | HRP20170903T1 (es) |
HU (1) | HUE034816T2 (es) |
LT (1) | LT2534132T (es) |
MX (1) | MX2012009186A (es) |
MY (1) | MY165238A (es) |
NZ (1) | NZ601422A (es) |
PE (1) | PE20121532A1 (es) |
PL (1) | PL2534132T3 (es) |
PT (1) | PT2534132T (es) |
RS (1) | RS56163B1 (es) |
RU (1) | RU2564022C2 (es) |
SG (1) | SG182763A1 (es) |
SI (1) | SI2534132T1 (es) |
TW (1) | TWI401243B (es) |
UA (1) | UA107954C2 (es) |
WO (1) | WO2011098398A1 (es) |
Families Citing this family (46)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7303676B2 (en) * | 2003-02-13 | 2007-12-04 | Zenon Technology Partnership | Supported biofilm apparatus and process |
GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
US8354444B2 (en) | 2008-09-18 | 2013-01-15 | Hoffmann-La Roche Inc. | Substituted pyrrolidine-2-carboxamides |
KR101485645B1 (ko) | 2009-10-14 | 2015-01-22 | 머크 샤프 앤드 돔 코포레이션 | p53 활성을 증가시키는 치환된 피페리딘 및 그의 용도 |
US8088815B2 (en) * | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
US20120010235A1 (en) * | 2010-07-12 | 2012-01-12 | Xin-Jie Chu | N-substituted pyrrolidines |
US8709419B2 (en) | 2010-08-17 | 2014-04-29 | Hoffmann-La Roche, Inc. | Combination therapy |
US9295669B2 (en) | 2010-12-14 | 2016-03-29 | Hoffman La-Roche Inc. | Combination therapy for proliferative disorders |
US8629133B2 (en) | 2011-03-10 | 2014-01-14 | Daiichi Sankyo Company, Limited | Dispiropyrrolidine derivatives |
WO2013062923A1 (en) | 2011-10-28 | 2013-05-02 | Merck Sharp & Dohme Corp. | MACROCYCLES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF |
US9062071B2 (en) | 2011-12-21 | 2015-06-23 | Merck Sharp & Dohme Corp. | Substituted piperidines as HDM2 inhibitors |
US8993614B2 (en) * | 2012-03-15 | 2015-03-31 | F. Hoffmann-La Roche Ag | Substituted pyrrolidine-2-carboxamides |
US20140200255A1 (en) * | 2012-03-19 | 2014-07-17 | Brian Higgins | Method for administration |
US9216170B2 (en) * | 2012-03-19 | 2015-12-22 | Hoffmann-La Roche Inc. | Combination therapy for proliferative disorders |
US20130245089A1 (en) * | 2012-03-19 | 2013-09-19 | Hoffmann-La Roche Inc. | Method for administration |
SG11201406889WA (en) | 2012-05-30 | 2015-02-27 | Hoffmann La Roche | Substituted pyrrolidine-2-carboxamides |
TWI586668B (zh) | 2012-09-06 | 2017-06-11 | 第一三共股份有限公司 | 二螺吡咯啶衍生物之結晶 |
RU2690663C2 (ru) | 2012-12-20 | 2019-06-05 | Мерк Шарп И Доум Корп. | Замещенные имидазопиридины в качестве ингибиторов hdm2 |
EP2948141A1 (en) * | 2013-01-22 | 2015-12-02 | F. Hoffmann-La Roche AG | Pharmaceutical composition with improved bioavailability |
ES2630392T3 (es) * | 2013-02-21 | 2017-08-21 | F. Hoffmann-La Roche Ag | Síntesis asimétrica de una pirrolidina-2-carboxamida sustituida |
US20140275562A1 (en) * | 2013-03-13 | 2014-09-18 | Dow Agrosciences Llc | Preparation of certain (substituted phenyl)-triazolyl-(substituted phenyl) molecules, and intermediates and insecticides related thereto |
ES2747073T3 (es) * | 2013-06-19 | 2020-03-10 | Hoffmann La Roche | Combinación de RO5503781, capecitabina y oxaliplatino para el tratamiento del cáncer |
RU2015152577A (ru) * | 2013-06-19 | 2017-07-24 | Ф. Хоффманн-Ля Рош Аг | Комбинация ro5503781 и капецитабина для лечения рака |
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BR112015031542A2 (pt) * | 2013-07-03 | 2017-07-25 | Hoffmann La Roche | métodos de previsão de reação de pacientes com câncer, método de tratamento de câncer, kit de previsão da reação ao tratamento e processos, métodos e usos inovadores |
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