AR076922A1 - Benzodiazepinas como inhibidores de pi3k/mtor, una composicion farmaceutica que las comprende, metodos para su fabricacion y su uso en el tratamiento del cancer. - Google Patents
Benzodiazepinas como inhibidores de pi3k/mtor, una composicion farmaceutica que las comprende, metodos para su fabricacion y su uso en el tratamiento del cancer.Info
- Publication number
- AR076922A1 AR076922A1 ARP100101819A ARP100101819A AR076922A1 AR 076922 A1 AR076922 A1 AR 076922A1 AR P100101819 A ARP100101819 A AR P100101819A AR P100101819 A ARP100101819 A AR P100101819A AR 076922 A1 AR076922 A1 AR 076922A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- ring
- alkyl
- hydrogen
- haloalkyl
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 title 1
- 101150097381 Mtor gene Proteins 0.000 title 1
- 108091007960 PI3Ks Proteins 0.000 title 1
- 102100023085 Serine/threonine-protein kinase mTOR Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 229910052739 hydrogen Inorganic materials 0.000 abstract 10
- 239000001257 hydrogen Substances 0.000 abstract 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 9
- 125000001188 haloalkyl group Chemical group 0.000 abstract 8
- 125000003342 alkenyl group Chemical group 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 150000002431 hydrogen Chemical group 0.000 abstract 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 6
- 125000000304 alkynyl group Chemical group 0.000 abstract 5
- 125000004429 atom Chemical group 0.000 abstract 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 4
- 125000002619 bicyclic group Chemical group 0.000 abstract 4
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 4
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 239000001301 oxygen Substances 0.000 abstract 4
- 229920006395 saturated elastomer Polymers 0.000 abstract 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 239000011593 sulfur Substances 0.000 abstract 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 3
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000000278 alkyl amino alkyl group Chemical group 0.000 abstract 2
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 125000005605 benzo group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 2
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 abstract 2
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910021386 carbon form Inorganic materials 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 abstract 1
- 125000000262 haloalkenyl group Chemical group 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000001841 imino group Chemical group [H]N=* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000006574 non-aromatic ring group Chemical group 0.000 abstract 1
- -1 phenyloxy Chemical group 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
- C07D413/02—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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Métodos de fabricacion y uso de los compuestos, en el tratamiento del cáncer. Reivindicacion 1: Un compuesto de Formula 1 a : o un estereoisomero simple o sus mezclas de isomeros y en forma adicional y opcional como una de sus sales aceptables desde el punto de vista farmacéutico, donde R1 es fenilo sustituido en forma opcional con uno, das, o tres grupos R6 o R1 es heteroarilo sustituido en forma opcional con uno, dos, o tres R7; R2 es -NR3R4; R3 es hidrogeno, alquilo, o alcoxicarbonilalquilo; y R4 es cicloalquilo sustituido en forma opcional, fenilo sustituido en forma opcional, fenilalquilo sustituido en forma opcional, heteroarilo sustituido en forma opcional, o heteroarilalquilo sustituido en forma opcional; o R3 y R4 junto con el nitrogeno al cual están unidos forman HET sustituido en forma opcional en cualquier átomo del anillo susceptible de sustituirse del anillo con R10, R10a, R10b, R10c, R10d, R10c, y R10f; HET es (a)un anillo de 5 a 8 miembros, monocíclico, saturado o parcialmente insaturado, pero no aromático que contiene en forma opcional un adicional de de uno o dos heteroátomos en el anillo que son en forma independiente oxígeno, azufre, o nitrogeno donde los átomos restantes del anillo son carbono; o (b)un anillo de 5 a 8 miembros, monocíclico, pero no aromático, parcialmente saturado que contiene en forma opcional un adicional de de uno o dos heteroátomos en el anillo que son en forma independiente oxígeno, azufre, o nitrogeno y los átomos restantes del anillo son carbono y cuyo anillo está fusionado a un anillo benzo; o (c) un anillo de 7 a 11 miembros bicíclico, o espirocíclico, en puente, fusionado que contiene en forma opcional un adicional de de uno o dos heteroátomos que son en forma independiente oxígeno, azufre, o nitrogeno y los átomos restantes del anillo son carbono y donde cada anillo del anillo de 7 a 11 miembros está saturado o parcialmente insaturado pero no totalmente aromático; o (d) un anillo de 7 a 11 miembros bicíclico, o espirocíclico, en puente, fusionado que contiene en forma opcional un adicional de de uno o dos heteroátomos en el anillo que son en forma independiente oxígeno, azufre, o nitrogeno y los átomos restantes del anillo son carbono donde cada anillo del anillo bicíclico de 7 a 11 miembros está saturado o parcialmente insaturado pero no totalmente aromático, y donde el anillo bicíclico de 7 a 11 miembros está fusionado a un anillo benzo; R5a y R5c son, en forma independiente, hidrogeno o alquilo; R5h es hidrogeno o halo; R5b es hidrogeno, amino, o halo; R5d, R5e, R5f, y son hidrogeno; cada R6, cuando R6 está presente, es, en forma independiente nitro; ciano; halo; alquilo; alquenilo; alquinilo; halo; haloalquilo; -OR8a; -NR8R8a; -C(O)NR8R8a; NRSC(O)OR9; -NR8C(O)R9 -NR8S(O)2R8a; -NR8C(O)NR8aR9 carboxi, -C(O)OR9 alquilcarbonilo; alquilo sustituido con uno o dos -C(O)NR8R8a; heteroarilo sustituido en forma opcional con 1, 2, o 3 R14 o heterocicloalquilo sustituido en forma opcional; cada R7, cuando R7 está presente, es, en forma independiente oxo; nitro; ciano; alquilo; alquenilo; alquinilo; halo; haloalquilo; hidroxialquilo; alcoxialquilo; -OR8a; -SR13 -S(O)R13; -S(O)2R13; -NR8R8a; -C(O)NR8R8a; -NR8C(O)OR9; -NR8C(O)R9-NR8S(O)2R8a; -NR8C(O)NR8aR8; carboxi; -C(O)OR9 alquilcarbonilo; -S(O)2NR8R9 alquilo sustituido con uno o dos -NR8R8a alquilo sustituido con uno o dos -NR8C(O)R8a cicloalquilo sustituido en forma opcional; cicloalquilalquilo sustituido en forma opcional; heterocicloalquilo sustituido en forma opcional; heterocicloalquilalquilo sustituido en forma opcional; heteroarilo sustituido en forma opcional; o heteroarilalquilo sustituido en forma opcional; R8 es hidrogeno, alquilo, alquenilo, alquinilo, hidroxialquilo, o haloalquilo; R8a es hidrogeno, alquilo, alquenilo, alquinilo, haloalquilo, hidroxialquilo, cianoalquilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, alcoxialquilo, cicloalquilo sustituido en forma opcional, cicloalquialquilo sustituido en forma opcional, heterocicloalquilo sustituido en forma opcional, heterocicloalquilalquilo sustituido en forma opcional, fenilo sustituido en forma opcional, fenilalquilo sustituido en forma opcional, heteroarilo sustituido en forma opcional, o heteroarilalquilo sustituido en forma opcional; R9 es alquilo, alquenilo, alquinilo, hidroxialquilo, alcoxialquilo, haloalquilo, o heterocicloalquilalquilo sustituido en forma opcional; R10, R10a, R10b, R10c, R10d, R10e, y R10f son, en forma independiente, hidrogeno; halo; alquilo; haloalquilo; haloalquenilo; hidroxialquilo; alquiltio; alquilsulfonilo; hidroxi; alcoxi; haloalcoxi; ciano; alcoxicarbonilo; carboxi; amino; alquilamino; dialquilamino; -C(O)R12, -C(O)NR11R11a cicloalquilo sustituido en forma opcional; cicloalquilalquilo sustituido en forma opcional; fenilo sustituido en forma opcional; fenilalquilo sustituido en forma opcional; feniloxi sustituido en forma opcional; feniloxialquilo sustituido en forma opcional; heterocicloalquilo sustituido en forma opcional; heterocicloalquilalquilo sustituido en forma opcional; heteroarilo sustituido en forma opcional; o heteroarilalquilo sustituido en forma opcional; o dos de R10, R10a, R10b, R10c, R10d, R10e, y R10f cuando están unidos al mismo carbono forman oxo, imino, o tiono; R11 hidrogeno, alquilo, o alquenilo; R11a hidrogeno, alquilo, o alquenilo; R12 es alquilo, o heteroarilo sustituido en forma opcional; R13 es alquilo o haloalquilo; y cada R14, cuando R14 está presente, es, en forma independiente amino, alquilamino, dialquilamino, acilamino, halo, hidroxi, alquilo, haloalquilo, hidroxialquilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, alcoxicarbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, o fenilo sustituido en forma opcional.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21714609P | 2009-05-26 | 2009-05-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076922A1 true AR076922A1 (es) | 2011-07-20 |
Family
ID=42634933
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101819A AR076922A1 (es) | 2009-05-26 | 2010-05-26 | Benzodiazepinas como inhibidores de pi3k/mtor, una composicion farmaceutica que las comprende, metodos para su fabricacion y su uso en el tratamiento del cancer. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8637499B2 (es) |
| EP (1) | EP2435426B8 (es) |
| JP (1) | JP2012528165A (es) |
| KR (1) | KR20120087808A (es) |
| CN (1) | CN102459248A (es) |
| AR (1) | AR076922A1 (es) |
| AU (1) | AU2010254200A1 (es) |
| BR (1) | BRPI1010896A2 (es) |
| CA (1) | CA2763008A1 (es) |
| ES (1) | ES2425091T3 (es) |
| IL (1) | IL216473A0 (es) |
| MX (1) | MX2011012584A (es) |
| NZ (1) | NZ596552A (es) |
| WO (1) | WO2010138487A1 (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5869222B2 (ja) | 2008-01-04 | 2016-02-24 | インテリカイン， エルエルシー | 特定の化学的実体、組成物および方法 |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| JP2012527474A (ja) * | 2009-05-22 | 2012-11-08 | エクセリクシス， インク． | 増殖性疾患に対するベンゾキサゼピンベースのｐｉ３ｋ／ｍｔ０ｒ阻害剤 |
| CA2812089C (en) | 2010-09-14 | 2020-02-18 | Exelixis Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| NZ608069A (en) | 2010-10-06 | 2014-06-27 | Glaxosmithkline Llc | Benzimidazole derivatives as pi3 kinase inhibitors |
| WO2012068096A2 (en) * | 2010-11-15 | 2012-05-24 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
| EP2640367A2 (en) * | 2010-11-15 | 2013-09-25 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
| WO2012071509A2 (en) * | 2010-11-24 | 2012-05-31 | Exelixis, Inc. | Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture |
| EP2643319A1 (en) * | 2010-11-24 | 2013-10-02 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
| MX347708B (es) | 2011-01-10 | 2017-05-09 | Infinity Pharmaceuticals Inc | Proceso para preparar isoquinolinonas y formas solidas de isoquinolinonas. |
| WO2012116237A2 (en) | 2011-02-23 | 2012-08-30 | Intellikine, Llc | Heterocyclic compounds and uses thereof |
| RU2456287C1 (ru) * | 2011-05-20 | 2012-07-20 | Николай Филиппович Савчук | Стимуляторы секреции инкретиновых гормонов, способы их получения и применения |
| PH12014500973A1 (en) | 2011-11-01 | 2014-06-16 | Exelixis Inc | Phosphatidylinositol 3-kinase inhibitors for the treatment of lymphoproliferative malignancies |
| FR2986232B1 (fr) * | 2012-01-26 | 2014-02-14 | Sanofi Sa | Derives heterocycliques bicycliques, leur preparation et leur application en therapeutique |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| FR2994572B1 (fr) * | 2012-08-17 | 2015-04-17 | Centre Nat Rech Scient | Pyrido[3,2-d]pyrimidines trisubstituees, leurs procedes de preparation et leurs utilisation en therapeutique |
| RU2702908C2 (ru) | 2012-11-01 | 2019-10-14 | Инфинити Фармасьютикалз, Инк. | Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы |
| US9938291B2 (en) | 2013-03-14 | 2018-04-10 | The Trustess Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
| EP2968303B1 (en) | 2013-03-14 | 2018-07-04 | The Trustees of Columbia University in the City of New York | Octahydrocyclopentapyrroles, their preparation and use |
| ES2705247T3 (es) | 2013-03-14 | 2019-03-22 | Univ Columbia | 4-fenilpiperidinas, su preparación y uso |
| WO2014151936A1 (en) | 2013-03-14 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles, their preparation and use |
| US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| AU2015253232B2 (en) | 2014-04-30 | 2020-10-01 | The Trustees Of Columbia University In The City Of New York | Substituted 4-phenylpiperidines, their preparation and use |
| CN111848643A (zh) * | 2015-07-02 | 2020-10-30 | 豪夫迈·罗氏有限公司 | 苯并氧氮杂*噁唑烷酮化合物及其使用方法 |
| US11028055B2 (en) * | 2015-11-30 | 2021-06-08 | Children's Medical Center Corporation | Compounds for treating proliferative diseases |
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| MX391135B (es) | 2016-06-24 | 2025-03-21 | Infinity Pharmaceuticals Inc | Terapias de combinacion. |
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| DE4102103A1 (de) | 1991-01-25 | 1992-08-20 | Bayer Ag | Substituierte benzoxazepine und benzthiazepine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln |
| US5272158A (en) | 1991-10-29 | 1993-12-21 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| WO1996026190A1 (en) * | 1995-02-22 | 1996-08-29 | Smithkline Beecham Corporation | Integrin receptor antagonists |
| US6011029A (en) * | 1996-02-26 | 2000-01-04 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
| BR0013608A (pt) | 1999-08-27 | 2002-05-21 | Procter & Gamble | Disponibilidade controlada de componentes de formulações, composições e métodos para lavar roupa empregando os mesmos |
| BR0013610A (pt) | 1999-08-27 | 2002-07-16 | Procter & Gamble | Componentes de formulções de ação rápida,composições e métodos para lavar roupa empregando os mesmos |
| MXPA02002124A (es) | 1999-08-27 | 2002-09-18 | Procter & Gamble | Componentes de formulacion de incremento de estabilidad y composiciones y metodos de lavanderia que emplean los mismos. |
| CN1384868A (zh) | 1999-08-27 | 2002-12-11 | 宝洁公司 | 稳定的配制组分、使用该组分的组合物和洗衣方法 |
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| CN101497612A (zh) | 2009-03-03 | 2009-08-05 | 北京华禧联合科技发展有限公司 | 一类新喹诺酮类化合物及其制备与用途 |
| US20100305093A1 (en) * | 2009-04-09 | 2010-12-02 | Exelixis, Inc. | Inhibitors of mTOR and Methods of Making and Using |
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- 2010-05-25 BR BRPI1010896A patent/BRPI1010896A2/pt not_active IP Right Cessation
- 2010-05-25 CA CA2763008A patent/CA2763008A1/en not_active Abandoned
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- 2010-05-25 ES ES10720869T patent/ES2425091T3/es active Active
- 2010-05-25 KR KR1020117031045A patent/KR20120087808A/ko not_active Withdrawn
- 2010-05-25 NZ NZ596552A patent/NZ596552A/en not_active IP Right Cessation
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- 2010-05-25 WO PCT/US2010/036032 patent/WO2010138487A1/en not_active Ceased
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- 2010-05-26 AR ARP100101819A patent/AR076922A1/es not_active Application Discontinuation
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| EP2435426A1 (en) | 2012-04-04 |
| JP2012528165A (ja) | 2012-11-12 |
| KR20120087808A (ko) | 2012-08-07 |
| NZ596552A (en) | 2014-02-28 |
| EP2435426B8 (en) | 2013-07-03 |
| EP2435426B1 (en) | 2013-05-22 |
| WO2010138487A1 (en) | 2010-12-02 |
| CN102459248A (zh) | 2012-05-16 |
| AU2010254200A1 (en) | 2011-12-08 |
| US8637499B2 (en) | 2014-01-28 |
| BRPI1010896A2 (pt) | 2019-09-24 |
| ES2425091T3 (es) | 2013-10-11 |
| CA2763008A1 (en) | 2010-12-02 |
| IL216473A0 (en) | 2012-01-31 |
| MX2011012584A (es) | 2012-02-21 |
| US20120258953A1 (en) | 2012-10-11 |
| HK1168349A1 (en) | 2012-12-28 |
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