AR057911A1 - Compuestos de pirimidinil benzotiofeno formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento - Google Patents
Compuestos de pirimidinil benzotiofeno formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamentoInfo
- Publication number
- AR057911A1 AR057911A1 ARP060105065A ARP060105065A AR057911A1 AR 057911 A1 AR057911 A1 AR 057911A1 AR P060105065 A ARP060105065 A AR P060105065A AR P060105065 A ARP060105065 A AR P060105065A AR 057911 A1 AR057911 A1 AR 057911A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- cycloalkyl
- halo
- hydroxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 16
- -1 Pyrimidinyl benzothiophene compound Chemical class 0.000 abstract 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 6
- 125000001475 halogen functional group Chemical group 0.000 abstract 6
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 3
- 125000003386 piperidinyl group Chemical group 0.000 abstract 3
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 2
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 101100240517 Caenorhabditis elegans nhr-11 gene Proteins 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 206010023774 Large cell lung cancer Diseases 0.000 abstract 1
- 208000034578 Multiple myelomas Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010033128 Ovarian cancer Diseases 0.000 abstract 1
- 206010061535 Ovarian neoplasm Diseases 0.000 abstract 1
- 206010035226 Plasma cell myeloma Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000029742 colonic neoplasm Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 208000005017 glioblastoma Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 201000009546 lung large cell carcinoma Diseases 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000004305 thiazinyl group Chemical group S1NC(=CC=C1)* 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000004950 trifluoroalkyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuesto de pirimidinil benzotiofeno de formula (1) en donde R1 es H, hidroxi, halo, metiltio, aminosulfonilo, pirid-2-ilamino, 3-,metilaminocarbonilfenilo, -C(O)NR8R9, -(CH2)0-1NHSO2R12, -CH2NHCONHR13, -NHC(O)R14, o pirrolidinonilo opcionalmente sustituido con etiloxicarbonilo; R2 es H, hidroxi, halo, ciano, alquilo C1-4 o alcoxi C1-4; R3 es H, halo o metilo; R4 es (a) -NR6R7 o (b) aminometilociclohexilo, piperidinilo, 2,2,6-6-tetrametilpiperidin-4-ilo; 2,2,6,6-tetrametilpiperidin-4- iletenilo, 4-alquilpiperidin(C1-4)-4-ilo, o pirrolidinilo; en donde (b) puede ser opcionalmente sustituido con un sustituyente seleccionado del grupo que consiste de alquenilo C2-4, cicloalquilo C3-6, C(O)R10, y alquilo C1-4 opcionalmente sustituido con halo, alcoxi C1-4 o cicloalquilo C3-6; R5 es H cuando n es 1-7 o hidroxi cuando n es 2-7; R6 es H o alquilo C1-4; R7 es seleccionado del grupo que consiste de H, alquilo C1-4, piperidin-4-ilo opcionalmente sustituido con alquilo C1-4, piperidinilcarbonilo opcionalmente sustituido con alquilo C1-4, pirrolidin-3-ilo opcionalmente sustituido con alquilo C1-4, y pirrolidinilocarbonilo opcionalmente sustituido con alquilo C1-4, alternativamente R6 y R7 junto con el N al cual están unidos, forman un anillo seleccionado del grupo que consiste de piperazinilo, homopiperazinilo, 4-dimetiloaminopiperidin-1-ilo, 3-dimetiloaminopirrolidin-1-ilo, o hexahidro-pirrol[3,4-c]pirrolilo; en donde el anillo puede ser opcionalmente sustituido del grupo que consiste de alquenilo C2-4, cicloalquilo C3-6, C(O)R10, y uno a tres sustituyentes alquilo C1-4 opcionalmente sustituidos con hidroxi; R8 es H o alquilo C1-4; R9 es H, alquilo C1-4, alcoxi C1-4, cicloalquilo C3-6, tiazolilo, imidazolilo, piridilo, fenilo opcionalmente sustituido con halo, 2-hidroxi-2-fenilo-etilo, imidazoliletilo, 6-cloropirid-3-ilmetilo, o furan-2-ilo-(alquilo C1-4); alternativamente R8 y R9 junto con el N al cual están unidos, forman un heterociclo seleccionado del grupo que consiste de morfolinilo y tiazinilo; R10 es H, alquilo C1-4, o NHR11; R11 es H o alquilo C1-4; R12 es alquilo C1-4, trifluoroalquilo C1-4, bencilo, o cicloalquilo C3-6; R13 es alquilo C1-4, cicloalquilo C3-6, o bencilo opcionalmente sustituido co alquilo C1-4, halo, o alcoxi C1-4; R14 es cicloalquilo C3-6, piperidinilo, indolilo metilo, o bencilo opcionalmente sustituido con 3-dimetilamino-2-hidroxipropoxi; siempre que cuando R4 es piperidinilo, R1 es -C(O)NR8R9; y n es 1-7 o una sal del mismo farmacéuticamente aceptable. Formulacion farmacéutica que lo comprende. Uso de dicho compuesto para la manufactura de un medicamento para el tratamiento de un cáncer seleccionado de mieloma multiple, cáncer de colon, cáncer de pulmon de célula grande, glioblastoma y cáncer de ovario, o para el tratamiento de enfermedades inflamatorias seleccionadas de artritis reumatoide y enfermedad pulmonar obstructiva cronica.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73809705P | 2005-11-18 | 2005-11-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR057911A1 true AR057911A1 (es) | 2007-12-26 |
Family
ID=38345605
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060105065A AR057911A1 (es) | 2005-11-18 | 2006-11-17 | Compuestos de pirimidinil benzotiofeno formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US7547691B2 (es) |
| EP (1) | EP1989200B1 (es) |
| JP (1) | JP2009516697A (es) |
| KR (1) | KR100990771B1 (es) |
| CN (1) | CN101309918B (es) |
| AR (1) | AR057911A1 (es) |
| AT (1) | ATE437873T1 (es) |
| AU (1) | AU2006337626B2 (es) |
| BR (1) | BRPI0618245A2 (es) |
| CA (1) | CA2629336A1 (es) |
| CR (1) | CR9947A (es) |
| DE (1) | DE602006008187D1 (es) |
| DK (1) | DK1989200T3 (es) |
| EA (1) | EA014426B1 (es) |
| EC (1) | ECSP088456A (es) |
| ES (1) | ES2329085T3 (es) |
| IL (1) | IL190489A0 (es) |
| MA (1) | MA30053B1 (es) |
| NO (1) | NO20082594L (es) |
| PE (1) | PE20070833A1 (es) |
| PL (1) | PL1989200T3 (es) |
| PT (1) | PT1989200E (es) |
| SI (1) | SI1989200T1 (es) |
| TN (1) | TNSN08227A1 (es) |
| TW (1) | TW200800201A (es) |
| WO (1) | WO2007092095A2 (es) |
| ZA (1) | ZA200803940B (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA95949C2 (ru) | 2006-03-31 | 2011-09-26 | Янссен Фармацевтика, Н.В. | Бензоимидазол-2-илпиримидины и пиразины как модуляторы рецептора гистамина h4 |
| US20080021217A1 (en) * | 2006-07-20 | 2008-01-24 | Allen Borchardt | Heterocyclic inhibitors of rho kinase |
| US8063212B2 (en) | 2006-12-21 | 2011-11-22 | Eli Lilly And Company | Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer |
| JP5166441B2 (ja) * | 2006-12-21 | 2013-03-21 | イーライ リリー アンド カンパニー | 癌治療用イミダゾリジノニルアミノピリミジン化合物 |
| PE20090216A1 (es) | 2007-05-16 | 2009-02-28 | Lilly Co Eli | Compuestos triazolil aminopirimidina |
| KR101131254B1 (ko) | 2007-05-16 | 2012-04-24 | 일라이 릴리 앤드 캄파니 | 트리아졸릴 아미노피리미딘 화합물 |
| US9371311B2 (en) | 2008-06-30 | 2016-06-21 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine derivatives |
| US8309720B2 (en) | 2008-06-30 | 2012-11-13 | Janssen Pharmaceutica Nv | Process for the preparation of substituted pyrimidine derivatives |
| KR101123178B1 (ko) * | 2009-04-09 | 2012-06-13 | (주)에스메디 | 2-아릴벤조싸이오펜 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물 |
| EP2467137A1 (en) | 2009-08-19 | 2012-06-27 | Ambit Biosciences Corporation | Biaryl compounds and methods of use thereof |
| RU2552999C2 (ru) | 2010-04-27 | 2015-06-10 | Хатчисон Медифарма Лимитед | Соединения пиримидинилиндола |
| JP2014512364A (ja) | 2011-04-07 | 2014-05-22 | コーネル ユニバーシティー | 水溶液中で二量体化できる単量体、およびその使用法 |
| US9245773B2 (en) | 2011-09-02 | 2016-01-26 | Taiwan Semiconductor Manufacturing Company, Ltd. | Semiconductor device packaging methods and structures thereof |
| CN103159742B (zh) * | 2011-12-16 | 2015-08-12 | 北京韩美药品有限公司 | 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用 |
| EP2812324B1 (en) | 2012-02-08 | 2021-09-01 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| CN105085434B (zh) * | 2014-05-09 | 2018-02-09 | 上海特化医药科技有限公司 | 硫乙拉嗪或其中间体的制备方法 |
| WO2017076888A1 (en) * | 2015-11-03 | 2017-05-11 | Janssen Pharmaceutica Nv | 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same |
| CN116283877A (zh) | 2016-07-29 | 2023-06-23 | 赛诺维信制药公司 | 化合物、组合物及其用途 |
| AU2017301767A1 (en) | 2016-07-29 | 2019-02-14 | Pgi Drug Discovery Llc | Compounds and compositions and uses thereof |
| WO2018140512A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
| EP3573970A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
| EP3573964A1 (en) * | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
| EP3630745A2 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Covalent inhibitors of kras |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| KR20200036008A (ko) | 2017-08-02 | 2020-04-06 | 선오비온 파마슈티컬스 인코포레이티드 | 이소크로만 화합물 및 이의 용도 |
| AU2019312670B2 (en) | 2018-08-01 | 2025-01-02 | Araxes Pharma Llc | Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer |
| MX2021010880A (es) | 2019-03-14 | 2022-01-18 | Sunovion Pharmaceuticals Inc | Sales de un compuesto de isocromanilo y formas cristalinas, procesos de preparacion, usos terapeuticos y composiciones farmaceuticas de las mismas. |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3752589A (en) * | 1988-05-16 | 1989-12-12 | Georgia State University Research Foundation, Inc. | Nucleic acid interacting unfused heteropolycyclic compounds |
| GB0308466D0 (en) | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
| EP1831207B1 (en) * | 2004-12-17 | 2012-11-14 | Amgen Inc. | Aminopyrimidine compounds as plk inhibitors |
-
2006
- 2006-10-23 TW TW095139053A patent/TW200800201A/zh unknown
- 2006-11-15 EA EA200801362A patent/EA014426B1/ru not_active IP Right Cessation
- 2006-11-15 AU AU2006337626A patent/AU2006337626B2/en not_active Ceased
- 2006-11-15 SI SI200630446T patent/SI1989200T1/sl unknown
- 2006-11-15 CA CA002629336A patent/CA2629336A1/en not_active Abandoned
- 2006-11-15 PT PT06850430T patent/PT1989200E/pt unknown
- 2006-11-15 PL PL06850430T patent/PL1989200T3/pl unknown
- 2006-11-15 BR BRPI0618245-3A patent/BRPI0618245A2/pt not_active IP Right Cessation
- 2006-11-15 JP JP2008541463A patent/JP2009516697A/ja not_active Ceased
- 2006-11-15 EP EP06850430A patent/EP1989200B1/en active Active
- 2006-11-15 WO PCT/US2006/060911 patent/WO2007092095A2/en not_active Ceased
- 2006-11-15 PE PE2006001456A patent/PE20070833A1/es not_active Application Discontinuation
- 2006-11-15 DK DK06850430T patent/DK1989200T3/da active
- 2006-11-15 ES ES06850430T patent/ES2329085T3/es active Active
- 2006-11-15 AT AT06850430T patent/ATE437873T1/de active
- 2006-11-15 KR KR1020087011830A patent/KR100990771B1/ko not_active Expired - Fee Related
- 2006-11-15 DE DE602006008187T patent/DE602006008187D1/de active Active
- 2006-11-15 US US12/093,024 patent/US7547691B2/en not_active Expired - Fee Related
- 2006-11-15 CN CN2006800428126A patent/CN101309918B/zh not_active Expired - Fee Related
- 2006-11-17 AR ARP060105065A patent/AR057911A1/es unknown
-
2008
- 2008-03-27 IL IL190489A patent/IL190489A0/en unknown
- 2008-04-29 CR CR9947A patent/CR9947A/es not_active Application Discontinuation
- 2008-05-08 ZA ZA200803940A patent/ZA200803940B/xx unknown
- 2008-05-16 EC EC2008008456A patent/ECSP088456A/es unknown
- 2008-05-16 TN TNP2008000227A patent/TNSN08227A1/en unknown
- 2008-06-10 NO NO20082594A patent/NO20082594L/no not_active Application Discontinuation
- 2008-06-13 MA MA31035A patent/MA30053B1/fr unknown
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