AR032467A1 - Derivados de piridina, procedimiento para prepararlos, el uso de dichos derivados para la preparacion de medicamentos y los medicamentos que contienen dichos derivados - Google Patents
Derivados de piridina, procedimiento para prepararlos, el uso de dichos derivados para la preparacion de medicamentos y los medicamentos que contienen dichos derivadosInfo
- Publication number
- AR032467A1 AR032467A1 ARP010103479A ARP010103479A AR032467A1 AR 032467 A1 AR032467 A1 AR 032467A1 AR P010103479 A ARP010103479 A AR P010103479A AR P010103479 A ARP010103479 A AR P010103479A AR 032467 A1 AR032467 A1 AR 032467A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- branched
- linear
- alkylamino
- aryl
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 2
- -1 phenylethyloxy, nitro, amino Chemical group 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000003282 alkyl amino group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 2
- DZBUGLKDJFMEHC-UHFFFAOYSA-N acridine Chemical compound C1=CC=CC2=CC3=CC=CC=C3N=C21 DZBUGLKDJFMEHC-UHFFFAOYSA-N 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 150000003254 radicals Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 abstract 1
- 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
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- GMLCDIVXKUWJFO-UHFFFAOYSA-N [C].C1=CC=NC=C1 Chemical compound [C].C1=CC=NC=C1 GMLCDIVXKUWJFO-UHFFFAOYSA-N 0.000 abstract 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 229940041181 antineoplastic drug Drugs 0.000 abstract 1
- 150000005840 aryl radicals Chemical class 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 238000002483 medication Methods 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 1
- 150000003222 pyridines Chemical class 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- AGGIJOLULBJGTQ-UHFFFAOYSA-N sulfoacetic acid Chemical class OC(=O)CS(O)(=O)=O AGGIJOLULBJGTQ-UHFFFAOYSA-N 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
Classifications
-
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
La presente se refiere a derivados de piridina de la formula general (1), a su preparacion y uso como medicamentos, especialmente para el tratamiento de tumores, en la cual: R, R1, R2, R3 pueden estar unidos opcionalmente a los átomos de carbono de piridina C1-9, son iguales o distintos y significan, independientemente entre sí, hidrogeno, alquilo C1-8 lineal o ramificado, cicloalquilo C3-7, alquilcarbonilo C1-8 lineal o ramificado, preferentemente acetilo, alcoxi C1-8 lineal o ramificado, halogeno, aril-alcoxi C1-8, preferentemente benciloxi o feniletiloxi, nitro, amino, mono-alquilamino C1-4, di-alquilamino C1-4, alcoxicarbonil C1-8-amino, alcoxicarbonilamino C1-6-alquilo C1-8, ciano, ciano C1-6-alquilo lineal o ramificado, carboxi, alcoxicarbonilo C1-8, alquilo C1-4 substituido con uno o varios átomos de fluor, preferentemente el grupo trifluorometilo, carboxi-alquilo C1-8 o alcoxicarbonil C1-8-alquilo C1-6, alquenilo C2-6, preferentemente alilo, alquinilo C2-6, preferentemente etinilo o propargilo, ciano-alquilo C1-6 lineal o ramificado, preferentemente cianometilo, arilo, donde el radical arilo puede estar insustituido o puede estar mono o polisustituido, de igual o distinta manera, con halogeno, alquilo C1-8 lineal o ramificado, cicloalquilo C3-7, carboci, alcoxicarbonilo C1-8 lineal o ramificado, preferentemente ter.-butoxicarbonilo, con trifluorometilo, hidroxi, alcoxi C1-8 lineal o ramificado, preferentemente metoxi o etoxi, benciloxi, nitro, amino, mono-alquilamino C1-4, di-alquilamino C1-4, ciano, ciano-alquilo C1-6 lineal o ramificado, donde adicionalmente R y R1 y/o R2 y R3 pueden formar un anillo 6 aromático condensado con el anillo de piridina, formándose un anillo de quinolina o acridina, que a su vez puede estar sustituido con los radicales R, R1, R2, y R3 con los significados mencionados con anterioridad en cualquier posicion del átomo de C en el anillo; R, R1, R2, R3 pueden ser hidroxi, R4 puede ser alquilo C1-20 que puede estar sustituido por CN o -C=NH(NH2), R4 puede ser carboxi o alcoxi C1-4-carbonilo, sales fisiologicamente aceptables pueden ser además sal de ácido metansulfonico o sal de ácido sulfoacético; Z es oxígeno o azufre, donde el radical sustituido en el heterociclo de piridina de formula (2) puede estar unido a los átomos C1-9 de la estructura del anillo de piridina; P y Q son, independientemente entre sí, oxígeno, o en cada caso, dos átomos de hidrogeno (es decir, -CH2-); X es nitrogeno o C-R5, donde R5 es hidrogeno o alquilo C1-6; n y m son, independientemente entre sí, un numero entero entre 0-3, con la condicion de que, en el caso de que n = 0, X sea un grupo CR5R6, donde R5 y R6 son, independientemente entre sí, hidrogeno o alquilo C1-6, y el átomo de nitrogeno adyacente al grupo C=Z esté sustituido con un átomo de hidrogeno o un grupo alquilo C1-6; R4 puede ser un radical alquilo C1-20 lineal o ramificado, que puede estar saturado o insaturado con uno hasta tres enlaces dobles o triples y que puede estar insustituido o sustituido opcionalmente en los átomos de C iguales o diferentes con uno, dos o más arilo, heteroarilo, halogeno, alcoxi C1-6, amino, mono-alquilamino C1-4 o di-alquilamino C1-4; un radical arilo C6-14, un radical aril C6-14-alquilo C1-4 o un radical heteroarilo C2-10 o heteroaril C2-10-alquilo C1-4 que contiene uno o varios heteroátomos seleccionados del grupo N, O y S, donde el radical alquilo C1-4 puede estar insustituido o puede estar mono o polisustituido, de igual o distinta manera, con alquilo C1-6, halogeno u oxo (=O) y el radical arilo C6-14 o heretoarilo C2-10 puede estar insustituido o puede estar mono o polisustituido, de igual o distinta manera, con alquilo C1-8 lineal o ramificado, cicloalquilo C3-7, halogeno, ciano, alcoxicarbonilamino C1-6, alcoxi C1-6, carboxi, alcoxicarbonilo C1-8, alquilo C1-6 lineal o ramificado sustituido con uno o varios átomos de fluor, preferentemente trifluorometilo, hidroxi, alcoxi C1-8 lineal o ramificado, preferentemente metoxi o etoxi, donde los átomos de oxígeno adyacentes también pueden estar unidos mediante grupos alquileno C1-2, preferentemente un grupo metileno, benciloxi, nitro, amino, mono-alquilamino C1-4, di-alquilamino C1-4, arilo, que a su vez puede estar insustituido o puede estar mono o polisustituido, de igual o distinta manera, con alquilo C1-8 lineal o ramificado, cicloalquilo C3-7, carboxi, alcoxicarbonilo C1-8 lineal o ramificado, con trifluorometilo, hidroxi, alcoxi C1-8 lineal o ramificado, preferentemente metoxi o etoxi, benciloxi, nitro, amino, mono-alquilamino C1-4, di-alquilamino C1-4, ciano, ciano-alquilo C1-6 lineal o ramificado; así como sus isomeros estructurales y estereoisomeros, especialmente tautomeros, diastereomeros y enantiomeros, y sus sales de tolerancia farmacéutica, especialmente sales de adicion ácida. También se describe el uso de dichos derivados para la preparacion de medicamentos, el procedimiento para preparar dichos derivados y los medicamentos que los contienen. Los compuestos de formula (1) son utiles como medicamentos anti-tumorales para el tratamiento de mamíferos, especialmente el ser humano.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10035908A DE10035908A1 (de) | 2000-07-21 | 2000-07-21 | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR032467A1 true AR032467A1 (es) | 2003-11-12 |
Family
ID=7649970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010103479A AR032467A1 (es) | 2000-07-21 | 2001-07-20 | Derivados de piridina, procedimiento para prepararlos, el uso de dichos derivados para la preparacion de medicamentos y los medicamentos que contienen dichos derivados |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US6638935B2 (es) |
| EP (1) | EP1305289A2 (es) |
| JP (1) | JP2004516243A (es) |
| KR (1) | KR20030015894A (es) |
| CN (1) | CN1447796A (es) |
| AR (1) | AR032467A1 (es) |
| AU (2) | AU8198901A (es) |
| BG (1) | BG107506A (es) |
| BR (1) | BR0112711A (es) |
| CA (1) | CA2353353A1 (es) |
| DE (1) | DE10035908A1 (es) |
| HU (1) | HUP0300743A2 (es) |
| IL (1) | IL153931A0 (es) |
| MX (1) | MXPA03000596A (es) |
| NO (1) | NO20030302L (es) |
| NZ (1) | NZ524156A (es) |
| PL (1) | PL361354A1 (es) |
| RU (1) | RU2003105238A (es) |
| SK (1) | SK1942003A3 (es) |
| WO (1) | WO2002008190A2 (es) |
| ZA (1) | ZA200300545B (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040014744A1 (en) * | 2002-04-05 | 2004-01-22 | Fortuna Haviv | Substituted pyridines having antiangiogenic activity |
| CN100509790C (zh) * | 2002-06-29 | 2009-07-08 | 赞塔里斯有限公司 | 芳基羰基哌嗪和杂芳基羰基哌嗪及其治疗良性和恶性肿瘤疾病的用途 |
| BRPI0407088A (pt) * | 2003-01-28 | 2006-01-24 | Aventis Pharma Sa | Produtos n-aril-heteroaromáticos, composições contendo os mesmos e seu uso |
| FR2855825B1 (fr) * | 2003-06-04 | 2008-08-22 | Aventis Pharma Sa | Produits aryl-heteroaromatiques, compositions les contenant et utilisation |
| PE20050226A1 (es) * | 2003-06-04 | 2005-05-18 | Aventis Pharma Sa | Productos aril-heteroaromaticos y composiciones que los contienen |
| US7592466B2 (en) | 2003-10-09 | 2009-09-22 | Abbott Laboratories | Ureas having antiangiogenic activity |
| FR2871157A1 (fr) * | 2004-06-04 | 2005-12-09 | Aventis Pharma Sa | Produits biaryl aromatiques, compositions les contenant et utilisation |
| EP1645556A1 (en) * | 2004-10-07 | 2006-04-12 | Boehringer Ingelheim International GmbH | Arylpiperazine-benzoylamide derivatives useful as pharmaceutical agents |
| AU2008210455A1 (en) * | 2007-01-31 | 2008-08-07 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as kinase inhibitors |
| CA2678577A1 (en) * | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| EP2183228B1 (en) * | 2007-07-26 | 2014-08-20 | Vitae Pharmaceuticals, Inc. | CYCLIC INHIBITORS OF 11ß -HYDROXYSTERIOD DEHYDROGENASE 1 |
| CA2704266A1 (en) * | 2007-11-02 | 2009-06-11 | Vertex Pharmaceuticals Incorporated | [1h- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase c-theta |
| AR069207A1 (es) * | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| CA2708303A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceuticals, Inc. | Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| TW200934490A (en) * | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| WO2009094169A1 (en) | 2008-01-24 | 2009-07-30 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5734666B2 (ja) * | 2008-02-11 | 2015-06-17 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤 |
| US8598160B2 (en) * | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| JP5538356B2 (ja) * | 2008-03-18 | 2014-07-02 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤 |
| WO2009134387A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| AR071236A1 (es) | 2008-05-01 | 2010-06-02 | Vitae Pharmaceuticals Inc | Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1 |
| CL2009001059A1 (es) * | 2008-05-01 | 2010-11-12 | Boehringer Ingelheim Int | Compuestos derivados de 1,3-oxazin-2-ona-3,6 sustituidos, inhibidores de la actividad de la 11-beta-hidroxiesteroide deshidrogenasa i; composicion farmaceutica que los comprende; utiles en el tratamiento de enfermedades tales como diabetes mellitus, entre otras. |
| CA2723032A1 (en) * | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| US8569337B2 (en) | 2008-07-23 | 2013-10-29 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| ES2402087T3 (es) | 2008-07-23 | 2013-04-26 | Vertex Pharmaceuticals Incorporated | Inhibidores de la pirazolopiridina quinasa |
| AU2009274023A1 (en) | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| US8846668B2 (en) | 2008-07-25 | 2014-09-30 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2010011314A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1 |
| MX2011001319A (es) * | 2008-08-06 | 2011-04-05 | Vertex Pharma | Inhibidores de aminopiridina cinasa. |
| CA2744946A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| TW201039034A (en) * | 2009-04-27 | 2010-11-01 | Chunghwa Picture Tubes Ltd | Pixel structure and the method of forming the same |
| UA109255C2 (ru) | 2009-04-30 | 2015-08-10 | Берінгер Інгельхайм Інтернешнл Гмбх | Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1 |
| KR20120061771A (ko) * | 2009-04-30 | 2012-06-13 | 비타이 파마슈티컬즈, 인코포레이티드 | 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제 |
| CA2760705A1 (en) | 2009-05-06 | 2010-11-11 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridines |
| EP2440537A1 (en) | 2009-06-11 | 2012-04-18 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| WO2011002910A1 (en) | 2009-07-01 | 2011-01-06 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2011094288A1 (en) | 2010-01-27 | 2011-08-04 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrazine kinase inhibitors |
| EP2528917B1 (en) | 2010-01-27 | 2016-10-19 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridines useful for the treatment of autoimmune, inflammatory or (hyper)proliferative diseases |
| MX2012008643A (es) | 2010-01-27 | 2013-02-26 | Vertex Pharma | Inhibidores de cinasas de pirazolopiridinas. |
| US8933072B2 (en) | 2010-06-16 | 2015-01-13 | Vitae Pharmaceuticals, Inc. | Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use |
| JP5813106B2 (ja) | 2010-06-25 | 2015-11-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン |
| PH12013500808A1 (en) | 2010-11-02 | 2015-10-07 | Boehringer Ingelheim Int | Pharmaceutical combinations for the treatment of metabolic disorders |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE791501A (fr) * | 1971-11-19 | 1973-05-17 | Albert Ag Chem Werke | Diamines cycliques n,n'-disubstituees et leur procede de preparation |
| JPS50151886A (es) * | 1974-05-29 | 1975-12-06 | ||
| HU175075B (hu) * | 1977-06-30 | 1980-05-28 | Egyt Gyogyszervegyeszeti Gyar | Sposob poluchenija piperazidov piridin-karbonovoj kisloty |
| EP0040793B1 (en) * | 1980-05-22 | 1985-08-28 | Masayuki Ishikawa | Novel quinazoline-dione compounds, process for production thereof and pharmaceutical use thereof |
| EP0318235A3 (en) * | 1987-11-25 | 1991-05-02 | Takeda Chemical Industries, Ltd. | Paf antagonist, 1,4-disubstituted piperazine compounds and production thereof |
| MX16687A (es) * | 1988-07-07 | 1994-01-31 | Ciba Geigy Ag | Compuestos de biarilo y procedimiento para su preparacion. |
| WO1995000497A1 (en) * | 1993-06-18 | 1995-01-05 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| CZ288002B6 (cs) * | 1995-01-11 | 2001-03-14 | Samjin Pharmaceutical Co., Ltd. | Piperazinové deriváty a farmaceutický prostředek s protinádorovou aktivitou je obsahující |
| ATE251141T1 (de) * | 1995-03-10 | 2003-10-15 | Berlex Lab | Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien |
| NZ329847A (en) * | 1996-06-29 | 1999-01-28 | Samjin Pharm Co Ltd | Piperazine derivatives and process for the preparation thereof |
| ES2125206B1 (es) * | 1997-07-21 | 1999-11-16 | Esteve Labor Dr | Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos. |
| WO1999043682A1 (en) * | 1998-02-26 | 1999-09-02 | Neurogen Corporation | 2-(het-)aryl-4-(cyclic amino substituted) heteroaryl fused pyridine derivatives, their preparation and their use as (ant-)agonists for gaba (a) brain receptors |
| CA2342251A1 (en) * | 1998-08-28 | 2000-03-09 | Scios Inc. | Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase |
| WO2000052001A1 (en) * | 1999-03-03 | 2000-09-08 | Samjin Pharmaceutical Co., Ltd. | Piperazine derivatives and process for the preparation thereof |
| US6469006B1 (en) * | 1999-06-15 | 2002-10-22 | Bristol-Myers Squibb Company | Antiviral indoleoxoacetyl piperazine derivatives |
| DE60022386T2 (de) * | 1999-12-16 | 2006-06-22 | Schering Corp. | Substituierte imidazole als neuropeptide y y5 rezeptor antagonisten |
-
2000
- 2000-07-21 DE DE10035908A patent/DE10035908A1/de not_active Withdrawn
-
2001
- 2001-07-18 WO PCT/EP2001/008262 patent/WO2002008190A2/de not_active Ceased
- 2001-07-18 IL IL15393101A patent/IL153931A0/xx unknown
- 2001-07-18 BR BR0112711-0A patent/BR0112711A/pt not_active IP Right Cessation
- 2001-07-18 AU AU8198901A patent/AU8198901A/xx active Pending
- 2001-07-18 KR KR10-2003-7000880A patent/KR20030015894A/ko not_active Withdrawn
- 2001-07-18 EP EP01960509A patent/EP1305289A2/de not_active Withdrawn
- 2001-07-18 PL PL36135401A patent/PL361354A1/xx unknown
- 2001-07-18 JP JP2002514097A patent/JP2004516243A/ja not_active Withdrawn
- 2001-07-18 HU HU0300743A patent/HUP0300743A2/hu unknown
- 2001-07-18 RU RU2003105238/04A patent/RU2003105238A/ru not_active Application Discontinuation
- 2001-07-18 NZ NZ524156A patent/NZ524156A/en unknown
- 2001-07-18 MX MXPA03000596A patent/MXPA03000596A/es unknown
- 2001-07-18 AU AU2001281989A patent/AU2001281989B2/en not_active Ceased
- 2001-07-18 SK SK194-2003A patent/SK1942003A3/sk not_active Application Discontinuation
- 2001-07-18 CN CN01814312A patent/CN1447796A/zh active Pending
- 2001-07-20 US US09/910,139 patent/US6638935B2/en not_active Expired - Fee Related
- 2001-07-20 CA CA002353353A patent/CA2353353A1/en not_active Abandoned
- 2001-07-20 AR ARP010103479A patent/AR032467A1/es unknown
-
2002
- 2002-01-21 ZA ZA200300545A patent/ZA200300545B/xx unknown
-
2003
- 2003-01-20 NO NO20030302A patent/NO20030302L/no unknown
- 2003-01-30 BG BG107506A patent/BG107506A/bg unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN1447796A (zh) | 2003-10-08 |
| KR20030015894A (ko) | 2003-02-25 |
| IL153931A0 (en) | 2003-07-31 |
| AU8198901A (en) | 2002-02-05 |
| MXPA03000596A (es) | 2003-05-14 |
| WO2002008190A3 (de) | 2002-08-01 |
| US6638935B2 (en) | 2003-10-28 |
| SK1942003A3 (en) | 2003-12-02 |
| DE10035908A1 (de) | 2002-03-07 |
| ZA200300545B (en) | 2003-02-12 |
| AU2001281989B2 (en) | 2005-05-12 |
| NO20030302L (no) | 2003-02-07 |
| JP2004516243A (ja) | 2004-06-03 |
| PL361354A1 (en) | 2004-10-04 |
| BG107506A (bg) | 2003-09-30 |
| BR0112711A (pt) | 2003-05-20 |
| EP1305289A2 (de) | 2003-05-02 |
| WO2002008190A2 (de) | 2002-01-31 |
| US20020111354A1 (en) | 2002-08-15 |
| NO20030302D0 (no) | 2003-01-20 |
| NZ524156A (en) | 2005-10-28 |
| HUP0300743A2 (hu) | 2003-10-28 |
| RU2003105238A (ru) | 2004-08-10 |
| CA2353353A1 (en) | 2002-01-21 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR032467A1 (es) | Derivados de piridina, procedimiento para prepararlos, el uso de dichos derivados para la preparacion de medicamentos y los medicamentos que contienen dichos derivados | |
| AR033383A1 (es) | Derivados de acridina, procedimiento para prepararlos, el uso de los mismos para la preparacion de medicamentos y los medicamentos que contienen dichos derivados | |
| AR033678A1 (es) | Derivados de quinolina, procedimiento para prepararlos, uso de los mismos para la preparacion de medicamentos y los medicamentos que contienen dichos derivados | |
| ECSP22012347A (es) | Derivados de 2-morfolinopiridina sustituidos como inhibidores de la cinasa atr | |
| AR034897A1 (es) | Derivados n-monoacilados de o-fenilendiaminas, sus analogos heterociclicos de seis miembros y su uso como agentes farmaceuticos | |
| ATE104279T1 (de) | 4-fluorbenzolderivate, herstellungsverfahren und diese enthaltende pharmazeutische zusammensetzungen. | |
| AR064608A1 (es) | Derivados de pirazolo-quinazolina sustituidos, composiciones farmaceuticas que los contienen. proceso para su preparacion y uso de los mismos como agentes anticancer. | |
| KR940007021A (ko) | 흥분성 아미노산 수용체 길항물질 | |
| AR069510A1 (es) | Arilo y heteroarilo imidazo[1,5-a]pirazinas fusionadas como inhibidores de la fosfodiesterasa 10 | |
| RU2006134003A (ru) | Серосодержащие соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с | |
| CO6160288A2 (es) | Composiciones farmaceuticas que comprenden nilotinib o su sal | |
| AR049126A1 (es) | Derivados de 5, 6, 7, 8 - tetrahidroimidazo[1,5a]piridina con actividad inhibitoria de la aldosterona sintasa, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento del hiperaldosterismo y del sindrome de cushing. | |
| AR042368A1 (es) | Un compuesto derivado de purina, su uso, un procedimiento para prepararlo y una composicion farmaceutica que lo comprende | |
| AR047682A1 (es) | Derivados tetrahidroisoquinolinilo de quinazolina e isoquinolina | |
| AR035325A1 (es) | Derivados de adamantano, un proceso para su preparacion, composicion farmaceutica, un proceso para la preparacion de dicha composicion, y el uso de dichos derivados para la fabricacion de un medicamento | |
| MX9203550A (es) | Derivados de 4-aminoquinolina y su uso como medicamentos. | |
| RU2006134005A (ru) | Новые соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с | |
| CY1110261T1 (el) | Παραγωγα της κουμαρινης που χρησιμοποιουνται σαν αντιπηκτικα | |
| AR036599A1 (es) | Un derivado de 2-pirimidinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4-ona y 7-pirimidinil-2,3-dihidroimidazo[1,2-a]pirimidin-5(1h)ona sustituidos, uso del mismo, un medicamento que lo comprende y un inhibidor de gsk3beta o gsk3beta y cdk5/p25 seleccionado entre el grupo de dicho derivado | |
| MX9303441A (es) | Procedimiento para la preparacion de acido clavulanico. | |
| TR199802344A2 (xx) | �kame edilmi� imidazolidin t�revleri | |
| BG100016A (bg) | Нiv протеазни инхибитори във фармацевтични комбинации за лечение на спин | |
| ES2566973T9 (es) | Uso de SNS-595 para tratar leucemia | |
| TR199701647A2 (xx) | �kame edilmi� purin t�revleri,bunlar�n imalat usul� | |
| BR0215017A (pt) | Lactamas como antagonistas da taquiquinina |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |