AR064358A1 - Procedimiento para la preparacion de derivados benzimida piperacinilo y diazepanilo - Google Patents
Procedimiento para la preparacion de derivados benzimida piperacinilo y diazepaniloInfo
- Publication number
- AR064358A1 AR064358A1 ARP070105628A ARP070105628A AR064358A1 AR 064358 A1 AR064358 A1 AR 064358A1 AR P070105628 A ARP070105628 A AR P070105628A AR P070105628 A ARP070105628 A AR P070105628A AR 064358 A1 AR064358 A1 AR 064358A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocyclyl
- group
- phenyl
- cycloalkyl
- Prior art date
Links
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
- C07D413/10—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 carbon chain containing aromatic rings
-
- 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
- A61K31/4965—Non-condensed pyrazines
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- 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
- C07D401/10—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 aromatic rings
-
- 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
- C07D403/10—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 carbon chain containing aromatic rings
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
La presente está dirigida a nuevos procedimientos para la preparacion de derivados benzamida diazepanilo y piperacinilo, utiles para el tratamiento de trastornos y condiciones mediante un receptor histamine, preferiblemente el receptor H3. Reivindicacion 1: Un procedimiento para la preparacion de un compuesto de formula (1) o una sal, éster, tautomero, solvato o amidas del mismo, farmacéuticamente aceptables, donde R1 está seleccionado del grupo que consiste en alquilo C1-10, alquenilo C3-8, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, (cicloalquilo C3-8)alquenilo C3-8 y (alquilcarbonilo C1-8)alquilo C1-8; n es un numero entero de 1 a 2; R2 y R3 están cada uno seleccionados independientemente del grupo que consiste en hidrogeno, fluor, cloro, bromo, nitro, trifluormetilo, metilo y alcoxi C1-3; m es un numero entero de 1 a 7; Q es NR8R9; donde R8 está seleccionado del grupo que consiste en hidrogeno, alquilo C1-6, alquenilo C3-6, carbociclilo de 3-9 miembros, heterociclilo de 3-12 miembros, fenilo, (heterociclilo de 6-9-miembros)alquileno C1-6 y (fenil)alquileno C1-6, y R9 está seleccionado del grupo que consiste en alquilo C1-6, alquenilo C3-6, carbociclilo de 6-9 miembros, heterociclilo de 3- 12 miembros (preferiblemente heterociclilo de 5-9 o 5-8 miembros, fenilo, (heterociclilo de 6-9-miembros)alquileno C1-6, y (fenil)alquileno C1-6; alternativamente, Q es un heterociclilo ligado a N, saturado, de 3-12 miembros, donde, además del nitrogeno de union a N, el heterociclilo de 3-12 miembros puede contener opcionalmente entre 1 y 3 heteroátomos adicionales seleccionados independientemente entre O, S, y N; donde Q (cuando Q es un heterociclilo ligado a N, saturado, de 3-12 miembros) está sustituido opcionalmente con 1-3 sustituyentes seleccionados independientemente del grupo que consiste en hidroxi, halo, carboxamida, alquilo C1-6, heterociclilo de 5-9 miembros o 6-9 miembros, -N(alquilo C1-6)(heterociclilo de 5-9 miembros o 6-9 miembros), -NH(heterociclilo de 5-9 miembros o 6-9 miembros), -O(heterociclilo de 5-9 miembros o 6-9 miembros), (heterociclilo de 5-9 miembros o 6-9 miembros)alquileno C1-3, alcoxi C1-6, (cicloalquilo C3-6)-O-, fenilo, (fenil)alquileno C1-3, y (fenil)alquileno C1-3-O-; donde cada uno de los grupos heterociclilo, fenilo, y alquilo anteriores pueden estar adicionalmente sustituidos opcionalmente con desde 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en trifluormetilo, metoxi, halo, nitro, ciano, hidroxi y alquilo C1-3; con la condicion de que las posiciones 5- y 6- en el anillo fenilo estén no sustituidas; con la condicion, además, que cuando R1 es metilo, entonces -(CH2)m-Q no es piperidin-1-ilmetilo; y donde cada uno de los grupos alquilo, alquileno, alquenilo, heterociclilo, cicloalquilo, carbociclilo y arilo anteriores, pueden estar, cada uno, sustituidos independientemente y opcionalmente con entre 1 y 3 sustituyentes independientemente seleccionados del grupo que consiste en trifluormetilo, metoxi, halo, amino, nitro, hidroxi y alquilo C1-3 que comprende hacer reaccionar un compuesto de formula (2) con un compuesto de formula (3); en presencia de un agente de acoplamiento de péptidos, en un solvente orgánico o mezcla de los mismos, para proveer el compuesto correspondiente de formula (1). Reivindicacion 7: Un procedimiento para la preparacion de un compuesto de formula (4) donde R1 está seleccionado del grupo que consiste en alquilo C1-10, alquenilo C3-8, cicloalquilo C3-8, (cicloalquilo C-38)alquilo C1-6, (cicloalquilo C3-8)alquenilo C3-8 y (alquilcarbonilo C1-8)alquilo C1-8; que comprende hacer reaccionar un compuesto de formula (5), donde X es hidrogeno o un grupo protector de nitrogeno y donde ambos sustituyentes Z son iguales y son un grupo saliente, con un compuesto de formula (6), en un solvente orgánico, para proveer el compuesto correspondiente de formula (4).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US87000306P | 2006-12-14 | 2006-12-14 | |
US11/953,262 US7893257B2 (en) | 2006-12-14 | 2007-12-10 | Process for the preparation of piperazinyl and diazepanyl benzamide derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
AR064358A1 true AR064358A1 (es) | 2009-04-01 |
Family
ID=39387172
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070105628A AR064358A1 (es) | 2006-12-14 | 2007-12-14 | Procedimiento para la preparacion de derivados benzimida piperacinilo y diazepanilo |
Country Status (33)
Country | Link |
---|---|
US (2) | US7893257B2 (es) |
EP (1) | EP2121636B1 (es) |
JP (2) | JP5385150B2 (es) |
KR (1) | KR101462891B1 (es) |
CN (1) | CN101605767A (es) |
AR (1) | AR064358A1 (es) |
BR (1) | BRPI0721088B8 (es) |
CA (2) | CA2880932A1 (es) |
CL (1) | CL2007003637A1 (es) |
CO (1) | CO6210827A2 (es) |
CR (1) | CR10928A (es) |
CY (1) | CY1118814T1 (es) |
DK (1) | DK2121636T3 (es) |
EA (1) | EA200970583A1 (es) |
EC (1) | ECSP099405A (es) |
ES (1) | ES2620818T3 (es) |
HR (1) | HRP20170621T1 (es) |
HU (1) | HUE032761T2 (es) |
IL (2) | IL199309A0 (es) |
LT (1) | LT2121636T (es) |
MX (1) | MX2009006472A (es) |
MY (1) | MY147320A (es) |
NO (1) | NO344305B1 (es) |
NZ (1) | NZ577603A (es) |
PH (1) | PH12012502236A1 (es) |
PL (1) | PL2121636T3 (es) |
PT (1) | PT2121636T (es) |
RS (1) | RS55866B1 (es) |
SG (1) | SG177207A1 (es) |
SI (1) | SI2121636T1 (es) |
TW (1) | TW200846004A (es) |
WO (1) | WO2008076685A2 (es) |
ZA (1) | ZA200904894B (es) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0324159D0 (en) | 2003-10-15 | 2003-11-19 | Glaxo Group Ltd | Novel compounds |
LT1976828T (lt) | 2005-12-29 | 2017-04-25 | Celtaxsys, Inc. | Diamino dariniai, kaip leukotrieno a4 hidrolazės inhibitoriai |
BRPI0721088B8 (pt) * | 2006-12-14 | 2021-05-25 | Janssen Pharmaceutica Nv | processo para a preparação de derivados de piperazinil e diazepanil benzamida |
AU2008294708B2 (en) | 2007-09-06 | 2012-03-15 | Glaxo Group Limited | Piperazine derivative having affinity for the histamine H3 receptor |
CA2707857C (en) | 2007-12-10 | 2016-09-13 | Novartis Ag | Spirocyclic amiloride analogues |
US8383657B2 (en) | 2007-12-21 | 2013-02-26 | Abbott Laboratories | Thiazolylidine urea and amide derivatives and methods of use thereof |
CA2905340C (en) | 2013-03-12 | 2022-05-31 | Celtaxsys, Inc. | Low dose oral formulations of acebilustat |
JP2016513681A (ja) | 2013-03-14 | 2016-05-16 | セルタクシス,インコーポレイテッド | ロイコトリエンa4加水分解酵素の阻害剤 |
JP6534650B2 (ja) | 2013-03-14 | 2019-06-26 | セルタクシス,インコーポレイテッド | ロイコトリエンa4加水分解酵素の阻害剤 |
BR112015022227A2 (pt) | 2013-03-14 | 2017-07-18 | Celtaxsys Inc | inibidores de leucotrieno a4 hidrolase |
CN108341792B (zh) * | 2018-04-28 | 2021-09-17 | 苏州莱克施德药业有限公司 | 一种Volasertib中间体1-环丙基甲基哌嗪的制备方法 |
CA3102077A1 (en) | 2018-05-31 | 2019-12-05 | Sanjeev AHUJA | Method of reducing pulmonary exacerbations in respiratory disease patients |
CN113372245B (zh) * | 2021-06-17 | 2023-01-13 | 仪征市海帆化工有限公司 | 一种n-苯甲酰基-o,o-对甲苯磺酰基-二乙醇胺的合成方法 |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2525223A (en) | 1948-05-25 | 1950-10-10 | American Cyanamid Co | Preparation of n-substituted piperazines |
DE818805C (de) | 1948-08-02 | 1951-10-29 | Rhone Poulenc Sa | Verfahren zur Herstellung von am Stickstoff durch eine Alkylgruppe monosubstituierten Piperazinen |
US3342816A (en) | 1965-06-01 | 1967-09-19 | Lilly Co Eli | Cyclopropylpiperazinoalkyl-phenothiazines |
DE3542002A1 (de) * | 1985-11-28 | 1987-06-04 | Bayer Ag | 1-cyclopropyl-6-fluor-1,4-dihydro-4-oxo-7- (1-piperazinyl)-3-chinolincarbonsaeuren, verfahren zu ihrer herstellung sowie diese enthaltende antibakterielle mittel |
DE3605005A1 (de) * | 1986-02-18 | 1987-08-20 | Basf Ag | Verfahren zur herstellung von n-methylpiperazin |
US6011029A (en) | 1996-02-26 | 2000-01-04 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
CA2235642C (en) * | 1998-05-15 | 2007-11-13 | Torcan Chemical Ltd. | Processes for preparing sildenafil |
EP1351946A2 (en) | 2000-09-01 | 2003-10-15 | Icos Corporation | Materials and methods to potentiate cancer treatment |
US6642226B2 (en) | 2001-02-06 | 2003-11-04 | Hoffman-La Roche Inc. | Substituted phenyl-piperidine methanone compounds |
DE10201240A1 (de) | 2002-01-15 | 2003-07-24 | Bayer Ag | Substituierte Alkyluracile und ihre Verwendung |
MX339074B (es) | 2002-10-23 | 2016-05-09 | Johnson & Johnson | Piperacinil y diacepanil benzamidas y benztioamidas. |
WO2005035534A1 (ja) * | 2003-10-08 | 2005-04-21 | Ono Pharmaceutical Co., Ltd. | 複素ビシクロ環および複素トリシクロ環化合物およびその医薬 |
GB0324159D0 (en) * | 2003-10-15 | 2003-11-19 | Glaxo Group Ltd | Novel compounds |
WO2006042103A2 (en) | 2004-10-05 | 2006-04-20 | Axys Pharmaceuticals, Inc. | Reversible inhibitors of cathepsin b |
CA2589748C (en) | 2004-12-24 | 2013-08-13 | Astrazeneca Ab | Heterocyclic compounds as ccr2b antagonists |
FR2885616B1 (fr) * | 2005-05-12 | 2007-06-22 | Servier Lab | Nouveaux derives de phenylpyridinylpiperazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
UA96424C2 (ru) | 2005-09-16 | 2011-11-10 | Янссен Фармацевтика Н.В. | Циклопропил амины как модуляторы н3 рецепторов гистамина |
US7795426B2 (en) * | 2005-10-31 | 2010-09-14 | Janssen Pharmaceutica Nv | Processes for the preparation of cyclopropyl-amide derivatives |
CA2628210A1 (en) * | 2005-10-31 | 2007-05-10 | Janssen Pharmaceutica N.V. | Novel processes for the preparation of piperazinyl and diazapanyl benzamide derivatives |
BRPI0721088B8 (pt) * | 2006-12-14 | 2021-05-25 | Janssen Pharmaceutica Nv | processo para a preparação de derivados de piperazinil e diazepanil benzamida |
-
2007
- 2007-12-10 BR BRPI0721088A patent/BRPI0721088B8/pt not_active IP Right Cessation
- 2007-12-10 ES ES07855037.3T patent/ES2620818T3/es active Active
- 2007-12-10 CA CA2880932A patent/CA2880932A1/en not_active Abandoned
- 2007-12-10 CA CA2672661A patent/CA2672661C/en active Active
- 2007-12-10 KR KR1020097014605A patent/KR101462891B1/ko active IP Right Grant
- 2007-12-10 US US11/953,262 patent/US7893257B2/en not_active Expired - Fee Related
- 2007-12-10 WO PCT/US2007/086936 patent/WO2008076685A2/en active Application Filing
- 2007-12-10 LT LTEP07855037.3T patent/LT2121636T/lt unknown
- 2007-12-10 DK DK07855037.3T patent/DK2121636T3/en active
- 2007-12-10 MY MYPI20092444A patent/MY147320A/en unknown
- 2007-12-10 JP JP2009541499A patent/JP5385150B2/ja not_active Expired - Fee Related
- 2007-12-10 RS RS20170402A patent/RS55866B1/sr unknown
- 2007-12-10 SI SI200731919A patent/SI2121636T1/sl unknown
- 2007-12-10 SG SG2011092046A patent/SG177207A1/en unknown
- 2007-12-10 MX MX2009006472A patent/MX2009006472A/es active IP Right Grant
- 2007-12-10 CN CNA2007800512756A patent/CN101605767A/zh active Pending
- 2007-12-10 EP EP07855037.3A patent/EP2121636B1/en active Active
- 2007-12-10 NZ NZ577603A patent/NZ577603A/en not_active IP Right Cessation
- 2007-12-10 PT PT78550373T patent/PT2121636T/pt unknown
- 2007-12-10 HU HUE07855037A patent/HUE032761T2/en unknown
- 2007-12-10 PL PL07855037T patent/PL2121636T3/pl unknown
- 2007-12-10 EA EA200970583A patent/EA200970583A1/ru unknown
- 2007-12-13 TW TW096147556A patent/TW200846004A/zh unknown
- 2007-12-14 AR ARP070105628A patent/AR064358A1/es active IP Right Grant
- 2007-12-14 CL CL200703637A patent/CL2007003637A1/es unknown
-
2009
- 2009-06-11 EC EC2009009405A patent/ECSP099405A/es unknown
- 2009-06-11 IL IL199309A patent/IL199309A0/en active IP Right Grant
- 2009-06-12 CO CO09061632A patent/CO6210827A2/es not_active Application Discontinuation
- 2009-07-10 NO NO20092634A patent/NO344305B1/no not_active IP Right Cessation
- 2009-07-13 ZA ZA200904894A patent/ZA200904894B/xx unknown
- 2009-07-14 CR CR10928A patent/CR10928A/es unknown
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2011
- 2011-01-10 US US12/987,370 patent/US8680273B2/en active Active
-
2012
- 2012-11-13 PH PH12012502236A patent/PH12012502236A1/en unknown
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2013
- 2013-08-05 JP JP2013162225A patent/JP2013241453A/ja active Pending
-
2014
- 2014-09-30 IL IL234893A patent/IL234893A/en active IP Right Grant
-
2017
- 2017-04-07 CY CY20171100420T patent/CY1118814T1/el unknown
- 2017-04-19 HR HRP20170621TT patent/HRP20170621T1/hr unknown
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