AR045950A1 - Compuestos derivados de piperazina, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos. - Google Patents
Compuestos derivados de piperazina, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos.Info
- Publication number
- AR045950A1 AR045950A1 ARP040103493A ARP040103493A AR045950A1 AR 045950 A1 AR045950 A1 AR 045950A1 AR P040103493 A ARP040103493 A AR P040103493A AR P040103493 A ARP040103493 A AR P040103493A AR 045950 A1 AR045950 A1 AR 045950A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alk
- atom
- absent
- groups
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title abstract 4
- 239000003814 drug Substances 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000004450 alkenylene group Chemical group 0.000 abstract 4
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 3
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 abstract 2
- 239000005977 Ethylene Substances 0.000 abstract 2
- -1 acenaphthyl Chemical group 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000006642 (C1-C6) cyanoalkyl group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 208000010412 Glaucoma Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 208000001647 Renal Insufficiency Diseases 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000005530 alkylenedioxy group Chemical group 0.000 abstract 1
- 125000004419 alkynylene group Chemical group 0.000 abstract 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000005331 diazinyl group Chemical group N1=NC(=CC=C1)* 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 1
- 201000006370 kidney failure Diseases 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 239000002461 renin inhibitor Substances 0.000 abstract 1
- 229940086526 renin-inhibitors Drugs 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a compuestos derivados de piperazina, composiciones farmacéuticas que los contienen y su uso en la fabricación de medicamentos. Los compuestos son apropiados en especial como inhibidores de la renina y también para ser usados en composiciones farmacéuticas y medicamentos para el tratamiento o prevención de la hipertensión, insuficiencia cardíaca, glaucoma, infarto de miocardio, insuficiencia renal y restenosis. Reivindicación 1: Compuestos de fórmula (1) o (2) en donde: R1 es arilo o heterociclilo; R2 es fenilo, naftilo, acenaftilo, ciclohexilo, piridilo, pirimidinilo, pirazinilo, oxopiridinilo, diazinilo, triazolilo, tienilo, oxazolilo, oxadiazolilo, tiazolilo, pirrolilo, furilo, tetrazolilo o imidazolilo, radicales que pueden estar sustituidos con 1-3 grupos halógeno, hidroxi, ciano, trifluorometilo, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6,. alcoxi C1-6-alquilo C1-6, cianoalquilo C1-6, carboxialquilo C1-6, alcanoiloxi 1-6-alquilo C1-6, alcoxicarboniloxi C1-6-alquilo C1-6, alcoxicarbonilo C1-6 o grupos alcoxi C1-6 o un grupo alquilendioxi C1-6 y/o con un radical L1-T1-L2-T2-L3-T3-L4-T4-L5-U; L1, L2, L3, L4 y L5 son, se modo independiente entre sí, un enlace, alquileno C1-8, alquenileno C2-8 o alquinileno C2-8 o están ausentes; T1, T2, T3 y T4 son, de modo independiente entre sí, (a) un enlace o están ausentes, o uno de los grupos (b) -CH(O)-, (c) -CH(OR6)-, (d) -CH(NR5R6)-, (e) -CO-, (f) -CR7R8-, (g) -O- o -NR6-, (h) - S(O)0-2-, (i) -SO2NR6-, (j) -NR6SO2-, (k) -CONR6-, (l)-NR6CO-, (m) -O-CO-, (n) -CO-O-, (o) -O-CO-O-, (p) -O-CO-NR6-, (q) -N(R6)-CO-N(R6)-, (r) -N(R6)-CO-O-, (s) pirrolidinileno, piperidinileno o piperazinileno, y (t) -C(R11)(R12)-, en donde los enlaces que parten de (b)-(t) llevan a un átomo de C saturado o aromático del grupo adyacente, en caso de que el enlace parte de un heteroátomo, y en donde no más de dos grupos (b)-(f), tres grupos (g)-(h) y un grupo (i)-(t) están ausentes; R3 es H, alquilo C1-6, alquenilo C1-6, alcoxi C1-6, hidroxialquilo C1-6, alcoxi C1-6-alquilo C1-6, bencilo, oxo o un grupo R4-Z1-X1-, en donde R4 es (a) H-, (b) alquilo C1-6-, (c) alquenilo C1-6, (d) hidroxialquilo C1-6, (e) polihidroxialquilo C1-6, (f) alquil C1-6-O-alquilo C1-6-, (g) arilo, (h) heterociclilo, (i) arilalquilo, (j) heterociclilalquilo, (k) ariloxialquilo, (l) heterocicliloxialquilo, (m) (R5,R6)N-(CH2)1-3-, (n) (R5,R6)N-, (o) alquil C1-6-S(O)0-2-, (p) aril-S(O)0-2, (q) heterociclil- S(O)0-2-, (r) HO-SO3- o sus sales, (s) H2N-C(NH)-NH-, y (t) NC-, y los enlaces que parten de (n)-(t) llevan a un átomo de C del grupo adyacente y este átomo de C está saturado, en caso de que el enlace parta de un heteroátomo; Z1 es (a) un enlace, está ausente, o es uno de los grupos, (b) alquileno C1-6, (c) alquenileno C1-6-, (d)-O-, -N(R11)-, -S(O)0-2-, (e) -CO-, (f) -O-CO-, (g) -O-CO-O-, (h) -O-CO-N(R11)-, (i) -N(R11)-CO-O-, (j) -CO-N(R11)-, (k) -N(R11)-CO-, (l) -N(R11)-CO-N-(R11)-, y (m) - CH(OR9)- y los compuestos que parten de (d) y (f)-(m) llevan a un átomo de C del grupo adyacente y este átomo de C está saturado, en caso de que el enlace parta de un heteroátomo; X1 es un enlace, está ausente o es -(CH2)1-3-; R5 y R6 son H, alquilo C1-6, alquenilo C1-6, arilalquilo C1-6 o acilo o, junto con el átomo de N al que están unidos, son un anillo heterocíclico de 5 o 6 miembros que puede contener un átomo de N, O o S adicional o un grupo -SO- o -SO2-, en donde el átomo de N adicional puede estar opcionalmente sustituido con radicales alquilo C1-6; R7 y R8 son junto con el átomo de C al que están unidos, un anillo de 3-7 miembros que puede contener uno o dos átomos de -O- o -S- o grupos -SO- o -SO2-; R9 es H, alquilo C1-6, cicloalquilo C3-8, alcoxi C1-6-alquilo C1-6, acilo o arilalquilo; R10 es carboxialquilo, alcoxicarbonilalquilo, alquilo o H, R11 es H o alquilo C1-6 R12 es H o alquilo C1-6; U es H, alquilo C1-6, cicloalquilo, ciano, cicloalquilo opcionalmente sustituido, arilo o heterociclilo; Q es etileno o está ausente (fórmula 1) o es etileno o metileno (fórmula 2); X es un enlace o un grupo >CH-R11, >CR9R11, >CHOR9, >CO o >C=NOR10; Z está ausente o es alquileno C1-6, alquenileno C1-6, hidroxialquilideno C1-6, -CH-R11-CO-NR9-, -O-, -S-, -NR9, -O-Alk-, -S-Alk-, -NR9-Alk-, -Alk-O-, -Alk-S- o -Alk-NR9-, en donde Alk es alquileno C1-6; y en donde (a) en caso de que Z sea -O- o -S-, X es -CR9R11- y R2 contiene un sustituyente L1-T1-L2- T2-L3-T3-L4-T4-L5-U o R3 es un sustituyente distinto de H tal como se definió con anterioridad; (b) en caso de que Z sea -O-Alk-, -S-Alk- o -NR9-Alk-, X es -CR9R11-; y (c) en caso de que X sea un enlace, Z es alquenileno C1-6, -Alk-O-, -Alk-S- o - Alk-NR9-; y sus sales de utilidad farmacéutica.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH17252003 | 2003-10-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045950A1 true AR045950A1 (es) | 2005-11-16 |
Family
ID=34438156
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103493A AR045950A1 (es) | 2003-10-09 | 2004-09-27 | Compuestos derivados de piperazina, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos. |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR045950A1 (es) |
| TW (1) | TW200528449A (es) |
| WO (1) | WO2005037803A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1707206A1 (de) * | 2005-03-31 | 2006-10-04 | Speedel Experimenta AG | Piperazinderivate zur inhibition von Beta-Sekretase, Cathepsin D, Plasmepsin ll und HIV-Protease und zur Behandlung von Malaria, Alzheimer und AIDS |
| GB0511063D0 (en) * | 2005-05-31 | 2005-07-06 | Novartis Ag | Organic compounds |
| WO2007034445A2 (en) * | 2005-09-26 | 2007-03-29 | Actelion Pharmaceuticals Ltd | Novel piperazine derivatives as renin inhibitors for cardiovascular events and renal insufficiency |
| WO2007049224A1 (en) * | 2005-10-25 | 2007-05-03 | Actelion Pharmaceuticals Ltd | Novel hexahydro- or octahydro-cyclopenta[c]pyrrole derivatives |
| WO2008074450A2 (en) * | 2006-12-20 | 2008-06-26 | Nicox S.A. | Non-peptidic renin inhibitors nitroderivatives |
| JP5092111B2 (ja) * | 2007-02-05 | 2012-12-05 | トーアエイヨー株式会社 | ブトキシアニリン誘導体 |
| WO2009022730A1 (ja) * | 2007-08-10 | 2009-02-19 | Nippon Chemiphar Co., Ltd. | Ｐ２ｘ４受容体拮抗剤 |
| TW200932241A (en) | 2007-12-05 | 2009-08-01 | Speedel Experimenta Ag | Organic compounds |
| UY33535A (es) * | 2010-08-13 | 2011-12-01 | Biolab Sanus Farmaceutuca Limitada | Derivados de 6,7-dihidro-3h-oxazolo[3,4]pirazin-5,8-diona |
| EP2814474B1 (en) | 2012-02-15 | 2020-11-18 | The United States of America, as Represented By the Secretery, Department of Health and Human Services | Methods of treating and preventing diseases and disorders of the central nervous system |
| AR099523A1 (es) * | 2014-02-24 | 2016-07-27 | Biolab Sanus Farmacêutica Ltda | Compuestos derivados de 6,7-dihidro-3h-oxazolo[3,4-a]pirazina-5,8-diona |
| US20250214980A1 (en) | 2022-03-14 | 2025-07-03 | Slap Pharmaceuticals Llc | Multicyclic compounds |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TR199800409T1 (xx) * | 1995-09-07 | 1998-05-21 | F.Hoffmann-La Roche Ag | Kalp ve b�brek yetersizli�inin tedavii�in yeni 4-(oksialkoksifenil)-3-oksi-piperidinler |
| US6376672B1 (en) * | 1999-04-27 | 2002-04-23 | Hoffmann-La Roche Inc. | Naphthalenylmethoxypiperidines as renin inhibitors |
| US6197959B1 (en) * | 1999-04-27 | 2001-03-06 | Hoffmann-La Roche Inc. | Piperidine derivatives |
| GB0119797D0 (en) * | 2001-08-14 | 2001-10-03 | Glaxo Group Ltd | Chemical compounds |
| US20040214832A1 (en) * | 2003-04-10 | 2004-10-28 | Cuiman Cai | Piperazine derivative renin inhibitors |
-
2004
- 2004-09-27 AR ARP040103493A patent/AR045950A1/es unknown
- 2004-10-07 TW TW093130312A patent/TW200528449A/zh unknown
- 2004-10-07 WO PCT/EP2004/052466 patent/WO2005037803A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| TW200528449A (en) | 2005-09-01 |
| WO2005037803A1 (en) | 2005-04-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |