MX2012004148A - Compuestos de dioxido de iminotiadiazina como inhibidores de la enzima de disociacion de la proteina precursora amiloide en el sitio beta, composiciones, y su uso. - Google Patents
Compuestos de dioxido de iminotiadiazina como inhibidores de la enzima de disociacion de la proteina precursora amiloide en el sitio beta, composiciones, y su uso.Info
- Publication number
- MX2012004148A MX2012004148A MX2012004148A MX2012004148A MX2012004148A MX 2012004148 A MX2012004148 A MX 2012004148A MX 2012004148 A MX2012004148 A MX 2012004148A MX 2012004148 A MX2012004148 A MX 2012004148A MX 2012004148 A MX2012004148 A MX 2012004148A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- sub
- compounds
- iminothiadiazine dioxide
- dioxide compounds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- IBIDQDPPONSSPQ-UHFFFAOYSA-N 1-imino-2H-thiadiazine Chemical compound N=S1NN=CC=C1 IBIDQDPPONSSPQ-UHFFFAOYSA-N 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 230000007170 pathology Effects 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/549—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 sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
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- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
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- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
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- C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
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- 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
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- 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
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- C07D239/12—Nitrogen atoms not forming part of a nitro radical
- C07D239/14—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
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Abstract
En sus muchas modalidades, la presente invención proporciona ciertos compuestos de dióxido de iminotiadiazina, incluyendo los compuestos de la Fórmula (I): (ver fórmula (I)) e incluyen sus estereoisómeros, y las sales farmacéuticamente aceptables de dichos compuestos, estereoisómeros, donde cada uno de R1, R2, R3, R4, R5, R9, el anillo A, el anillo B, m, n, p, -L1-,-L2-, y -L3- se selecciona independientemente y según lo definido en esta invención; se ha descubierto, sorprendentemente, que los compuestos de dióxido de iminotiadiazina novedosos de la invención exhiben propiedades las cuales se espera que los convierta en ventajosos como inhibidores de BACE y/o para el tratamiento y prevención de diversas patologías relacionadas con la producción de ß-amiloides ("Aß"); también se describen composiciones farmacéuticas que comprenden uno o más de dichos compuestos (solos y en combinación con uno o más otros agentes activos), y métodos para su preparación y uso en el tratamiento de patologías asociadas con la proteína amiloide beta (Aß), incluyendo la enfermedad de Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24968509P | 2009-10-08 | 2009-10-08 | |
| PCT/US2010/051553 WO2011044181A1 (en) | 2009-10-08 | 2010-10-06 | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012004148A true MX2012004148A (es) | 2012-05-08 |
Family
ID=43857101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012004148A MX2012004148A (es) | 2009-10-08 | 2010-10-06 | Compuestos de dioxido de iminotiadiazina como inhibidores de la enzima de disociacion de la proteina precursora amiloide en el sitio beta, composiciones, y su uso. |
Country Status (40)
| Country | Link |
|---|---|
| US (6) | US8729071B2 (es) |
| EP (2) | EP2485736B1 (es) |
| JP (4) | JP5592494B2 (es) |
| KR (3) | KR101759856B1 (es) |
| CN (2) | CN104744403A (es) |
| AR (1) | AR078534A1 (es) |
| AU (1) | AU2010303591B2 (es) |
| BR (1) | BR112012008014B1 (es) |
| CA (1) | CA2774579C (es) |
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