AR091981A1 - Dihidropiridona p1 como inhibidores del factor xia - Google Patents
Dihidropiridona p1 como inhibidores del factor xiaInfo
- Publication number
- AR091981A1 AR091981A1 ARP130102764A ARP130102764A AR091981A1 AR 091981 A1 AR091981 A1 AR 091981A1 AR P130102764 A ARP130102764 A AR P130102764A AR P130102764 A ARP130102764 A AR P130102764A AR 091981 A1 AR091981 A1 AR 091981A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- optionally substituted
- alkyl
- heterocycle
- carbocycle
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
- C07C53/16—Halogenated acetic acids
- C07C53/18—Halogenated acetic acids containing fluorine
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
Abstract
Estos compuestos son inhibidores selectivos del factor XIa o inhibidores duales de FXIa y calicreína plasmática. También composiciones farmacéuticas que comprenden estos compuestos y a métodos para tratar trastornos tromboembólicos y/o inflamatorios mediante su uso. Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o un estereoisómero, un tautómero o una sal de aquel aceptable desde el punto de vista farmacéutico, en donde: el anillo A se selecciona independientemente de un arilo de 6 miembros y un heterociclo de 5 a 6 miembros, en donde el arilo y el heterociclo se sustituyen opcionalmente, cuando la valencia lo permite, con uno o más R⁴; el anillo B se selecciona independientemente de un arilo de 6 miembros y un heterociclo de 5 a 10 miembros, en donde el arilo y el heterociclo se sustituyen opcionalmente, cuando la valencia lo permite, con uno o más R³; el anillo C se selecciona independientemente de los compuesto de fórmula (2) y (3); - - - - es un enlace opcional; G¹ se selecciona independientemente de carbociclo C₃₋₁₀ y un heterociclo de 5 a 10 miembros, en donde el carbociclo y el heterociclo se sustituyen opcionalmente, cuando la valencia lo permite, con uno o más R⁸; X se selecciona independientemente de alquileno C₄₋₈ y alquenileno C₄₋₈, en donde el alquileno y el alquenileno se sustituyen con R¹ y R²; de manera alternativa, uno o más de los átomos de carbono del alquileno y alquenileno se pueden reemplazar por O, C=O, S(O)ₚ, S(O)ₚNH, NH y N(alquilo C₁₋₄); X¹ se selecciona independientemente de CR⁷ y N; Y se selecciona independientemente de -NH-C(O)- y -C(O)-NH-; R¹ y R² se seleccionan independientemente de H, halógeno, haloalquilo, alquilo C₁₋₆ (opcionalmente sustituido con R⁶), hidroxilo y alcoxi (opcionalmente sustituido con R⁶), y cicloalquilo C₃₋₆ opcionalmente sustituido con R⁶; opcionalmente, cuando R¹ y R² se unen al mismo átomo de carbono, forman juntos un grupo oxo o cicloalquilo C₃₋₆; opcionalmente, cuando R¹ y R² se unen a átomos de carbono adyacentes entre sí, forman juntos un enlace o un carbociclo; R³ se selecciona independientemente de H, NO₂, =O, halógeno, haloalquilo, alquilo C₁₋₄ (opcionalmente sustituido con R⁶), alquenilo C₂₋₄ (opcionalmente sustituido con R⁶), alquinilo C₂₋₄ (opcionalmente sustituido con R⁶), CN, -(CH₂)ₙ-OR⁵, -(CH₂)ₙ-NR⁵R⁵, -(CH₂)ₙ-C(O)OR⁵, -(CH₂)ₙ-NR⁹C(O)OR⁵, -(CH₂)ₙ-NR⁹C(O)R⁵, -(CH₂)ₙ-NR⁹C(N-CN)NHR⁵, -(CH₂)ₙ-NR⁹C(NH)NHR⁵, -(CH₂)ₙ-N=CR⁹NR⁵R⁵, -(CH₂)ₙ-NR⁹C(O)NR⁵R⁵, -(CH₂)ₙ-C(O)NR⁵R⁵, (CH₂)ₙ-NR⁹C(S)NR⁹C(O)R⁵, -(CH₂)ₙ-S(O)ₚR¹², -(CH₂)ₙ-S(O)ₚNR⁵R⁵, -(CH₂)ₙ-NR⁹S(O)ₚNR⁵R⁵, -(CH₂)ₙ-NR⁹S(O)ₚR¹², -(CH₂)ₙ-carbociclo C₃₋₁₀ y -(CH₂)ₙ-heterociclo de 4 a 10 miembros, en donde el carbociclo y el heterociclo se sustituyen opcionalmente con R⁶; opcionalmente, dos grupos R³ adyacentes en el carbociclo y heterociclo pueden formar un anillo opcionalmente sustituido con R⁶; R⁴ se selecciona independientemente de H, OH, NH₂, halógeno, CN, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, -CH₂OH, -CO₂H, -CH₂CO₂H, -CO₂(alquilo C₁₋₄), -C(O)NH₂, -C(O)NH(alquilo C₁₋₄), -C(O)N(alquilo C₁₋₄)₂, S(O)₂NH₂, cicloalquilo C₃₋₆, arilo y un heterociclo de 5 a 6 miembros, en donde el cicloalquilo, arilo y heterociclo se sustituyen opcionalmente con R⁶; R⁵ se selecciona independientemente de H, alquilo C₁₋₄ (opcionalmente sustituido con halógeno, hidroxilo, alcoxi, carboxi, alcoxicarbonilo, amino, amino sustituido), -(CH₂)ₙ-carbociclo C₃₋₁₀ y -(CH₂)ₙ-heterociclo de 4 a 10 miembros, en donde el carbociclo y el heterociclo se sustituyen opcionalmente con R⁶; de manera alternativa, R⁵ y R⁵, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico opcionalmente sustituido con R⁶; R⁶ se selecciona independientemente de -(CH₂)ₙ-OH, =O, -(CH₂)ₙNH₂, -(CH₂)ₙCN, halógeno, alquilo C₁₋₆, -(CH₂)ₙ-C(=O)OH, -(CH₂)ₙ-C(=O)O-alquilo C₁₋₄, -(CH₂)ₙ-O-alquilo C₁₋₄, -(CH₂)ₙ-carbociclo C₃₋₁₀, -(CH₂)ₙ-heterociclo de 4 a 10 miembros y -O-heterociclo de 4 a 10 miembros, en donde el carbociclo y el heterociclo se sustituyen opcionalmente con R¹⁰; R⁷ se selecciona independientemente de H, hidroxilo, alcoxi, halógeno, alquilo C₁₋₃; R⁸ se selecciona independientemente de H, halógeno, CN, NH₂, alquilo C₁₋₆, haloalquilo, haloalquilcarbonilamina, alquilcarbonilo, alcoxi, haloalcoxi, -(CH₂)ₙ-arilo, -(CH₂)ₙ-cicloalquilo C₃₋₆ y -(CH₂)ₙ-heterociclo de 4 - 6 miembros; opcionalmente, dos grupos R⁸ adyacentes en el carbociclo y heterociclo pueden formar un anillo opcionalmente sustituido con R¹⁰; R⁹ es H o alquilo C₁₋₆; R¹⁰ se selecciona independientemente de alquilo C₁₋₆ (opcionalmente sustituido con R¹¹), alquenilo C₂₋₆, alquinilo C₂₋₆, -(CH₂)ₙ-cicloalquilo C₃₋₆ (opcionalmente sustituido con R¹¹), -O-heterociclo de 4 a 10 miembros (opcionalmente sustituido con R¹¹), F, Cl, Br, CN, NO₂, =O, CO₂H, -(CH₂)ₙ-O-alquilo C₁₋₅, -(CH₂)ₙ-OR¹¹ y -(CH₂)ₙ-NR¹¹R¹¹; R¹¹, en cada caso, se selecciona independientemente de H, alquilo C₁₋₅, -(CH₂)ₙ-OH, cicloalquilo C₃₋₆ y fenilo, o R¹¹ y R¹¹, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico opcionalmente sustituido con alquilo C₁₋₄; R¹² es alquilo C₁₋₆ opcionalmente sustituido con R¹¹; m es un entero seleccionado independientemente de 0 y 1; n, en cada caso, es un entero seleccionado independientemente de 0, 1, 2, 3 y 4; p, en cada caso, es un entero seleccionado independientemente de 0, 1 y 2; siempre que se excluyan los compuestos de fórmula (4) en donde el anillo A se selecciona independientemente del grupo de fórmulas (5); - - - - es un enlace opcional; R¹ se selecciona independientemente de H, hidroxilo y alquilo C₁₋₄; R², en cada caso, se selecciona independientemente de H e hidroxilo; R⁴ se selecciona independientemente de H, OH, F, O-alquilo C₁₋₄ y CN; R⁸ᵃ se selecciona independientemente de H, F, Cl y Br; R⁸ᵇ se selecciona independientemente de H y F; y R⁸ᶜ se selecciona independientemente de H, F y Cl.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261679197P | 2012-08-03 | 2012-08-03 | |
US201361787081P | 2013-03-15 | 2013-03-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR091981A1 true AR091981A1 (es) | 2015-03-11 |
Family
ID=48949290
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP130102764A AR091981A1 (es) | 2012-08-03 | 2013-08-02 | Dihidropiridona p1 como inhibidores del factor xia |
Country Status (26)
Country | Link |
---|---|
US (2) | US9409908B2 (es) |
EP (1) | EP2880026B1 (es) |
JP (1) | JP6082463B2 (es) |
KR (1) | KR20150038372A (es) |
CN (2) | CN108250199B (es) |
AR (1) | AR091981A1 (es) |
AU (1) | AU2013296259A1 (es) |
BR (1) | BR112015002081A2 (es) |
CA (1) | CA2880866A1 (es) |
CY (1) | CY1119004T1 (es) |
DK (1) | DK2880026T3 (es) |
EA (1) | EA028581B1 (es) |
ES (1) | ES2623175T3 (es) |
HR (1) | HRP20170506T1 (es) |
HU (1) | HUE032622T2 (es) |
IL (1) | IL237011A0 (es) |
LT (1) | LT2880026T (es) |
MX (1) | MX361759B (es) |
PL (1) | PL2880026T3 (es) |
PT (1) | PT2880026T (es) |
RS (1) | RS55975B1 (es) |
SG (1) | SG11201500271UA (es) |
SI (1) | SI2880026T1 (es) |
TW (1) | TW201410667A (es) |
UY (1) | UY34960A (es) |
WO (1) | WO2014022767A1 (es) |
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TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子xia抑制劑之新穎巨環化合物 |
TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為xia因子抑制劑之環狀p1接合劑 |
EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
US9079929B2 (en) | 2011-10-14 | 2015-07-14 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
JP6033319B2 (ja) | 2011-10-14 | 2016-11-30 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 第XIa因子阻害剤としての置換テトラヒドロイソキノリン化合物 |
WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
RS57039B1 (sr) | 2012-10-12 | 2018-05-31 | Bristol Myers Squibb Co | Kristalni oblici inhibitora faktora xia |
US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
FR3010076B1 (fr) * | 2013-09-02 | 2016-12-23 | Centre Nat De La Rech Scient - Cnrs - | Inhibiteurs de metalloproteases, leurs procedes de preparation et leurs utilisations therapeutiques |
US9777001B2 (en) * | 2014-01-31 | 2017-10-03 | Bristol-Myers Squibb Company | Macrocycles with aromatic P2′ groups as factor xia inhibitors |
NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
EP3189047B1 (en) | 2014-09-04 | 2018-12-26 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
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BR112018008506B8 (pt) * | 2015-10-29 | 2023-12-05 | Merck Sharp & Dohme | Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos |
CN109195973A (zh) | 2016-03-02 | 2019-01-11 | 百时美施贵宝公司 | 具有因子xia抑制活性的二酰胺大环类化合物 |
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