AR106241A1 - Inhibidores de calicreína plasmática humana - Google Patents
Inhibidores de calicreína plasmática humanaInfo
- Publication number
- AR106241A1 AR106241A1 ARP160103021A ARP160103021A AR106241A1 AR 106241 A1 AR106241 A1 AR 106241A1 AR P160103021 A ARP160103021 A AR P160103021A AR P160103021 A ARP160103021 A AR P160103021A AR 106241 A1 AR106241 A1 AR 106241A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- nrcrd
- nhc
- optionally substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 25
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 13
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 229910003827 NRaRb Inorganic materials 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
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- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- 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
- A61P7/10—Antioedematous agents; Diuretics
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- 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
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- 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
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- 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Pyrrole Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto representado mediante la fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, en donde, independientemente para cada caso: R¹ representa -OH, -ORᶜ, -NH₂, -NHRᶜ, -NRᶜRᵈ, alquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, halo, haloalquilo, cicloalquilo, (cicloalquil)alquilo, -C(O)Rᶜ, -C(O)OH, -C(O)ORᶜ, -OC(O)Rᶜ, -C(O)NH₂, -C(O) NHRᶜ, -C(O)NRᶜRᵈ, -NHC(O)Rᶜ o -NRᶜC(O)Rᵈ; o dos casos geminales de R¹ tomados junto con el carbono al que están unidos representan -C(O)-; o dos casos vecinos o geminales de R¹ tomados juntos forman un anillo carbocíclico o heterocíclico fusionado o espirocíclico opcionalmente sustituido; W es un enlace, -C(O)NH-, -C(O)N(Rᶜ)-, -C(O)O-, -CH₂- o -C(O)-; R² representa arilo, heteroarilo, aralquilo, heteroaralquilo, cicloalquilo, heterocicloalquilo, (cicloalquil)alquilo) o (heterocicloalquil)alquilo opcionalmente sustituido; V representa arilo o heteroarilo opcionalmente sustituido; Z está ausente o representa uno o más sustituyentes seleccionados independientemente del grupo que consiste en halo, haloalquilo, -NO₂, -CN, -C(O)Rᶜ, -C(O)OH, -C(O)ORᶜ, -OC(O)Rᶜ, -C(O)NH₂, -C(O)NHRᶜ, -C(O)NRᶜRᵈ, -NHC(O)Rᶜ, -N(Rᶜ)C(O)Rᵈ, -OS(O)ₚ(Rᶜ), -NHS(O)ₚ(Rᶜ) y -NRᶜS(O)ₚ(Rᶜ); X representa -C(NH₂)-, -C(NH(Rᶜ))-, -C(NRᶜRᵈ)-, -C(NHS(O)ₚRᶜ)-, -C(NHC(O)Rᶜ)-, -C(NHC(O)NH₂)-, C(NHC(O)NHRᶜ)-, -C(NHC(O)NRᶜRᵈ)-, -C(OH)-, -C(O(alquil))-, -C(N₃)-, -C(CN)-, -C(NO₂)-, -C(S(O)ₙRᵃ)-, -C[-C(=O)Rᶜ]-, C[-C(=O)NRᶜRᵈ]-, -C[-C(=O)SRᶜ]-, -C[-S(O)Rᶜ]-, -C[-S(O)₂Rᶜ]-, -C[S(O)(ORᶜ)]-, -C[-S(O)₂(ORᶜ)]-, -C[-SO₂NRᶜRᵈ]-, -C(halógeno)-, -C(alquilo), -C((cicloalquil)alquilo), -C(alquenil)-, -C(alquinil)- o -C(aralquil)-; R³ representa arilo, heteroarilo, cicloalquilo o heterocicloalquilo opcionalmente sustituido; R³ᵃ está ausente o representa uno o más sustituyentes seleccionados independientemente del grupo que consiste en halo, hidroxi, alquilo, -CF₃, -OCF₃, alcoxi, arilo, heteroarilo, ariloxi, amino, aminoalquilo, -C(O)NH₂, ciano, -NHC(O)alquilo, -SO₂-alquilo, -SO₂NH₂, cicloalquilo, -(CH₂)ʳORᵃ, -NO₂, -(CH₂)ʳNRᵃRᵇ, -(CH₂)ʳC(O)Rᵃ, -NRᵃC(O)Rᵇ, -C(O)NRᶜRᵈ, -NRᵃC(O)NRᶜRᵈ, -C(=NRᵃ)NRᶜRᵈ, -NHC(=NRᵃ)NRᶜRᵈ, -NRᵃRᵇ, -SO₂NRᶜRᵈ, -NRᵃSO₂NRᶜRᵈ, -NRᵃSO₂-alquilo, -NRᵃSO₂Rᵃ, -S(O)ₚRᵃ, -(CF₂)ʳCF₃, -NHCH₂Rᵃ, -OCH₂Rᵃ, -SCH₂Rᵃ, -NH(CH₂)₂(CH₂)ʳRᵃ, -O(CH₂)₂(CH₂)ʳRᵃ o -S(CH₂)₂(CH₂)ʳRᵃ; Y representa un enlace; o -Y-R⁴ representa -alquilen-R⁴, -CH₂C(O)-R⁴, -CH₂NH-R⁴, -CH₂N(alquil)-R⁴, -CRᵃRᵇ-R⁴, -NH-R⁴, -NHCH₂-R⁴, -NHC(O)-R⁴, -N(alquil)-R⁴, -N(alquil)CH₂-R⁴, -N((CH₂)₂OH)-R⁴, -N((cicloalquil)alquil)R⁴, -heterociclil-R⁴, -OR⁴, -OCH₂-R⁴, -OC(O)-R⁴, -OC(O)NRᵃRᵇ, -SCH₂R⁴ o -SR⁴ opcionalmente sustituido; R⁴ representa hidrógeno, hidroxi, alquilo, cicloalquilo, (heterocicloalquil)alquilo, (cicloalquil)alquilo, -CH₂OH, -CH(alquil)OH, -CH(NH₂)CH(alquilo)₂, arilo, aralquilo, heteroarilo, heteroaralquilo, -CH₂S(alquilo), amino o ciano opcionalmente sustituido; o -(CRᵃRᵇ)ʳ(CRᵃRᵇ)ₚ- fusionado a la posición 4 del anillo que tiene Z para formar un anillo heterocíclico de 5 a 7 miembros con sustituyentes opcionales; o cuando R³ es fenilo, R⁴ puede representar -NRᵃ-fusionado a la posición orto a X en ese fenilo; cada Rᵃ y Rᵇ es independientemente H alquilo, alquenilo, alquinilo, aralquilo, (cicloalquil)alquilo, -C(=O)Rᶜ, -C(=O)ORᶜ, -C(=O)NRᶜRᵈ, -C(=O)SRᶜ, -S(O)Rᶜ, -S(O)₂Rᶜ, -S(O)(ORᶜ) o -SO₂NRᶜRᵈ; Rᶜ y Rᵈ representan, independientemente en cada caso, alquilo, alquenilo, alquinilo, haloalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, cicloalquilo, (cicloalquil)alquilo, heterocicloalquilo, (heterocicloalquil)alquilo, -C(O)alquilo o -S(O)ₚ(alquilo) opcionalmente sustituido; o Rᶜ y Rᵈ se pueden tomar juntos para formar un anillo heterocíclico opcionalmente sustituido; el resto de fórmula (2) puede representar un compuesto del grupo de fórmulas (3); r es 0, 1, 2 ó 3; n es un entero del 0 al 6; p es 0, 1 ó 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562235754P | 2015-10-01 | 2015-10-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR106241A1 true AR106241A1 (es) | 2017-12-27 |
Family
ID=58424336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160103021A AR106241A1 (es) | 2015-10-01 | 2016-09-30 | Inhibidores de calicreína plasmática humana |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US10562850B2 (es) |
| EP (2) | EP3355890B1 (es) |
| JP (2) | JP6916171B2 (es) |
| KR (1) | KR20180058815A (es) |
| CN (2) | CN114591212A (es) |
| AR (1) | AR106241A1 (es) |
| AU (2) | AU2016330926B2 (es) |
| CA (1) | CA2999164A1 (es) |
| CO (1) | CO2018004572A2 (es) |
| CY (1) | CY1124907T1 (es) |
| DK (2) | DK3355890T3 (es) |
| EA (2) | EA038492B1 (es) |
| ES (1) | ES2905401T3 (es) |
| FI (1) | FI4019022T3 (es) |
| HK (1) | HK1254865A1 (es) |
| HR (2) | HRP20220059T1 (es) |
| HU (1) | HUE057106T2 (es) |
| IL (3) | IL291268B2 (es) |
| LT (2) | LT4019022T (es) |
| MA (1) | MA43052B1 (es) |
| MD (1) | MD3355890T2 (es) |
| MX (2) | MX2018003930A (es) |
| MY (1) | MY198346A (es) |
| PH (1) | PH12018500678A1 (es) |
| PL (2) | PL3355890T3 (es) |
| PT (2) | PT3355890T (es) |
| RS (2) | RS62807B1 (es) |
| SG (1) | SG10202003705WA (es) |
| SI (2) | SI4019022T1 (es) |
| TW (2) | TWI796714B (es) |
| WO (1) | WO2017059178A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3355890B1 (en) * | 2015-10-01 | 2021-11-10 | Biocryst Pharmaceuticals, Inc. | Human plasma kallikrein inhibitors |
| WO2019028362A1 (en) * | 2017-08-04 | 2019-02-07 | Dyax Corp. | INHIBITORS OF PLASMATIC KALLIKREIN AND USES THEREOF |
| EP3841086A4 (en) | 2018-08-20 | 2022-07-27 | Achillion Pharmaceuticals, Inc. | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF MEDICAL DISORDERS RELATED TO COMPLEMENT FACTOR D |
| CN110938077B (zh) * | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
| TW202144331A (zh) * | 2020-02-13 | 2021-12-01 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
| CN116444485B (zh) * | 2023-03-30 | 2024-01-23 | 广西中医药大学 | 吡啶基取代不对称脲的非金属催化、免柱层析合成方法 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4559157A (en) | 1983-04-21 | 1985-12-17 | Creative Products Resource Associates, Ltd. | Cosmetic applicator useful for skin moisturizing |
| LU84979A1 (fr) | 1983-08-30 | 1985-04-24 | Oreal | Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux |
| LU86084A1 (fr) | 1985-09-20 | 1987-04-02 | Faco Sa | Apparei de massage electrique |
| US5102417A (en) | 1985-11-07 | 1992-04-07 | Expandable Grafts Partnership | Expandable intraluminal graft, and method and apparatus for implanting an expandable intraluminal graft |
| US4800882A (en) | 1987-03-13 | 1989-01-31 | Cook Incorporated | Endovascular stent and delivery system |
| US4820508A (en) | 1987-06-23 | 1989-04-11 | Neutrogena Corporation | Skin protective composition |
| US4886062A (en) | 1987-10-19 | 1989-12-12 | Medtronic, Inc. | Intravascular radially expandable stent and method of implant |
| US4992478A (en) | 1988-04-04 | 1991-02-12 | Warner-Lambert Company | Antiinflammatory skin moisturizing composition and method of preparing same |
| US4938949A (en) | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
| WO1990013332A1 (en) | 1989-05-11 | 1990-11-15 | Cedars-Sinai Medical Center | Stent with sustained drug delivery |
| DE69110787T2 (de) | 1990-02-28 | 1996-04-04 | Medtronic, Inc., Minneapolis, Minn. | Intraluminale prothese mit wirkstoffeluierung. |
| US5419760A (en) | 1993-01-08 | 1995-05-30 | Pdt Systems, Inc. | Medicament dispensing stent for prevention of restenosis of a blood vessel |
| US5429634A (en) | 1993-09-09 | 1995-07-04 | Pdt Systems | Biogenic implant for drug delivery and method |
| EP0719334A1 (en) * | 1993-09-14 | 1996-07-03 | Genentech, Inc. | Pharmaceutical compositions containing ecotin and homologs thereof |
| US6774278B1 (en) | 1995-06-07 | 2004-08-10 | Cook Incorporated | Coated implantable medical device |
| CA2262117A1 (en) * | 1996-08-16 | 1998-02-19 | The Dupont Merck Pharmaceutical Company | Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof |
| EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| ATE439360T1 (de) * | 2001-09-21 | 2009-08-15 | Bristol Myers Squibb Co | Lactamhaltige verbindungen und ihre derivate als faktor-xa-hemmer |
| US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| US6770729B2 (en) | 2002-09-30 | 2004-08-03 | Medtronic Minimed, Inc. | Polymer compositions containing bioactive agents and methods for their use |
| DE10301300B4 (de) * | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| US7122557B2 (en) | 2003-03-18 | 2006-10-17 | Bristol-Myers Squibb Company | Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors |
| MXPA05010444A (es) * | 2003-04-03 | 2005-11-04 | Merck Patent Gmbh | Compuestos de carbonilo. |
| DE10315377A1 (de) * | 2003-04-03 | 2004-10-14 | Merck Patent Gmbh | Carbonylverbindungen |
| US7199149B2 (en) | 2003-10-01 | 2007-04-03 | Bristol Myers Squibb Company | Monocyclic and bicyclic lactams as factor Xa inhibitors |
| DE102004014945A1 (de) * | 2004-03-26 | 2005-10-13 | Merck Patent Gmbh | Prolinylderivate |
| 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 |
| US20140378474A1 (en) | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| EP2807156A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | Aminopyridine derivatives as plasma kallikrein inhibitors |
| EA029899B1 (ru) | 2012-06-04 | 2018-05-31 | Идорсиа Фармасьютиклз Лтд | Производные бензимидазол-пролина |
| GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| CN106103453A (zh) | 2014-01-14 | 2016-11-09 | 大日本住友制药株式会社 | 缩合5‑噁唑烷酮衍生物 |
| BR112016020199A8 (pt) | 2014-03-07 | 2021-07-20 | Biocryst Pharm Inc | composto inibidor de calicreína plasmática de humano, composição farmacêutica compreendendo o referido composto, kit e seu uso |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| SG10201907699YA (en) | 2015-02-27 | 2019-09-27 | Verseon Corp | Substituted pyrazole compounds as serine protease inhibitors |
| EP3355890B1 (en) * | 2015-10-01 | 2021-11-10 | Biocryst Pharmaceuticals, Inc. | Human plasma kallikrein inhibitors |
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