AR113794A1 - TRPC6 INHIBITORS - Google Patents
TRPC6 INHIBITORSInfo
- Publication number
- AR113794A1 AR113794A1 ARP180103108A ARP180103108A AR113794A1 AR 113794 A1 AR113794 A1 AR 113794A1 AR P180103108 A ARP180103108 A AR P180103108A AR P180103108 A ARP180103108 A AR P180103108A AR 113794 A1 AR113794 A1 AR 113794A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- cycloalkyl
- halo
- optionally substituted
- Prior art date
Links
- 102000003623 TRPC6 Human genes 0.000 title 1
- 108050001421 Transient receptor potential channel, canonical 6 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 238000000034 method Methods 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 abstract 1
- 239000005977 Ethylene Substances 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- 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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—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
- C07D213/02—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a compuestos de fórmula (1), y a sales farmacéuticamente aceptables de los mismos, en la que R¹ a R⁷, A, Y y L son tal como se definen en el presente documento. También se refiere a composiciones farmacéuticas que comprenden estos compuestos, a métodos de uso de estos compuestos en el tratamiento de diversas enfermedades y trastornos, procedimientos para preparar estos compuestos y productos intermedios útiles en estos procedimientos. Reivindicación 1: Compuesto de fórmula (1), en el que L está ausente o es metileno o etileno; Y es CH o N; A es CH o N; R¹ se selecciona del grupo que consiste en: alquilo C₁₋₆ opcionalmente sustituido con de 1 a 3 grupos seleccionados independientemente del grupo que consiste en halo, cicloalquilo C₃₋₆ y cicloalquilo OC₃₋₆; fenilo opcionalmente sustituido con de 1 a 3 grupos seleccionados independientemente del grupo que consiste en CF₃, halo, cicloalquilo C₃₋₆, cicloalquilo OC₃₋₆, alquilo OC₁₋₆ opcionalmente sustituido con de uno a tres halo; y cicloalquilo C₃₋₆ opcionalmente sustituido con de 1 a 3 grupos seleccionados independientemente del grupo que consiste en halo y alquilo C₁₋₆ opcionalmente sustituido con de 1 a 3 halo; R² se selecciona del grupo que consiste en H, alquilo C₁₋₆, OCF₃, cicloalquilo C₃₋₆, alquilo OC₁₋₆, cicloalquilo OC₃₋₆; R³ se selecciona del grupo que consiste en H, alquilo C₁₋₆, cicloalquilo C₃₋₆, cicloalquilo OC₃₋₆; en el que cada uno del alquilo C₁₋₆, cicloalquilo C₃₋₆, cicloalquilo OC₃₋₆ del grupo R³ pueden sustituirse opcionalmente con de uno a tres grupos cada uno seleccionado independientemente del grupo que consiste en halo, OH, alquilo OC₁₋₆, alquilo SC₁₋₆, N(alquilo C₁₋₆)₂; y en el que de uno a tres átomos de carbono del alquilo C₁₋₆ del grupo R³ pueden reemplazarse opcionalmente por uno o dos restos seleccionados del grupo que consiste en NH, N(alquilo C₁₋₆), O y S; R⁴ y R⁵ se seleccionan cada uno independientemente del grupo que consiste en H o alquilo C₁₋₆; R³ y R⁴ pueden, junto con el átomo al que se incorporan, unirse para formar un anillo carbociclilo de 3 a 9 miembros que puede contener opcionalmente de uno a tres heteroátomos seleccionados del grupo que consiste en N, O y S; o R³ y R⁵ pueden formar juntos un anillo bicíclico de 3 a 9 miembros que puede contener opcionalmente de uno a tres heteroátomos seleccionados del grupo que consiste en N, O y S; R⁶ se selecciona del grupo que consiste en H, alquilo C₁₋₆, CN, CF₃, OCF₃, cicloalquilo C₃₋₆, alquilo OC₁₋₆, y cicloalquilo OC₃₋₆; R⁷ se selecciona del grupo que consiste en H y alquilo OC₁₋₆; o una sal farmacéuticamente aceptable del mismo.The present refers to compounds of formula (1), and pharmaceutically acceptable salts thereof, where R¹ to R⁷, A, Y and L are as defined herein. It also relates to pharmaceutical compositions comprising these compounds, to methods of using these compounds in the treatment of various diseases and disorders, methods for preparing these compounds, and useful intermediates in these procedures. Claim 1: Compound of formula (1), in which L is absent or is methylene or ethylene; Y is CH or N; A is CH or N; R¹ is selected from the group consisting of: C₁₋₆ alkyl optionally substituted with 1 to 3 groups independently selected from the group consisting of halo, C₃₋₆ cycloalkyl, and OC₃₋₆ cycloalkyl; phenyl optionally substituted with 1 to 3 groups independently selected from the group consisting of CF₃, halo, C₃₋₆ cycloalkyl, OC₃₋₆ cycloalkyl, OC₁₋₆ alkyl optionally substituted with one to three halo; and C₃₋₆ cycloalkyl optionally substituted with 1 to 3 groups independently selected from the group consisting of halo and C₁₋₆ alkyl optionally substituted with 1 to 3 halo; R² is selected from the group consisting of H, C₁₋₆ alkyl, OCF₃, C₃₋₆ cycloalkyl, OC₁₋₆ alkyl, OC₃₋₆ cycloalkyl; R³ is selected from the group consisting of H, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, OC₃₋₆ cycloalkyl; wherein each of the C₁₋₆ alkyl, C₃₋₆ cycloalkyl, OC₃₋₆ cycloalkyl of the R³ group may be optionally substituted with one to three groups each independently selected from the group consisting of halo, OH, OC₁₋₆ alkyl, SC₁₋₆ alkyl, N (C₁₋₆ alkyl) ₂; and wherein one to three carbon atoms of the C₁₋₆ alkyl of the group R³ may optionally be replaced by one or two moieties selected from the group consisting of NH, N (C₁₋₆ alkyl), O and S; R⁴ and R⁵ are each independently selected from the group consisting of H or C₁₋₆ alkyl; R³ and R⁴ may, together with the atom to which they are incorporated, join to form a 3- to 9-membered carbocyclyl ring that may optionally contain one to three heteroatoms selected from the group consisting of N, O, and S; or R³ and R⁵ may together form a 3 to 9 membered bicyclic ring that may optionally contain one to three heteroatoms selected from the group consisting of N, O and S; R⁶ is selected from the group consisting of H, C₁₋₆ alkyl, CN, CF₃, OCF₃, C₃₋₆ cycloalkyl, OC₁₋₆ alkyl, and OC₃₋₆ cycloalkyl; R⁷ is selected from the group consisting of H and alkyl OC₁₋₆; or a pharmaceutically acceptable salt thereof.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762577883P | 2017-10-27 | 2017-10-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR113794A1 true AR113794A1 (en) | 2020-06-10 |
Family
ID=71523229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180103108A AR113794A1 (en) | 2017-10-27 | 2018-10-25 | TRPC6 INHIBITORS |
Country Status (2)
| Country | Link |
|---|---|
| AR (1) | AR113794A1 (en) |
| MA (2) | MA52370B1 (en) |
-
2018
- 2018-10-25 MA MA52370A patent/MA52370B1/en unknown
- 2018-10-25 MA MA50457A patent/MA50457B1/en unknown
- 2018-10-25 AR ARP180103108A patent/AR113794A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MA52370B1 (en) | 2022-12-30 |
| MA52370A (en) | 2022-03-30 |
| MA50457A (en) | 2020-09-02 |
| MA50457B1 (en) | 2023-06-28 |
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