AR070206A1 - Derivados de carboxamidas azabiciclicas su preparacion y su aplicacion en terapeutica - Google Patents
Derivados de carboxamidas azabiciclicas su preparacion y su aplicacion en terapeuticaInfo
- Publication number
- AR070206A1 AR070206A1 ARP090100166A ARP090100166A AR070206A1 AR 070206 A1 AR070206 A1 AR 070206A1 AR P090100166 A ARP090100166 A AR P090100166A AR P090100166 A ARP090100166 A AR P090100166A AR 070206 A1 AR070206 A1 AR 070206A1
- Authority
- AR
- Argentina
- Prior art keywords
- cycloalkyl
- alkylene
- alkyl
- aryl
- group
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 24
- 125000002947 alkylene group Chemical group 0.000 abstract 24
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 23
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 abstract 13
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 12
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 229910052757 nitrogen Inorganic materials 0.000 abstract 11
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 11
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 10
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 9
- 125000001072 heteroaryl group Chemical group 0.000 abstract 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000005529 alkyleneoxy group Chemical group 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 4
- -1 C (O) NR4R5 Chemical group 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 150000003573 thiols Chemical class 0.000 abstract 3
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 125000004001 thioalkyl group Chemical group 0.000 abstract 2
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical group C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 abstract 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 1
- XQFRJNBWHJMXHO-RRKCRQDMSA-N IDUR Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(I)=C1 XQFRJNBWHJMXHO-RRKCRQDMSA-N 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 102000003566 TRPV1 Human genes 0.000 abstract 1
- 101150016206 Trpv1 gene Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000005110 aryl thio group Chemical group 0.000 abstract 1
- XYOVOXDWRFGKEX-UHFFFAOYSA-N azepine Chemical compound N1C=CC=CC=C1 XYOVOXDWRFGKEX-UHFFFAOYSA-N 0.000 abstract 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000005366 cycloalkylthio group Chemical group 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- AEOCXXJPGCBFJA-UHFFFAOYSA-N ethionamide Chemical compound CCC1=CC(C(N)=S)=CC=N1 AEOCXXJPGCBFJA-UHFFFAOYSA-N 0.000 abstract 1
- 230000002496 gastric effect Effects 0.000 abstract 1
- 125000005368 heteroarylthio group Chemical group 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 150000003951 lactams Chemical class 0.000 abstract 1
- 238000002483 medication Methods 0.000 abstract 1
- 230000002503 metabolic effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 230000007170 pathology Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 abstract 1
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
- C07D471/04—Ortho-condensed systems
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- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
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- 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
- A61P17/04—Antipruritics
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- 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
- A61P17/06—Antipsoriatics
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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
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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
- A61P25/24—Antidepressants
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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
- 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
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- 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
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- 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
- A61P27/14—Decongestants or antiallergics
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Biotechnology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Procedimiento de preparacion, compuestos intermediarios, medicamentos, composicion farmacéutica y su uso para tratar patología donde estén implicados receptores de tipo TRPV1, dolor inflamacion, trastornos metabolicos, urologicos, ginecologicos, gastrointestinales, respiratorios, soriasis herpes etc. Reivindicacion 1: Compuesto que responde a la formula (1) en la que X1, X2, X3 y X4 representan, independientemente el uno del otro, un átomo de nitrogeno o un grupo C-R1; entendiéndose que cuando uno de X1, X2, X3 y X4 representa un átomo de nitrogeno, los demás corresponden a un grupo C-R1; Z1, Z2, Z3 y Z4 representan, independientemente el uno del otro, un átomo de nitrogeno, un átomo de carbono o un grupo C-R2, uno, al menos, de Z1, Z2, Z3 y Z4 corresponde a un átomo de nitrogeno y uno de Z1, Z2, Z3 y Z4, corresponde a un átomo de carbono, estando unido al átomo de nitrogeno de la amida o de la tioamida de formula (1); Ra y Rb forman junto con los átomos de carbono a los que están unidos un ciclo de cinco eslabones, conteniendo este ciclo un átomo de nitrogeno y átomos de carbono, estando este ciclo parcialmente saturado o insaturado y estando sustituido opcionalmente con uno o varios sustituyentes R3; W representa un átomo de oxígeno o de azufre; n es igual a 0, 1, 2 o 3; Y representa un arilo o un heteroarilo sustituido opcionalmente con uno o varios grupos elegidos entre un átomo de halogeno, un grupo alquilo C1-6, cicloalquilo 3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, hidroxi, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquileno C1-6-O-, fluoroalcoxi C1-6, ciano, C(O)NR4R5, nitro, NR4R5, tioalquilo C1-6, tiol, -S(O)-alquilo C1-6, -S(O)2-alquilo C1-6, SO2NR4R5, NR6C(O)R7, NR6SO2R5, C(O)NR4R5, OC(O)NR4R5, -Si-(alquil C1-6)3, -SF5, arilo-alquileno C1-5 o arilo, heteroaril-alquileno C1-5 o heteroarilo; estando los grupos alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquileno C1-6-O- sustituidos opcionalmente con un grupo hidroxi, alcoxi C1-6 o NR4R5, estando los grupos arilo y heteroarilo sustituidos opcionalmente con uno o varios sustituyentes R9 idénticos o diferentes el uno del otro; R1 se elige entre un átomo de hidrogeno, un átomo de halogeno, alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, ariloxi-alquilo C1-6, heteroariloxi-alquilo C1-6, aril-alquilenoxi C1-3-alquilo C1-6, heteroaril-alquilenoxi C1-3-alquilo C1-6, ariltio-alquilo C1-6, heteroariltio-alquilo C1-6, arilaIquileno C1-3-tio-alquilo C1-6, heteroaril-alquileno C1-3-tio-alquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquilenoxi C1-3, fluoroalcoxi C1-6, ciano, C(O)NR4R5, nitro, NR4R5, tioalquilo C1-6, cicloalquiltio C3-7, cicloalquil C3-7-alquileno C1-3-tio, -S(O)-alquilo C1-6, -S(O)-cicloalquilo C3-7, -S(O)-alquileno C1-3-cicloalquilo C3-7, alquilo C1-6-S(O)2, fluoroalquiIo C1-6-S(O)2, cicIoalquil C3-7-S(O)2, cicloalquil C3-7-alquileno C1-3-S(O)2, SO2NR4R5, -Si-(alquil C1-6)3, -SF5, NR6C(O)R7, NR6SO2R8, C(O)NR4R5, OC(O)NR4R5, arilo, heteroarilo, aril-alquileno C1-5, heteroaril-alquileno C1-5, ariloxi, ariltio, heteroariloxi o heteroariltio; estando los grupos heteroarilo o arilo sustituidos opcionalmente con uno o varios sustituyentes R9, idénticos o diferentes el uno del otro; R2 representa un átomo de hidrogeno, un átomo de halogeno, un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquileno C1-3-O-, hidroxi, tiol, fluoroalcoxi C1-6; R3, representa, cuando está unido a un átomo de carbono, un átomo de hidrogeno, un grupo hidroxi, tiol, alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquilenoxi C1-3; alcoxi C1-6-alquileno C1-3, cicloalquiloxi C3-7-alquileno C1-3, cicloalquil C3-7-alquilenoxi C1-3-alquileno C1-3, C(O)NR4R5, C(O)O-alquilo C1-6, CO2H, o un grupo oxo o tio; pudiendo estar los grupos alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7- alquilenoxi C1-3, alcoxi C1-6-alquileno C1-3, cicloalquiloxi C3-7-alquileno C1-3, cicloalquil C3-7-alquilenoxi C1-3-alquileno C1-3 sustituidos con un grupo hidroxi, alcoxi C1-6 o NR4R5; o R3, representa, cuando está unido a un átomo de nitrogeno, un átomo de hidrogeno, un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, arilo-C(O)-, alquilo C1-6-C(O)-, cicloalquil C3-7-C(O)-, cicloalquil C3-7-alquileno C1-3-C(O)-, fluoroalquilo C1-6-C(O)-, arilo-S(O), alquilo C1-6-S(O)-, fluoroalquilo -C1-6-(O)-, arilo-S(O)2-, alquilo C1-6-S(O)2, fluoroalquilo C1-6-S(O)2-, cicloalquil C3-7-S(O)2, cicloalquil C3-7-alquileno C1-3-S(O)2, alquilo C1-6-O-C(O)-, arilo-alquilo C1-3-O-C(O)-, cicloalquil C3-7-O-C(O)-, cicloalquil C3-7-alquileno C1-3-O-C(O)-, fluoroalquilo C1-6-O-C(O)-, arilo-O-C(O)-, heteroaril-O-C(O)-, heteroarilo o arilo; estando los grupos heteroarilo y arilo sustituidos opcionalmente con uno o varios sustituyentes R9; pudiendo estar los grupos alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, sustituidos con un grupo hidroxi, alcoxi C1-6 o NR4R5; R4 y R5, representan, independientemente el uno del otro, un átomo de hidrogeno o un grupo alquilo C1-6, cicloalquilo C3-7, cicIoalquil C3-7-alquileno C1-3, arilo-alquileno C1-5 o arilo, o R4 y R5 forman junto con el átomo de nitrogeno al que están unidos un grupo azetidina, pirrolidina, piperidina, azepina, morfolina, tiomorfolina, piperacina, homopiperacina estando el grupo NR4R5 sustituido opcionalmente con un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, arilo-alquileno C 1-6, arilo, heteroarilo, arilo-S(O)2, aIquilo C1-6-S(O)2-, fluoroalquilo C1-6-S(O)2, cicloalquil C3-7-S(O)2-, cicloalquil C3-7-alquileno C1-3S(O)2-, arilo-C(O)-, alquilo C1-6-C(O)-, cicloalquil C3-7-C(O)-, cicloalquil C3-7-alquileno C1-3-C(O)-, fluoroalquilo C1-6-C(O)-, hidroxi, alquiloxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquilenoxi C1-3, fluoroalquilo C1-6, ariloxi-alquileno C1-6, ariloxi, heteroariloxi-alquileno C1-6, heteroariloxi; R6 y R7 representan, independientemente el uno del otro, un átomo de hidrogeno, un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, arilo-alquileno C1-6 o arilo; estando el grupo arilo sustituido opcionalmente con uno o varios sustituyentes elegidos entre un átomo de halogeno, un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquilenoxi C1-3, fluoroalcoxi C1-6, nitro o ciano; o R6 y R7 forman juntos una lactama de 4 a 7 eslabones que comprende el átomo de nitrogeno y el grupo C(O) a los que están unidos; R8 representa un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, arilo-alquileno C1-6 o arilo; estando el grupo arilo sustituido opcionalmente con uno o varios sustituyentes elegidos entre un átomo de halogeno, un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, fluoroalquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquilenoxi C1-3, fluoroalcoxi C1-6, nitro o ciano; o R6 y R8 forman juntos una sultama de 4 a 7 eslabones que comprende el átomo de nitrogeno y el grupo S(O)2 a los que están unidos; R9 representa un átomo de halogeno, un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil-C3-7-alquileno C1-3, fluoroalquilo C1-6, alcoxi C1-6, cicloalquiloxi C3-7, cicloalquil C3-7-alquilenoxi C1-3, fluoroalcoxi C1-6; estando estos grupos sustituidos opcionalmente con un grupo OH, alcoxi C1-6 o NR4R5 o bien R9 representa un grupo nitro, ciano o NR4R5; pudiendo estar el o los átomos de azufre del compuesto de formula general (1) en forma oxidada; pudiendo estar el o los átomos de nitrogeno del compuesto de formula general (1) en forma oxidada en el estado de base o de sal de adicion a un ácido, así como en el estado de hidrato o de solvato. Reivindicacion 14: Compuesto de la formula general (2A), (2B), (2C), (2D), (2E), (2F), (2G) o (2H).
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| EA027068B1 (ru) | 2013-04-03 | 2017-06-30 | Янссен Сайенсиз Айрлэнд Юси | Производные n-фенилкарбоксамида и их применение в качестве лекарственных препаратов для лечения гепатита b |
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| EA035500B1 (ru) | 2013-05-17 | 2020-06-25 | Янссен Сайенсиз Айрлэнд Юси | Производные сульфамоилтиофенамида и их применение в качестве медикаментов для лечения гепатита b |
| DK3024819T3 (en) | 2013-07-25 | 2018-06-06 | Janssen Sciences Ireland Uc | GLYOXAMIDE-SUBSTITUTED PYRROLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICINES FOR TREATING HEPATITIS B |
| KR102290189B1 (ko) | 2013-10-23 | 2021-08-17 | 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 | 카르복스아미드 유도체 및 ｂ형 간염 치료용 의약으로서의 이의 용도 |
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| US10875876B2 (en) | 2015-07-02 | 2020-12-29 | Janssen Sciences Ireland Uc | Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B |
| WO2017024018A1 (en) | 2015-08-05 | 2017-02-09 | Vitae Pharmaceuticals, Inc. | Modulators of ror-gamma |
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| FR2926555B1 (fr) | 2008-01-22 | 2010-02-19 | Sanofi Aventis | Derives bicycliques de carboxamides azabicycliques, leur preparation et leur application en therapeutique |
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