ZA201803367B - Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders - Google Patents

Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders

Info

Publication number
ZA201803367B
ZA201803367B ZA2018/03367A ZA201803367A ZA201803367B ZA 201803367 B ZA201803367 B ZA 201803367B ZA 2018/03367 A ZA2018/03367 A ZA 2018/03367A ZA 201803367 A ZA201803367 A ZA 201803367A ZA 201803367 B ZA201803367 B ZA 201803367B
Authority
ZA
South Africa
Prior art keywords
tlr7
polycyclic
antagonists
treatment
immune disorders
Prior art date
Application number
ZA2018/03367A
Other languages
English (en)
Inventor
A Sherer Brian
Brugger Nadia
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of ZA201803367B publication Critical patent/ZA201803367B/en

Links

Classifications

    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine 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
    • A61K31/495—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
    • A61K31/505—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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—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
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
ZA2018/03367A 2015-12-17 2018-05-21 Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders ZA201803367B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562268765P 2015-12-17 2015-12-17
US201662353603P 2016-06-23 2016-06-23
PCT/US2016/067112 WO2017106607A1 (en) 2015-12-17 2016-12-16 Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders

Publications (1)

Publication Number Publication Date
ZA201803367B true ZA201803367B (en) 2021-08-25

Family

ID=58191545

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2018/03367A ZA201803367B (en) 2015-12-17 2018-05-21 Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders

Country Status (29)

Country Link
US (7) US10399957B2 (enExample)
EP (3) EP3889146A1 (enExample)
JP (3) JP6882299B2 (enExample)
KR (2) KR20250043596A (enExample)
CN (2) CN113603675A (enExample)
AU (3) AU2016371014B2 (enExample)
CA (1) CA3005766A1 (enExample)
CL (1) CL2018001624A1 (enExample)
DK (1) DK3889145T3 (enExample)
ES (2) ES2981114T3 (enExample)
FI (1) FI3889145T3 (enExample)
HR (1) HRP20240355T1 (enExample)
HU (1) HUE066591T2 (enExample)
IL (4) IL259751B (enExample)
LT (1) LT3889145T (enExample)
MX (2) MX2021006804A (enExample)
MY (2) MY196319A (enExample)
NZ (1) NZ742476A (enExample)
PH (1) PH12018501068A1 (enExample)
PL (1) PL3889145T3 (enExample)
PT (1) PT3889145T (enExample)
RS (1) RS65319B1 (enExample)
SG (2) SG11201804170RA (enExample)
SI (1) SI3889145T1 (enExample)
SM (1) SMT202400141T1 (enExample)
TW (3) TWI886474B (enExample)
UA (1) UA124802C2 (enExample)
WO (1) WO2017106607A1 (enExample)
ZA (1) ZA201803367B (enExample)

Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2021006804A (es) * 2015-12-17 2023-01-13 Merck Patent Gmbh Antagonistas policiclicos del receptor 7/8 tipo toll (tlr7/8) y uso de los mismos en el tratamiento de trastornos inmunitarios.
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
RS63776B1 (sr) 2016-07-14 2022-12-30 Crinetics Pharmaceuticals Inc Modulatori somatostatina i njihove upotrebe
RU2758686C2 (ru) * 2016-08-08 2021-11-01 Мерк Патент Гмбх Антагонисты tlr7/8 и их применение
MA46535A (fr) 2016-10-14 2019-08-21 Prec Biosciences Inc Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b
WO2018089695A1 (en) * 2016-11-11 2018-05-17 Dynavax Technologies Corporation Toll-like receptor antagonist compounds and methods of use
CN110944990B (zh) 2017-07-18 2024-06-18 默克专利股份公司 Tlr7/8拮抗剂及其用途
CN117659025A (zh) * 2017-10-30 2024-03-08 科罗拉多州立大学董事会法人团体 Toll样受体8（tlr8）特异性拮抗剂及其制备方法和用途
CA3086172A1 (en) * 2017-12-19 2019-06-27 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof
WO2019123339A1 (en) 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
AU2018392213B2 (en) 2017-12-20 2021-03-04 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein
CN111699187A (zh) 2018-02-12 2020-09-22 豪夫迈·罗氏有限公司 用于治疗和预防病毒感染的新的砜化合物和衍生物
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ， インコーポレイテッド Ｈｂｖ複製阻害剤としての置換ピロリジン化合物
EP3774883A1 (en) 2018-04-05 2021-02-17 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis b virus protein x
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
TW202014193A (zh) 2018-05-03 2020-04-16 捷克科學院有機化學與生物化學研究所 包含碳環核苷酸之2’3’－環二核苷酸
WO2019233941A1 (en) * 2018-06-05 2019-12-12 F. Hoffmann-La Roche Ag Tetrahydro-1 h-pyrazino[2,1 -ajisoindolylquinoline compounds for the treatment of autoimmune disease
US11713327B2 (en) 2018-06-12 2023-08-01 Hoffmann-La Roche Inc. Heteroaryl heterocyclyl compounds for the treatment of autoimmune disease
CN112585134A (zh) * 2018-06-13 2021-03-30 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的吡啶基杂环基化合物
BR112020026681A2 (pt) 2018-06-27 2021-04-06 Bristol-Myers Squibb Company Compostos naftiridinona substituídos úteis como ativadores de célula t
ES2950007T3 (es) 2018-06-27 2023-10-04 Bristol Myers Squibb Co Compuestos de naftiridinona útiles como activadores de células T
EP3818052A1 (en) * 2018-07-06 2021-05-12 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
JPWO2020017569A1 (ja) * 2018-07-17 2021-12-02 日本ケミファ株式会社 Ｔ型カルシウムチャネル阻害剤
JP7366994B2 (ja) * 2018-07-23 2023-10-23 エフ． ホフマン－ラ ロシュ アーゲー 自己免疫疾患治療用の新規ピペラジン化合物
MX2021000093A (es) * 2018-07-31 2021-03-25 Merck Patent Gmbh Antagonistas del receptor de tipo toll 7/8 (tlr7/8) y usos de los mismos.
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
WO2020043271A1 (en) 2018-08-28 2020-03-05 F. Hoffmann-La Roche Ag Novel pyrrolidinyl amide compounds for the treatment of autoimmune disease
US11639352B2 (en) 2018-09-04 2023-05-02 Hoffman-La Roche Inc. Benzothiazole compounds for the treatment of autoimmune diseases
WO2020048595A1 (en) * 2018-09-06 2020-03-12 F. Hoffmann-La Roche Ag Novel cyclic amidine compounds for the treatment of autoimmune disease
WO2020048596A1 (en) * 2018-09-06 2020-03-12 F. Hoffmann-La Roche Ag Novel pyrazolopyridine compounds for the treatment of autoimmune disease
JP2022501326A (ja) * 2018-09-07 2022-01-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 自己免疫疾患の治療のための新規ピロリジンアミン化合物
CN112673007A (zh) * 2018-09-11 2021-04-16 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的吡唑并吡啶胺化合物
EP3623369B1 (en) 2018-09-12 2023-10-25 F. Hoffmann-La Roche AG Novel morpholinyl amine compounds for the treatment of autoimmune disease
US20210395239A1 (en) * 2018-09-27 2021-12-23 Hoffmann-La Roche Inc. Heterocyclyl compounds for the treatment of autoimmune disease
TWI721624B (zh) 2018-10-31 2021-03-11 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
CA3117556A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds as hpk1 inhibitors
CN109516925B (zh) * 2018-10-31 2021-07-16 陕西慧康生物科技有限责任公司 一种谷氨酸-1-甲酯-5-叔丁酯的合成方法
US20210300924A1 (en) * 2018-11-09 2021-09-30 Hoffmann-La Roche Inc. 5-[6-[[3-(4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)azetidin-1-yl]methyl]morpholin-4-yl]quinoline-8-carbonitrile derivatives and similar compounds as tlr7-9 antagonists for treating systemic lupus erythematosus
CN109369571A (zh) * 2018-12-04 2019-02-22 无锡市赛乐新材料科技有限公司 一种含氟取代的7-溴-4-醛基苯并噻二唑及其合成方法
US10689360B1 (en) 2019-01-30 2020-06-23 Insilico Medicine Ip Limited TLR inhibitors
US11008303B2 (en) 2019-01-30 2021-05-18 Insilico Medicine Ip Limited TLR 9 inhibitors
US11807622B2 (en) 2019-01-30 2023-11-07 Insilico Medicine Ip Limited TLR 9 inhibitors
JP7637328B2 (ja) 2019-02-07 2025-02-28 ベイジーン リミテッド Ｔｌｒ７アゴニストとしてのイミダゾ［２，１－ｆ］［１，２，４］トリアジン－４－アミン誘導体
WO2020178770A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
JP7350871B2 (ja) 2019-03-07 2023-09-26 インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． ２’３’－環状ジヌクレオチドおよびそのプロドラッグ
EP3935065A1 (en) 2019-03-07 2022-01-12 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
JP2022081710A (ja) * 2019-03-29 2022-06-01 ユーティアイ リミテッド パートナーシップ 関節リウマチを治療するためのｔ型カルシウムチャネル阻害剤の使用
WO2020203609A1 (ja) * 2019-03-29 2020-10-08 日本ケミファ株式会社 掻痒を治療するためのｔ型カルシウムチャネル阻害剤の使用
SG11202110401WA (en) * 2019-04-09 2021-10-28 Hoffmann La Roche Hexahydro-1h-pyrazino[1,2-a]pyrazine compounds for the treatment of autoimmune disease
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
CN112094224B (zh) * 2019-06-18 2022-08-26 浙江医药股份有限公司新昌制药厂 一种带保护基的3-取代-5-氨基哌啶的制备方法
EP4017476A1 (en) 2019-08-19 2022-06-29 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
CN112430208A (zh) * 2019-08-26 2021-03-02 东莞市东阳光仿制药研发有限公司 一种pf-06651600中间体的制备方法
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
EP4028125A1 (en) * 2019-09-10 2022-07-20 F. Hoffmann-La Roche AG Novel quinoline compounds for the treatment of autoimmune disease
EP4031539A1 (en) 2019-09-16 2022-07-27 F. Hoffmann-La Roche AG Piperidinyl amine compounds for the treatment of autoimmune disease
MY208114A (en) 2019-09-30 2025-04-16 Gilead Sciences Inc Hbv vaccines and methods treating hbv
US11884647B2 (en) 2019-10-18 2024-01-30 The Regents Of The University Of California Compounds and methods for targeting pathogenic blood vessels
WO2021084022A1 (en) * 2019-10-31 2021-05-06 F. Hoffmann-La Roche Ag Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease
EP4058452B1 (en) * 2019-11-12 2025-07-09 F. Hoffmann-La Roche AG Hydropyrazino[1,2-b]isoquinoline compounds for the treatment of autoimmune disease
CN114728976B (zh) * 2019-11-19 2024-08-16 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的氢-1H-吡咯并[1,2-a]吡嗪化合物
WO2021099285A1 (en) * 2019-11-19 2021-05-27 F. Hoffmann-La Roche Ag Triazatricycle compounds for the treatment of autoimmune disease
WO2021099406A1 (en) * 2019-11-20 2021-05-27 F. Hoffmann-La Roche Ag Spiro(isobenzofuranazetidine) compounds for the treatment of autoimmune disease
PH12022551012A1 (en) * 2019-11-26 2023-03-06 Hoffmann La Roche 1,8-naphthyridin-2-one compounds for the treatment of autoimmune disease
PH12022551260A1 (en) 2019-11-28 2024-06-03 Bayer Ag Substituted aminoquinolones as dgkalpha inhibitors for immune activation
EP4069693B1 (en) 2019-12-03 2024-03-20 F. Hoffmann-La Roche AG Hydropyrido[1,2-alpha]pyrazine compounds for the treatment of autoimmune diseases
CN116057068A (zh) 2019-12-06 2023-05-02 精密生物科学公司 对乙型肝炎病毒基因组中的识别序列具有特异性的优化的工程化大范围核酸酶
CN114846014B (zh) 2019-12-18 2025-06-13 英特维特国际股份有限公司 包含氮杂吲哚结构的驱虫化合物
BR112022012222A2 (pt) 2019-12-23 2022-09-13 Bristol Myers Squibb Co Derivados de piperazina substituídos úteis como ativadores de células t
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
WO2021188959A1 (en) 2020-03-20 2021-09-23 Gilead Sciences, Inc. Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
CN116018139A (zh) * 2020-05-14 2023-04-25 默克医疗保健股份两合公司 用于冠状病毒感染治疗的tlr7/8拮抗剂
US20230301981A1 (en) * 2020-06-15 2023-09-28 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof
US20240350492A1 (en) 2020-07-10 2024-10-24 Ting Therapeutics Llc Methods for the Prevention and Treatment of Hearing Loss
WO2022022489A1 (zh) * 2020-07-27 2022-02-03 江苏恒瑞医药股份有限公司 吲哚稠环类衍生物、其制备方法及其在医药上的应用
WO2022028389A1 (zh) * 2020-08-03 2022-02-10 江苏恒瑞医药股份有限公司 稠三环类衍生物、其制备方法及其在医药上的应用
CN114057754B (zh) * 2020-08-07 2023-05-16 江苏恒瑞医药股份有限公司 含氮桥环类衍生物、其制备方法及其在医药上的应用
CA3191084A1 (en) 2020-09-09 2022-03-17 Gerald Burke Formulations of a somatostatin modulator
WO2022067462A1 (en) * 2020-09-29 2022-04-07 Beigene (Beijing) Co., Ltd. Process for preparing inhibitors of kras g12c
KR102513463B1 (ko) * 2020-11-26 2023-03-29 주식회사 에스앤케이테라퓨틱스 엔도솜 톨-유사 수용체를 제어하는 신규 소분자 화합물 및 이를 이용한 자가면역질환 치료제
TW202227442A (zh) 2020-11-26 2022-07-16 大陸商江蘇恆瑞醫藥股份有限公司 稠合三環化合物、其製備方法及其在醫藥上的應用
CN115109032B (zh) * 2021-03-18 2023-09-05 成都百裕制药股份有限公司 喹啉衍生物及其在医药上的应用
AU2022257039A1 (en) 2021-04-16 2023-10-05 Gilead Sciences, Inc. Thienopyrrole compounds
TW202348237A (zh) 2021-05-13 2023-12-16 美商基利科學股份有限公司 TLR8調節化合物及抗HBV siRNA療法之組合
JP7686091B2 (ja) 2021-06-23 2025-05-30 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
CA3222277A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
EP4359389A1 (en) 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
AU2022298639C1 (en) 2021-06-23 2025-07-17 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2023039464A1 (en) 2021-09-10 2023-03-16 Gilead Sciences, Inc. Thienopyrrole compounds
CN115160296B (zh) * 2022-08-08 2024-05-28 西安市第五医院 一种n-取代喹啉-4-胺类化合物及其制备、药物组合物和应用
CN115650881B (zh) * 2022-09-06 2025-01-17 浙江医药股份有限公司新昌制药厂 一种利用微反应器合成喹诺酮类化合物中间体的工艺方法
WO2024153063A1 (zh) 2023-01-18 2024-07-25 苏州科睿思制药有限公司 Enpatoran的晶型及其制备方法和用途
WO2025201636A1 (en) 2023-03-31 2025-10-02 Syngenta Crop Protection Ag Pesticidally-active 2,2-dihalocyclopropyl compounds
WO2025214612A1 (en) 2023-04-14 2025-10-16 Syngenta Crop Protection Ag Pesticidally-active 2,2-dihalocyclopropyl compounds
WO2025032195A1 (en) 2023-08-09 2025-02-13 Merck Patent Gmbh Crystalline form h1 of 5-((3r,55)-3-amino-5- trifluoromethyl-piperidin-1-yl)-quinoline-8-carbonitrile hemihydrate
WO2025032197A1 (en) 2023-08-09 2025-02-13 Merck Patent Gmbh Crystalline form of 5-((3r,5s)-3-amino-5-trifluoromethyl-piperidin-1-yl)-quinoline-8-carbonitrile
WO2025032190A1 (en) 2023-08-09 2025-02-13 Merck Patent Gmbh Crystalline form a1 of 5-((3r,55)-3-amino-5- trifluoromethyl-piperidin-1-yl)-quinoline-8-carbonitrile hcl
WO2025160132A1 (en) * 2024-01-23 2025-07-31 Maplight Therapeutics, Inc. Gpr6 inverse agonists
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240244A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection
US20250345389A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1020252A (en) * 1911-04-26 1912-03-12 Arthur H Bell Brooder.
US1016829A (en) * 1911-05-19 1912-02-06 Abraham Hurwitz Device for setting pallet-jewels.
US1227293A (en) * 1914-04-10 1917-05-22 Charles H Morison Safety-catch for cuff-buttons.
US1271680A (en) * 1918-01-15 1918-07-09 Emanuel W Dunn Heater.
US1367747A (en) * 1919-05-07 1921-02-08 George B Keplinger Bath-brush
DE812911C (de) 1945-03-12 1951-09-06 Rhone Poulenc Sa Verfahren zur Herstellung von neuen substituierten Derivaten des Piperidins
CH578535A5 (en) 1973-05-11 1976-08-13 Ciba Geigy Ag Quinoline-3-carboxylic acid derivs - with e.g. analgesic, antinociceptive, antiinflammatory and antiallergic props
US4933447A (en) * 1987-09-24 1990-06-12 Ss Pharmaceutical Co., Ltd. Quinoline derivatives
FR2798656B1 (fr) 1999-09-17 2004-12-17 Aventis Pharma Sa Derives de la quinolyl propyl piperidine, leur preparation et les compositions qui les contiennent
JP2005511625A (ja) 2001-11-14 2005-04-28 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング 向精神薬としてのピラゾール誘導体
GB0206033D0 (en) 2002-03-14 2002-04-24 Pfizer Ltd Compounds useful in therapy
WO2003105850A1 (en) 2002-06-18 2003-12-24 Abbott Laboratories 2-aminoquinolines as melanin concentrating hormone receptor antagonists
WO2004016576A1 (ja) 2002-08-12 2004-02-26 Takeda Pharmaceutical Company Limited 縮合ベンゼン誘導体および用途
CA2505873A1 (en) 2002-11-12 2004-05-27 Pfizer Products Inc. Quinoline derivatives
GB0227240D0 (en) 2002-11-21 2002-12-31 Glaxo Group Ltd Compounds
GB0229281D0 (en) * 2002-12-16 2003-01-22 Novartis Ag Organic compounds
US20050124625A1 (en) * 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
JPWO2005087749A1 (ja) 2004-03-15 2007-08-09 協和醗酵工業株式会社 ２−アミノキナゾリン誘導体
US20060211752A1 (en) 2004-03-16 2006-09-21 Kohn Leonard D Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
US20070004679A1 (en) 2004-05-17 2007-01-04 Nathalie Schlienger Androgen receptor modulators and methods of treating disease using the same
AU2005247405A1 (en) 2004-05-17 2005-12-08 Acadia Pharmaceuticals Inc. Androgen receptor modulators and method of treating disease using the same
JP2006056882A (ja) * 2004-07-23 2006-03-02 Tanabe Seiyaku Co Ltd ピラゾロピリミジン化合物
CN101023083A (zh) * 2004-07-23 2007-08-22 田边制药株式会社 含氮的稠合双环化合物
US20080081817A1 (en) 2004-07-23 2008-04-03 Tanabe Seiyaku Co., Ltd. Nitrogenous Fused Bicyclic Compound
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
GB0510810D0 (en) 2005-05-26 2005-06-29 Novartis Ag Organic compounds
GB0526042D0 (en) 2005-12-21 2006-02-01 Syngenta Participations Ag Chemical compounds
WO2007097289A1 (ja) 2006-02-20 2007-08-30 Takeda Pharmaceutical Company Limited 新規医薬
HUE033894T2 (en) 2006-08-23 2018-01-29 Kudos Pharm Ltd 2-Methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as MTOR inhibitors
EP1903038A1 (de) * 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
US20100004452A1 (en) 2006-09-26 2010-01-07 Barbara Bertani 5-quinolinone derivatives as 5ht1a receptor modulators for treating sexual dysfunction, cognition impairment, psychotic disorders, anxiety, depression, etc.
CL2008001002A1 (es) 2007-04-11 2008-10-17 Actelion Pharmaceuticals Ltd Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana.
PT2164825E (pt) 2007-06-05 2014-06-24 Sanofi Sa Derivados de di(hetero)arilciclo-hexano, sua preparação, sua utilização e composições farmacêuticas compreendendo os mesmos
CA2725416A1 (en) 2008-05-12 2009-11-19 Amnestix, Inc. Compounds for improving learning and memory
JP2011526931A (ja) 2008-07-03 2011-10-20 エグゼリクシス， インコーポレイテッド Ｃｄｋモジュレーター
US8735424B2 (en) * 2008-09-02 2014-05-27 Novartis Ag Bicyclic kinase inhibitors
WO2010063352A1 (en) 2008-12-01 2010-06-10 Merck Patent Gmbh 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer
KR20110117705A (ko) 2009-02-11 2011-10-27 더 리전트 오브 더 유니버시티 오브 캘리포니아 톨-유사 수용체 조정제 및 질병의 치료
EP2401275B1 (en) * 2009-02-24 2013-07-24 Respiratorius AB Naphthyridine derivatives having bronchodilating activity
WO2011009015A1 (en) 2009-07-16 2011-01-20 Mallinckrodt Inc. (+) - morphinans as antagonists of toll-like receptor 9 and therapeutic uses thereof
US20120214803A1 (en) * 2011-02-18 2012-08-23 Vifor (International) Ag Novel Sulfonaminoquinoline Hepcidin Antagonists
WO2013060881A1 (en) 2011-10-27 2013-05-02 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Pyridopyrimidines and their therapeutic use
WO2014086453A1 (en) 2012-12-07 2014-06-12 Merck Patent Gmbh Azaheterobicyclic compounds
CA2916298C (en) 2013-06-26 2021-10-12 Abbvie Inc. Primary carboxamides as btk inhibitors
TWI529171B (zh) * 2013-07-29 2016-04-11 赫孚孟拉羅股份公司 １，７－萘啶衍生物
RU2718876C2 (ru) 2013-08-23 2020-04-15 Ньюфарма, Инк. Некоторые химические соединения, композиции и способы
SG10201704327RA (en) * 2013-10-14 2017-06-29 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds
MX363708B (es) * 2013-10-14 2019-03-29 Eisai R&D Man Co Ltd Compuestos de quinolina selectivamente sustituidos.
CN104557913B (zh) 2013-10-28 2017-02-08 上海汇伦生命科技有限公司 吡啶并嘧啶类化合物，其制备方法和用途
CA2933466A1 (en) * 2013-12-13 2015-06-18 Takeda Pharmaceutical Company Limited Pyrrolo[3,2-c]pyridine derivatives as tlr inhibitors
WO2015092592A1 (en) 2013-12-17 2015-06-25 Pfizer Inc. Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors
US9938282B2 (en) 2014-02-05 2018-04-10 Stereokem, Inc. Expedient synthesis of sitagliptin
NZ724691A (en) 2014-03-24 2018-02-23 Guangdong Zhongsheng Pharmaceutical Co Ltd Quinoline derivatives as smo inhibitors
CN104945377A (zh) 2014-03-24 2015-09-30 南京明德新药研发股份有限公司 作为smo抑制剂的喹啉衍生物
AR100137A1 (es) 2014-04-22 2016-09-14 Hoffmann La Roche Compuestos 4-amino-imidazoquinolina
GB201411236D0 (en) 2014-06-25 2014-08-06 Takeda Pharmaceutical Novel compounds
US10590086B2 (en) 2014-11-03 2020-03-17 Iomet Pharma Ltd. Pharmaceutical compound
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
WO2016087593A1 (en) 2014-12-05 2016-06-09 Syngenta Participations Ag Novel fungicidal quinolinylamidines
MA41169A (fr) 2014-12-17 2017-10-24 Acraf Composés antibactériens à large spectre d'activité
US10167270B2 (en) 2015-07-01 2019-01-01 Northwestern University Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity
WO2017031427A1 (en) 2015-08-19 2017-02-23 3-V Biosciences, Inc. COMPOUNDS AND METHODS FOR INHIBITING mTOR
MX2021006804A (es) 2015-12-17 2023-01-13 Merck Patent Gmbh Antagonistas policiclicos del receptor 7/8 tipo toll (tlr7/8) y uso de los mismos en el tratamiento de trastornos inmunitarios.
RU2758686C2 (ru) 2016-08-08 2021-11-01 Мерк Патент Гмбх Антагонисты tlr7/8 и их применение
CN110944990B (zh) 2017-07-18 2024-06-18 默克专利股份公司 Tlr7/8拮抗剂及其用途
CA3086172A1 (en) 2017-12-19 2019-06-27 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof
MX2021000093A (es) * 2018-07-31 2021-03-25 Merck Patent Gmbh Antagonistas del receptor de tipo toll 7/8 (tlr7/8) y usos de los mismos.

Also Published As

Publication number Publication date
NZ742476A (en) 2022-09-30
HRP20240355T1 (hr) 2024-06-07
LT3889145T (lt) 2024-04-10
EP3889146A1 (en) 2021-10-06
TWI736566B (zh) 2021-08-21
PT3889145T (pt) 2024-04-02
MX2018006637A (es) 2018-08-01
NZ777345A (en) 2025-02-28
RU2018123698A (ru) 2020-01-17
TW202332674A (zh) 2023-08-16
US20190330183A1 (en) 2019-10-31
KR20180094939A (ko) 2018-08-24
US20200095222A1 (en) 2020-03-26
TW201730175A (zh) 2017-09-01
AU2016371014B2 (en) 2021-07-01
IL279752B (en) 2022-12-01
JP2021098703A (ja) 2021-07-01
CA3005766A1 (en) 2017-06-22
DK3889145T3 (da) 2024-03-18
IL279751A (en) 2021-01-31
US20170174653A1 (en) 2017-06-22
JP2023126574A (ja) 2023-09-07
MY210123A (en) 2025-08-28
PH12018501068A1 (en) 2019-01-21
EP3390389A1 (en) 2018-10-24
AU2016371014A1 (en) 2018-05-31
EP3390389B1 (en) 2021-05-19
US20230303514A1 (en) 2023-09-28
IL259751A (en) 2018-07-31
JP7317878B2 (ja) 2023-07-31
IL279752B2 (en) 2023-04-01
MY196319A (en) 2023-03-24
HUE066591T2 (hu) 2024-08-28
JP6882299B2 (ja) 2021-06-02
KR102787063B1 (ko) 2025-03-26
ES2981114T3 (es) 2024-10-07
US10544122B2 (en) 2020-01-28
BR112018011556A2 (pt) 2018-11-27
CN113603675A (zh) 2021-11-05
RU2018123698A3 (enExample) 2020-04-02
AU2023285714A1 (en) 2024-01-18
WO2017106607A1 (en) 2017-06-22
CN108699032B (zh) 2022-07-22
IL259751B (en) 2021-06-30
TW202229253A (zh) 2022-08-01
SI3889145T1 (sl) 2024-05-31
AU2021218041B2 (en) 2023-10-05
SMT202400141T1 (it) 2024-05-14
CN108699032A (zh) 2018-10-23
RS65319B1 (sr) 2024-04-30
TWI886474B (zh) 2025-06-11
KR20250043596A (ko) 2025-03-28
UA124802C2 (uk) 2021-11-24
CL2018001624A1 (es) 2018-09-21
IL279752A (en) 2021-01-31
TWI804003B (zh) 2023-06-01
EP3889145A1 (en) 2021-10-06
US20210115013A1 (en) 2021-04-22
EP3889145B1 (en) 2024-02-21
MX385424B (es) 2025-03-18
US10947213B1 (en) 2021-03-16
SG11201804170RA (en) 2018-06-28
ES2883285T3 (es) 2021-12-07
AU2021218041A1 (en) 2021-10-07
US10696649B2 (en) 2020-06-30
JP2018537501A (ja) 2018-12-20
FI3889145T3 (fi) 2024-05-14
US10399957B2 (en) 2019-09-03
SG10202001146PA (en) 2020-03-30
PL3889145T3 (pl) 2024-07-01
US11629134B2 (en) 2023-04-18
MX2021006804A (es) 2023-01-13
IL279751B (en) 2021-06-30
US20250059157A1 (en) 2025-02-20

Similar Documents

Publication Publication Date Title
ZA201803367B (en) Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
IL275463A (en) TLR7/8 antagonists and their use
IL271492A (en) Use of cannabidiol in the treatment of multiple sclerosis complex
IL290150A (en) Compounds and methods for treating chronic pain
IL271117B (en) Diazabicyclic mutated imidazopyrimidines and their use in the treatment of respiratory disorders
HUE066864T2 (hu) Helyettesített pirazolo(1,5-a)pirimidinek és alkalmazásuk orvosi rendellenességek kezelésében
GB2542155B (en) Use of cannabidiol in the treatment of mental disorders
IL261932A (en) Use of probiotics in the treatment and/or prevention of eczema
HRP20180260T1 (hr) Dimer buprenorfina i njegova uporaba u liječenju gastrointestinalnih poremećaja
IL275349A (en) Use of hM4Di in the treatment of seizure disorders
PT3302454T (pt) Composições para utilização no tratamento da doença de parkinson e distúrbios associados
ZA201905402B (en) Compounds and their use in the treatment of schistosomiasis
IL274838A (en) Use of MIR101 or MIR128 in the treatment of seizure disorders
ZA201600312B (en) Therapeutic agents for use in the prophylaxis and/or treatment of hyperkinetic movement disorders
PT3408287T (pt) Gdf15 em glaucoma e respetivos métodos de utilização
PL3148990T3 (pl) Związki tiazolidynonu i ich zastosowanie w leczeniu zaburzeń psychiatrycznych neurologicznych i stanów zapalnych, w szczególności stanów zapalnych układu nerwowego
HK40063935A (zh) 多环tlr7/8拮抗剂及其在治疗免疫失调中的用途
GB201603510D0 (en) Compositions for use in the treatment of neurological disease
IL261240B (en) Preparations useful in the prevention and/or treatment of inflammation and pain
PT3148990T (pt) Compostos de tiazolidinona e seu uso no tratamento de condições psiquiátricas ou distúrbios neurológicos e inflamação, particularmente neuroinflamação